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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 575 journals)
Showing 401 - 253 of 253 Journals sorted alphabetically
Microbial Drug Resistance     Hybrid Journal   (Followers: 3)
Molecular Informatics     Hybrid Journal   (Followers: 5)
Molecular Pharmacology     Hybrid Journal   (Followers: 2)
Molekul     Open Access   (Followers: 1)
Natural Product Communications     Open Access  
Nature Reviews Drug Discovery     Full-text available via subscription   (Followers: 318)
Naunyn-Schmiedeberg's Archives of Pharmacology     Hybrid Journal  
NeuroMolecular Medicine     Hybrid Journal  
Neuropharmacology     Hybrid Journal   (Followers: 6)
Neuropsychopharmacology     Hybrid Journal   (Followers: 18)
Neuropsychopharmacology Reports     Open Access  
Nigerian Journal of Natural Products and Medicine     Full-text available via subscription  
OA Drug Design & Delivery     Open Access  
OA Medical Hypothesis     Open Access  
Obesity Facts     Open Access   (Followers: 8)
Open Pharmacoeconomics & Health Economics Journal     Open Access  
Open Pharmacology Journal     Open Access  
OpenNano     Open Access   (Followers: 1)
Orbital - The Electronic Journal of Chemistry     Open Access   (Followers: 1)
Oriental Pharmacy and Experimental Medicine     Partially Free   (Followers: 2)
Pain and Therapy     Open Access   (Followers: 3)
Particulate Science and Technology: An International Journal     Hybrid Journal   (Followers: 1)
PDA Journal of Pharmaceutical Science and Technology     Full-text available via subscription   (Followers: 36)
Pediatric Drugs     Full-text available via subscription   (Followers: 4)
Pediatric Pharmacology     Open Access   (Followers: 1)
Pharmaceutica Analytica Acta     Open Access  
Pharmaceutical Biology     Open Access  
Pharmaceutical Care-La Farmacoterapia     Open Access  
Pharmaceutical Chemistry Journal     Hybrid Journal  
Pharmaceutical Development and Technology     Hybrid Journal   (Followers: 21)
Pharmaceutical Executive     Full-text available via subscription   (Followers: 6)
Pharmaceutical Fronts     Open Access   (Followers: 6)
Pharmaceutical Historian     Open Access  
Pharmaceutical Journal     Free   (Followers: 8)
Pharmaceutical Journal of Sri Lanka     Open Access  
Pharmaceutical Medicine     Full-text available via subscription   (Followers: 4)
Pharmaceutical Nanotechnology     Hybrid Journal  
Pharmaceutical Patent Analyst     Full-text available via subscription   (Followers: 3)
Pharmaceutical Research     Hybrid Journal   (Followers: 97)
Pharmaceutical Statistics     Hybrid Journal   (Followers: 16)
Pharmaceutical Technology     Full-text available via subscription   (Followers: 6)
Pharmaceuticals     Open Access   (Followers: 4)
Pharmacia     Open Access  
PharmacoEconomics     Full-text available via subscription   (Followers: 26)
PharmacoEconomics & Outcomes News     Full-text available via subscription   (Followers: 4)
PharmacoEconomics German Research Articles     Full-text available via subscription  
PharmacoEconomics Spanish Research Articles     Hybrid Journal   (Followers: 1)
Pharmacoepidemiology and Drug Safety     Hybrid Journal   (Followers: 34)
Pharmacogenetics and Genomics     Hybrid Journal   (Followers: 1)
Pharmacogenomics     Hybrid Journal   (Followers: 7)
Pharmacogenomics and Personalized Medicine     Open Access   (Followers: 2)
Pharmacogenomics Journal     Hybrid Journal   (Followers: 5)
Pharmacognosy Communications     Partially Free  
Pharmacognosy Magazine     Open Access   (Followers: 2)
Pharmacognosy Research     Open Access   (Followers: 2)
Pharmacological Reports     Hybrid Journal  
Pharmacological Research     Hybrid Journal   (Followers: 1)
Pharmacological Research - Modern Chinese Medicine     Open Access  
Pharmacological Reviews     Hybrid Journal   (Followers: 2)
Pharmacology     Full-text available via subscription  
Pharmacology & Therapeutics     Hybrid Journal   (Followers: 3)
Pharmacology & Pharmacy     Open Access   (Followers: 1)
Pharmacology Biochemistry and Behavior     Hybrid Journal   (Followers: 2)
Pharmacology Research & Perspectives     Open Access  
Pharmacon : Jurnal Farmasi Indonesia     Open Access  
Pharmacopsychiatry     Hybrid Journal   (Followers: 3)
Pharmacotherapy The Journal of Human Pharmacology and Drug Therapy     Hybrid Journal   (Followers: 38)
Pharmactuel     Open Access   (Followers: 1)
Pharmacy     Open Access   (Followers: 4)
Pharmacy & Pharmacology     Open Access  
Pharmacy Education     Full-text available via subscription   (Followers: 11)
Pharmacy Practice (Internet)     Open Access   (Followers: 8)
Pharmakon : Arzneimittel in Wissenschaft und Praxis     Full-text available via subscription   (Followers: 1)
PharmaNutrition     Hybrid Journal   (Followers: 3)
PharmaTutor     Open Access  
Pharmazeutische Industrie     Full-text available via subscription   (Followers: 11)
Pharmazeutische Zeitung     Full-text available via subscription   (Followers: 15)
Pharmazie in Unserer Zeit (Pharmuz)     Hybrid Journal   (Followers: 18)
Physiology International     Full-text available via subscription   (Followers: 3)
Plant Products Research Journal     Full-text available via subscription  
Planta Medica     Hybrid Journal   (Followers: 4)
Planta Medica International Open     Open Access  
Prescriber     Hybrid Journal   (Followers: 9)
Progress in Neuro-Psychopharmacology and Biological Psychiatry     Hybrid Journal   (Followers: 8)
Psychiatry and Clinical Psychopharmacology     Open Access   (Followers: 1)
Psychopharmacology     Hybrid Journal   (Followers: 16)
Pulmonary Pharmacology & Therapeutics     Hybrid Journal   (Followers: 2)
PZ Prisma : Materialien zur Fort- und Weiterbildung     Full-text available via subscription  
Redox Report     Open Access  
Regulatory Mechanisms in Biosystems     Open Access   (Followers: 1)
Regulatory Toxicology and Pharmacology     Hybrid Journal   (Followers: 41)
Research & Reviews : A Journal of Drug Design & Discovery     Full-text available via subscription  
Research & Reviews : A Journal of Pharmaceutical Science     Full-text available via subscription  
Research & Reviews : A Journal of Pharmacognosy     Full-text available via subscription  
Research & Reviews : A Journal of Pharmacology     Full-text available via subscription   (Followers: 1)
Research in Pharmaceutical Sciences     Open Access   (Followers: 3)
Research in Social and Administrative Pharmacy     Hybrid Journal   (Followers: 3)
Research Journal of Pharmacognosy     Open Access  
Research Results in Pharmacology     Open Access  
Reviews of Physiology, Biochemistry and Pharmacology     Hybrid Journal   (Followers: 4)
Reviews on Clinical Pharmacology and Drug Therapy     Full-text available via subscription  
Revista Colombiana de Ciencias Químico-Farmacéuticas     Open Access  
Revista Cubana de Plantas Medicinales     Open Access   (Followers: 1)
Revista de Ciências Farmacêuticas Básica e Aplicada     Open Access  
Revista Mexicana de Ciencias Farmaceuticas     Open Access  
Revue de Médecine et de Pharmacie     Full-text available via subscription  
Safety and Risk of Pharmacotherapy     Open Access   (Followers: 1)
Saudi Pharmaceutical Journal     Open Access  
Scandinavian Journal of Clinical and Laboratory Investigation     Hybrid Journal   (Followers: 8)
Scientia Pharmaceutica     Open Access  
Seminars in Hematology     Hybrid Journal   (Followers: 12)
Seminars in Oncology Nursing     Full-text available via subscription   (Followers: 10)
Separation Science plus (SSC plus)     Hybrid Journal  
Side Effects of Drugs Annual     Full-text available via subscription   (Followers: 2)
Skin Pharmacology and Physiology     Full-text available via subscription   (Followers: 6)
Substance Abuse : Research and Treatment     Open Access   (Followers: 5)
Suchttherapie     Hybrid Journal   (Followers: 1)
Sustainable Chemistry and Pharmacy     Full-text available via subscription   (Followers: 1)
Synfacts     Hybrid Journal   (Followers: 5)
SynOpen     Open Access  
The Botulinum J.     Hybrid Journal  
The Brown University Psychopharmacology Update     Hybrid Journal   (Followers: 2)
The Medical Letter     Full-text available via subscription   (Followers: 18)
The Pink Sheet     Full-text available via subscription   (Followers: 12)
The Pink Sheet Daily     Full-text available via subscription   (Followers: 5)
Therapeutic Advances in Drug Safety     Open Access   (Followers: 3)
Therapeutic Advances in Psychopharmacology     Open Access   (Followers: 4)
Therapeutic Advances in Vaccines     Hybrid Journal   (Followers: 1)
Therapeutic Drug Monitoring     Hybrid Journal   (Followers: 5)
Therapeutic Innovation & Regulatory Science     Hybrid Journal   (Followers: 7)
Thérapie     Full-text available via subscription   (Followers: 1)
TheScientist     Free   (Followers: 6)
Toxicological & Environmental Chemistry     Hybrid Journal   (Followers: 2)
Toxicological Research     Hybrid Journal  
Toxicological Sciences     Hybrid Journal   (Followers: 11)
Toxicology     Hybrid Journal   (Followers: 19)
Toxicology and Applied Pharmacology     Hybrid Journal   (Followers: 25)
Toxicology and Industrial Health     Hybrid Journal   (Followers: 6)
Toxicology in Vitro     Hybrid Journal   (Followers: 12)
Toxicology International     Full-text available via subscription   (Followers: 5)
Toxicology Letters     Hybrid Journal   (Followers: 16)
Toxicology Mechanisms and Methods     Hybrid Journal   (Followers: 9)
Toxicology Research     Partially Free   (Followers: 8)
Toxicon     Hybrid Journal   (Followers: 5)
Toxicon : X     Open Access  
Toxin Reviews     Hybrid Journal  
Translational Psychiatry     Open Access   (Followers: 14)
Trends in Peptide and Protein Sciences     Open Access  
Trends in Pharmacological Sciences     Full-text available via subscription   (Followers: 21)
Tropical Journal of Pharmaceutical Research     Open Access  
Ukrainian Biopharmaceutical Journal     Open Access  
Vascular Pharmacology     Hybrid Journal   (Followers: 2)
World Mycotoxin Journal     Hybrid Journal   (Followers: 3)
Yakugaku Zasshi     Open Access   (Followers: 1)
Zeitschrift für Phytotherapie     Hybrid Journal   (Followers: 1)
Актуальні питання фармацевтичної та медичної науки та практики     Open Access  
Фармацевтичний часопис     Open Access  

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Pharmacia
Number of Followers: 0  

  This is an Open Access Journal Open Access journal
ISSN (Print) 0428-0296 - ISSN (Online) 2603-557X
Published by Pensoft Homepage  [58 journals]
  • Investigating the effect of Fenofibrate on biomarkers of vascular
           inflammation in L-NAME induced hypertensive rats

    • Abstract: Pharmacia 69(2): 459-465
      DOI : 10.3897/pharmacia.69.e81078
      Authors : Begard Berzinji, Kawa Dizaye : This study aims to evaluate the impact of fenofibrate on the levels of (IL-6, hsCRP, Lp-PLA2, sCD40L, and cystatin C) in hypertensive rats. Twenty-four rats were divided into two groups each of twelve. The first group served as the normotensive group, while the second group was regarded as the hypertensive group. Each group was further divided into two subgroups (control and treated). The control subgroups only received a placebo and the treated subgroups were given fenofibrate 30 mg/kg daily orally by gastric gavage for 4 weeks. The level of hsCRP, IL6, and Lp-PLA2 significantly increased, but sCD40L and cystatin C levels were not changed in hypertensive rats. Fenofibrate has significantly reduced the levels of hsCRP and Lp-LPA2 in hypertensive rats while IL6 and sCD40s have not been changed in both groups. In conclusion, Fenofibrate has revealed a pleiotropic anti-inflammatory effect by reducing the level of hsCRP and Lp-LPA2 in hypertensive rats. HTML XML PDF
      PubDate: Thu, 19 May 2022 10:48:19 +030
       
  • Study of intestinal microbial flora of local chickens to investigate
           the effect of probiotics Bacillus subtilis and Bacillus coagulans on the
           expression of ctxM and luxS pathogenic genes in isolates of Escherichia
           coli

    • Abstract: Pharmacia 69(2): 453-457
      DOI : 10.3897/pharmacia.69.e80807
      Authors : Zahra Elahianfiroz, Majid Baseri Salehi, Masood Ghane : Background and objective: Antibiotics are widely used worldwide. However, due to the emergence of antibiotic resistance in a wide range of microorganisms, their use worldwide has failed. Probiotics are suggested as complementary and alternative medicine. The present study aimed to investigate the effects of probiotics isolated from local chickens on the expression of luxS and ctxM genes in resistant Escherichia coli. Materials and methods: 300 fecal samples were taken from patients referring to Imam Khomeini Hospital in Tehran during May–September 2016 and Escherichia coli samples were isolated using specific culture media and biochemical tests and then the presence of luxS and ctxM genes were identified using PCR with specific primers. In order to extract the probiotics forming spores, the intestinal contents of 10 poultry that had not used any antibiotics and probiotics were cultured, isolated, and identified using biochemical and PCR methods. Commercial strains of Bacillus subtilis and Bacillus coagulans were purchased to compare their effects with native bacteria. These strains were then co-cultured with resistant Escherichia coli strains containing ctxM and luxS genes. Real-time PCR was used to evaluate the effect of these probiotics on gene expression Results: The results indicated that 40 isolates (7.5%) of Escherichia coli were obtained from the 300 fecal samples. Thirteen samples (32.5%) were outpatients and 27 (67.5%) were inpatients. All isolates were isolated from men and women aged 21–62. Four Escherichia coli strains were isolated from patients carrying ctxM and luxS genes. Isolation of Bacillus coagulans and Bacillus subtilis from samples was confirmed by biochemical and molecular experiments. The commercial and native strains of Bacillus coagulans reduced the expression of the luxS and ctxM genes by 3.60, 3.30, 1.58, and 2.70 times respectively. Also, the commercial and native strains of Bacillus subtilis decreased the expression of the luxS and ctxM genes by 1.37, 1.10, 2.20, and 2.80 times respectively. The results of statistical analysis showed a significant relationship between the presence of native and commercial probiotics in culture and reduced expression of ctxM and luxS genes. Conclusion: According to the results, supplements of Bacillus coagulans and Bacillus subtilis increase the effect of antibiotics resistance in Escherichia coli by reducing the expression of resistance genes. HTML XML PDF
      PubDate: Thu, 19 May 2022 10:47:43 +030
       
  • Phytochemical extraction and comparative analysis of antioxidant
           activities of Areca catechu L. nut extracts

    • Abstract: Pharmacia 69(2): 447-451
      DOI : 10.3897/pharmacia.69.e77829
      Authors : Ajesh Kumar A, S.S. Syed Abuthahir, Hassan Y. Aboul-Enein : FRAP assay proved all the extracts of Areca catechu L. nut have antioxidant properties because IC50 values of all the extracts of the same were less than that of ascorbic acid. Remaining antioxidant assays like DPPH radical scavenging assay, H2O2 scavenging assay, and Fe2+ chelating assay showed more antioxidant properties in ethyl acetate extract and nonpolar solvent extracts like n- hexane, and chloroform respectively. Antioxidant properties of Areca catechu L. nut varied depending upon the different solvent extract. HTML XML PDF
      PubDate: Thu, 19 May 2022 10:47:10 +030
       
  • Determination of amino acids of plants from Angelica L. genus by
           HPLC method

    • Abstract: Pharmacia 69(2): 437-446
      DOI : 10.3897/pharmacia.69.e83705
      Authors : Liliia Budniak, Liudmyla Slobodianiuk, Svitlana Marchyshyn, Ihor Potishnyi : One of the tasks of pharmaceutical science is to find new sources of effective drugs. Such sources include plants such as Angelica archangelica L. and Angelica sylvestris L., which have been used for many years to treat various diseases in folk medicine. Because the chemical composition of these plants is poorly understood, the aim of our study was to investigate the amino acid composition of the leaves of A. archangelica L. and A. sylvestris L. The amino acids of the leaves of the study species of the genus Angelica L. were determined by the HPLC method. Eighteen free and nineteen bound amino acids were identified in the leaves of A. archangelica L. The A. sylvestris L. leaves contained nineteen free and the same amount of bound amino acids. High concentrations of free and bound amino acids such as L-glutamic acid and L-aspartic acid predominate in A. archangelica L. and A. sylvestris L. This allowed these amino acids to be considered distinguishing markers of the study plants. Character metabolic processes in which these amino acids take part may be associated with the medicinal properties of these plants pursuant to their use in medicine and, therefore, may contribute to the insight of their therapeutic properties. HTML XML PDF
      PubDate: Mon, 16 May 2022 17:31:20 +030
       
  • The effectiveness of the use of polypeptide drugs and their effect on
           the metabolic parameters of oral fluid in patients with generalized
           periodontitis in depending on blood type

    • Abstract: Pharmacia 69(2): 429-435
      DOI : 10.3897/pharmacia.69.e82421
      Authors : Yurii Bandrivsky, Orysia Bandrivska, Nataliia Malko, Larysa Posolenyk, Oksana Vydoinyk, Maryana Iskiv : The article presents the results of treatment of 157 patients with generalized periodontitis depending on blood type using polypeptide drugs. The concentration of total protein, C – reactive protein, IgG, TRACP, BSALP, albumin, amylase, lipase, Ca, Fe was determined in the oral fluid. The treatment allowed to reduce the content of total protein, C – reactive protein, TRACP in the oral fluid with increasing levels of calcium, Fe, BSALP, in relation to the relevant data before treatment. And also, polypeptide drugs helped to increase the level of albumin in representatives of 0 (I) and A (II) blood type in the oral fluid; contributed to a decrease: glucose, IgG with increasing activity, amylase and lipase in carriers of B (III) and AB (IV) blood type in the oral fluid, in relation to the values before treatment. The dynamics of indicators of oral fluid metabolism with the help of polypeptide drugs, convincingly proves the effectiveness of their use in the treatment of generalized periodontitis in patients with different blood type. HTML XML PDF
      PubDate: Mon, 16 May 2022 13:24:48 +030
       
  • Synthesis, docking study, and structure activity relationship of novel
           anti-tumor 1, 2, 4 triazole derivatives incorporating 2-(2, 3- dimethyl
           aminobenzoic acid) moiety

    • Abstract: Pharmacia 69(2): 415-428
      DOI : 10.3897/pharmacia.69.e83158
      Authors : Hiba Alsaad, Ammar Kubba, Lubna H. Tahtamouni, Ali H. Hamzah : A series of 1,2,4 triazole derivatives (H7-12) have been synthesized by reacting an excess of hydrazine hydrate with carbothioamide derivatives (H1-6). The final compounds (HB1-HB6) were synthesized by reacting the triazole derivatives with mefenamic acid using DCC as a coupling agent. The chemical structures were confirmed by FT-IR, 1H, and 13C-NMR spectra, and some physicochemical properties were determined. The cytotoxicity of the different compounds (HB1-HB6) was evaluated by the MTT assay against two human epithelial cancer cell lines, A549 lung carcinoma and Hep G2 hepatocyte carcinoma, and one normal human cell line WI-38 lung fibroblasts. The mode of cell killing (apoptosis versus necrosis), as well as the effect on cell cycle phases were evaluated via flow cytometry. Additionally, EGFR tyrosine kinase inhibition assay was performed. The results presented in the current study indicate that the six tested compounds exhibited cytotoxicity against both cancer cell lines, and the lowest IC50 was achieved with compound HB5 against Hep G2 cancer cells which was found to be highly selective against cancer cells. HB5-treated Hep G2 cells were arrested at the S and G2/M cell cycle phases. Compound HB5 caused cell killing via apoptosis rather than necrosis, and this was achieved by inhibiting EGFR tyrosine kinase activity needed for cell proliferation, and cell cycle progression. In silico pre-ADMET studies confirmed all final compounds don’t cause CNS side effects, with little liver dysfunction effect. HTML XML PDF
      PubDate: Wed, 11 May 2022 16:33:00 +030
       
  • Method development and validation of cabozantinib by LC-MS/MS

    • Abstract: Pharmacia 69(2): 407-413
      DOI : 10.3897/pharmacia.69.e82684
      Authors : Punna Venkateshwarlu, Mehul M. Patel : The objective of this method is to be simple, precise, and economical performed by LC-MS/MS instrument. The mass spectrometric determination was performed using electrospray ionization in the positive mode with multiple reaction monitoring (MRM) mode and precursor to product ion transition to product ion of m/z 502.2 > 323 for cabozantinib. The effective separation of cabozantinib was achieved X-Bridge (2.1 mm × 100 mm, 3.5 µ) column and the mobile phase composition is 0.2% formic acid: acetonitrile (40:60 v/v), pumped at 0.12 ml/min flow rate. The Rt of cabozantinib was found to be 1.34 minutes. The LOD and LOQ were found at 1.5 ng/ml and 5 ng/ml concentrations and linearity concentrations were in a range of 5 ng/ml to 75 ng/ml with a regression correlation coefficient of 0.999. The % RSD value of accuracy was observed at 1.2–2.0. The marketed formulation assay was found to be 99.82%. The developed method and validation parameters were accepted as per USFDA guidelines. HTML XML PDF
      PubDate: Tue, 10 May 2022 18:22:48 +030
       
  • Serum monitoring of carbamazepine in patients with epilepsy and
           clinical implications

    • Abstract: Pharmacia 69(2): 401-406
      DOI : 10.3897/pharmacia.69.e82425
      Authors : Angel T. Alvarado, Gustavo Paredes, Gregoriana García, Alexis Morales, Ana María Muñoz, María Saravia, Ricardo Losno, María R. Bendezú, Haydee Chávez, Jorge A. García, Mario Pineda, Luis Sullón-Dextre : Carbamazepine is a drug with a narrow therapeutic range that requires clinical monitoring, since its toxic effects are not easily predictable, and the therapeutic level can vary. Our study aimed to monitor the serum level and determine the concentration/dose relationship of carbamazepine in people with epilepsy, analyzing its clinical implication. It is observed that 90.48% of the study volunteers present serum level values (4.3–10.4 mg/L) within the therapeutic range (4–12 mg/L); 7.14% present supratherapeutic levels (12.7–14.4 mg/L), 2.38% subtherapeutic (0.93 mg/L). The findings indicate a negative correlation (r = -0.616; r2 = 0.379; p = 0.001), between the dose (mg/day) and the dose ratio (mg/L/mg/day); and a positive correlation (r = 0.544; r2 = 0.296; p = 0.002), between the dose (mg/day)-serum concentration (mg/L). ANOVA and Tukey’s test mean difference is significant (p
      PubDate: Tue, 10 May 2022 18:21:02 +030
       
  • HPLC-DAD assay of phenols profile in Antennaria dioica (L.) Gaertn

    • Abstract: Pharmacia 69(2): 393-399
      DOI : 10.3897/pharmacia.69.e81654
      Authors : Roksolana Basaraba, Alona Savych, Svitlana Marchyshyn, Nataliіa Muzyka, Pavlina Ilashchuk : Antennaria dioica (Asteraceae family) – is a perennial herb, commonly found in dry grasslands and sandy or stony places from Eurasian areas. It is known in traditional medicine as antioxidant, diuretic, choleretic and anti-inflammatory remedy. This species should be reconsidered as possible sources of phenols, mainly flavonoids and hydroxycinnamic acids. Thus, the aim of this study was to validate a chromatographic method for detection of phenols and their identification in A. dioica herb. HPLC-DAD method was evaluated in terms of linearity, precision, repeatability, accuracy, LOD and LOQ. The calibration curves of thirteen reference substances were linear (R2 > 0.99) over the range of 5–400 µg/mL, the LODs and the LOQs were in the range of 0.1–0.3 µg/mL and 0.2–1.0 µg/mL, respectively. During HPLC-DAD assay two flavones – luteolin, apigenin; flavonol – quercetin and three its glycosides – rutin, hyperoside and isoquercitrin; coumarins: coumarin and umbelliferone; five hydroxycinnamic acids – chlorogenic, caffeic, p-coumaric, trans-ferulic and rosmarinic were identified in A. dioica herb. This phytochemical study of A. dioica confirms that this plant material is a rich source of phenolic compounds. HTML XML PDF
      PubDate: Tue, 10 May 2022 18:19:19 +030
       
  • Dynamics insights into aggregation of phospholipid species with
           cholesterol and vitamin C

    • Abstract: Pharmacia 69(2): 385-391
      DOI : 10.3897/pharmacia.69.e81435
      Authors : Dwi Hudiyanti, Sherllyn Meida Christa, Nur Hanna Mardhiyyah, Daru Seto Bagus Anugrah, Tatik Widiarih, Parsaoran Siahaan : This paper provides dynamic insight into the aggregation profile of systems containing six different phospholipid species, cholesterol, and vitamin C thru Coarse-Grain Molecular Dynamics (CGMD) simulations. The simulation used 42 systems, and each system was composed of 220 molecules of each phospholipid species, a varied number of cholesterol molecules (0, 11, 22, 33, 66, 88), and 10 vitamin C molecules. The phospholipid species were DLPE, DOPE, DLiPE, DOPS, DLiPS, and DLiPC. We found curved bilayer, toroidal bilayer, concave micelle, disc-like bilayer, planar bilayer, and liposome structures in the systems during the 40 ns simulation. The systems with a ratio cholesterol:phospholipid between 15% and 40% formed liposomes regardless of the phospholipid species. Cholesterol is positioned in the liposome bilayer while vitamin C is encapsulated in the aqueous core of liposomes for all cholesterol compositions. The cholesterol influences the liposome formation of various phospholipid species and the encapsulation of vitamin C in the liposome structure. HTML XML PDF
      PubDate: Tue, 10 May 2022 18:17:41 +030
       
  • Inhibitory effects on HepG2 cell proliferation and induction of cell
           cycle arrest by Chromolaena odorata leaf extract and fractions

    • Abstract: Pharmacia 69(2): 377-384
      DOI : 10.3897/pharmacia.69.e80498
      Authors : Hanifah Yusuf, Marhami Fahriani, Cut Murzalina, Rumaisa Dhifa Mawaddah : Concern about the side effects of liver cancer treatment has driven studies on anticancer to find compounds from plants that can act as chemotherapy. The anticancer activity of Chromolaena odorata against colorectal cancer, lung cancer, leukemia, cervical cancer, breast cancer, and liver cancer has been proven. However, this plant’s mechanism that can inhibit liver cancer cell growth is still undetermined. This study aims to investigate the anticancer activity of C. odorata against HepG2 cells. Extraction of C. odorata leaves was done by maceration method using 80% ethanol and further fractionated. Total flavonoid and major compound of the crude extract were determined by aluminum chloride colorimetric assay and Liquid Chromatography-Mass Spectrometry method. The IC50 and proliferation analysis was performed by MTT assay. Cell cycle was analyzed by using flowcytometry. Total flavonoid of 1.95% and compounds such as 5,7,8,3ʹ,4ʹ-Pentamethoxyflavonone, 1-Carboethoxy-β-carboline, 3-Methylcanthin-2, 6- dion, Canthin-6-one were found in C. odorata. The proliferation of HepG2 was significantly lower after 72 hours of incubation with ½ IC50 of C. odorata fractions. HepG2 cells treated with C. odorata extract and fractions were accumulated in the G0-G1 phase. These results indicated that C. odorata leaves could inhibit the proliferation of HepG2 cells and induce cell cycle arrest. HTML XML PDF
      PubDate: Tue, 10 May 2022 18:15:02 +030
       
  • Inhibitory effects of Moringa oleifera leaves extract on xanthine
           oxidase activity from bovine milk

    • Abstract: Pharmacia 69(2): 363-375
      DOI : 10.3897/pharmacia.69.e77740
      Authors : Hasnah Natsir, Abdur Rahman Arif, Abdul Wahid Wahab, Prastawa Budi, Rugaiyah Andi Arfah, Arwansyah Arwansyah, Ahmad Fudholi, Ni Luh Suriani, Achmad Himawan : Moringa oleifera is a tropical plant in the Moringaceae family that contains a lot of bioactive compounds. This study aimed to isolate and characterize the enzyme xanthine oxidase (XO), and conducted inhibitory tests on XO using methanol extracts of M. oleifera leaves. The xanthine oxidase enzyme isolated from bovine milk was characterized to determine the optimum pH, temperature, and substrate concentration. XO inhibition was evaluated by in vitro and in silico methods. The results of XO isolation and characterization of bovine milk showed the optimum conditions at pH 6.5, substrate concentration of 0.1 mM, and temperature 35 °C with an activity rate of 32.47 mU/mL; 21.55 mU/mL, and 21.94 mU/mL. Inhibition analysis results on methanol extract of M. oleifera leaves showed the highest activity decrease at the extract concentration of 160 ppm, with a relative inhibition value of 21.35%, while allopurinol as a positive control has a relative value inhibition of 61.21%. Relative value inhibition indicated the potential of M. oleifera leaves as a source of medicinal plants for gout sufferers. Additionally, a computational analysis was performed to observe the molecular interaction between the primary compounds of M. oleifera leaves, i.e., 5-O-acetyl-thio-octyl-β-L-rhamnofuranoside, quinic acid, and 2-dimethyl(trimethylsilylmethyl)silyloxymethyltetrahydrofuran, and XO using the molecular docking method. The finding implied that these compounds are bound to the catalytic sites of XO by hydrogen bonds and hydrophobic interactions, indicating the primary compounds of M. oleifera leaves could become XO inhibitors to treat gout disease. HTML XML PDF
      PubDate: Thu, 14 Apr 2022 18:15:49 +030
       
  • Synthesis, in silico prediction of sites of metabolism and in-vitro
           hepatotoxicity evaluationofnew seriesN’-substituted
           3-(1,3,7-trimethyl-xanthin-8-ylthio)propanehydrazides

    • Abstract: Pharmacia 69(2): 351-361
      DOI : 10.3897/pharmacia.69.e83535
      Authors : Javor Mitkov, Magdalena Kondeva-Burdina, Maya Georgieva, Alexander Zlatkov : New series of 3-(1,3,7-trimethyl-xanthin-8-ylthio)propanehydrazide derivatives were designed and synthesized. The targed compounds were obtained in yields of 54 to 100% and their structures were elucidated by FTIR,1H NMR,13C NMR, MS and microanalyses. The tested compounds were subjected to in silico prediction of sites of metabolism (SOMs). The predictions show thatthe main metabolic changes will be primarily related to oxidation of the sulfur atom in the side chain, carried out under the action of CYP2C19, as well as O-demethylation of compounds containing methoxy groups.The N-demethylation of the xanthine fragment was determined to be regulated by CYP1A2, CYP2C9, CYP2D6 and CYP3A4. Theperformed in vitro studies confirmed for two of the tested compounds to be low hepatotoxic, due to the presented prooxidant effects at subcellular level (isolated rat liver microsomes). These results highlight these molecules as promising hydrazide-hydrazone structures for the design of compounds with low hepatotoxicity. HTML XML PDF
      PubDate: Wed, 13 Apr 2022 18:54:07 +030
       
  • Measuring medication adherence of hypertensive patients with
           monotherapy treatment in a community health center by utilizing medication
           possession ratio

    • Abstract: Pharmacia 69(2): 345-350
      DOI : 10.3897/pharmacia.69.e82330
      Authors : Irma Melyani Puspitasari, Laila Nur Azizah, Rano Kurnia Sinuraya, Sofa Dewi Alfian, Rizky Abdulah : Adherence is a particular concern in treating hypertension, and non-adherence to antihypertensive drugs might cause uncontrolled hypertension. This study aimed to measure retrospectively the medication adherence of hypertensive patients with monotherapy treatment in a community health center (Puskesmas) in Bandung city, Indonesia. The retrospective patient data from 2011 to 2015 were obtained from an electronic prescription database. The patient data of those diagnosed with hypertension, >18 years old, and who received mono-antihypertensive therapy within a 12-month period were included in this study. To assess medication adherence, the medication possession ratio (MPR) was applied. Out of 780 patients, 93.6% of patients showed poor adherence, about 5.8% showed intermediate adherence, and 0.6% of patients had high adherence. Males and females showed different levels of adherence (p
      PubDate: Tue, 12 Apr 2022 14:52:03 +030
       
  • HPLC-FLD analysis of amino acids content in Chrysanthemum
           morifolium

    • Abstract: Pharmacia 69(2): 337-343
      DOI : 10.3897/pharmacia.69.e82097
      Authors : Alona Savych, Olha Polonets, Liubov Morozova, Kateryna Syrovatko, Tetiana Recun : Chrysanthemum morifolium (Asteraceae family) have long been used as a tonic, antioxidant, antipyretic, analgesic, sedative, antitumor, neuroprotector, hepatoprotector and cardioprotector agent. This species should be reconsidered as possible sources of many biocompounds, especially amino acids. Thus, the aim of this study was to validate the chromatographic method for detection of amino acids and their identification in flowers and leaves of Ch. morifolium of variant Pectoral. HPLC-FLD method was evaluated in terms of linearity, precision, repeatability, accuracy, LOD and LOQ. The calibration curves of all analytical standards of amino acids were linear (R2 > 0.99) over the range of 0.015–0.625 μmol/mL, the LODs and the LOQs were in the range of 0.001–0.096 µg/mL and 0.004–0.321 µg/mL, respectively. During the HPLC-FLD assay ten amino acids in free form and fifteen amino acids after hydrolysis in Ch. morifolium flowers were identified. Besides, twelve amino acids were detected in free form and fourteen amino acids after hydrolysis in Ch. morifolium leaves. The results of HPLC-FLD analysis showed that the predominant amino acid was L-proline in both types of herbal raw materials. Its total content was 31.67±0.02 μg/mg in Ch. morifolium flowers and 18.56±0.02 μg/mg in Ch. morifolium leaves. This phytochemical study confirms that flowers and leaves of Ch. morifolium (Pectoral) are rich sources of amino acids and can exhibit a wide range of pharmacological activities. HTML XML PDF
      PubDate: Tue, 12 Apr 2022 14:51:21 +030
       
  • Formulation and in vitro evaluation of inosine acedoben dimepranol
           tablets

    • Abstract: Pharmacia 69(2): 319-325
      DOI : 10.3897/pharmacia.69.e81442
      Authors : Krum Kafedjiiski : The present work was carried out to formulate and evaluate immediate release tablets of Inosine Acedoben Dimepranol (IAD). Tablets were prepared by wet granulation process to overcome the poor compression properties of IAD powder and produce high-dose tablets. Various type of binders and disintegrants like Povidone K-30, K-25, wheat starch, mannitol were used to prepare some series of tablets. Granules were evaluated for pre-compression parameters and tablets were evaluated for post- compression parameters. The composition batch № IAD L03 was the best for producing IAD 500 mg tablets. The optimal lubricant is glycerol dibehenate at a concentration of 3.08%. Optimized formulation was evaluated for in-vitro dissolution test. Stability studies were performed for the selected composition. HTML XML PDF
      PubDate: Fri, 8 Apr 2022 17:57:35 +0300
       
  • Peculiar features of bone marrow cell proliferation in Djungarian
           hamsters with genetic disorders under thiotepa effect

    • Abstract: Pharmacia 69(2): 327-335
      DOI : 10.3897/pharmacia.69.e77353
      Authors : Sergey Kuzin, Denis Bogomolov, Iza Berechikidze, Svetlana Larina, Tatyana Sakharova : The paper aims to examine the proliferation of bone marrow cell pool in Djungarian hamsters and the subsequent restoration of their genetic stability after the action of thiotepa (TT). The study involved 36 animals, of which 16 were in the control group (injected with 0.25 ml of physiological solution), and 20 in the experimental group (0.25 ml of thiotepa at a dose of 1.5 mg per 1 kg of body weight). The maximum number of cells with CA amounting to 30.0% was observed 13 hours after TT injection (p≤0.05 between the control and experimental groups) and rapidly declined to 5.7% over subsequent periods by the 37th hour of the experiment (p≤0.05). The results suggest that the restoration of cell pool genetic stability is largely associated with the cell selection mechanisms, which confers an advantage over cell proliferation without chromosome anomalies. HTML XML PDF
      PubDate: Fri, 8 Apr 2022 11:20:34 +0300
       
  • Anti-inflammatory activity of Sabicea brevipes Wernharm
           (Rubiaceae)

    • Abstract: Pharmacia 69(2): 311-317
      DOI : 10.3897/pharmacia.69.e82311
      Authors : Emmanuel Ifeanyi Attah, Samson Chibuzo Ugwuagbo, Sampath Chinnam, Fabian Ifeanyi Eze, Charles Okeke Nnadi, Matthias Onyebuchi Agbo, Wilfred Obonga, Mithun Rudrapal, Sanjay G. Walode, Aatika Nizam, Ranjan Kumar Sahoo, Atul R. Bendale, Shubham J. Khairnar, Mohini R. Jagtap : Over the years, medicinal plants have been employed in the treatment of inflammation and related ailments. This study evaluated the anti-inflammatory potential of the aerial parts of S. brevipes. The extracts and fractions were further evaluated for anti-inflammatory activity in carrageenan-induced rat model at varying doses (200 and 400 mg/kg doses, orally) for 5 h of treatment. The result of the phytochemical screening showed the presence of alkaloids, terpenoids, glycosides, flavonoids and tannins in the aerial parts of the plant. The in vivo anti-inflammatory study exhibited inhibition of 42% and 44%, 47% and 36%, 33% and 31%, and 43% and 42% for methanol extract n-hexane fraction, ethyl acetate fraction, and methanol fraction, at 200 and 400 mg/kg doses, respectively. The positive control (diclofenac sodium) showed an inhibition value of 51% at 5 mg/kg dose. Finally, it is concluded that S. brevipes possesses anti-inflammatory potential which validates the enthnomedicinal claim of the plant. HTML XML PDF
      PubDate: Thu, 7 Apr 2022 19:03:37 +0300
       
  • The use of complex marketing analysis and QSPR methodology for the
           necessity of a drug development grounding for the treatment of type 2
           diabetes mellitus with increased bioavailability

    • Abstract: Pharmacia 69(2): 303-310
      DOI : 10.3897/pharmacia.69.e79179
      Authors : Inna Kovalevska, Olena Ruban, Alina Volkova, Alla Kotvitska, Alina Cherkashyna : In order to guarantee qualitative medical and pharmaceutical care it is necessary for all participants of the process to provide consistent interconnected actions, including the use of modern approaches in pharmacotherapy, assessment of the urgent needs of the population in medicines (drugs), development and introduction of modern qualitative, safe and effective drugs into the market. Today, one of the key indicators in determining the population‘s need for drugs is the epidemiological indicators in a particular region and their dynamics. In recent years, the actuality of optimal and effective approaches developing in the prevention and treatment of socially significant diseases, including diabetes mellitus (DM), has been increasingly emphasized at the global level. All actions that are proposed for the development of standardized guidelines, treatment protocols, programs for on-time detection and prevention of diabetes are aimed at forming a system of measures are patient-oriented, based on understanding the patient‘s problems, lifestyle, habits, income and expenses for treatment, as well as other components associated with achieving optimal results for patients. HTML XML PDF
      PubDate: Thu, 7 Apr 2022 19:02:40 +0300
       
  • Atorvastatin ascorbic acid cocrystal strategy to improve the safety and
           efficacy of atorvastatin

    • Abstract: Pharmacia 69(2): 295-302
      DOI : 10.3897/pharmacia.69.e80072
      Authors : Sunil Kumar Karumuri Taraka, Praveen Kumar Pasala, Ranjan Kumar Sahoo, Umesh D. Laddha, Shubham J. Khairnar, Atul R. Bendale, Mithun Rudrapal : The study was aimed to investigate the effect of dissolution enhancement on the hypolipidemic effect and hepatotoxicity of the drug in hyperlipidemic rats. Atorvastatin ascorbic acid cocrystals were prepared by phase solution methods and characterized by Fourier transformation infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, X-Ray powder diffraction. Results of characterization confirmed that atorvastatin ascorbic acid cocrystals exhibited particle size was 221 nm. In in vitro study, results of dissolution test showed that the release of atorvastatin was increased to 1.6 folds. From In vivo study results, it was observed that in atorvastatin ascorbic acid cocrystals treated rats, serum total cholesterol, triglycerides, liver transaminase levels were significantly decreased, and liver glutathione activity was increased. In conclusion, atorvastatin ascorbic acid cocrystals therapy exhibited less hepatotoxicity in presence of ascorbic acid when compared to atorvastatin alone therapy and also the efficacy of therapy was improved. HTML XML PDF
      PubDate: Tue, 5 Apr 2022 14:24:07 +0300
       
  • Theranostic nanomachines for cancer treatment

    • Abstract: Pharmacia 69(2): 285-293
      DOI : 10.3897/pharmacia.69.e80595
      Authors : Alexandre Loukanov, Ayano Kuribara, Chavdar Filipov, Svetla Nikolova : Multifunctional programmed nanomachines with theranostic functions demonstrated great potential in the clinical practice of oncology, as well as the personalized nanomedicine. The reason is because such nanoagents with combined diagnostic and therapeutic functions were found to be highly effective for cancer treatment. The appropriate design of nanomachines allows them to overcome the biological barriers of proliferative tumors and to distinguish the cancer cells from their normal counterparts. Moreover, the use of biocompatible and biodegradable precursors for construction of nanomachines minimize significantly the caused adverse effects to the normal tissue cells, which is a main problem of the chemotherapy. In addition, the utilization of theranostic nanomachines also enables an improved selectivity to the cancer in respect to its intrinsic complexity, heterogeneity, and dynamic evolution. Here we present the programmable functions and performance of the microenvironment-responsive nanomachines at a molecular level for cancer imaging and therapy. HTML XML PDF
      PubDate: Tue, 5 Apr 2022 14:23:28 +0300
       
  • Understanding the combination of fractional factorial design and
           chemometrics analysis for screening super-saturable quercetin-self nano
           emulsifying components

    • Abstract: Pharmacia 69(2): 273-284
      DOI : 10.3897/pharmacia.69.e80594
      Authors : Galih Pratiwi, Aninditha Rachmah Ramadhiani, Shaum Shiyan : Quercetin is formulated in a super saturable - self-nano emulsifying (SS-SNE) to increase its stability and bioavailability. This study focuses on the screening design for SS-SNE components with a fractional factorial design (FrFD) approach and chemometric analysis. The FrFD method was chosen because it provides comprehensive benefits. The oil components used are canola and grape seed oil. Croduret 50-SS was selected as a surfactant and PEG 400 as a co-surfactant. The interaction of SNE components was evaluated using FTIR-ATR instrumentation. SNE droplet morphology was observed using a transmission electron microscope (TEM). The selected formulas were grape seed oil as oil phase at 19.6%, croduret at 60%, and PEG 400 as co-surfactant with a concentration of 16.6%. The selected formula has a droplet size of 133.27 nm, PDI of 0.181, the zeta potential of 17.00 mV, electrophoretic mobility of 1.332 µmcm/Vs, emulsification time of 10.05 seconds, a viscosity of 370.147 mPa.s, and a drug load of 31.70 mg/mL. The components of grape seed oil, croduret, and PEG 400 resulted in a quercetin carrier SNE formula that met the criteria. FrFD design and chemometric analysis in the screening process can help determine the selected formula very effectively and efficiently. HTML XML PDF
      PubDate: Tue, 5 Apr 2022 14:22:44 +0300
       
  • Development and validation of an RP-HPLC method for analysis of
           2-(5-(4-chlorophenyl)-3-(ethoxycarbonyl)-2-methyl-1H-pyrrol-1-yl)propanoic
           acid and its impurities under different pH

    • Abstract: Pharmacia 69(2): 265-271
      DOI : 10.3897/pharmacia.69.e80843
      Authors : Vania Maslarska, Stanislav Bozhanov, Stanislava Vladimirova, Lily Peikova, Diana Tzankova, Maya Georgieva : A simple, fast and selective stability indicating RP-HPLC method was applied for following the degradation and appearance of impurities of previously synthesized 2-(5-(4-chlorophenyl)-3-(ethoxycarbonyl)-2-methyl-1H-pyrrol-1-yl)propanoic acid. The chromatographic separation was achieved on a C18 column (150×4 mm i.d., 5 μm) using a mobile phase consisting of Acetonitrile: Phosphate buffer, pH=3, (50:50% v/v) with isocratic elution at a flow rate of 1.0 mL min−1 and temperature of the column of 30 °C applying a UV/VIS detector at 225 nm. The method was validated according to the ICH guidelines. A process related impurity was determined at pH 9.0 corresponding to ethyl 2-acetyl-4-(4-chlorophenyl)-4-oxobutanoate. No change in the structure was detected at pH = 7.4. HTML XML PDF
      PubDate: Tue, 5 Apr 2022 14:21:56 +0300
       
  • Drug therapy monitoring (TDM) of Digoxin: safety and efficacy
           review

    • Abstract: Pharmacia 69(2): 261-264
      DOI : 10.3897/pharmacia.69.e81467
      Authors : Rony Abdi Syahputra, Urip Harahap, Aminah Dalimunthe, M. Pandapotan Nasution, Denny Satria : Digoxin was developed as a novel medication for the treatment of heart failure and atrial fibrillation (AF) 200 years ago. This investigation began with a PubMed and Google Scholar search for various papers using the terms digoxin safety and efficacy, digoxin in heart failure, and digoxin in atrial fibrillation. Digoxin should be administered at a dose of 0.5–0.7 ng/mL in individuals with heart failure and reduced ejection fraction. Digoxin should be administered to decrease hospital readmissions, although SDC, creatinine, and potassium levels should be continuously maintained to limit the risk of toxicity. Digoxin may be used in conjunction with diuretics, spironolactone, ACE inhibitors, or beta-blockers. It is preferable to take digoxin on a regular basis. Digoxin should not be used in the pre-excitation syndrome because it can result in the rapid development of accessory route conductors, which can finally result in ventricular fibrillation. Due to the narrow therapeutic index of digoxin, it requires appropriate treatment and continuous monitoring. HTML XML PDF
      PubDate: Tue, 5 Apr 2022 14:21:09 +0300
       
  • The development of a novel ultrashort antimicrobial peptide
           nanoparticles with potent antimicrobial effect

    • Abstract: Pharmacia 69(1): 255-260
      DOI : 10.3897/pharmacia.69.e81954
      Authors : Ali Salama : Conventional antibiotics are facing significant microbial resistance, which has recently reached previously unnoticed critical levels. As a result of this situation, a large proportion of antimicrobial agents currently used in the clinic have significantly reduced therapeutic potential. Antimicrobial peptides (AMPs) may offer the medical community an alternative strategy to traditional antibiotics in the fight against microbial resistance. Current research efforts are focused on developing technologies that may reduce AMP toxicity while retaining their potent antimicrobial activity and possibly improving their delivery. The ionotropic gelation method was used to encapsulate a novel in-house designed potent ultrashort antimicrobial peptide (USAMP) into chitosan-based nanoparticles (CS-NPs) in this study. WRWRWR -CS-NPs were tested for antibacterial kinetics against two strains of Staphylococcus aureus for four days, and the developed WRWRWR -CS-NPs showed a 3-log decrease in the number of colonies when compared to CS-NP and a 5-log decrease when compared to control bacteria. Loaded WRWRWR into CS-NPs could represent an innovative approach to develop delivery systems based on NPs technology for achieving potent antimicrobial effects against multi-drug resistant and biofilm forming bacteria with negligible systemic toxicity and reduced synthetic costs that are obstructing the clinical development of AMPs generally. HTML XML PDF
      PubDate: Wed, 23 Mar 2022 17:19:57 +020
       
  • Interaction between endocannabinoids and the adrenergic system before
           and after stress-exposure

    • Abstract: Pharmacia 69(1): 249-254
      DOI : 10.3897/pharmacia.69.e80550
      Authors : Hristina Hristova Nocheva, Eleonora Nikolaeva Encheva-Stoykova, Evgeni Evgeniev Grigorov : Cold stress-induced analgesia (c-SIA) has been evaluated in male Wistar rats injected with cannabinoid receptors type 1 and a2-adrenergic receptor agonists and antagonists in different combinations before or after stress exposure. The aim of the study was to evaluate whether the endogenous cannabinoid and the adrenergic systems influenced c-SIA, and the patterns of their potential interaction. Exogenous administration of anandamide and Clonidine together, before or after stress exposure, increased c-SIA even with differences in the time of manifestation of the effect, its duration and the degree. The two systems differently contribute to c-SIA pathogenesis and mediation. Administered before stress exposure cannabinoids and the adrenergic system seem to oppose each other: the latter rather potentiates, while cannabinoids suppress c-SIA. Administered after stress exposure, instead, the two systems appear to exert a synergistic effect, and antagonization of each one of them abolishes the analgesic effect. HTML XML PDF
      PubDate: Thu, 17 Mar 2022 09:29:01 +020
       
  • Phytochemical analysis and anti-allergic activity of a combined herbal
           medicine based on bur-marigold, calendula and hawthorn

    • Abstract: Pharmacia 69(1): 237-247
      DOI : 10.3897/pharmacia.69.e77624
      Authors : Semen Kotov, Tetyana Gontova, Nadiia Kononenko, Elina Chernyavski, Valentyna Chikitkina : Using an experimentally selected extractant for balanced extraction of flavonoids, polysaccharides and polyphenols from bur-marigold herb, calendula flowers and hawthorn leaves and flowers, 3 suitable dry extracts and 1 combined extract in the selected ratio of raw materials were obtained. It was concluded that it was reasonable to standardize the combined herbal extract on the content of flavonoids in terms of luteolin-7-glucoside and content of polyphenols in terms of pyrogallol by UV method and the content of terpenoid compounds, in terms of oleanolic acid by densitometric method. The combined extract at a dose of 30 mg/kg in the model of anaphylactic shock has showed antiallergic activity at the level of tesalin and exceeds diazoline; the ability of the combined extract to reduce the permeability of skin capillaries at the level of the tesalin has established on the model of active cutaneous anaphylaxis and it significantly exceeded diazoline; the combined extract did not differ in membrane-stabilizing properties from the effect of desloratadine and was significantly superior to the reference drugs diazolin and tesalin in the test of indirect degranulation of mast cells. As a result, it was concluded that the mechanism of anti-allergic action of the combined extract is probably associated not only with antihistamine properties but also with the ability to stabilize cell membranes. HTML XML PDF
      PubDate: Mon, 14 Mar 2022 10:04:00 +020
       
  • Patient satisfaction with clinical pharmacy services and the affecting
           factors: a literature review

    • Abstract: Pharmacia 69(1): 227-236
      DOI : 10.3897/pharmacia.69.e80261
      Authors : Yuliandani Yuliandani, Sofa Dewi Alfian, Irma Melyani Puspitasari : Service quality is measured to assess the consistency of medical services provided to fulfill patient expectations. This article provides an overview of patient satisfaction with clinical pharmacy services and the influencing factors. A literature search from MEDLINE and EBSCO databases was performed with the keywords “patient satisfaction”, “pharmacy service”, “hospital pharmacy service”, and “clinical pharmacy service”. The inclusion criteria for articles are original articles, full papers, articles in English, and published in 2011–2021. A total of 25 articles from 1,118 articles discussed patient satisfaction with clinical pharmacy services such as counseling, drug therapy monitoring, patient support programs, and pharmaceutical care. Generally, patients are satisfied with clinical pharmacy services such as counseling, drug therapy monitoring, patient support programs, and pharmaceutical care. The most influencing factors with clinical pharmacy services are the quality, convenience, ease of information, and confidence in pharmacist competence. Pharmacists should equip themselves with the appropriate knowledge and competencies in clinical pharmacy services for benefits their patients. HTML XML PDF
      PubDate: Tue, 8 Mar 2022 10:22:44 +0200
       
  • Molecular docking and dynamic simulations study for repurposing of
           multitarget coumarins against SARS-CoV-2 main protease, papain-like
           protease and RNA-dependent RNA polymerase

    • Abstract: Pharmacia 69(1): 211-226
      DOI : 10.3897/pharmacia.69.e77021
      Authors : Mai E. Shoman, Amer Ali Abd El-Hafeez, Moteb Khobrani, Abdullah A. Assiri, Sultan S. Al Thagfan, Eman M. Othman, Ahmed R. N. Ibrahim : Proteases and RNA-Dependent RNA polymerase, major enzymes which are essential targets involved in the life and replication of SARS-CoV-2. This study aims at in silico examination of the potential ability of coumarins and their derivatives to inhibit the replication of SARS-Cov-2 through multiple targets, including the main protease, papain-like protease and RNA-Dependent RNA polymerase. Several coumarins as biologically active compounds were studied, including coumarin antibiotics and some naturally reported antiviral coumarins. Aminocoumarin antibiotics, especially coumermycin, showed a high potential to bind to the enzymes’ active site, causing possible inhibition and termination of viral life. They demonstrate the ability to bind to residues essential for triggering the crucial cascades within the viral cell. Molecular dynamics simulations for 50 ns supported these data pointing out the formation of rigid, stable Coumermycin/enzyme complexes. These findings strongly suggest the possible use of Coumermycin, Clorobiocin or Novobiocin in the fight against COVID-19, but biological evidence is still required to support such suggestions. HTML XML PDF
      PubDate: Tue, 8 Mar 2022 10:22:13 +0200
       
  • Inhibition of the phytopathogenic fungi Curvularia lunata BM and
           Ganoderma sp. TB4 by antifungal compounds produced by Bacillus siamensis
           LDR grown on hanjeli (Coix lacryma-jobi L.) starch

    • Abstract: Pharmacia 69(1): 203-210
      DOI : 10.3897/pharmacia.69.e80180
      Authors : Iman Santoso, Qonita Gina Fadhilah, Syella Dwi Safitri, Sri Handayani, Andi Eko Maryanto, Yasman Yasman : Bacillus siamensis LDR was tested for its potential as a biocontrol agent against the phytopathogenic fungi Curvularia lunata BM and Ganoderma sp. TB4. Fermentation of B. siamensis LDR for the production of antifungal compound was performed in modified Czapex-Dox broth using hanjeli (Coix lacryma-jobi L.) starch as carbon source. The Bacillus siamensis LDR inoculum was 105 CFU/ mL, and fermentation was conducted for up to 16 days. Antibiosis assay conducted to test the antifungal activity of filtrate medium. The results showed inhibition of C. lunata BM and Ganoderma sp. TB4 were 47.08% and 85.99%, respectively on 14th day of fermentation. Antifungal assay of the crude extract from filtrate medium revealed growth inhibition of C. lunata BM (60.70%) and Ganoderma sp. TB4 (65.25%). Thin layer chromatography of the crude extract revealed pink-colored spots indicative of lipopeptide compounds. Analysis of the crude extract by ultraperformance liquid chromatography-mass spectrometry was tentatively identified as iturin A, bacillomycin F, and surfactin. HTML XML PDF
      PubDate: Mon, 7 Mar 2022 18:31:47 +0200
       
  • Antibacterial activity of Medan Butterfly pea (Clitoria ternatea L.)
           corolla extract against Streptococcus mutans ATCC®25175™ and
           Staphylococcus aureus ATCC®6538™

    • Abstract: Pharmacia 69(1): 195-202
      DOI : 10.3897/pharmacia.69.e77076
      Authors : Denny Satria, Ervina Sofyanti, Pitu Wulandari, Fajarini, Sri Dewi Pakpahan, Stephanie Artha Limbong : Streptococcus mutans (S. mutans) and Staphylococcus aureus (S. aureus) pathogenicity that alter biofim, has become one of risk factor in orthodontic treatment. The medicinal plant’s Butterfly pea efficacy as an antibacterial agent should be confirmed in dentistry. The purpose of this study is to investigate the antibacterial activity of Medan butterfly pea corolla extract (BPCE) against S. mutans ATCC®25175™ and S. aureus ATCC®6538™. This is a laboratory experiment with Post Test Only Group Design. The minimum inhibitory concentration of BPCE is 6.25 mg/mL. The best concentration of butterfly pea extract to inhibit biofilm formation (antibiofilm) is 100 mg/mL. There was a significant difference (p < 0.05) for antibiofilm activity assays and determination of intramembrane cellular leakage. Although Medan BPCE was inadequate enough in forming antibiofilm and caused intramembrane leakage of S. mutans and S. aureus, further studies in exploring the potential morphological traits of these herbs related to orthodontic products are quite promising. HTML XML PDF
      PubDate: Fri, 4 Mar 2022 16:26:09 +0200
       
  • Oral acute toxicity study extract ethanol of balakka fruit
           (Phyllanthus emblica)

    • Abstract: Pharmacia 69(1): 187-194
      DOI : 10.3897/pharmacia.69.e81280
      Authors : Endy Juli Anto, Rony Abdi Syahputra, Hendrika Andriana Silitonga, Putri Cahaya Situmorang, Sony Eka Nugaraha : Phyllanthus emblica (PE) is a plant widely found in Indonesia, especially in Sumatra island, and in India. This study followed the OECD No. 420. The groups were divided based on gender, male and female rats. Male rats were divided into 6 groups, which were male/female control, male/female 2000 mg/kgBW, and male/female 5000 mg/kgBW. This study revealed that the ethanol extract of Phyllanthus emblica (EEPE) doses of 2000 mg/kgBW and 5000 mg/kgBW did not cause histological changes in the heart, liver, testes, ovaries, and kidneys, and did not cause changes to the hematological parameters, kidney biochemical parameters, liver biochemical parameters, and electrolyte parameters both in male and female rats. The results show that the LD50 of EEPE is higher than 5000 mg/kgBW. In short, this study provides information regarding the antioxidant activity and the safe use of EEPE. The LD50 of extract ethanol of Phyllanthus emblica is higher than 5000 mg/kgBW. HTML XML PDF
      PubDate: Tue, 22 Feb 2022 10:16:23 +020
       
  • Thymol exerts antioxidant, anti-inflammatory, and anti-apoptotic
           protective effects against gentamicin nephrotoxicity in rats

    • Abstract: Pharmacia 69(1): 181-186
      DOI : 10.3897/pharmacia.69.e77338
      Authors : Amr A. Fouad, Nardin A. Moussa, Mustafa M. Abdul Kareem, Usama I. Akl, Manal I. Abdelghany, Asmaa M. Abdel-Aziz : The renoprotective effect of thymol (TML) was investigated in rats challenged with gentamicin (GN). Rats received TML (20 mg/kg/day, p.o.) for 15 days, and GN (80 mg/kg/day, i.p.) starting from the 8th day. TML significantly lowered serum creatinine and neutrophil gelatinase-associated lipocalin, and renal malondialdehyde, nitric oxide, tumor necrosis factor-α, interleukin-18, Bax, caspase-3, and caspase-9 in GN-challenged rats. In addition, TML caused a significant increment of renal total antioxidant capacity in rats received GN. Moreover, TML significantly ameliorated GN-induced histopathological kidney tissue injury, and significantly decreased nuclear factor-κB p65 and kidney injury molecule-1 expressions in kidneys of GN-challenged rats. It was concluded that TML guarded against CN-induced nephrotoxicity in rats via inhibition of oxidative stress, inflammation, and apoptosis. HTML XML PDF
      PubDate: Tue, 22 Feb 2022 10:15:48 +020
       
  • The role of pharmacists’ interventions in improving drug-related
           problems, blood pressure, and quality of life of patients with stage 5
           chronic kidney disease

    • Abstract: Pharmacia 69(1): 175-180
      DOI : 10.3897/pharmacia.69.e79781
      Authors : Peri, Azizah Nasution, Alwi Thamrin Nasution : This six-month cohort study analyzed the impact of pharmacy interventions (PI) on drug-related problems (DRPs), blood pressure (BP), and quality of life (QoL) among patients with stage 5 chronic kidney disease (CKD) (n = 83) admitted to Pirngadi Hospital, Medan, Indonesia period February to July 2021. DRPs, BP, and QoL of the patients were analyzed before and after PI. DRPs were analyzed applying PCNE version 9, BP scores were extracted from the patients’ medical records. Their QoL was assessed using a WHOQoL questionnaire. The impacts of PI on the incidence of DRPs, BP, and the patients’ QoL were analyzed applying Wilcoxon Signed Rank and Friedman test in the SPSS program version 23.0. The number of DRPs was significantly reduced from 470 before PI to 162 following PI (p = 0.000). The patients’ QoL improved significantly from 40 ± 9.87 before PI to 69 ± 12. 45 after PI, p = 0.000. PI is crucial to improve the outcomes of CKD patients. HTML XML PDF
      PubDate: Fri, 18 Feb 2022 10:11:53 +020
       
  • Quantitative analysis of fatty acids and monosaccharides composition in
           Chamerion angustifolium L. by GC/MS method

    • Abstract: Pharmacia 69(1): 167-174
      DOI : 10.3897/pharmacia.69.e76687
      Authors : Liudmyla Slobodianiuk, Liliia Budniak, Halyna Feshchenko, Andriy Sverstiuk, Yuri Palaniza : Chamaenerion angustifolium L. widely known as fireweed, has significant natural resources in Ukraine. It has long been used in folk medicine as a sedative, analgesic, astringent, antimicrobial, anti-inflammatory, antisclerotic, wound healing, and diaphoretic agent. These properties are the result of the availability of many groups of biologically active compounds such as flavonoids, hydroxycinnamic acids, tannins, ascorbic acid, polyphenols, macro- and microelements. The aim of the study was to determine the content of fatty acids and monosaccharides of the herb. The qualitative composition and quantitative content of these biologically active compounds were determined using a GC/MS method. The results of the analysis showed that the herb of fireweed has monosaccharides, such as D-ribose, D-arabinose, D-mannose, D-glucose, D-galactose, and Myo-inositol. D-glucose presented in raw materials in the highest amount, it is content in the herb was 11.23 mg/kg. Among fatty acids, the mono-, polyunsaturated and saturated acids were determined. The content of polyunsaturated fatty acids of the total fatty acids was 53.19%, monounsaturated – 4.92%, and saturated – 41.89%. Linolenic, palmitic, and linoleic acids dominated among the determined twelve fatty acids, their content was 1.82 mg/kg, 1.74 mg/kg, and 1.10 mg/g. HTML XML PDF
      PubDate: Fri, 18 Feb 2022 10:11:22 +020
       
  • Immunogenesis in patients with medium and severe coronavirus infection
           – dynamics in different age groups

    • Abstract: Pharmacia 69(1): 157-165
      DOI : 10.3897/pharmacia.69.e81063
      Authors : Petar Atanasov, Stefka Ivanova, Yozlem Kobakova, Maria Moneva-Sakelarieva, Danka Obreshkova, Valentina Petkova, Pavlina Laleva-Jordanova : The results of a one-year prospective study, during which the process of immunogenesis in patients over 18 years of age with moderate and severe coronavirus infection was monitored and analyzed in clinical and paraclinical (clinical laboratory) aspects, are summarized and presented. The study included 2683 patients, all treated in the Clinic of Internal Diseases at the University Multiprofile Hospital for Active Treatment and Emergency Medicine “N. I. Pirogov” EAD, Sofia for the period from April 2020 to December 2020. Patients were followed for one year after recovering from moderate to severe coronavirus infection. Patients are grouped into four age categories as follows: 18–45 years; 46–65 years; 66–80 years and over 80 years. The results of our study show that during the study period in 97% of patients the level of anti-SARS-CoV2, rose and in the remaining three percent it was flat or followed by subsequent waning (in less than 1% of patients), but does not reach critically low levels (i. e. below the positivity conditional threshold). The level of IgG reached a peak and then waned, but on the other hand, as mentioned above, the amount of Ig-Total tested shows a significant increase. This trend is observed in all age groups, with a difference in the level of IgG and Ig-Total depending on age. The results of the additional screening in the target period in terms of virulence and virus segregation, categorically rule out the suspicion of the presence of “silent spreader”. During the follow-up period, no patients were re-hospitalized due to recurrence of Coronavirus infection (re-infection and illness). HTML XML PDF
      PubDate: Wed, 16 Feb 2022 14:10:24 +020
       
  • Development and validation of RP-HPLC method for analytical
           characterization of the anabolic steroid Methenolone acetate in food
           supplements

    • Abstract: Pharmacia 69(1): 151-155
      DOI : 10.3897/pharmacia.69.e78176
      Authors : Diana Tzankova, Alexandrina Mateeva, Javor Mitkov, Lily Peikova, Maya Georgieva : Nutritional supplements are concentrated sources of nutrients, vitamins and minerals with a nutritional or physiological effect, the purpose of which is to supplement the normal nutritional balance. A necessity of the health risk associated with their unregulated usage requires development of suitable fast and precise methods for their evaluation. As an answer to this a novel RP-HPLC method for analytical characterization of the anabolic steroid Methenolone acetate in food supplement was developed. The method is based on separation and evaluation performed on an analytical column Kintex 5µm EVO C18 (100 × 4.6 mm) with mobile phase acetonitrile:water = 60:40, v/v; flow rate of 1.0 mL/min and UV-detection at 240 nm and column temperature, at 25 °C. The method has proved to be specific, linear, accurate and precise. The method identified a presence of both Methenolone and Methenolone acetate in the evaluated sample. HTML XML PDF
      PubDate: Tue, 15 Feb 2022 16:56:21 +020
       
  • Socioeconomic impacts on medication adherence among patients with
           hypertension: A multicentre cross-sectional study in Lombok, Indonesia

    • Abstract: Pharmacia 69(1): 143-149
      DOI : 10.3897/pharmacia.69.e78441
      Authors : Adji Prayitno Setiadi, Sari Widiyastuti, IGA Dewi Mariati, Bruce Sunderland, Yosi Irawati Wibowo : Socioeconomic impacts on adherence are understudied, particularly in disadvantaged areas. This study aimed to evaluate socioeconomic factors on medication adherence among patients with hypertension in Lombok, Indonesia. A cross-sectional survey was conducted in all six public hospital outpatient clinics in Lombok in 2017. Data was obtained using a validated questionnaire to which the Morisky Green Levine Adherence Scale (MGLS) questionnaire was used to assess medication adherence. Binary logistic regression was performed to determine independent socioeconomic associations. A total of 693 patients with hypertension were included (response rate 84%). The majority had low adherence (76.2%). Significant independent associations were reported between setting and education with adherence (rural versus urban setting: odds ratio 3.54, p
      PubDate: Fri, 4 Feb 2022 15:33:48 +0200
       
  • Synthesis and antioxidant properties of new (2,4- and
           3,4-dimethoxyphenyl)-1,2,4-triazoles

    • Abstract: Pharmacia 69(1): 135-142
      DOI : 10.3897/pharmacia.69.e74107
      Authors : Dmitro V. Dovbnya, Andriy H. Kaplaushenko, Yuliia S. Frolova, Evheniy S. Pruglo : The purpose of the work is to develop preparative methods for the synthesis of ((5-(2,4- and 3,4-dimethoxyphenyl)-3H-1,2,4-triazole-3-yl)thio)aceto(propano-, butano-, benzo)nitriles, to investigate the reaction of acid hydrolysis, to receive the physical-chemical properties of the synthesized compounds, and to study antioxidant activity of new compounds. Preparative methods for the synthesis of (5-(2,4- and 3,4-dimethoxyphenyl)-3H-1,2,4-triazole-3-yl)thio)aceto(propano-, butano-, benzo)nitriles have been developed for which studied the reaction of acid hydrolysis, resulting in the production of carboxylic acids. The structure of the obtained substances was confirmed by modern physical-chemical methods. The antioxidant activity of the synthesized compounds was evaluated in vitro by the method of the non-enzymatic initiation of BOD with salts of iron (II). HTML XML PDF
      PubDate: Wed, 2 Feb 2022 18:50:02 +0200
       
  • Effect of gold nanoparticles on the expression of efflux pump mexA and
           mexB genes of Pseudomonas aeruginosa strains by Quantitative real-time PCR
           

    • Abstract: Pharmacia 69(1): 125-133
      DOI : 10.3897/pharmacia.69.e77608
      Authors : Keramat Dorri, Farzan Modaresi, Mohammad Reza Shakibaie, Elham Moazamian : Antibiotic-resistant Pseudomonas aeruginosa infections are usually difficult to treat, and there are limited antibiotics for treating them. Increased antibiotic resistance of this bacterium, especially in a multidrug form, has caused many problems for treatment. Nowadays, metal nanoparticles are considered as appropriate alternatives to antibiotics. The objective of the present study was to investigate the effect of gold nanoparticles on the expression of MexB and MexA genes in Pseudomonas aeruginosa isolates.Pseudomonas aeruginosa isolate was identified using biochemical tests and an API kit. The antibiotic sensitivitytest for different antibiotics was performed withthe Kirby-Bauer test according to the CLSI standard. The presence of MexB and MexA genes was assessed by PCR. The effect of gold nanoparticles was investigated by microdilution to evaluate the minimum inhibitory concentration, and the expression of MexB and MexA treated genes was done with silver nanoparticles by the Real-Time PCR method.40 Pseudomonas aeruginosa isolates were detected and identified. These isolates showed significant resistance to various antibiotics. All strains were carriers of MexB and MexA genes, and finally, in the expression of MexB and MexA genes,a significant decrease in the expression of these genes was observed in the samples treated with gold nanoparticles compared to non-treated samples.One of the mechanisms of antibacterial activity of gold nanoparticles is through reducing the expression of mexA and mexB genes and thus reducing the number of active efflux pumps at the cell surface. HTML XML PDF
      PubDate: Tue, 25 Jan 2022 10:44:30 +020
       
  • In vitro production of flavonoids in cultures of Gypsophila
           glomerata

    • Abstract: Pharmacia 69(1): 107-111
      DOI : 10.3897/pharmacia.69.e77769
      Authors : Pavlinka Popova, Yancho Zarev, Aleksandar Shkondrov, Ilina Krasteva, Iliana Ionkova : Effects of increased concentration of calcium chloride on growth and production of flavonoids in newly established shoot and callus Gypsophila glomerata cultures were studied. The highest impact of CaCl2 on the growth index was determined in callus cultures (GI = 0.92), while in shoot cultures calcium treatment reduced the amount of biomass (GI = 0.38). Total flavonoids in shoot cultures grown on MS medium and MS medium supplemented with double amount of CaCl2 were 0.36 mg/g d. w. In both callus cultures, 2 mg/g d. w. total flavonoids were quantified. Shoots and callus grown on non-modified media accumulated 0.02 mg/g d. w. quercetin derivatives. Unlike these, both shoots and callus grown on calcium-enriched media accumulated 0.03 and 0.05 mg/g d. w. of isorhamnetin derivatives. In vitro shoot cultures grown on MS medium enriched in twice the amount of CaCl2 accumulated the highest amount of saponarin (0.138 mg/mg d. w.). HTML XML PDF
      PubDate: Fri, 21 Jan 2022 16:04:13 +020
       
  • Potential of hydroxybenzoic acids from Graptopetalum paraguayense for
           inhibiting of herpes simplex virus DNA polymerase – metabolome
           profiling, molecular docking and quantum-chemical analysis

    • Abstract: Pharmacia 69(1): 113-123
      DOI : 10.3897/pharmacia.69.e79467
      Authors : Nadezhda Todorova, Miroslav Rangelov, Ivayla Dincheva, Ilian Badjakov, Venelin Enchev, Nadezhda Markova : According to our previous investigation the total methanol extract from Graptopetalum paraguayense E. Walther demonstrates a significant inhibitory effect on herpes simplex virus type 1 (HSV-1). To clarify what causes this inhibitory activity on HSV-1, a metabolic profile of the plant was performed. Three main fractions: non-polar substances, polar metabolites and phenolic compounds were obtained and gas chromatography–mass spectrometry (GC-MS) analysis was carried out. Since it is well known that phenolic compounds show a significant anti-herpes effect and that viral DNA polymerase (DNApol) appears to play a key role in HSV virus replication, we present a docking and quantum-chemical analysis of the binding of these compounds to viral DNApol amino acids. Fourteen different phenolic acids found by GC-MS analyses, were used in molecular docking simulations. According to the interaction energies of all fourteen ligands in the DNApol pockets based on docking results, density functional theory (DFT) calculations were performed on the five optimally interacting with the receptor acids. It was found that hydroxybenzoic acids from phenolic fraction of Graptopetalum paraguayense E. Walther show a good binding affinity to the amino acids from the active site of the HSV DNApol, but significantly lower than that of acyclovir. The mode of action on virus replication of acyclovir (by DNApol) is different from that of the plant phenolic acids one, probably. HTML XML PDF
      PubDate: Fri, 21 Jan 2022 10:30:19 +020
       
  • Specificity of clinical trials of some osteoporosis medicines

    • Abstract: Pharmacia 69(1): 99-106
      DOI : 10.3897/pharmacia.69.e79258
      Authors : Stefka Ivanova, Valentina Petkova : Clinical trials of medicinal products related to the prevention and treatment of osteoporosis cover all activities, operations, methods and means for obtaining summary data and their interpretation in order to reveal the nature of the procedures, as well as certain relationships and dependencies of interest imposed the relevant study. The main objectives of the analysis are to characterize the relationships and dependencies, to measure the significance of these relationships, to model statistically significant relationships and dependencies. An important condition for conducting the statistical analysis is that the data are comparable, i.e. to be based on unambiguously defined features and criteria for their internal content. Objective: This work covers a documentary analysis of conducted clinical trials of drugs for the treatment of osteoporosis, as well as an analysis of the conducted clinical trials of the drug. Denosumab. Methods: Gathering primary empirical information, allowing for: objectification of certain facts; for retrospective study of events and phenomena in a long period; allows to determine the direction of development of the process of clinical trials and processes. The applied statistical analysis covers activities, operations, methods and means for obtaining summary data and for their interpretation in order to reveal the nature of the procedures, as well as certain connections and dependencies. Results: Studies show that clinical trials of osteoporosis products have the following limitations: gender differentiation – although the disease occurs in both sexes, studies in female patients are more common, patients are required to are in menopause, in some studies it is required as including criteria – the presence of a fracture due to osteoporosis, the age characteristic of patients is on average 45–80 years. All analyzed drugs show a positive effect on the state of bone density and bone structure. Conclusion: All analyzed medicinal products show a positive effect on the state of bone density and bone structure but the process is irreversible, so early prevention associated with early diagnosis would lead to earlier treatment measures in the early stages of the disease, which in turn, it would lead to long-term savings in indirect and difficult-to-estimate costs for society as a whole. HTML XML PDF
      PubDate: Thu, 20 Jan 2022 17:28:46 +020
       
  • Contribution to the microscopic identification of Zingiber
           officinale

    • Abstract: Pharmacia 69(1): 93-97
      DOI : 10.3897/pharmacia.69.e78304
      Authors : Anna Gavrilova, Genadi Gavrilov, Dora Trifonova : Zingiber officinale Roscoe has a very long history of use throughout the world, both as a spice and as a medicinal plant. During the last two years in the midst of a global pandemic of SARS-CoV-2 the use of various herbal products with ginger rhizome as active ingredient increased because of its numerous health beneficial properties. A detailed characteristic of the crude powdered drug is presented by microscopic photographs for the first time. Although the structure of ginger rhizome is relatively simple and well-studied, the presented results in combination with the detailed analysis of the literature provide additional insight to the pharmacopoeial guidelines for the identification of ginger powder. HTML XML PDF
      PubDate: Wed, 19 Jan 2022 16:42:27 +020
       
  • Potency of moringa (Moringa oleifera L.) leaves extract containing
           quercetin as a depigmentation agent inhibiting the tyrosinase enzyme using
           in-silico and in-vitro assay

    • Abstract: Pharmacia 69(1): 85-92
      DOI : 10.3897/pharmacia.69.e73132
      Authors : Ni Putu Linda Laksmiani, I Wayan Agus Widiantara, Andrew Borneo Salian Pawarrangan : Hyperpigmentation is a disorder of facial skin pigments due to an increase in the process of melanogenesis, which can cause a darkening of skin color. A flavonoid compound with potential as a skin-lightening agent is quercetin, commonly found in Moringa oleifera L. leaves. This study aims to determine quercetin’s affinity and molecular mechanism on tyrosinase enzyme target proteins using an in-silico molecular docking method. Docking of quercetin with the tyrosinase enzyme produced a bond energy value of -7.08 kcal/mol. In comparison, the tropolone as a native ligand with the tyrosinase enzyme produced -4.79 kcal/mol. Quercetin has a strong affinity for the tyrosinase enzyme, indicated by the bond energy results from docking. Quercetin extraction from Moringa oleifera L. leaves using three different extraction methods: maceration, soxhlation, and reflux were made. The chromatogram from the TLC-Densitometry method showed the identification result in maceration and soxhlation extract containing quercetin, while reflux extract did not contain quercetin. The highest quercetin was obtained in the maceration method with a level of 21.57% w/w, while the soxhlation received quercetin as much as 18.49% w/w. In-vitro tests were carried out using a spectrophotometric method using a comparison of kojic acid. The in-vitro test found that IC50 from kojic acid was 48.90 µg/mL and IC50 of the extract from moringa leaf maceration of 115.36 µg/mL. Based on this research, quercetin compounds in Moringa oleifera L. leaves from maceration can potentially be skin-lightening agents. HTML XML PDF
      PubDate: Wed, 19 Jan 2022 16:41:40 +020
       
  • Impact of acacia arabica topical gel on skin wound healing: An
           experimental study

    • Abstract: Pharmacia 69(1): 77-83
      DOI : 10.3897/pharmacia.69.e72595
      Authors : Eman Abdullah, Sara Taha, Noor Sulaiman, Muna Ahmed : Aim of the study: To estimate the influence of Acacia Arabica gel abstract on skin wound healing. Material and method: 28male adult rabbits were included, 2 incisions of 1cm length were made on the skin of the rabbit’s back, one is treated by acacia gel while another left for normal healing, histopathological examination was done at 24h, 3, 7 and 14 days intervals. Results: The inflammatory reactions showed no significant results for both the control group and the study group during the study intervals. Granulation tissue in the control group was absent after 24h but increased to become profound after 7 days then become moderate, while the study group showed scanty granulation tissue from the first day and increased through study intervals. Re-epithelialization mean scores in the study group were higher than control one. Conclusions: Acacia arabica has the efficacy of hastening the wound healing process. HTML XML PDF
      PubDate: Tue, 11 Jan 2022 17:18:27 +020
       
  • Analysis of amino acids content in the plant components of the
           antidiabetic herbal mixture by GC-MS

    • Abstract: Pharmacia 69(1): 69-76
      DOI : 10.3897/pharmacia.69.e77251
      Authors : Alona Savych, Svitlana Marchyshyn, Liudmila Mosula, Oksana Bilyk, Ihor Humeniuk, Alexandra Davidenko : Medicinal plants and their combinations due to the wide range of biologically active substances can influence on various links of the pathogenetic mechanism of development of DM type 2 and its complications. One of such combinations is an antidiabetic herbal mixture (Urticae folia, Rosae fructus, Myrtilli folia, Menthae folia and Taraxaci radices) with established hypoglycaemic, hypolipidemic, antioxidant, hepatoprotective, pancreatoprotective activity in previous pharmacological studies in vivo and in vitro and defined phytochemical composition. Thus, the aim of this study was to identify and establish the content of amino acids in the plant components of antidiabetic herbal mixture. The amino acids were separated by GC-MS method with pre-column derivatization. The calibration curves of twenty CRS of amino acids were linear (R2 > 0.98) over the range of 1–100 µg/mL, the LODs and the LOQs were in the range of 0.01–0.07 µg/mL and 0.02–0.20 µg/mL, respectively. The results of analysis showed that the predominant essential amino acid was L-proline in Taraxaci radices, Urticae folia, Rosae fructus and Menthae folia, its total content was 101.46 mg/g, 25.31 mg/g, 23.04 mg/g and 19.30 mg/g, respectively. In addition, it was established total content of essential amino acid – L-leucine that can stimulate insulin secretion in β-cells of the pancreas. Its total content was 58.51 mg/g in Taraxaci radices, 9.58 mg/g in Myrtilli folia, 4.68 mg/g in Rosae fructus, 2.99 mg/g in Urticae folia and 0.79 mg/g in Menthae folia. Chromatographic examination also revealed L-phenylalanine, an essential amino acid important for antidiabetic therapy that can increase insulin secretion, stimulate proliferation and neogenesis of β-cells of the pancreas and reduce insulin resistance. Its total content was 13.42 mg/g in Myrtilli folia, 2.23 mg/g in Rosae fructus, 1.478 mg/g in Urticae folia, 1.46 mg/g in Taraxaci radices and 0.52 mg/g in Menthae folia. This phytochemical study shows, which plant material forms the amino acid composition and content in the finished herbal mixture and due to which biologically active substances the antidiabetic activity of this phytocomposition is manifested. HTML XML PDF
      PubDate: Fri, 7 Jan 2022 10:43:04 +0200
       
  • Study of the dissolution kinetics of drugs in solid dosage form with
           lisinopril and atorvastatin and intestinal permeability to assess their
           equivalence in vitro

    • Abstract: Pharmacia 69(1): 61-67
      DOI : 10.3897/pharmacia.69.e77319
      Authors : Nataliia Shulyak, Kateryna Liushuk, Oksana Semeniuk, Nadiya Yarema, Tetyana Uglyar, Dariya Popovych, Andriy Sverstiuk, Roman Ciciura, Liliya Logoyda : Atorvastatin and lisinopril are a successful combination for the treatment of patients with chronic heart failure and hypertension. Study of the dissolution kinetics of drugs in solid dosage form with lisinopril and atorvastatin and intestinal permeability to assess their equivalence in vitro were described. In medium with hydrochloric acid pH 1.2, in the medium of acetate buffer solution with a pH of 4.5 and in the medium phosphate buffer solution with a pH of 6.8 for 15 min more than 85% of the active substance passes into solution, hence the dissolution profiles these drugs in these environments are similar, and the drugs in them are “very quickly soluble”. Among the in vitro models that make it possible to assess the degree of absorption of API, the most widely used culture of adenocarcinoma cells of the colon – Caco-2. The development of the analytical methodology and its validation is the final stage of both the dissolution study and the Caco-2 test, as well as the biowaver procedure. It plays the most important role in the reliability of the results for all the above procedures and tests. To study permeability, method LC-MS/MS was developed. According to the obtained results, atorvastatin and lisinopril showed low permeability. The values ​​of recovery of transport of test and control substances through the monolayer of cells of the Caco-2 line indicate that the results of the experiment can be considered reliable. The equivalence of the drugs “Lisinopril”, tablets of 10 mg and “Atorvastatin”, tablets of 10 mg, belongs to class III BCS proven by in vitro studies. HTML XML PDF
      PubDate: Fri, 7 Jan 2022 10:41:48 +0200
       
  • Repurposing – second life for drugs

    • Abstract: Pharmacia 69(1): 51-59
      DOI : 10.3897/pharmacia.69.e72548
      Authors : Porkodi Ayyar, Umamaheswari Subramanian : Drug repurposing refers to finding new indications for existing drugs. The paradigm shift from traditional drug discovery to drug repurposing is driven by the fact that new drug pipelines are getting dried up because of mounting Research & Development (R&D) costs, long timeline for new drug development, low success rate for new molecular entities, regulatory hurdles coupled with revenue loss from patent expiry and competition from generics. Anaemic drug pipelines along with increasing demand for newer effective, cheaper, safer drugs and unmet medical needs call for new strategies of drug discovery and, drug repurposing seems to be a promising avenue for such endeavours. Drug repurposing strategies have progressed over years from simple serendipitous observations to more complex computational methods in parallel with our ever-growing knowledge on drugs, diseases, protein targets and signalling pathways but still the knowledge is far from complete. Repurposed drugs too have to face many obstacles, although lesser than new drugs, before being successful. HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:30:50 +0200
       
  • Detection and development of a quantitation method for undeclared
           compounds in antidiabetic biologically active additives and its validation
           by high performance liquid chromatography

    • Abstract: Pharmacia 69(1): 45-50
      DOI : 10.3897/pharmacia.69.e76247
      Authors : Virab Gurgen Kirakosyan, Avetis Hovhannes Tsaturyan, Lilit Eduard Poghosyan, Ella Vardan Minasyan, Hayk Razmik Petrosyan, Lusine Yurik Sahakyan, Tatevik Hovhannes Sargsyan : An isocratic, high-performance liquid chromatography (HPLC) quantitation method was developed for the quantitative determination of metformin, glibenclamide, gliclazide, glimepiride in some antidiabetic biologically active additives. A Nucleosil C18, 5 μm, 4.6 mm × 150 mm, column with mobile phase containing buffer (10 mm Na2HPO4, 10 mm sodium dodecyl sulfate): acetonitrile = 68 : 32 (V/V), pH = 7.5 was used. The flow rate was 1.0 mL/min, and effluents were monitored at 226 nm. The retention times of gliclazide glibenclamide, glimepiride and metformin, were 2.203, 4.587, 5.667 and 10.182 min, respectively. Linearity was studied by preparing standard solutions of gliclazide, glibenclamide, glimepiride and metformin at the concentration range of 50% to 150% of working concentration from a stock solution. The method was successfully applied to the estimation of gliclazide, glibenclamide, glimepiride and metformin in some antidiabetic biologically active additives. This method was validated to confirm its system suitability, selectivity, linearity, precision and accuracy according to international conference on harmonization (ICH) guidelines. HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:29:45 +0200
       
  • Specialized nutrition for athletes: evaluation of ergogenic action
           using the principles of evidence-based medicine

    • Abstract: Pharmacia 69(1): 37-44
      DOI : 10.3897/pharmacia.69.e76599
      Authors : L. M. Gunina, Ye. B. Shustov, I. F. Belenichev, N. L. Vysochina, R. V. Golovashchenko, O.V. Morozova : The aim is to form a balanced position regarding the ergogenic characteristics of new sports food products in the modern practice of training highly qualified athletes on the basis of clinical-experimental evaluation of the effectiveness of special purpose real food additives. Materials and methods. Studies were carried out on laboratory animals (36 Wistar rats at the age of 3 months weighing 150–200 g and 16 Svetlogorsk mini-pigs) as well as on 102 high-qualified representatives of cyclic sports (all men aged 19–26) − members of national teams such as swimming (25), cross-country athletics (53), and skiing (24). As a control group, we studied 25 athletes of the same gender (all men), age and qualifications who received a placebo (starch capsules) for a long time during exercise. Placebo-controlled studies have been conducted on laboratory animals and athletes in compliance with the principles of bioethics. Results. It has been established that in the experiment the application of a new specialized food product MioActiv has a positive effect on the physical performance of animals and delays the onset of fatigue, which significantly exceeds the corresponding characteristics in the placebo group. Athletes also showed an increase in speed when passing competitive distances by 18.7–21.4% (p < 0,05), as well as a significant increase in mental endurance indicators (p < 0,05). The approbation of the innovative pre-workout pharmacological nutrient complex Pre-Fuse also showed the high efficacy and safety of this product with a positive effect of increasing the performance and endurance of animals, as well as the parameters of mental performance of athletes in the main groups, in contrast to the data in the placebo control groups. Conclusions. An analysis of the prescription components of new types of ergogenic sports nutrition and the presented results of preclinical and clinical studies conducted on the basis of the evidence-based medicine paradigm regarding the effectiveness of specialized products indicate the complex action of these funds on various aspects of both physical and mental performance. From the materials presented in the article, it can be seen that specialized sports nutrition products of an ergogenic orientation can provide significant assistance in increasing sports results. HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:29:01 +0200
       
  • Indicators of endothelial function and systemic immune inflammatory
           response in patients with chronic heart failure and coexisting primary
           hypothyroidism

    • Abstract: Pharmacia 69(1): 31-35
      DOI : 10.3897/pharmacia.69.e77225
      Authors : Yuliia Ihorivna Mykula, Iryna Hryhorivna Kupnovytska, Oksana Ihorivna Danulyk : Chronic heart failure is one of the leading causes of death globally, affecting 1.5 to 2% of the total world population and 2.9 to 3.9% of the total Western European population. Chronic heart failure often progresses rapidly in coexistence with endocrine pathology, namely hypothyroidism, that results in a more rapid development and further progression of endothelial dysfunction and the development of a systemic inflammatory response. The aim of our research was to study the levels of endothelin-1, C-reactive protein, tumor necrosis factor α and their correlation with the levels of thyroid-stimulating hormone, thyroxine in patients with chronic heart failure and coexisting hypothyroidism. There were examined 38 patients with chronic heart failure and coexisting hypothyroidism and 42 patients with chronic heart failure without hypothyroidism. The serum levels of endothelin-1, C-reactive protein, tumor necrosis factor α were determined by the enzyme-linked immunosorbent assay, while the levels of thyroid-stimulating hormone and thyroxine were determined by the electrochemiluminescence immunoassay. In patients with chronic heart failure and coexisting hypothyroidism, the levels of endothelin-1, C-reactive protein, and tumor necrosis factor α were 2.9, 1.5 and 2.27 times higher than those in patients without hypothyroidism. In Group I, there was a moderate positive correlation between the serum levels of endothelin-1 and thyroid-stimulating hormone and a weak negative correlation between the levels of thyroxine and endothelin-1. In Group II, there was a weak correlation between the levels of endothelin-1 and thyroid-stimulating hormone and no correlation between the levels of thyroxine and endothelin-1. In Group I, there was a strong positive correlation between C-reactive protein and thyroid-stimulating hormone levels as well; in Group II, no similar correlation was found. In Group I, there was found a moderate negative correlation between tumor necrosis factor α and thyroxine levels. According to our results, there was a close correlation between the markers of endothelial dysfunction, immune inflammatory response, and single markers of hypothyroidism. HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:27:49 +0200
       
  • Improvement of in vitro antioxidant activity of kaempferol by
           encapsulation in copolymer micelles

    • Abstract: Pharmacia 69(1): 25-29
      DOI : 10.3897/pharmacia.69.e77678
      Authors : Denitsa Aluani, Magdalena Kondeva-Burdina, Alexandra Tosheva, Krassimira Yoncheva, Virginia Tzankova : Antioxidant capacity of poorly soluble natural antioxidant kaempferol, in particular free or loaded in two types of cationic micelles, was studied on non-enzyme induced lipid peroxidation (LPO) in vitro. The micelles were based on triblock copolymers - poly(2-(dimethylamino)ethyl methacrylate-b-poly(propylene oxide)-b-poly(2-(dimethylamino)ethyl methacrylate (PDMAEMA-PPO-PDMAEMA) and poly(2-(dimethylamino)ethyl methacrylate-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate (PDMAEMA-PCL-PDMAEMA). The lipid peroxidation was induced by incubating of rat liver microsomes with iron sulphate and ascorbic acid (Fe2+/AA). The effect of free and micellar kaempferol (at concentrations 25, 50 and 75 μg/ml) was assessed after 20 min incubation time. In the non-enzyme lipid peroxidation model, the kaempferol-loaded micelles significantly decreased the formation of malondialdehyde (MDA). The effect of kaempferol loaded in PDMAEMA-PCL-PDMAEMA micelles was more pronounced, showing an improved antioxidant activity in the conditions of oxidative stress and lipid peroxidation in vitro. HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:26:54 +0200
       
  • HPLC determination of Escitalopram in tablet dosage forms

    • Abstract: Pharmacia 69(1): 21-24
      DOI : 10.3897/pharmacia.69.e77878
      Authors : Stefan Balkanski : Purpose: A simple, specific, precise, and accurate reversed phase liquid chromatographic (RP-LC) method has been developed for the determination of Escitalopram in tablet dosage form. Methods: The chromatographic separation was achieved on a LiChrosorb C18, 250 mm x 4.6 mm, 5 μm column at a detector wavelength of 270 nm and a flow rate of 1.0 ml/min. The mobile phase was composed of methanol, acetonitrile (70:30 v/v). The retention time of Escitalopram was 5.49 min. The method was validated for the parameters like specificity, linearity, precision, accuracy, limit of quantitation and limit of detection. Results: The method was found to be specific as no other peaks of impurities and excipients were observed. The square of correlation coefficient (R2) was 0.9999 while relative standard deviations were found to be
      PubDate: Wed, 5 Jan 2022 11:26:04 +0200
       
  • Development of new HPLC method for identification of metabolic
           degradation of N-pyrrolylhydrazide hydrazones with determined MAO- B
           activity in cellular cultures

    • Abstract: Pharmacia 69(1): 15-20
      DOI : 10.3897/pharmacia.69.e78417
      Authors : Alexandrina Mateeva, Lily Peikova, Magdalena Kondeva-Burdina, Maya Georgieva : In this research, a new rapid PR- HPLC method was developed for the determination of metabolites in isolated rat hapatocytes. The chromatographic parameters, including the stationary and mobile phases, outlet pressure, temperature and flow rate, were optimized. The method identified two initial from the synthesis molecules in higher concentration and one new unidentified structure as products of the hepatocytic processing of the evaluated analyte. The results identified as first step of metabolism the hydrolysis of the hydrazone group. Further investigations should be aimed into determining the next metabolic transformations, predicted by the in silico application of the web server SMARTCyp. HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:24:55 +0200
       
  • Investigating matrix interference in the pharmacopeial limit test for
           aluminum in citric acid: a re-examination, for revision of the method

    • Abstract: Pharmacia 69(1): 9-13
      DOI : 10.3897/pharmacia.69.e78631
      Authors : Theerasak Rojanarata, Kittithat Maithongdee, Nattapong Yuwansri, Sirada Kaewprasert, Thana Thanayutsiri, Noppharat Phadungcharoen, Akhayachatra Chinsriwongkul : In many pharmacopoeias, the limit test used for determining the level of aluminum in citric acid labeled for use in the manufacture of dialysate, is based on solvent extraction using 8-hydroxyquinoline and measurement of fluorescence. However, the fluorescence intensity (F.I.) readout from the extract of citric acid samples has been found to be highly dubious, showing low value, and even lower than that of a blank solution. The aim of this work therefore was to examine what effects the matrix has on the test. The comparison of the two standard curves of aluminum solutions in water, against those prepared in citric acid solutions revealed that they differed greatly in terms of slope and y-intercept. In addition, the F.I. values on the plot of the citric acid solution were much lower than that prepared in the water. In another experiment, a decrease in the F.I. of aluminum solution was clearly seen when the co-existing concentration of citric acid was increased. The results inferred that citric acid interfered with the test due to its acidity and metal-chelating capabilities. Based on this evidence, the pharmacopeial limit test for aluminum in citric acid should be revised; otherwise, it could yield results that underestimate aluminum levels and lead to inaccurate conclusions HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:24:05 +0200
       
  • Comparative assessment of clinical trials, indications, pharmacokinetic
           parameters and side effects of approved platinum drugs

    • Abstract: Pharmacia 69(1): 1-7
      DOI : 10.3897/pharmacia.69.e78813
      Authors : Stefka Ivanova : Platinum complexes are among the most commonly applied anticancer agents. The aim of current work is collection, analysing and comparative estimation of clinical trials and pharmacological indications of currently approved for application platinum detivatives: Cisplatin, Carboplatin, Oxaliplatin, Nedaplatin (Japan), Lobaplatin (China), Heptaplatin (North Korea), and Satraplatin. The other aim of the study includes the summarizing of the hystoric data for the stages of the developlement of these drugs, and the comparison of pharmacokimetic parameters, side effecs and the dose-liniting factors of the drugs. The observational study on pharmacokinetic parameters shows that protein binding decreases in order: 95% (Cisplatn); 90% (Oxaliplatin); 50% (Nedaplatin); low (Carboplatin). For every of Cisplatin, Carboplatin, Oxaliplatin have been reported more than 1000 clinical trials; for Lobaplatin, Nedaplatin, Satraplatin - about 10 trials. The differenses in dose-limiting effects are: neuro-, nephro-, ototoxicity (Cisplatin); neurotoxicity (Oxaliplatin); nephrotoxicity (Heptaplatin); myelosuppression: thrombocytopenia, neutropenia, leukopenia (Carboplatin, Nedaplatin, Satraplatin). HTML XML PDF
      PubDate: Wed, 5 Jan 2022 11:23:04 +0200
       
  • The state of pro- and antioxidant systems in rats with DMH-induced
           colon carcinogenesis on the background of extracorporeal detoxification

    • Abstract: Pharmacia 68(4): 941-946
      DOI : 10.3897/pharmacia.68.e71840
      Authors : Oksana Kachur, Liudmyla Fira, Petro Lykhatskyі, Dmytro Fira, Iryna Stechyshyn : Aim: Cancer is one of the leading causes of death in the world. The aim of this research was to study the indices of pro- and antioxidant systems in rats with dimethylhydrazine (DMH)-induced colon carcinogenesis on the background of the enterosorbent AUT-M use. Materials and methods: The study was performed on 70 white male rats weighing 200–250 g. Adenocarcinoma of the colon was simulated by subcutaneous injection of the DMH (Sigma-Aldrich Chemie, Japan) at a dose of 7.2 mg/kg once a week during 7 months. Enterosorbent AUT-M was administered intragastrically daily for 21 days after simulation of carcinogenesis at a dose of 1 ml of suspension per 100 g of animal body weight. The state of the pro- and antioxidant systems was studied by the content of oxidative modification of proteins products (OMP), the activity of superoxide dismutase (SOD), catalase (CAT), contents of ceruloplasmin (CP) and reduced glutathione (GSH). Results: It was found that DMH-induced colon carcinogenesis in rats is accompanied by disorders in the antioxidant defense system and activation of free radical oxidation processes. Enterosorbent AUT-M provides a significant reduction in the content of OMP370 and OMP430 in both blood serum and liver homogenate of rats. Moreover, the use of enterosorbent AUT-M demonstrated a significant increase in the activity of SOD, CAT, content of GSH and a decrease in CP content in investigated tissues. Conclusion: The use of enterosorbent AUT-М demonstrated prominent potential suppression for oxidative stress and positive effect on antioxidant defense system in rats with DMH-induced colon carcinogenesis. HTML XML PDF
      PubDate: Wed, 15 Dec 2021 12:00:45 +020
       
  • Development and validation of standardization methods of aqueous
           sapropel extract

    • Abstract: Pharmacia 68(4): 933-939
      DOI : 10.3897/pharmacia.68.e71783
      Authors : Oksana Strus, Mariana Fedorovska, Serhii Holota, Natalia Polovko : Methodological bases and uniform standardization criteria of humic compounds as substances for drug products have not been developed yet. This is due to the structural complexity of humic compounds, the variety of ways to extract them from natural objects, the impossibility of using many classical methods of analytical chemistry to identify and quantify humic substances (HS), the lack of standard samples. The identification of humic acids (HA) in the aqueous sapropel extract (ASE) is identified after extracting from ASE by alkaline hydrolysis by the quantification method. After further precipitation with a concentrated sulfuric acid solution characteristic dark brown color is appeared. It was carried out the HA extraction from the sample of ASE, the precipitation of HA, the oxidation of HA and Mohr’s salt titration in accordance with the methodology developed on the basis of SSTU 7083:2009. It was determined that the total mass fraction of HA in the ASE sample was 83.8 mg/g± 0.12%. The methods of identification and quantification of the total mass of HA in ASE have been developed and validated. The ASE has been standardized. HTML XML PDF
      PubDate: Wed, 15 Dec 2021 12:00:18 +020
       
  • Physicochemical and phytochemical standardization, and antibacterial
           evaluation of Cassia alata leaves from different locations in Indonesia

    • Abstract: Pharmacia 68(4): 947-956
      DOI : 10.3897/pharmacia.68.e76835
      Authors : Marissa Angelina, Ainul Mardhiyah, Rizna Triana Dewi, Sofa Fajriah, Nusaibah Muthiah, Yasmin Ekapratiwi, Indah D. Dewijanti, Sukirno, Jamilah, Sri Hartati : Physicochemical analysis for simplicia and extract, respectively: water content 2.12–4% for simplicia; drying losses 3.93–5.47% and 8.51–19.76%; total ash 5.14–9.41% and 6.22–17.07%; total ash acid-insoluble content 0.29–5.41% and 0.52–3.82%; total ash water-soluble content 1.26–7.14% and 1.43–8.54%; water-soluble content 19.60–39.43% and 58.45–77.51%; ethanol-soluble content 13.99–33.76% and 59.79–75.39%. The phytochemical analysis showed that the extracts contain alkaloids, flavonoids, saponins, tannins, and terpenoids. Total flavonoids and total phenolics content were 9.86–15.74% QE/g and 6.67–7.65% GAE/g, respectively. Based on LC-MS results, the extract contained emodin, kaempferol, kaempferol-3,7-diglucoside, and kaempferol-3-O-β-D-glucopyranoside. The extracts possessed antibacterial activity against bacteria tested. HTML XML PDF
      PubDate: Wed, 15 Dec 2021 09:40:48 +020
       
  • Flavonoids in in vitro cultures of Astragalus hamosus

    • Abstract: Pharmacia 68(4): 927-931
      DOI : 10.3897/pharmacia.68.e76460
      Authors : Aleksandar Shkondrov, Pavlinka Popova, Iliana Ionkova, Ilina Krasteva : Astragalus hamosus contains valuable biologically active compounds, incl. flavonoids. The possibility for in vitro cultivation of the species as a source of important flavonoids was studied. Shoot and callus cultures were established and successfully cultivated on different nutrition media, complemented or not with growth regulators. An ultra-high performance liquid chromatography – high-resolution electrospray ionisation mass spectrometry (UHPLC-HRESIMS) qualitative and quantitative analysis of non-purified methanol extracts of these cultures was performed. It was found that the cultures produced rutin in comparable quantity. Interestingly, both shoots and callus cultures accumulated the rare triglycosides alcesefoliside and mauritianin. The quantity of mauritianin, biosynthesized in shoots, was significantly higher to that in callus cultures. Alcesefoliside, was in lower quantity, compared to mauritianin. In addition, callus cultures produced alcesefoliside trice as the shoots, besides their lower level of differentiation. These findings could serve as initial research to establish the value of in vitro cultures from A. hamosus as an alternative mean of production of pharmaceutically important flavonol glycosides. HTML XML PDF
      PubDate: Fri, 10 Dec 2021 15:56:34 +020
       
  • Morpho-functional indicators changes of rats’ myocardium in
           experimental doxorubicin-induced chronic heart failure and its
           pharmacological modulation with new 4-amino-1,2,4-triazole derivative

    • Abstract: Pharmacia 68(4): 919-925
      DOI : 10.3897/pharmacia.68.e75298
      Authors : Pavlo G. Bak, Igor F. Belenichev, Liudmyla I. Kucherenko, Andrei V. Abramov, Olga V. Khromylоva : Bromide 1 - (β-phenylethyl)-4-amino-1,2,4-triazolium (Hypertril) has the properties of a beta-blocker and of NO-mimetic, is assigned to the IV class of toxicity. All these effects make Hypertril a promising drug for the treatment of cardiovascular diseases. The aim of this paper was to study the cardioprotective action of Hypertril in terms of the effect on the morpho-functional parameters of the myocardium in rats with experimental chronic heart failure (CHF). CHF was modeled on 80 white outbred rats weighing 190–220g by administering doxorubicin at a cumulative dose of 15 mg/kg. Hypertril and the reference drug metoprolol succinate were administered within 30 days after CHF modeling, intragastrically at doses of 3.5 mg/kg and 15 mg/kg. Morphometric analysis of the cellular structure of the myocardium was carried out on an Axioskop microscope (Zeiss, Germany), in an automatic mode using a macro program developed in a specialized programming environment VIDAS-2.5 (Kontron Elektronik, Germany). The administration of Hypertril to animals with CHF led to an increase in the density of nuclei of cardiomyocytes, the area of myocardiocyte nuclei, an increase in the nuclear cytoplasmic ratio and an increase in the concentration of RNA in the nuclei and cytoplasm of cardiomyocytes compared with the group of untreated animals, which indicated the presence of a pronounced cardioprotective effect in the drug candidate. In terms of such indicators as the density of surviving cardiomyocytes and the content of RNA in them, the nuclear-cytoplasmic ratio of Hypertril is significantly (p < 0.05) superior to metoprolol. HTML XML PDF
      PubDate: Fri, 10 Dec 2021 15:54:38 +020
       
  • Determination of TLC fingerprint biomarker of Ipomoea batatas (L.) Lam
           leaves extracted with ethanol and its potential as antihyperglycemic agent
           

    • Abstract: Pharmacia 68(4): 907-917
      DOI : 10.3897/pharmacia.68.e71334
      Authors : Putu Sanna Yustiantara, Ni Kadek Warditiani, Pande Made Nova Armita Sari, Ni Luh Kade Arman Anita Dewi, Yan Ramona, I Made Jawi, I Made Agus Gelgel Wirasuta : Antihyperglycemic activity of Ipomoea batatas (L.) leaves has been studied for years. As many naturally found varieties of such plant species have been used as herbal medicines, there is a need to establish a fingerprint biomarker standardization method. Our research combined TLC fingerprints and chemometric analysis to determine biomarkers in leaf ethanol extract of Ipomoea batatas (L.) (EIBL). We predicted the main constituents of anthocyanin glycosides and their acylated derivates in the leaf ethanol extract of such plants using ESI-MS. The EIBL that contained identified biomarkers has succeeded in providing an antihyperglycemic effect in experimental using STZ-induced rats. This study also found a linear correlation between doses of flavonoid derivates as antioxidant agents with their antihyperglycemic activities. Therefore, this biomarker information can be used as a model to predict the dose-responses of the antihyperglycemic activities produced by other leaf ethanol extracts of I. batatas. HTML XML PDF
      PubDate: Fri, 10 Dec 2021 15:53:34 +020
       
  • Comparison of efficacies of full and abbreviated cascade impactors in
           aerosol characterization of nebulized salbutamol sulfate produced by a jet
           nebulizer

    • Abstract: Pharmacia 68(4): 899-905
      DOI : 10.3897/pharmacia.68.e76072
      Authors : Nattika Nimmano, Safura Binti Mohd Mohari : The properties of aerosols generated from salbutamol sulfate solution (1 mg/mL) using an air-jet nebulizer were evaluated using Next Generation Impactor (NGI), a full cascade impactor, and Fast Screening Impactor (FSI), an abbreviated impactor measurement (AIM). Both impactors were operated under the same experimental conditions. The samples were recovered and assayed using validated high performance liquid chromatography (HPLC). The study investigated AIM-Human Respiratory Tract (HRT) concept by comparing key parameters of aerosolization i.e. fine particle dose (FPD) and fine particle fraction (FPF) measured using FSI, with NGI as baseline. The results showed that FSI yielded different but comparable values for FPD and FPF, indicating that it is alternative impactor to NGI. Despite the fact that FSI could not replace NGI, it may be used as an alternative impactor for simple and rapid aerosol characterization of formulations in some pharmaceutical development and quality control processes. HTML XML PDF
      PubDate: Fri, 10 Dec 2021 14:54:59 +020
       
  • Frequency of CYP2D6*3 and *4 and metabolizer phenotypes in three
           mestizo Peruvian populations

    • Abstract: Pharmacia 68(4): 891-898
      DOI : 10.3897/pharmacia.68.e75165
      Authors : Angel T. Alvarado, Roberto Ybañez-Julca, Ana María Muñoz, César Tejada-Bechi, Roberto Cerro, Luis Abel Quiñones, Nelson Varela, César André Alvarado, Erick Alvarado, María R. Bendezú, Jorge A. García : Wild type genotypes (CYP2D6) and their allelic variants have been described in a sample of a Peruvian mestizo population. The global allele frequency was 0.015 for CYP2D6*3 and 0.051 for CYP2D6*4. The percentages of genotypes described were 97% CYP2D6*1/*1 and 3.0% CYP2D6*1/*3; 90.60% for CYP2D6*1/*1, 8.55% CYP2D6*1/*4 and 0.85% CYP2D6*4/*4. The allelic frequencies of CYP2D6*3 in the Lima subpopulations were 0.022 and 0.010 for Junin; CYP2D6*4 of 0.048, 0.060, and 0.050 for residents of Lima, Junín, and Tacna, respectively. The Hardy-Weinberg equilibrium test for the studied population showed that both frequencies are in equilibrium, p
      PubDate: Wed, 8 Dec 2021 11:47:23 +0200
       
  • Antibiotic overuse in obstetric and gynecologic procedures at Zagazig
           university hospitals: A prospective observational study

    • Abstract: Pharmacia 68(4): 883-889
      DOI : 10.3897/pharmacia.68.e71923
      Authors : Ahmed M. Magdy, Mahmoud A. Seksaka, Gehan F. Balata : Surgical site infection (SSI) constitutes a major problem in healthcare in terms of healthcare cost, morbidity and mortality. Surgical antibiotic prophylaxis (SAP) is one of the effective strategies for SSI prevention. Poor adherence to SAP guidelines across different countries has been observed. Misuse of prophylactic antibiotics threatens patient safety and leads to an increase in the acquisition of antibiotic resistance. The aim of this study was to assess the utilization of SAP in obstetric and gynecologic procedures in terms of indication for prophylaxis, antibiotic selection, timing of administration and prophylaxis duration. A prospective observational study was conducted at the obstetrics and gynecology department of Zagazig University Hospital during the period from January 2020 to June 2020. Medical records of 264 women were recorded and evaluated. The American Society of Health-System Pharmacists (ASHP) therapeutic guidelines, World Health Organization (WHO) recommendations and The American College of Obstetricians and Gynecologists (ACOG) practice bulletin were used for data evaluation and hence women were stratified into two groups. For women who underwent procedures in which guidelines recommended the use of SAP (200 patients; 75.75%), 198 women (99%) received preoperative prophylaxis. None of women (0%) received the recommended first line antibiotic by guidelines while the most commonly used prophylactic antibiotics were Cefotaxime (86 patients; 43.43%) and Ampicillin-sulbactam (62 patients; 31.31%). Preoperative antibiotic prophylaxis timing was 0-60 minutes before skin incision. All women received postoperative prophylaxis that extended to an average of 7 days. Regarding the other group who underwent procedures in which prophylactic antibiotics weren’t recommended by guidelines (64 patients; 24.24%), 37 women (57.81%) followed the guidelines and didn’t receive SAP while 27 women (42.18%) received SAP. Poor adherence to guidelines recommendations regarding prophylactic antibiotic selection and prophylaxis duration was observed. High utilization rate of prophylactic antibiotics in procedures that didn’t require their use was reported.. HTML XML PDF
      PubDate: Mon, 22 Nov 2021 10:03:48 +020
       
  • Quercetin effects on adaptive immune response in experimental
           periodontitis of bacterial-immune genesis

    • Abstract: Pharmacia 68(4): 877-882
      DOI : 10.3897/pharmacia.68.e70883
      Authors : Andrii Demkovych, Yurii Bondarenko, Vitaliy Shcherba, Vitalii Luchynskyi, Volodymyr Vitkovskyy, Volodymyr Machogan : In the article was studied the effects of flavonol quercetin on indices of adaptive immune response in experimental animals on the 14th day of the experimental bacterial-immune periodontitis development. Indices of immune protection were determined by the relative number of lymphocytes with CD3+, CD4+, CD8+, CD19+, CD16+ and immunoregulatory index (CD4+ / CD8+) in intact animals and on the 14th day of inflammatory process development in periodontal tissues as well as the therapeutic effects of flavonol quercetin. As a result of the study, characterized changes associated with the activity of both the cell-mediated and humoral-immune response were found, both in the development of experimental periodontitis, and apply of flavonol. In particular, there was an increase in the animal’s blood relative amount of CD8+, CD16+ cells on the 14th day, and content of CD3+, CD4+, CD19+ was decreased. In this case, the immunoregulatory index (CD4+ / CD8+) as an important index of immunological activity was decreased. The apply of flavonol quercetin in the period development of bacterial-immune periodontitis animals functional activity of the T-cell line of the immune system was increased, as evidenced percentage increase of B- and T-cells due to T-helper cells decrease as well as T-killers content during this period of inflammatory reaction in the periodontal complex, in comparison with animals, which were not treated. HTML XML PDF
      PubDate: Thu, 18 Nov 2021 15:40:07 +020
       
  • Characterization and analysis of the antidiabetic activities of sulphated
           polysaccharide extract from Caulerpa lentillifera

    • Abstract: Pharmacia 68(4): 869-875
      DOI : 10.3897/pharmacia.68.e73158
      Authors : Sofa Fajriah, Ilmi Fadhilah Rizki, Ellya Sinurat : Caulerpa lentillifera is a type of green seaweed that is cultivated in tropical and subtropical areas. The objectives of this study were to determine the characteristics of the sulfated polysaccharides from C. lentillifera and evaluate its antidiabetic activity. In the initial process of this study, samples were macerated with ethanol (1:10). Then, the maceration residue was extracted with an accumulator at 75 °C for three hours. The crude extract yield was 4.16% based on weight seaweed. Ion chromatography purification with DEAE-Sepharose resin provided a yield of 14.8% of crude extract. The monomer analysis of C. lentillifera from the crude extract and purified extract revealed that galactose monomers were dominant and glucose was a minor component. The total carbohydrate and sulfate contents of purified C. lentillifera were higher than those of crude C. lentillifera. Bioactivity tests revealed that purified polysaccharides had higher antidiabetic activity against α-glucosidase enzyme than crude ones with IC50 values of 134.81± 2.0 µg/mL. Purified sulfated polysaccharides of C. lentillifera could potentially be used as an antidiabetic medication. HTML XML PDF
      PubDate: Fri, 12 Nov 2021 17:31:53 +020
       
  • Determination of amino acids content of the Tagetes lucida Cav. by GC/MS

    • Abstract: Pharmacia 68(4): 859-867
      DOI : 10.3897/pharmacia.68.e73325
      Authors : Liudmyla Slobodianiuk, Liliia Budniak, Svitlana Marchyshyn, Liliya Kostyshyn, Maria Ezhned : Plant raw materials are widely used for the prevention and treatment providing of many diseases. The interest is the in-depth research of the flowers, leaves, and herb of Tagetes lucida. Therefore, the study aimed to determine the content of primary metabolites, namely amino acids in the raw materials of this plant. The amino acids composition and content in flowers, leaves, and herb were determined by the GC/MS method. The results of the study revealed that the raw material of Tagetes lucida contains more bound and less free amino acids. Free and bound L-proline, L-isoleucine were present in all the analyzed samples in the greatest amount (1.909 mg/g and 20.999 mg/g, 0.804 mg/g and 18.908 mg/g in the flowers; 2.721 mg/g and 18.973 mg/g, 3.459 mg/g and 28.518 mg/g in the leaves; 6.436 mg/g and 18.817 mg/g, 0.245 mg/g and 0.222 mg/g in the herb). Another free amino acid with a high content in flowers (1.321 mg/g) and herb (0.825 mg/g) of Tagetes lucida was L-aspartic acid. In addition, high content of L-phenylalanine in bound form was found in the leaves (11.843 mg/g) of the study plant. These amino acids to be considered distinguishing markers of the Tagetes lucida. This research contributes to already known information of Tagetes lucida use as herbal medicine, nutraceutical, and food reinforcement. HTML XML PDF
      PubDate: Thu, 11 Nov 2021 19:22:42 +020
       
  • Assessment of the effects of metformin and glibenclamide on the
           concentration of selected trace elements in type 2 diabetic patients

    • Abstract: Pharmacia 68(4): 845-849
      DOI : 10.3897/pharmacia.68.e72080
      Authors : Jehan A. Mohammad, Ammar A. Y. Almulathanon, Fatimah Haitham Fathi : Metformin and glibenclamide may have beneficial effects on the levels of trace elements in diabetic patients. The aim of the current study was to assess the effects of metformin and glibenclamide on the concentrations of copper (Cu), zinc (Zn) and magnesium (Mg) in patients with type 2 diabetes mellitus. The metformin-treated patients showed significantly lower serum Cu levels compared with the untreated and glibenclamide groups. In addition, treatment with metformin was associated with a significant increase in serum concentrations of Zn compared to the newly diagnosed patients, whereas it did not show a noticeable alteration in the serum level of Mg. In contrast, the glibenclamide treated group revealed significantly higher Zn and Mg levels compared with the newly diagnosed group, while the serum level of Cu was not significantly modified. In conclusion, treatment with metformin led to a reduction in serum Cu and an increase in serum Zn concentrations, whereas glibenclamide treatment displayed enhancement in serum Zn and Mg levels. HTML XML PDF
      PubDate: Wed, 10 Nov 2021 16:44:55 +020
       
  • Non-extractive spectrophotometric determination of valsartan in pure form
           and in pharmaceutical products by ion-pair complex formation with
           bromophenol blue and methyl red

    • Abstract: Pharmacia 68(4): 851-858
      DOI : 10.3897/pharmacia.68.e73559
      Authors : Kateryna Peleshok, Bohdana Bondar, Liubomyr Kryskiw, Tetyana Kucher, Olha Poliak, Liliya Logoyda : Two simple, rapid, green non extractive spectrophotometric methods are described for the estimation of valsartan in tablet dosage form. The determination is based on the ion-pair formation using the dyes, bromophenol blue (BPB) and methyl red (MR). Valsartan forms ion-pair complex selectively with the dyes, as indicated by the formation of a coloured complex with BPB at pH 5.5 with λmax at 424 nm and MR at pH 4.3 with λmax at 494 nm. For both methods, optimal spectrophotometric conditions were established. The linear relationship was found between absorbance at λmax and concentration of drug in the range 8–24 µg/mL for BPB and 4–20 µg/mL for MR. Regression analysis of Beer’s law plot at 424 nm yielded the regression equation, y = 0.0102x + 01636 (BPB) and at 494 nm y = 0.0222x – 0.0063 (MR). High values of correlations coefficient (R2 = 0.9988 (BPB) and R2 = 0.9991 (MR)) and small values of intercept validated the linearity of calibration curve and obedience to Beer’s law. The LOD and LOQ values were calculated to be 1.03 µg/mL and 3.43 µg/mL respectively (BPB) and 0.68 µg/mL and 2.26 µg/mL respectively (MR). Intra-day and inter-day accuracy and precision, robustness were in acceptable limits. The proposed methods were applied for the quantification of valsartan in tablets pertaining to three commercial formulations. Analytical eco-scale for greenness assessment of the proposed spectrophotometric methods showed that both methods corresponds to excellent green analysis with a score of 89. HTML XML PDF
      PubDate: Wed, 10 Nov 2021 16:44:24 +020
       
  • Evaluation of the antifungal activity of marine actinomycetes isolates
           against the phytopathogenic fungi Colletotrichum siamense KA: A
           preliminary study for new antifungal compound discovery

    • Abstract: Pharmacia 68(4): 837-843
      DOI : 10.3897/pharmacia.68.e72817
      Authors : Qonita Gina Fadhilah, Iman Santoso, Andi Eko Maryanto, Sarini Abdullah, Yasman Yasman : Marine actinomycetes are being explored to discover potential actinomycetes that produce antifungal compounds. In a previous study, marine actinomycetes isolates from the mangrove ecosystem were found to inhibit growth of the phytopathogenic fungi Colletotrichum siamense KA. In this study, the three of these isolates with the highest antagonistic activity—SM11, SM14, and SM15—were evaluated for their antifungal activity using antibiosis assay. The fermentation was performed in SCB:PDB medium (1:1) for 6, 9, and 12 days. The results showed that SM14 was the strongest potential isolate; it inhibited the growth of C. siamense KA on average up to 64.90% for 12 days on PDA filtrate medium. Molecular identification showed SM14 was closely related to Streptomyces sanyensis, but had differences in morphological and biochemical characteristics compared to SM11 or SM15. This indicated that the three isolates were different strains and may challenge further research on identifying and analyzing their antifungal compounds. HTML XML PDF
      PubDate: Tue, 9 Nov 2021 13:03:25 +0200
       
  • Anticancer activity of Mandragora autumnalis: an in vitro and in vivo
           study

    • Abstract: Pharmacia 68(4): 827-835
      DOI : 10.3897/pharmacia.68.e71695
      Authors : Asma Ismail Mahmod, Wamidh H. Talib : Ethanol crude extract and four solvent fractions were extracted from M. autumnalis leave to evaluate their anticancer effect in both models: in vitro and in vivo. The in vitro assessments were conducted using the MTT method in five cancer cell lines and one normal cell line. Ethanol extract and n-hexane fraction showed antitumor activity against MCF-7 breast cancer cells with IC₅₀ values of 0.1 and 0.4 mg/ml, respectively, and low cytotoxicity against normal VERO cell line (IC₅₀ value > 4 mg/ml). Furthermore, expression levels of VEGF were tested in MCF-7 cells treated with M. autumnalis using Human VEGF Simple Step ELISA Kit. The results indicated downregulation of VEGF expression in the treated cells compared to the control group. Additionally, the LD₅₀ of M. autumnalis ethanol extract was calculated by applying an acute toxicity assay. Balb/C mice were inoculated with EMT6/p breast cancer cells and then treated with (137 mg/kg/day intraperitoneal injection) of ethanol extract for ten days. Interestingly, a significant (p < 0.001) reduction occurred in the tumor size of the treated group comparing to the control. Treatment in vivo toxicity was evaluated by measuring liver and kidney parameters. The tumor-bearing mice treated with the M. autumnalis extract showed normal serum level of AST, ALT, and creatinine. The results indicate that M. autumnalis has antitumor properties in both models in vitro and in vivo. However, further molecular investigation is required to understand the molecular bearings of M. autumnalis’ activity. HTML XML PDF
      PubDate: Wed, 27 Oct 2021 09:42:28 +030
       
  • Polyphenols content of selected medical plants and food supplements
           present at Bulgarian market

    • Abstract: Pharmacia 68(4): 819-826
      DOI : 10.3897/pharmacia.68.e71460
      Authors : Petya Koleva, Silvia Tsanova-Savova, Slaveyka Paneva, Stefan Velikov, Zaharina Savova : Background: Medicinal plants are a rich source of antioxidant polyphenols and in particular flavonoids. Materials and methods: In the present study 5 Bulgarian medical plants and 5 food supplements, present at the Bulgarian market, are analyzed for their Total phenolic, Total flavonoids and selected individual flavonoids content. A HPLC method was developed and validated for simultaneous determination of (+)-catechin, (-)-epicatechin and rutin in plant and supplements, using PDA detection. Results: The results show that polyphenols in the selected food supplements are lower than those of the medical plants analyzed. Mentha piperita and Melissa officinalis have the highest polyphenols content (67.38 and 65.17 mg GAE/g; 54.59 and 57.76 mg RE/g respectively). Rutin was detected in all samples analyzed, reaching highest levels in Mentha piperita (7332.5 µg/g), followed by fruits of Sambucus nigra (2818.7 µg/g). Conclusion: The results of the study are a practical contribution to a more complete characterization of the polyphenolic composition in Bulgarian medicinal plants. HTML XML PDF
      PubDate: Wed, 20 Oct 2021 13:23:46 +030
       
  • Spectrophotometric methods for the determination of lisinopril in
           medicines

    • Abstract: Pharmacia 68(4): 811-818
      DOI : 10.3897/pharmacia.68.e72991
      Authors : Nataliia Shulyak, Kateryna Budzivula, Tetyana Kucher, Liubomyr Kryskiw, Olha Poliak, Liliya Logoyda : Two simple, rapid and green spectrophotometric methods are described for the determination of lisinopril medicines. The determination is based on the reaction of the primary amino group of the lisinopril with ninhydrin in aqueous medium (Method I) and reaction on the carboxylic group of the lisinopril with copper (II) sulfate (Method II). For both methods, optimal spectrophotometric conditions were established. The linear relationship was found between absorbance at λmax and concentration of drug in the range 40–60 µg/mL (Method I) and 0.592–2.072 mg/mL (Method II). Regression analysis of Beer’s law plot at 400 nm yielded the regression equation, y = 7.4929x – 0.0545 (Method I) and at 730 nm y = 0.0443x – 0.0832 (Method II). High values of correlations coefficient (R2 = 0.9917 (Method I) and R2 = 0.999 (Method II)) and small values of intercept validated the linearity of calibration curve and obedience to Beer’s law. The LOD and LOQ values were calculated to be 6.91 µg/mL and 23.01 µg/mL respectively (Method I) and 0.11 mg/mL and 0.36 mg/mL respectively (Method II). Intra-day and inter-day accuracy and precision were in acceptable limits. The proposed methods were applied for the quantification of lisinopril in tablets pertaining to three commercial formulations. Analytical eco-scale for greenness assessment of the proposed spectrophotometric methods showed that both methods correspond to excellent green analysis. HTML XML PDF
      PubDate: Mon, 18 Oct 2021 11:39:48 +030
       
  • Commodity analysis of medical products used in adult incontinence

    • Abstract: Pharmacia 68(4): 805-809
      DOI : 10.3897/pharmacia.68.e73181
      Authors : Tetiana Diadiun, Inna Baranova, Safol Musozoda, Dmytro Semeniv, Svetlana Zaporozhska : There are problems people don’t want to talk about, and one of them is incontinence in adults. This is a fairly common and delicate problem. It negatively affects human life. This most often applies to people with disabilities and bedridden patients. People have to change their usual way of life, give up their favorite activities, there is a constant need to stay at home. Walking, attending events are difficult. All this has a corresponding effect on the psychological health of a person. In such a situation, it is advisable to use diapers for adults. This is a modern hygienic product that is intended to make life easier for people suffering from various forms of incontinence. Diapers are similar in shape to baby diapers, but they are adapted to the size of an adult. This is a great option for the care of patients who are bedfast or in a wheelchair. HTML XML PDF
      PubDate: Thu, 14 Oct 2021 10:04:33 +030
       
  • The investigation of antimicrobial activity of some s-substituted
           bis-1,2,4-triazole-3-thiones

    • Abstract: Pharmacia 68(4): 797-804
      DOI : 10.3897/pharmacia.68.e65761
      Authors : Yevhen Karpun, Volodymyr Parchenko, Tetiana Fotina, Denys Demianenko, Anatolii Fotin, Volodymyr Nahornyi, Natalia Nahorna : New S-substituted 4-alkyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol derivatives have been designed, synthesized and studied their antimicrobial activity on 11 standard Gram-positive and Gram-negative microorganism strains. Their spectral and physicochemical parameters were established using modern comprehensive methods of analysis, including 1H NMR spectroscopy, GC-MS and elemental analysis.It has been found that compound 2a exhibits strong suppression of 5 test strains (MBC = 15.6 µg/mL). Compound 4a showed moderate inhibition of Salmonella pullorum, Escherichia coli O2, Salmonella enteritidis strains (MBC = 31.25 µg/mL) Compound 6a was sensitive toward ten tested bacteria at 31.25 µg/mL concentration. HTML XML PDF
      PubDate: Tue, 12 Oct 2021 15:13:09 +030
       
  • Potentially inappropriate medications use and its associated factors among
           geriatric patients: a cross-sectional study based on 2019 Beers Criteria

    • Abstract: Pharmacia 68(4): 789-795
      DOI : 10.3897/pharmacia.68.e73597
      Authors : Heba Khader, Luai Z. Hasoun, Ahmad Alsayed, Mahmoud Abu-Samak : The aims of this study were to estimate the prevalence of potentially inappropriate medications (PIMs) in a community-dwelling Jordanian population of geriatrics according to the 2019 American Geriatrics Society Beers Criteria, to identify the most used PIMs and factors independently associated with PIMs use. This was an observational, descriptive, cross-sectional study. The sample population included 386 participants. Data were collected by face-to-face interviews. A total of 2894 medications were evaluated. The prevalence of patients using at least one PIM was 49.2%. The most used PIMs were proton pump inhibitors (24.6%) and long-acting sulfonylurea (20.5%). Participants who had diabetes mellitus, peptic ulcer, or irritable bowel syndrome had significantly higher numbers of PIMs. The use of PIMs was high in Jordanian geriatric patients. The results of this study might help healthcare providers to detect high-risk patients and reconsider the necessity of using PIMs to decrease the risk of adverse drug events. HTML XML PDF
      PubDate: Fri, 8 Oct 2021 15:42:48 +0300
       
  • Coupling Ifosfamide to nanoemulsion-based clove oil enhances its toxicity
           on malignant breast cancer and cervical cancer cells

    • Abstract: Pharmacia 68(4): 779-787
      DOI : 10.3897/pharmacia.68.e68291
      Authors : Sahar M. AlMotwaa : The anticancer effects of chemotherapeutic agents may be accentuated, and their side effects minimized by combining them with essential oils in nanocarrier systems. This study aimed to incorporate ifosfamide (IF) into nanoemulsion-based clove oil (IF-CLV). The nano-emulsion (NE) formulas were characterized with Zetasizer. The cytotoxicity of the formulated NEs against cervical (HeLa) and breast (MCF-7) cancer cell lines was determined using MTT assay, light microscopy, and DAPI staining. The z – average diameters of NE-CLV and IF-CLV were 63.1±1.00 and 89.4±2.64 nm, while Zeta potential values were – 4.39±0.4 and – 11.65±1.1mV, respectively. Cytotoxicity studies revealed that relative to free IF, NE-CLV and IF-CLV were highly toxic on HeLa and MCF-7cells, in a dose-dependent manner. The half-maximal inhibitory concentration (IC50) values of NE-CLV against HeLa and MCF-7 have decreased 38 and 27 folds, while the corresponding IC50 values of IF-CLV have decreased 57 and 35 folds, respectively. These results suggest that the incorporation of IF into NE-based clove oil produces potent therapeutic effects against cancer cell lines. HTML XML PDF
      PubDate: Fri, 8 Oct 2021 15:39:47 +0300
       
  • Preclinical safety evaluation of drone brood homogenate and justification
           of pharmacological action

    • Abstract: Pharmacia 68(4): 771-777
      DOI : 10.3897/pharmacia.68.e70678
      Authors : Bohdana Pavliuk, Iryna Stechyshyn, Mariana Chubka, Taras Hroshovyi : The problem of studying the metabolic syndrome, as well as its integration into other pathological processes, despite large-scale research, remains relevant. The complexity of the interaction of different links in pathogenesis requires scientists to find new tools and methods for both diagnosis and treatment. Drone brood homogenate, which is a multifactorial pharmacological agent in terms of chemical composition, seems to be promising to study for today. And the lack of contraindications and a wide age range makes it an excellent object of research. The current study evaluated the pharmacological aspects of safety: acute toxicity, effects on the functional and motor activity of the gastrointestinal tract, as well as local irritation of the gastric mucosa, the secretory function of the stomach. All experiments were performed according to the classical methods. The specific pharmacological activity of the drone brood homogenate was determined in comparison with metformin in the experimental fructose metabolic syndrome. Animals obtained from the Vivarium of I.Horbachevsky Ternopil National Medical University were used to implement the set goals. Working with animals was met all bioethical requirements. The study found that the lyophilized drone brood homogenate does not have a local irritant effect and does not cause ulcers on the surface of the gastric mucosa, does not affect the secretory function of the stomach and motor-evacuatory activity of the gastrointestinal tract and is a low-toxic substance, indicating the possibility of its long-term safe use. As expected, glucose, insulin, and HOMA index were significantly increased in animals that were simulated metabolic syndrome. The use of drone brood homogenate by animals contributed to a relatively positive effect on selected indicators of the metabolic syndrome. Accordingly, drone brood homogenate is a promising active pharmaceutical ingredient for the normalization of biochemical disorders in metabolic syndrome. HTML XML PDF
      PubDate: Fri, 8 Oct 2021 08:04:46 +0300
       
  • Rare disease patients’ needs: an up-to-date analysis and future
           directions

    • Abstract: Pharmacia 68(4): 763-770
      DOI : 10.3897/pharmacia.68.e73240
      Authors : Maria Kamusheva, Petya Milushewa : The interest to rare diseases has increased in the recent decades. Legislation seeks to facilitate patients’ access to innovative and effective treatment and to define incentives for pharmaceutical and biotechnology companies to develop new medicines for rare diseases.The current review presents the current knowledge and adopted solutions in the field of rare diseases and discusses the future issues and unmet needs that should be resolved for affected patients and their families. Along with the positive trends in the field of rare diseases, there are still issues related to diagnosis and inequal care for some patients groups that should be solved over the next decade. The innovative digital health methods, which have been improved continuously in the recent years, implementation of improved versions of patient-centered policy plans and programs and investment in advanced therapies could move forward the rare diseases to new horizons giving them the opportunity to overcome the main barriers and challenges in the whole journey of the patients – from diagnosis through treatment to follow-up. HTML XML PDF
      PubDate: Wed, 6 Oct 2021 15:17:02 +0300
       
  • Preliminary in vitro study of anti-oxidant activity and anti-diabetic
           potential of plant extracts from 4 herbal substances not traditionally
           used for treatment of diabetes mellitus

    • Abstract: Pharmacia 68(4): 755-762
      DOI : 10.3897/pharmacia.68.e72769
      Authors : Dora Trifonova, Anna Gavrilova, Galina Dyakova, Genadi Gavrilov, Maya Yotova, Stefan Nikolov : The focus of the presented study is the in vitro anti-oxidant activity and anti-diabetic potential of water extracts from the following four herbal substances, not traditionally used for treatment of diabetes mellitus – leaves of Sambucus ebulus L. and Prunus mahaleb L., and flowering stems of Cichorium intybus L. and Satureja kitaibelii Wierzb. ex Heuff. The water extracts are obtained through ultrasonication. The extract of S. kitaibelii stands out due to its highest values in all studied indicators – total phenolic content, scavenging potential (DPPH, ABTS) and α-glucosidase inhibitory activity which was six times higher than acarbose. The extract of C. intybus also showed significant α-glucosidase inhibitory activity compared to acarbose. The flowering stems of both species are promising sources of biologically active substances for blood sugar control in diabetes mellitus. HTML XML PDF
      PubDate: Tue, 5 Oct 2021 09:14:57 +0300
       
  • Frequency of CYP1A1*2A polymorphisms and deletion of the GSMT1 gene in a
           Peruvian mestizo population

    • Abstract: Pharmacia 68(4): 747-754
      DOI : 10.3897/pharmacia.68.e71621
      Authors : Angel Tito Alvarado, Ana María Muñoz, María Saravia Bartra, Milton Valderrama-Wong, Daniela González, Luis Abel Quiñones, Nelson Varela, María Rocío Bendezú, Jorge Antonio García, Berta Loja-Herrera : The polymorphic variants of CYP1A1 and the deletion of GSTM1 are present in the Peruvian mestizo population. Wild type and mutated genotypes (WT/*2A and *2A/ *2A) were identified, whose allele frequencies are 0.31 (T allele) and 0.69 (C allele), respectively; 53% with wild type GSTM1 (+) and 47% with null GSTM1. The frequency in Iquiteño emigrants was 0.72 CYP1A1*2A and 25% GSTM1 (-); from Lima 0.67 CYP1A1*2A and 33% of GSTM1 (-). The Hardy-Weinberg equilibrium test for the studied population showed that both frequencies are out of balance, p > .05. The presence of the risk allele of the CYP1A1*2A polymorphism and the deletion in the GSTM1 gene are high, which could be indicative of a phase I and II metabolic imbalance in this group of Peruvian populations, with potential risks of activating agents procarcinogens thus affecting the incidence of tumor pathologies with an environmental component. HTML XML PDF
      PubDate: Tue, 5 Oct 2021 09:14:19 +0300
       
  • Comparative evaluation of cystatin C and neutrophil gelatinase-associated
           lipocalin in patients with thalassemia major versus thalassemia intermedia
           

    • Abstract: Pharmacia 68(4): 741-746
      DOI : 10.3897/pharmacia.68.e71475
      Authors : Marwa Mohammed, Jehan Mohammad, Zainab Fathi, Muzahim Al-Hamdany, Nasih Alkazzaz : Kidney disorders are long-term complications in thalassemia patients, especially with the high life expectancy of these patients. Proper evaluation of kidney impairment in β-thalassemia patients can be difficult due to higher intake of iron chelators, resulting in renal impairment. Early biomarkers of renal disease are used for the diagnosis of tubular and glomerular abnormalities. The current study was conducted on 88 individuals, 25 healthy people and 63 β-thalassemia patients. Circulating levels of urea, creatinine, cystatin C and neutrophil gelatinase-associated lipocalin were measured in all groups. Compared to healthy control, patients with thalassemia major and intermedia showed a significant increase in both cystatin C and NGAL levels, with no effects on creatinine levels. Furthermore, urea levels were markedly higher in patients with thalassemia major compared to control. As early renal dysfunction markers, cystatin C and NGAL should be routinely evaluated in thalassemia patients major and intermedia. HTML XML PDF
      PubDate: Mon, 4 Oct 2021 10:08:47 +0300
       
  • Quantitative analysis of biologically active substances and the
           investigation of antioxidant and antimicrobial activities of some extracts
           of Osage orange fruits

    • Abstract: Pharmacia 68(4): 731-739
      DOI : 10.3897/pharmacia.68.e70180
      Authors : Ani Slavik Dadayan, Lala Ashot Stepanyan, Tatevik Hovhannes Sargsyan, Anahit Mkhitar Hovhannisyan, Slavik Arshak Dadayan : Biologically active substances, the antioxidant and antimicrobial activity of aqueous, 70% ethylate and ethyl acetate extracts of fruits of maclura orange (Osage Orange), a representative of the Moraceae genus growing in the Ararat region of Armenia have been studied. It is found that plant extracts are rich in a wide range of pharmacologically active substances, in particular, tannins, flavonoids, organic acids, vitamins, anthocyanins, micro- and microelements, etc. Based on the investigations performed, extracts of maclura orange can be recommended as a source of biologically active substances (BAS), as well as a preventive and corrective agent in deficiency or imbalance of macro- and microelements in tissue and cellular structures in various pathological processes in the body. An ethanol extract of maclura fruits exhibits the antimicrobial activity against Bacillus subtilis 1820, E. Coli 5002, Serratia marcescens 5251 and Staphylococcus aureus ATCC-6538 strains. Maclura extracts can be used as an environmentally friendly source of antioxidants against early aging. HTML XML PDF
      PubDate: Fri, 1 Oct 2021 14:08:17 +0300
       
  • Analysis of carbohydrates content in the plant components of antidiabetic
           herbal mixture by GC-MS

    • Abstract: Pharmacia 68(4): 721-730
      DOI : 10.3897/pharmacia.68.e69107
      Authors : Alona Savych, Maryna Duchenko, Yulia Shepeta, Alexandra Davidenko, Olha Polonets : Medicinal plants and their combinations due to the wide range of biologically active substances can influence on various links of the pathogenetic mechanism of development of diabetes mellitus and its complications. One of such combinations is an antidiabetic herbal mixture (Urticae folia, Rosae frucrus, Myrtilli folia, Menthae folia and Taraxaci radices) with established hypoglycemic, hypolipidemic, antioxidant, hepatoprotective, pancreatoprotective activity in previous pharmacological study in vivo. Thus, the aim of this study was to identify and establish the content of carbohydrates in free and bound form in the plant components of antidiabetic herbal mixture. The carbohydrates were separated by gas chromatography-mass spectrometry after conversion into volatile derivatives as aldononitrile acetate. The monomeric composition of polysaccharides was studied after their hydrolysis to form monosaccharides and polyalcohols. The results of the quantitative study showed that the predominant carbohydrate in free form was saccharose in Urticae folia, L-fructose in Myrtilli folia, Rosae frucrus, Taraxaci radices and Menthae folia, L-glucose in Rosae frucrus. Concerning the determination of monomers of polysaccharides after hydrolysis, L-glucose prevailed in all plant components of antidiabetic herbal mixture. The chromatographic study revealed a number of polyalcohols that are important for the treatment and prevention of progression of diabetes mellitus and its complications, namely, mannitol and myo-inositol. HTML XML PDF
      PubDate: Fri, 1 Oct 2021 08:07:35 +0300
       
  • COVID-19 pandemic impact on the pharmaceutical sector in Bulgaria

    • Abstract: Pharmacia 68(3): 713-720
      DOI : 10.3897/pharmacia.68.e71638
      Authors : Veselina Ivanova, Deyan Pavlov, Tolya Assenova, Emily Terzieva, Petya Milushewa, Alime Djemadan, Gergana Vladimirova, Maria Dimitrova, Maria Kamusheva : In December, 2019 in Wuhan, Hubei Province, China, a new, unknown strain of coronavirus called SARS-CoV-2 was identified. The virus has spread rapidly to other countries around the world, among which the most affected were Italy, Spain and the United States. As a result, in March 2020 The WHO has declared the new coronavirus epidemic a global pandemic. Despite timely measures and efforts to reduce morbidity, up to date, confirmed cases are 119,452,269, while the number of deaths reached 2,647,662 people. The COVID-19 pandemic has affected all areas of human life – health, social, economic. In each of them, a number of restrictions and obligations were imposed, including wearing of masks, use of disinfectants, education in an online environment, limited work in restaurants and shops. The health sector was particularly affected, and all actors in the pharmaceutical system had to reorganize and adapt their activities in the name of a common goal – ending the COVID-19 pandemic. HTML XML PDF
      PubDate: Wed, 15 Sep 2021 11:22:05 +030
       
  • Evaluation the effects of insulin on oxidant/antioxidant status in type 1
           diabetic patients

    • Abstract: Pharmacia 68(3): 699-704
      DOI : 10.3897/pharmacia.68.e70495
      Authors : Ammar A. Y. Almulathanon, Jehan A. Mohammad, Thikra Ali Allwash : Earlier works have revealed increased generation of reactive oxygen species (ROS) and decreased antioxidant levels in type 1 diabetes mellitus (T1DM). The current study aimed to investigate the effect of mixed insulin therapy on oxidative stress and antioxidant status in patients with T1DM. This study involved 75 participants who were divided into three groups: 20 healthy subjects as a control, 25 newly diagnosed patients with T1DM (without treatment) and 30 patients with T1DM treated with insulin (regular and Human Neutral Protamine Hagedorn (NPH)) twice daily. Fasting serum glucose (FSG), serum concentrations of insulin, malondialdehyde (MDA), catalase (CAT), reduced glutathione (GSH), and vitamins (C and E) were measured in all participants. Compared with the healthy control, serum glucose and MDA concentrations were observed to be significantly higher, while significantly lower concentrations of CAT, GSH, and vitamins (C and E) were found in both the treated and untreated diabetic groups. Although insulin therapy caused a significant decrease in blood sugar with a marked elevation in the levels of insulin, CAT, GSH and vitamin E compared to the untreated patients, the changes in the levels of MDA and vitamin C between diabetic groups were not significant. Moreover, the level of insulin resistance was significantly increased in insulin-treated patients as compared to the control and untreated diabetic groups. In conclusion, twice daily treatment with regular and NPH insulin can ameliorate hyperglycemia and improve antioxidant levels in patients with T1DM. However, the insulin regimen used in this study did not reveal a beneficial effect on oxidative stress and insulin resistance. Hence, exogenous antioxidants (vitamins C and E) can be used in combination with insulin to control these parameters. HTML XML PDF
      PubDate: Fri, 10 Sep 2021 18:07:52 +030
       
  • Effect of lisinopril therapy on serum leptin, oxidative stress and
           C-reactive protein in hypertensive patients

    • Abstract: Pharmacia 68(3): 705-711
      DOI : 10.3897/pharmacia.68.e73140
      Authors : Zeina A. Althanoon, Isam H. Mahmood : The pathogenesis of essential hypertension through the interaction with elements of the rennin angiotensin aldosterone system is affected by oxidative stress and inflammation. The present study aimed to assess the effects of ACE-Inhibitor, lisinopril, on blood pressure, lipid profiles (total cholesterol, triglycerides, LDL and HDL), MDA, and TAS, hsCRP, and serum leptin levels n hypertensive patients. A case control study included 100 newly diagnosed mild to moderate hypertensive patients and another 100 apparently healthy aged and sex matched subjects as controls. The patients were treated with 10 mg lisinopril orally per day for three months’ duration. Venous blood sample was taken to test levels of MDA, GSH and TAS, hsCRP, lipid profiles and leptin in the serum before and after lisinopril therapy for both patients and controls. Systolic and diastolic blood pressure were also assessed before and after lisinopril therapy for both patients and controls. In hypertensive patients treated with lisinopril, markers of oxidative stress (MDA, TAS and GSH), high sensitive C-reactive protein and leptin were all found to be decreased significantly after drug treatment (p < 0.01). Lisinopril affectively lowered systolic and diastolic BP values (p < 0.01). A significant decrease in lipid profile (p < 0.01) with a significant increase in HDL-C and TAS levels (p < 0.01) were found in lisinopril treated group in comparison with their values before treatment. Lisinopril may be used as a treatment for high blood pressure, as well as for the insulin resistance, hyperleptinemic, and low-grade inflammatory states that are associated with the disease. HTML XML PDF
      PubDate: Fri, 10 Sep 2021 11:57:10 +030
       
  • The role of resistin and its relation to other pathogenetic factors of the
           chronic kidney disease development

    • Abstract: Pharmacia 68(3): 693-698
      DOI : 10.3897/pharmacia.68.e70680
      Authors : Nataliia Gubina, Irina Kupnovytska, Vasil Mishchuk, Nataliia Hladka : Chronic kidney disease (CKD) is the leading cause of death from non-communicable diseases, and its prevalence in 2017 ranged from 8.5 to 9.8%. Depending on the stage of CKD, stage 1 was diagnosed in 3.5%, stage 2 in 3.2% and stage 3 in 7.6%, while stages 4 and 5 took place in 0.4 and 0.1% of the world’s population respectively. Obesity also contributes to the increase in the prevalence and severity of CKD, and their combination occurs in 3.1% of patients. Kidney damage and their structural and functional changes in patients with obesity are associated with high metabolic activity of adipose tissue, due to the synthesis of adipocytokines, including resistin. The purpose of the work: to study changes of resistin level in the blood in patients with early stages of chronic kidney disease, its relation to the level of endothelin, markers of lipid metabolism and inflammation. Materials and methods: 70 patients with stage 1 and 88 patients with stage 2 of CKD with different stages of obesity were examined. Glomerular filtration rate (GFR) was calculated by the formula CKD-EPI based on creatinine, cystatin C and their combination (CKD-EPIcysC / cr). The levels of cystatin C, resistin, tumor necrosis factor-alpha (TNF-α) and endothelin-1 were determined by enzyme-linked immunosorbent assay. Determination of total cholesterol and low-density lipoprotein cholesterol levels in the blood serum was performed by colorimetric method. Statistical analysis of the results was performed with the help of Statistica 6.0 statistical software package using Student’s t-test and Spearman’s rank correlation coefficient. Results: an increase of the resistin level in the blood by 1.3 times in the patients with stage 1 CKD and by 1.6 times in the patients with stage 2 CKD and obesity was determined (p1.2 < 0.05), and there was a weak correlation between its concentration in the blood and body mass index. A significant average negative correlation between resistin and GFR was detected. Increased serum resistin level correlates with increased TNF-α. In patients of both groups, the level of resistin and LDL increases simultaneously, and the correlation between them increases as CKD progresses. Similar changes are observed with respect to increasing concentrations of resistin and endothelin-1. Thus, an increase of resistin level in the blood in patients with the early stages of CKD initiates a number of pathological changes, such as systemic inflammation, hyperlipidemia and endothelial dysfunction. HTML XML PDF
      PubDate: Wed, 8 Sep 2021 11:56:44 +0300
       
  • A novel derivative of picolinic acid induces endoplasmic reticulum
           stress-mediated apoptosis in human non-small cell lung cancer cells:
           synthesis, docking study, and anticancer activity

    • Abstract: Pharmacia 68(3): 679-692
      DOI : 10.3897/pharmacia.68.e70654
      Authors : Ali H. Abbas, Ammar A. Razzak Mahmood, Lubna H. Tahtamouni, Zainab A. Al-Mazaydeh, Majdoleen S. Rammaha, Fatima Alsoubani, Rheda I. Al-bayati : Thirteen new derivatives of picolinic acid (4–7) were designed and synthesized from the starting parent molecule, picolinic acid. The new compounds were characterized by ATR-FTIR, 1HNMR, and CHNS analysis. A molecular docking study was performed to evaluate the binding affinity of the synthesized compounds toward EGFR kinase domain that indicated occupation of the critical site of EGFR kinase pocket and excellent positioning of the compounds in the pocket. The cytotoxic activity of the compounds against two human cancer cell lines (A549 and MCF-7), the non-tumorigenic MCF10A cell line, and white blood cells (WBC) was evaluated using the MTT assay. Compound 5 showed anticancer activity against A549 lung cancer cells (IC50 = 99.93 µM) but not against MCF-7 breast cancer cells or normal cells. Compound 5 mediated cytotoxicity in A549 lung cancer cells by inducing apoptotic cell death, as suggested by fragmented nuclei after DAPI staining, and agarose gel electrophoresis. Moreover, compound 5 triggered the activation of caspases 3, 4 and 9. However, compound 5 treatment did not affect the release of cytochrome c from the mitochondria to the cytosol, as compared to the vehicle-treated control cells. Nevertheless, compound 5-treated cells reported greater release of smac/DIABLO to the cytosol. In the same context, both compound 5 and thapsigargin (specific inhibitor of sarco/endoplasmic reticulum Ca2+-ATPase (SERCA)) enhanced eIF2 phosphorylation, reflecting the activation of the atypical ER stress pathway and the potential applicability of compound 5 in lung cancer treatment. HTML XML PDF
      PubDate: Wed, 8 Sep 2021 11:56:30 +0300
       
  • Dermatitis in community pharmacies: a survey on italian pharmacists’
           management and implications on corticophobia

    • Abstract: Pharmacia 68(3): 671-677
      DOI : 10.3897/pharmacia.68.e70452
      Authors : Corrado Giua, Nicolina P. Floris, Michele Schlich, Enrico Keber, Carlo Gelmetti : Community pharmacists represent an important resource for the promotion of a safer and more effective self-management of common skin diseases, as well as the provision of educational support on therapies prescribed by clinicians, ultimately improving patients’ adherence. In this study, a semi-structured survey was administered to 154 Italian community pharmacists, in order to acquire information on their counseling activity on dermatological disorders. Collected data provide an overview on the frequency and methodology of counseling offered in Italian community pharmacies, identifying knowledge gaps and misbeliefs. In particular, an overall negative opinion on topical corticosteroid therapy emerged among pharmacists, unveiling a phenomenon previously described as corticophobia. Starting from this observation, we discuss the risks for patients’ adherence, associated with corticophobia among pharmacists. Lastly, we briefly report on the main tools desired by pharmacists to improve their education on dermatology, envisioning their implementation with the aim of a more effective counseling. HTML XML PDF
      PubDate: Wed, 8 Sep 2021 11:55:10 +0300
       
  • The effect of intranasal administration of an IL-1b antagonist (RAIL) on
           the state of the nitroxydergic system of the brain during modeling of
           acute cerebrovascular accident

    • Abstract: Pharmacia 68(3): 665-670
      DOI : 10.3897/pharmacia.68.e71243
      Authors : Bogdan S. Burlaka, Igor F. Belenichev, Olga I. Ryzhenko, Victor P. Ryzhenko, Olena G. Aliyeva, Lyudmyla V. Makyeyeva, Olena O. Popazova, Pavlo G. Bak : Introduction: This study was designed to evaluate the effect activity of RAIL-gel in comparison with Citicoline on nitroxydergic system during acute cerebrovascular accident. Methods: In this study, 80 white nonlinear rats were randomly assigned to 4 groups (20 rats in each): 1) intact; 2) control - untreated with acute cerebrovascular accident (ACVA), examined on the 4th day; 3) animals with ACVA, receiving RAIL, examined on the 18th day; 4) animals with ACVA, treated with Citicoline, examined on the 4th day. The expression of inducible NOS was determined by Western blotting. The nitrosative stress marker, nitrotyrosine, was determined using the ELISE kit NITROTYROSINE (kit no. HK501-02, series 12825k1212-k). To assess the state of iNOS mRNA expression, we used the method of polymerase chain reaction with reverse transcription in real time (RT-PCR). Results: Our research demonstrated that course administration of the RAIL and Citicoline to animals with ACVA for 4 days leads to the stabilization of the parameters of the brain nitroxydergic system. However, Citicoline does not provide a full effect on the shifts of the NO system in the brain. It does not have the proper effect on such an important link in the pathogenesis of ischemic brain damage as nitrosative stress. RAIL leads to a significant decrease in NOS activity due to its inducible form (decrease in the expression of iNOS and iNOS mRNA) and a decrease in NO metabolits, and inhibition of nitrosative stress (decrease in nitrotyrosine). Conclusion: IL-1b antagonist RAIL (Intranal Gel) significantly exceeds Citicoline in terms of the severity of the effect on the nitroxydergic system indicators. HTML XML PDF
      PubDate: Wed, 8 Sep 2021 11:54:38 +0300
       
  • Simultaneous quantification of the major flavonoids from wild spinach by
           UHPLC-HRMS and their neuroprotective effects in a model of H2O2-induced
           oxidative stress on SH-SY5Y cells

    • Abstract: Pharmacia 68(3): 657-664
      DOI : 10.3897/pharmacia.68.e71030
      Authors : Zlatina Kokanova-Nedialkova, Denitsa Aluani, Virginia Tzankova, Paraskev Nedialkov : A modified UHPLC-HRMS method for simultaneous quantification of eight flavonoids from the aerial parts of the wild spinach (Chenopodium bonus-henricus L.) was re-validated for specificity, the limit of detection and quantitation limit, linearity, accuracy, and precision. The glycosides of spinacetin (Chbhnf-04, Chbhnf-06, and Chbhnf-08) and patuletin (Chbhnf-01) were the predominant compounds. The total amount of assayed flavonoids from the aerial parts of a title plant was estimated to be 1.82% and 1.4% in two different populations from Vitosha Mountain (Bulgaria). The neuroprotective properties of compounds Chbhnf-02, Chbhnf-04, Chbhnf-06, Chbhnf-07, Chbhnf-08 were further assessed using a model of H2O2-induced oxidative stress on human neuroblastoma SH-SY5Y cells. All tested flavonoids demonstrated statistically significant neuroprotective activity close to that of silibinin. Patuletin (Chbhnf-07) and spinacetin (Chbhnf-08) triglycosides showed the most protective effects at the lowest concentration of 50 µM. HTML XML PDF
      PubDate: Wed, 8 Sep 2021 11:53:55 +0300
       
  • The impact of chirality on the analysis of alkaloids in plant

    • Abstract: Pharmacia 68(3): 643-656
      DOI : 10.3897/pharmacia.68.e71101
      Authors : Ngoc-Van Thi Nguyen, Kim-Ngan Huynh Nguyen, Kien Trung Nguyen, Kyeong Ho Kim, Hassan Y. Aboul-Enein : Most of the alkaloids are chiral compounds and are clinically administered as the racemic mixture, even though its enantiomers have been known to exert different pharmacological activity. The determination of the enantiomeric composition of alkaloid-containing plants is subject to severe attention from pharmacological and toxicological points of view. This review gives an overview of the chiral analysis of alkaloids that were used in theoretical studies and applications for plants in recent years. HTML XML PDF
      PubDate: Tue, 7 Sep 2021 11:54:20 +0300
       
  • Biomarkers of iron status in allopurinol-treated renal stone patients

    • Abstract: Pharmacia 68(3): 633-642
      DOI : 10.3897/pharmacia.68.e70275
      Authors : Adnan A. Zainal, Ibrahim M. Faisal, Abdulla A. Ahmad : Limited evidence exists on the effect of xanthine oxidase inhibitors in nephrolithiasis patients on iron status markers, beyond their effects on urate. The aim of this study was to investigate whether allopurinol therapy was associated with a significant impact on parameters related to iron status, in patients with renal stones. Allopurinol treatment was associated with a nonsignificant decline in serum uric acid. There were no significant differences in serum levels of transferrin and ferritin after treatment with allopurinol compared to pre-treatment levels. A non-significant fall in serum levels of haptoglobin was registered. The drug was associated with a significant rise in serum iron levels. Serum uric acid and iron did not show a significant correlation with any parameter in the study. Allopurinol exerted an overall non-significant effect on iron metabolism in nephrolithiasis patients, save for serum iron, this entails lack of untoward effects in populations with-iron related conditions. HTML XML PDF
      PubDate: Tue, 7 Sep 2021 11:53:40 +0300
       
  • Effects of flavonol quercetin on syndrome of endogenous intoxication in
           experimental periodontitis

    • Abstract: Pharmacia 68(3): 627-632
      DOI : 10.3897/pharmacia.68.e67341
      Authors : Andrii Demkovych, Vitaliy Shcherba, Olha Yaremchuk, Halyna Stoikevych, Volodymyr Machogan, Vitalii Luchynskyi : The article presents the results of study effect of quercetin on the indicators of endogenous intoxication syndrome under conditions of experimental periodontitis. One of the key links in the pathogenesis of any inflammatory disease, including maxillofacial area, is endogenous intoxication, an important pathophysiological mechanism of which is the activation of lipid peroxidation. The experimental animals were treated by intramuscular injections with water-soluble quercetin for 7 days. For further research the blood serum was selected in which was determined the content of middle molecular weight molecules and erythrocyte intoxication index. Excessive lipoperoxidation was accompanied by accumulation of peroxidation products and depletion of antioxidant reserves, which led to accumulation of toxic substances. That is why the study of the level of middle molecular weight molecules and erythrocyte intoxication index in simulated bacterial-immune periodontitis is a reliable criterion. Quercetin was able to reduce the expression of endogenous intoxication syndrome in experimental bacterial-immune periodontitis. HTML XML PDF
      PubDate: Tue, 24 Aug 2021 11:51:48 +030
       
  • Pharmacists’ strategies to detect, resolve, and prevent DRPs in CKD
           patients

    • Abstract: Pharmacia 68(3): 619-626
      DOI : 10.3897/pharmacia.68.e65136
      Authors : Ni Made Susilawati, Eli Halimah, Siti Saidah : Pharmacists have undergone obstacles in the process of detecting, resolving, and preventing CKD patients’ DRPs. Thus, optimal strategies were needed. A total of 19 articles were included based on the article searching process. Based on the articles, it can be concluded: The strategies of detecting DRPs in CKD patients were carried out through medication reconciliation and medication review. The outcomes of these strategies were the number of DRPs/patients and types of DRPs detected. Strategies to resolve and prevent DRPs in CKD patients were conducted through interprofessional collaboration, education, and counselling. The outcome of these strategies was a change in the patients’ DRPs status. Optimization of detection, resolution, and prevention strategies were performed by improving pharmacists’ professional hard and soft-skills as well as modifying the pharmaceutical care delivery model. A decrease in the number of DRPs/patients and a change in DRPs status were reported as the outcomes of optimizing this process. HTML XML PDF
      PubDate: Mon, 23 Aug 2021 10:43:17 +030
       
  • Effect of esomeprazole on lipid profile in patients with peptic ulcer

    • Abstract: Pharmacia 68(3): 613-617
      DOI : 10.3897/pharmacia.68.e70292
      Authors : Eman Abdullah, Sarraa Dhiaa, Khalaf Saleh, Marwan Merkhan : Esomeprazole; a newly introduced PPI has been widely prescribed by healthcare providers due to its improved pharmacokinetic profile. Most users could have other diseases and the PPIs are indicated as acid-suppressor to minimize gastric side effects of polypharmacy. A high percentage of users could suffer from cardiovascular diseases and lipid dysmetabolism. Hence, this study was designed to determine the impact of long-term use of esomeprazole on lipid profile in a normal subject other than having peptic ulcer for which esomeprazole has been indicated. Results confirmed that esomeprazole reduced triglyceride and HDL levels and elevated total cholesterol level and correspondingly LDL level was elevated, however, no effect was noticed with VLDL. To sum up, esomeprazole impaired lipid metabolism in apparently normal healthy individuals apart from having peptic ulcer for which the esomeprazole was indicated, this finding rise a caution during prescribing esomeprazole for the patient with multiple diseases and polypharmacy including cardiovascular ailments. HTML XML PDF
      PubDate: Tue, 17 Aug 2021 10:57:52 +030
       
  • Commodity analysis of compression products for varicose veins

    • Abstract: Pharmacia 68(3): 607-611
      DOI : 10.3897/pharmacia.68.e67587
      Authors : Tetiana Diadiun, Inna Baranova, Svitlana Kovalenko, Rymma Yeromenko, Mykola Rybalkin : Compression therapy occupies a key place in the complex treatment and prevention of chronic venous insufficiency of the lower extremities. Today the pharmaceutical market of Ukraine is represented by a wide range of compression products. Popular in Ukraine are manufacturers of compression products from the Baltic region, Ukraine, there are also Russian, but leading in quality are Germany, USA, and Italy. A survey of consumers and pharmacy practitioners has been performed. The results obtained indicate that compression products for varicose veins treatment are inferior to medicinal products in sales. The main motive for buying a compression product is a doctor’s prescription. The most popular compression garments are stockings. HTML XML PDF
      PubDate: Mon, 9 Aug 2021 12:12:36 +0300
       
 
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