 Subjects -> PHARMACY AND PHARMACOLOGY (Total: 575 journals)
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- Sci. Pharm., Vol. 91, Pages 29: Escherichia coli (Lilly) and Saccharomyces
cerevisiae (Novo) rDNA Glucagon: An Assessment of Their Actions When
Supplied Selectively to Periportal Cells in the Bivascularly Perfused Rat
Liver
Authors: Lívia Bracht, Jorgete Constantin, Rosane Marina Peralta, Adelar Bracht
First page: 29
Abstract: The actions of Eli Lilly-rDNA glucagon and Novo Nordisk-rDNA glucagon on glycogen catabolism and related parameters were investigated using the bivascularly perfused rat liver. The technique allows glucagon to be supplied to a selective portion of the hepatic periportal region (≈39%) when the former is infused into the hepatic artery in retrograde perfusion. Both glucagon preparations were equally effective in influencing metabolism (glucose output, glycolysis and O2 uptake) when supplied to all cells along the liver sinusoids. When only a selective periportal region of the liver was supplied with the hormone, however, the action of Novo Nordisk-rDNA glucagon was proportional to the accessible cell space, whereas the action of Eli Lilly-rDNA glucagon greatly exceeded the action that was expected for the accessible space. Chromatographically, both rDNA preparations were not pure, but their impurities were not the same. The impurities in Eli Lilly-rDNA glucagon resembled those found in the similarly acting pancreatic Eli Lilly glucagon. It was concluded that the space-extrapolating action of Eli Lilly-rDNA glucagon is caused by a yet-to-be-identified impurity. The hypothesis was raised that an impurity in certain glucagon preparations can enhance cell-to-cell propagation of the glucagon signal, possibly via gap junctional communication.
Citation: Scientia Pharmaceutica
PubDate: 2023-06-24
DOI: 10.3390/scipharm91030029
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 30: Impact of Compressional Force,
Croscarmellose Sodium, and Microcrystalline Cellulose on Black Pepper
Extract Tablet Properties Based on Design of Experiments Approach
Authors: Chaowalit Monton, Thaniya Wunnakup, Jirapornchai Suksaeree, Laksana Charoenchai, Natawat Chankana
First page: 30
Abstract: This study aimed to prepare tablets of black pepper extract using the Design of Experiments (DOE) approach. The levels of three factors—compressional force, croscarmellose sodium (CCS), and microcrystalline cellulose (MCC)—were screened using the one-factor-at-a-time technique, followed by the DOE utilizing the Box–Behnken design. The respective variations for each factor were as follows: compressional force (1500–2500 psi), CCS (1–3%), and MCC (32–42%). The results indicated that compressional force significantly decreased tablet thickness and friability, while increasing hardness and prolonging disintegration time. CCS significantly shortened disintegration time but did not affect tablet thickness, hardness, and friability. MCC, on the other hand, significantly increased tablet thickness and hardness, while significantly decreasing friability. Furthermore, the study observed interactions among factors and quadratic effects of each factor, which significantly influenced tablet properties. The optimal tablet formulation consisted of 2.2% CCS, 37% MCC, and a compressional force of 2000 psi. These tablets had a weight of 198.39 ± 0.49 mg, a diameter of 9.67 ± 0.01 mm, a thickness of 1.98 ± 0.02 mm, a hardness of 7.36 ± 0.24 kP, a friability of 0.11 ± 0.02%, and a disintegration time of 5.59 ± 0.39 min. The actual values obtained using the optimal conditions closely matched the predicted values, with a low percent error (less than 5%). In conclusion, the application of the DOE approach successfully developed tablets of black pepper extract, which can be utilized as food supplement products.
Citation: Scientia Pharmaceutica
PubDate: 2023-06-27
DOI: 10.3390/scipharm91030030
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 31: Analytical Investigation of Forced
Oxidized Anti-VEGF IgG Molecules: A Focus on the Alterations in Antigen
and Receptor Binding Activities
Authors: Ayhan Parlar, Busra Gurel, Mehmet Reşit Sönmez, Meral Yüce
First page: 31
Abstract: Alterations in the biological activity of the molecules under stress conditions have not been documented as widely in the literature yet. This study was designed to reveal the functional impacts of various oxidation conditions on a model mAb, a commercial anti-VEGF IgG molecule. The responses to antigen binding, cell proliferation, FcRn receptors, and C1q binding, which rarely appear in the current literature, were investigated. The authors report peptide mapping data, post-translational modification (PTM) analysis, cell proliferation performance, and antigen (VEGF), C1q, and FcRn binding activities of the mAb under various stress conditions. The oxidation-prone site of the mAb was determined as Met252 in the DTLMISR peptide. The VEGF binding activity and anti-cell proliferation activity of the mAbs did not alter, while C1q and FcRn binding capacity significantly decreased under oxidative stress conditions. The full report is vital for many scientific and industrial processes about mAbs. The authors recommend performing functional analyses in addition to the structural studies while investigating the impacts of stress factors on therapeutic mAbs.
Citation: Scientia Pharmaceutica
PubDate: 2023-06-28
DOI: 10.3390/scipharm91030031
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 32: Structural Aspect of
Hydroxyethyl-Starch–Anticancer-Drug-Conjugates as State-of-the-Art
Drug Carriers
Authors: Koushik Chandra, Sansa Dutta, Haradhan Kolya, Chun-Won Kang
First page: 32
Abstract: Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, target-oriented drug-delivery systems (DDS) or pulsatile drug-delivery systems (PDDS) have recently been developed as an alternative tool that takes care of the entire pharmacodynamic activities of drug action. Hydroxyethyl starch (HES) has emerged as an effective clinical tool for delivering anticancer agents into target cells. These systems have demonstrated significant potential as anticancer drug carrier conjugates through their innate pharmacokinetic properties with their safety profile. This review focuses primarily on the structural aspect during the use of HES or HES-based polymers as carriers for delivering well-known anticancer drugs. This review also indicates a perspective on the long-term research needed for the sake of improving modern drug-delivery systems based on HES polymers and in the form of nanocarriers.
Citation: Scientia Pharmaceutica
PubDate: 2023-06-29
DOI: 10.3390/scipharm91030032
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 33: Chromobacterium Violaceum: A Model for
Evaluating the Anti-Quorum Sensing Activities of Plant Substances
Authors: Petya D. Dimitrova, Tsvetozara Damyanova, Tsvetelina Paunova-Krasteva
First page: 33
Abstract: In the new antibiotic era, the exponential increase in multiresistant bacterial strains has become the main global health problem. Many researchers have focused their efforts on exploring novel or combined strategies for combating bacterial resistance. Good knowledge of the molecular mechanisms of resistance and bacterial virulence factors as key targets provides us with a good basis for resolving the problem. One particularly attractive and promising strategy is to attack the main regulatory “network” of bacterial virulence determinants known as quorum sensing (QS). The inhibition of QS signals will be a novel means of screening more effective quorum-sensing inhibitors (QSIs) and will play a key role in the use of next-generation antimicrobials in the battle against resistance. This motivated the present review to provide a comprehensive clarification of the regulatory mechanisms of quorum-sensing signaling pathways in Chromobacterium violaceum and the discovery of potential plant quorum-sensing inhibitors.
Citation: Scientia Pharmaceutica
PubDate: 2023-07-03
DOI: 10.3390/scipharm91030033
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 34: In Vitro Cytotoxicity and Antioxidant
Studies of Dovyallis caffra-Mediated Cassiterite (SnO2) Nanoparticles
Authors: Jerry O. Adeyemi
First page: 34
Abstract: Many medicinal plants found in Africa, such as Dovyallis caffra, have been reported to contain various bioactive compounds, which have been found to reduce metal salts into their corresponding metal-based nanoparticles. In this paper, the evaluation of synthesis, characterization, and biological properties of Dovyallis caffra-mediated cassiterite (SnO2) nanoparticles was carried out. The physicochemical properties of the synthesized material were investigated using X-ray diffraction (XRD), energy dispersive X-ray analysis (EDX), scanning electron microscopy (SEM), and transmission electron microscopy (TEM) techniques. The characterization studies revealed that the material possessed a single tetragonal cassiterite SnO2 phase, having a cluster-like foam appearance and an irregular spherical morphology with diameters ranging from 6.57 to 34.03 nm. The biological screening revealed that the prepared cassiterite (SnO2) nanoparticles exhibited cytotoxicity against the MCF-7 breast cancer cells, with an IC50 value of 62.33 µg mL−1, better than the standard drug 5-fluorouracil, with an IC50 value of 71.21 µg mL−1. The radical scavenging potential of the nanoparticles, using the DPPH assay, showed that it possessed a slightly better activity than ascorbic acid, a common antioxidant. These results suggest that the Dovyallis caffra-mediated cassiterite (SnO2) nanoparticles possess the potential to simultaneously generate and scavenge excess ROS, which in turn results in the exhibition of good cytotoxicity and antioxidant properties.
Citation: Scientia Pharmaceutica
PubDate: 2023-07-07
DOI: 10.3390/scipharm91030034
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 35: Adjuvant Oligonucleotide Vaccine Increases
Survival and Improves Lung Tissue Condition of B6.Cg-Tg (K18-ACE2)2
Transgenic Mice
Authors: Volodymyr V. Oberemok, Kateryna V. Laikova, Kseniya A. Yurchenko, Ilya A. Novikov, Tatyana P. Makalish, Anatolii V. Kubyshkin, Oksana A. Andreeva, Anastasiya I. Bilyk
First page: 35
Abstract: The main problem in creating anti-coronavirus vaccines that target mainly proteins of the outer membrane of the virus is the rapid variability in the RNA genome of the pathogen that encodes these proteins. In addition, the introduction of technologies that can affordably and quickly produce flexible vaccine formulas that easily adapt to the emergence of new subtypes of SARS-CoV-2 is required. Universal adjuvant oligonucleotide vaccines based on conserved regions of the SARS-CoV-2 genome can take into account the dynamics of rapid changes in the virus genome, as well as be easily synthesized on automatic DNA synthesizers in large quantities in a short time. In this brief report, the effectiveness of four phosphorothioate constructs of the La-S-so-type adjuvant oligonucleotide vaccine is evaluated on B6.Cg-Tg (K18-ACE2)2 transgenic mice for the first time. In our primary trials, the oligonucleotide vaccine increased the survival rate of animals infected with SARS-CoV-2 and also reduced the destructive effects of the virus on the lung tissue of mice, activating both their innate and adaptive immunity. The obtained results show that the development of adjuvant oligonucleotide vaccine constructs of the La-S-so type is an affordable and efficient platform for the prevention of coronavirus infections, including those caused by SARS-CoV-2.
Citation: Scientia Pharmaceutica
PubDate: 2023-07-12
DOI: 10.3390/scipharm91030035
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 36: Computational Assessment of Cannflavin A
as a TAK1 Inhibitor: Implication as a Potential Therapeutic Target for
Anti-Inflammation
Authors: Sarunya Chuanphongpanich, Satapat Racha, Banthita Saengsitthisak, Pichai Pirakitikulr, Kannika Racha
First page: 36
Abstract: TAK1 (transforming growth factor-beta-activated kinase 1) is a crucial therapeutic target in inflammation-related diseases. This study investigated the inhibitory potential of cannflavin A, a flavonoid found in Cannabis sativa, against TAK1. Through in silico approaches, including drug-likeness analysis, ADMET assessment, molecular docking, and molecular dynamics simulation, the binding affinity and stability of cannflavin A were evaluated. The results demonstrate that cannflavin A exhibits excellent ADMET properties and displays superior binding affinity and stability at the ATP binding site of TAK1 when compared to the known inhibitor takinib. Notably, the decomposition of binding free energy unveils critical amino acid residues involved in TAK1 binding, underscoring the inhibitory effect of cannflavin A through TAK1 inhibition. These findings highlight the potential of cannflavin A as a TAK1 inhibitor and its significant implications for the development of targeted therapies in inflammation-related diseases. Through modulating inflammatory signaling pathways, cannflavin A holds promise for more effective and tailored treatment strategies, particularly in rheumatoid arthritis. This study contributes to the current understanding of cannflavin A’s application and provides a foundation for further research and innovative approaches in targeted therapies for inflammatory conditions.
Citation: Scientia Pharmaceutica
PubDate: 2023-07-17
DOI: 10.3390/scipharm91030036
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 37: Chitosan-Based Nanocarriers for Delivery
of Remdesivir
Authors: Viktoria Milkova, Kamelia Kamburova, Petar Martinov, Neli Vilhelmova-Ilieva, Viktor Rashev
First page: 37
Abstract: Stable multicomponent capsules for the delivery of remdesivir (Veklury®) are produced through subsequent electrostatic adsorption of oppositely charged components on oil emulsion droplets. For the first time, the encapsulation and release of the medicine Veklury® from polymer capsules was reported. In this study, the effect of the physicochemical properties of chitosan on the size and stability of the produced structures is investigated, on the loaded amount of drug and on the kinetics of drug release in conditions close to the physiological ones. Microbiological studies of the capsules and their constituents were performed via in vitro assays against HCT-8 cell lines and human coronavirus HCoV-OC43. A detailed analysis was performed on the influence of the properties of produced capsules on cytotoxicity against the chosen cell line, as well as their effect on the replication cycle of the virus, the virucidal activity of the samples against the viability of the extracellular virions, and their effect on viral adsorption on the cell membrane.
Citation: Scientia Pharmaceutica
PubDate: 2023-08-09
DOI: 10.3390/scipharm91030037
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 38: PBPK Evaluation of Sofosbuvir Dose in
Pediatrics Using Simcyp®
Authors: Rania Elkeeb, Anomeh Avartoomian, Amira S. Gouda, Ahmed M. Abdel-Megied, Ola Abdallah, Eman Atef
First page: 38
Abstract: The aim of the study is to evaluate the effectiveness of the pediatric sofosbuvir weight-based dosing strategy in providing an equitable drug exposure compared to the marketed dose. The physiologically based pharmacokinetic (PBPK) modeling and simulation is a valuable tool in assessing drug dosing and toxicity in populations with physiological, pathological, and genetic pharmacokinetic (PK) variability. The PBPK model of the sofosbuvir compound was developed using Simcyp® V20. The model was developed and verified using the published sofosbuvir’s physicochemical properties and clinical data from multiple studies on healthy adult volunteers, hepatitis C virus (HCV)-infected adults, and HCV-infected pediatrics. The AUC and Cmax fold ratio of (predicted/observed) fell within the acceptable range of 0.5–2 in all tested adults’ data, confirming the successful development of the sofosbuvir Simcyp® compound model. Using this model, a weight-based dosing regimen of 6 mg/kg in pediatric patients was simulated and compared to the 150 mg and 200 mg approved dose for 3–6 and 6–12 y/o pediatric patients, respectively. No dose adjustment was recommended in patients ages 6–12 y/o. However, compared to the approved 150 mg for 3–6 y/o, the weight base dose provided an equitable drug exposure to adults. Further clinical studies are warranted to verify this finding.
Citation: Scientia Pharmaceutica
PubDate: 2023-08-10
DOI: 10.3390/scipharm91030038
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 39: Compounded Hair Solutions and Foams
Containing Minoxidil: Does the Color Change Impact Stability'
Authors: Hudson C. Polonini, Carolina C. V. Silva
First page: 39
Abstract: An increasing number of pharmacies around the world are producing hair solutions and foams containing minoxidil for alopecia, commonly using ready-to-use vehicles such as TrichoSolTM or TrichoFoamTM. However, it is paramount to determine the chemical and microbiological compatibility of these formulations so they can be safely implemented as vehicles of choice. Also, these products usually suffer from a change of color over time, which leads to many patients prematurely discontinuing treatment. As long-term treatment is recommended, this study aimed to assess the physical–chemical and microbiological stability and investigate the color change of compounded minoxidil formulations. For that, HPLC analyses and antimicrobial effectiveness testing were conducted in a bracketed study covering concentrations from 1.0% to 7.0% of minoxidil. HPLC, pH, and metals in 5.0% minoxidil compounded products were determined using ICP-MS to evaluate the mechanisms involved in their color change. The stability of the products varied from 120 to 380 days. The color change was remarkably noticeable, but apart from this parameter, no other quality attribute was affected throughout this period, including minoxidil content, which presented only minor fluctuations. No precipitation was observed, and pH was relatively stable. It is not expected that this yellow color will impact effectiveness. Finally, we created an indicative color chart of the behavior of minoxidil in the studied vehicles.
Citation: Scientia Pharmaceutica
PubDate: 2023-08-15
DOI: 10.3390/scipharm91030039
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 40: Hepatoprotective Activity, In Silico
Analysis, and Molecular Docking Study of Verbascoside from Leucophyllum
frutescens in Rats with Post-Necrotic Liver Damage
Authors: Osmar Antonio Jaramillo-Morales, Erik Díaz-Cervantes, Lisa Dalla Via, Aida Nelly Garcia-Argaez, Josué Vidal Espinosa-Juárez, José Carlos Ovando-Zambrano, Victor Manuel Muñoz-Pérez, Carmen Valadez-Vega, Mirandeli Bautista
First page: 40
Abstract: There is an urgent need for scientists to verify the pharmacological properties of medicinal plants. Leucophyllum frutescens (Lf) belongs to the family Scrophulariaceae, and it is used in the treatment of airway diseases such as cough, tuberculosis, and asthma. The methanolic extract of the aerial parts of Lf allows for the isolation and identification of verbascoside (Vb). This study aimed to evaluate the hepatoprotective effect of Vb, a caffeoyl phenylethanoid glycoside (CPG), on post-necrotic liver damage induced by thioacetamide (TA) via in vivo and in silico studies, with the latter considering a cancerous process. The aerial parts of Lf were extracted by maceration using hexane methanol (5 L/500 g/8 days). Vb was isolated from methanol extract at approximately 30%. Wistar rats were intragastrically pretreated or not with a single dose of Vb (20 mg/kg) for four days. On the fourth day, a single dose of TA (6.6 mmol/kg) was intraperitoneally injected. Blood samples and parameters related to liver damage, like AST and ALT, were obtained. Vb significantly reduced the level of liver injury following thioacetamide-induced necrosis. This was corroborated by in silico assay and docking studies, demonstrating that Vb can interact with a HeLa target through hydrogen bonds and electrostatic interactions, achieving better performance than commercial chemotherapeutic Taxol®, by 0.34 kcal/mol. AST and ALT were significantly lower in the rats pretreated with Vb. Furthermore, Vb did not induce cytotoxicity and had a median lethal dose (LD50) greater than 5000 mg/kg. These results suggest that Vb may be used as an alternative to reduce liver damage.
Citation: Scientia Pharmaceutica
PubDate: 2023-08-16
DOI: 10.3390/scipharm91030040
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 41: Preliminary Screening of South African
Plants for Binding Affinity to the Serotonin Reuptake Transporter and
Adenosine A1/A2A Receptors
Authors: Andisiwe Mnqika, Adeyemi O. Aremu, H. D. Janse van Rensburg, Makhotso Lekhooa
First page: 41
Abstract: In South African traditional medicine, Gomphocarpus fruticosus (L.) W.T. Aiton, Hypoxis hemerocallidea Fisch. & C.A. Mey., and Leonotis leonurus. (L.) R.Br. have been recorded among different ethnic groups to be a valuable herbal remedy for the management of depression-related conditions. The current study investigated the affinity of these three plants toward the serotonin reuptake transporter (SERT) and adenosine A1/A2 receptors. Six solvents (water, methanol, acetone, dichloromethane, petroleum ether, and hexane) were used to extract the selected plants. We established that eight extracts exerted potential affinity based on the applied in vitro binding experiment. The methanol and acetone extracts of Hypoxis hemerocallidea had 60% specific binding of [3H]citalopram, an indication that almost 40% of the plant extracts were bound to the SERT. For the adenosine receptor binding assays, methanol and hexane extracts of Leonotis leonurus were the most active, with rA1Ki values of 0.038 and 0.176 mg/mL, respectively. In addition, the dichloromethane extract of Gomphocarpus fruticosus had an rA1Ki value of 6.46 mg/mL. Extracts from the more polar solvents methanol and dichloromethane had higher binding affinity. Additionally, these plant extracts acted as antagonists at the adenosine A1 receptor. Overall, the current findings provide an indication of the potential antidepressant effects of some of the tested extracts based on their binding to the receptors evaluated. However, a combination of other in vitro assays is needed to establish possible mechanisms of action. In addition, computational analysis and profiling of plant extracts is crucial to identify the bioactive compounds with a higher affinity to the receptors. Ultimately, in vivo studies remain essential to allow for an in-depth elucidation of the mechanisms of action.
Citation: Scientia Pharmaceutica
PubDate: 2023-08-22
DOI: 10.3390/scipharm91030041
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 42: Flavonol Glycosides from Eugenia uniflora
Leaves and Their In Vitro Cytotoxicity, Antioxidant and Anti-Inflammatory
Activities
Authors: Ayodeji Oluwabunmi Oriola, Gugulethu Mathews Miya, Moganavelli Singh, Adebola Omowunmi Oyedeji
First page: 42
Abstract: In view of the extensive use of Eugenia uniflora leaves for the management of tumours and other chronic inflammatory diseases in traditional medicine, an activity-guided fractionation of its leaf ethanolic extract led to the isolation of two flavonol glycosides. Cytotoxicity study was based on the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) viability assay against the non-tumourigenic human embryonic kidney (HEK-293) cells, and the cancerous liver (Hep-G2) and cervical (HeLa) cell lines. Antioxidant tests were carried out using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and hydrogen peroxide (H2O2) radical scavenging assays, while an in vitro anti-inflammatory test was conducted using egg albumin denaturation (EAD) assay. Based on comprehensive spectroscopic and spectrometric evidence, the compounds were elucidated as myricitrin (1) and a newly described compound, 5,7-dihydroxy-3-(3,4,5-trihydroxy-6-methyltetrahydropyran-2-yloxy)-2-(2,4,5-trihydroxyphenyl)chromen-4-one, named “unifloratrin (2)”. The cytotoxicity of myricitrin (1) was comparable to 5-fluorouracil (standard drug), with a CC50 of 8.5 ± 2.2 µg/100 µL against HeLa cells. It also demonstrated better antioxidant activity, with an IC50 of 6.23 ± 1.09, 22.01 ± 2.59 and 30.46 ± 1.79 µM against DPPH, NO and H2O2 free radicals, respectively. At 20 µg/mL and an incubation time of 2 h, myricitrin was comparable to diclofenac (standard drug) in anti-inflammatory activity. This report may serve as a justification for the ethnomedicinal use of E. uniflora, while flavonol glycosides, such as myricitrin (1), could be further exploited as a candidate cytotoxic agent.
Citation: Scientia Pharmaceutica
PubDate: 2023-08-24
DOI: 10.3390/scipharm91030042
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 43: Ethnobotanical Review of Selected
Medicinal Plants in Guam for the Treatment of Urinary Tract Ailments and
Their Pharmacological Properties
Authors: Sahena Ferdosh
First page: 43
Abstract: The Chamorro healers of Guam have more than a thousand years of history of using herbs and medicinal plants for the treatment of common ailments. The objective of this study is to review the bioactive compounds and pharmacological properties of medicinal plants which are used for urinary tract health by local healers. Literature searches were performed using Google Scholar, ScienceDirect, PubMed, and SpringerLink, by using several keywords, including “medicinal plants in Guam”, “traditional uses”, “bioactive compounds”, “pharmacological properties”, and “urinary tract infections”. This review highlights the traditional uses, bioactive compounds, and pharmacological properties of five medicinal plant species, namely Euphorbia hirta, Phyllanthus amarus, Premna serratifolia, Psidium guajava, and Urena lobata. Phenolics, alkaloids, terpenoids, essential oils, and polypeptides are the leading secondary metabolites reported in different plant extracts, which have been found to have significant antimicrobial, antioxidant, anti-inflammatory, antidiabetic, and anticancer properties. The therapeutic claims made about medicinal plants in Guam are well supported by the literature, having similar applications and pharmacological properties in other regions of the world. These medicinal plants have a lot of unexplored potential that might be utilized to develop more potent drugs for the treatment of infectious diseases, as well as food and herbal supplements.
Citation: Scientia Pharmaceutica
PubDate: 2023-09-01
DOI: 10.3390/scipharm91030043
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 44: Old Dogs with New Tricks: Antiparasitic
Potential of Structurally Diverse 5-Nitrofuran and 5-Nitrothiophene Imines
and Acyl Hydrazones
Authors: Ibrahim S. Al Nasr, Waleed S. Koko, Tariq A. Khan, Rainer Schobert, Bernhard Biersack
First page: 44
Abstract: Miscellaneous imines and acyl hydrazones were prepared from 5-nitrofuraldehyde and 5-nitrothiophene-2-carboxaldehyde. Their activities against Toxoplasma gondii and Leishmania major parasites were evaluated. Promising antiparasitic effects and selectivities were observed for certain acyl hydrazones and imines. Cobalt(II) and copper(II) complexes conserved the high anti-Toxoplasma activities of 3-hydroxy-2-naphthoic carboxyl hydrazone (2a). In addition, sound activities against L. major promastigotes were observed for various analogs of 2a (2b and 2i) and pyrid-2-ylpyrazole-based imines (3g and 3h). Relatively low toxicities to kidney cells and macrophages indicate promising selectivity profiles for these compounds.
Citation: Scientia Pharmaceutica
PubDate: 2023-09-19
DOI: 10.3390/scipharm91030044
Issue No: Vol. 91, No. 3 (2023)
- Sci. Pharm., Vol. 91, Pages 17: Fabrication of Direct Compressible Tablets
Containing Chatuphalathika Extract Obtained through Microwave-Assisted
Extraction: An Optimization Approach
Authors: Chaowalit Monton, Piyapa Keawchay, Chantisa Pokkrong, Pariyakorn Kamnoedthapaya, Abhiruj Navabhatra, Jirapornchai Suksaeree, Thaniya Wunnakup, Natawat Chankana, Thanapat Songsak
First page: 17
Abstract: This research sought to optimize the microwave-assisted extraction of Chatuphalathika as an herbal recipe maximizing the active compounds and the antioxidant activity by the Box–Behnken design. Three factors—microwave power, time, and cycle—were varied. Eight responses—extraction yield, total phenolic content, gallic acid content, corilagin content, chebulagic acid, chebulinic acid, IC50 from DPPH assay, and IC50 from FRAP assay—were monitored. Furthermore, cytotoxicity was evaluated to ensure the safety of the extract. After that, the optimized extract was compressed into tablets. The results showed that the optimal condition of the microwave-assisted extraction gave the simultaneous maximum extraction yield, total phenolic content, and antioxidant activity with a microwave power of 450 W for 30 s and 3 cycles. The extract obtained from the optimal condition exhibited a good safety profile although a concentration of 5 mg/mL was used. The optimized tablets were achieved when a compression force of 1500 psi and magnesium stearate of 1% were applied, and no sodium starch glycolate was added. In conclusion, the optimal green extraction method could be used for the extraction of the Chatuphalathika. Furthermore, the fabrication of Chatuphalathika tablets was successful, as the tablets had low friability with a short disintegration time.
Citation: Scientia Pharmaceutica
PubDate: 2023-03-23
DOI: 10.3390/scipharm91020017
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 18: Medicinal Chemistry of Quinazolines as
Anticancer Agents Targeting Tyrosine Kinases
Authors: Mohamed F. Zayed
First page: 18
Abstract: Cancer is a large group of diseases that can affect any organ or body tissue due to the abnormal cellular growth with the unknown reasons. Many of the existing chemotherapeutic agents are highly toxic with a low level of selectivity. Additionally, they lead to development of therapeutic resistance. Hence, the development of targeted chemotherapeutic agents with low side effects and high selectivity is required for cancer treatment. Quinazoline is a vital scaffold well-known to be linked with several biological activities. The anticancer activity is one of the prominent biological activities of this scaffold. Several established anticancer quinazolines work by different mechanisms on the various molecular targets. The aim of this review is to present different features of medicinal chemistry as drug design, structure activity relationship, and mode of action of some targeted anticancer quinazoline derivatives. It gives comprehensive attention on the chemotherapeutic activity of quinazolines in the viewpoint of drug discovery and its development. This review provides panoramic view to the medicinal chemists for supporting their efforts to design and synthesize novel quinazolines as targeted chemotherapeutic agents.
Citation: Scientia Pharmaceutica
PubDate: 2023-03-28
DOI: 10.3390/scipharm91020018
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 19: Mapping Protein Targets of Carnosol, a
Molecule Identified in Rosmarinus officinalis: In Silico Docking Studies
and Network Pharmacology
Authors: María Taboada-Alquerque, Danilo Pajaro-Valenzuela, Karina Caballero-Gallardo, Alejandro Cifuentes, Elena Ibáñez, Maicol Ahumedo-Monterrosa, Elena E. Stashenko, Jesus Olivero-Verbel
First page: 19
Abstract: Carnosol is a natural diterpene present in Rosmarinus officinalis L. (rosemary) with anti-tumor and anti-inflammatory properties. Despite its importance, the pharmacological mechanisms underlying the interactions between carnosol and human targets are still unclear. The goal was to identify plausible human target for carnosol and the network pharmacology. Rosemary was analyzed using HPLC-QTOF-MS/MS. Potential carnosol targets were identified using docking and a public database (CTD). Carnosol was screened against 708 human proteins using AutoDock Vina, and affinity values were used as prioritization criteria. The targets set was uploaded to WebGestalt to obtain Gene Ontology (GO) and KEGG pathway enrichment analysis. HPLC-QTOF-MS/MS analyses allowed the tentative annotation of nine chemicals, with carnosol being the most ionized. There were 53 plausible targets for carnosol, with 20 identified using virtual screening, including Hsp90α (−10.9 kcal/mol), AKR1C3 (−10.4 kcal/mol), and Hsp90β (−10.4 kcal/mol), and 33 identified from CTD. The potential targets for carnosol identified with PPI and molecular docking were HSP90AA1, MAPK1, MAPK3, CAT, JUN, AHR, and CASP3. GO terms and KEGG pathways analysis found that carnosol is closely related to infection (Chagas, influenza A, toxoplasmosis, and pertussis) and inflammation (IL-17 and TNF signaling pathway and Th-17 cell differentiation). These results demonstrated that carnosol may induce an immuno-inflammatory response.
Citation: Scientia Pharmaceutica
PubDate: 2023-04-10
DOI: 10.3390/scipharm91020019
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 20: In Vitro and Ex Vivo Models for Screening
Topical Anti-Inflammatory Drugs
Authors: Juan Luis Pérez-Salas, Martha Rocío Moreno-Jiménez, Nuria Elizabeth Rocha-Guzmán, Rubén Francisco González-Laredo, Luis Medina-Torres, José Alberto Gallegos-Infante
First page: 20
Abstract: Skin inflammation occurs as an immune response to various stimuli such as ultraviolet light, irritants, or any type of skin barrier injury. Finding safe and effective drugs to combat skin inflammation remains a research challenge. Ethical and legal considerations in animal testing encourage the development of in vitro and ex vivo models for the detection of skin inflammation. This report presents an updated review of non-animal study models available for screening drugs with anti-inflammatory potential. It includes a description of the basic methods used to inhibit protein denaturation and red blood cell membrane stability. Three in vitro inhibition assay methods for enzymes relevant to the skin inflammatory process are then described. The development of cell culture models is described: relatively simple and easy-to-produce two-dimensional (2D) skin cell cultures that allow assessment of response to a given stimulus, three-dimensional (3D) cell cultures that better mimic human skin physiology by more accurately replicating mechanical and chemical signals, and vascularized 3D skin models with dynamic perfusion and microfluidic devices known as skin on a chip. Finally, ex vivo skin models are presented that could more accurately represent human skin in terms of structure, cell signaling mechanisms, and absorption effects. Although the current development of models without the use of animals is promising, improvements and refinements are needed to make the models more suitable as screening platforms for topical anti-inflammatory drugs.
Citation: Scientia Pharmaceutica
PubDate: 2023-04-17
DOI: 10.3390/scipharm91020020
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 21: Development of Methods of Quality Control
of the Tablet «Ramipril»
Authors: Kateryna Typlynska, Yuliya Kondratova, Liliya Logoyda
First page: 21
Abstract: Our main target was to develop methods for the quality control of the tablet «ramipril» according to the indicators of «Quantitative determination», «Impurities» and «Dissolution». New, precise, accurate and green HPLC methods were developed for the determination of ramipril and its impurities in tablets. The separation was accomplished using a diode array detector at 210 nm with an isocratic and gradient mobile phase consisting of a 0.2 g/L solution of sodium hexanesulfonate (pH 2.7) and the acetonitrile and chromatographic columns Acclaim 120 C18 and Inertsil ODS-3. The developed method was validated in accordance with ICH guidelines. The analysis of impurities was performed within a run duration of less than 25 min, which is about a two times shorter than that of the official Ph. Eur. method. The analysis of ramipril in tablets was performed with a run duration of less than 4.5 min, which is about three times shorter than that of the official USP method. The developed methods were successfully applied for the quality control of the tablet «ramipril» according to the indicators of «Quantitative determination», «Impurities» and «Dissolution». In addition, they proved its superiority over the reported methods in terms of greenness using different assessment tools.
Citation: Scientia Pharmaceutica
PubDate: 2023-04-21
DOI: 10.3390/scipharm91020021
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 22: Photoprotector Effect of Emulsions with
Yerba-Mate (Ilex paraguariensis) Extract
Authors: Juliana Andriolli Ribeiro, Ederlan Magri, Itamar Luís Gonçalves, Karina Paese, Juliana Roman, Alice Teresa Valduga
First page: 22
Abstract: Yerba-mate contains in its composition a high concentration of phenolic compounds. This class of secondary metabolites exhibits strong values of molar absorptivity on ultraviolet and visible wavelengths. This study evaluated the effect of yerba-mate extracts on the in vitro solar protection factor (SPF) value of sunscreen formulations. The sunscreen formulations were prepared to have non-ionic lotion as a basis and yerba-mate extract and/or avobenzone as active agents. The SPF and resveratrol protective effect of the formulations were determined by UV-vis spectrometry. A synergic effect between the yerba-mate extract and avobenzone on the SPF was found. Yerba-mate extract at 5% improved the SPF of the avobenzone 5% formulation from 28.46 ± 5.45 to 40.48 ± 0.84. Yerba-mate extract at 5% avoided resveratrol degradation by ultraviolet radiation. At this same concentration, avobenzone produced a smaller effect than yerba-mate extracts in resveratrol protection. The formulations with yerba-mate + avobenzone presented smaller changes in pH values during 12 days of storage. The spreadability profile of yerba-mate and avobenzone formulations was similar to the profile of avobenzone formulations. The results reported here show the suitability of the yerba-mate extract use in photoprotective formulations, highlighting their in vitro effect and opening possibilities for new investigations exploring this property.
Citation: Scientia Pharmaceutica
PubDate: 2023-04-23
DOI: 10.3390/scipharm91020022
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 23: Comparative Evaluation of Metformin and
Metronidazole Release from Oral Lyophilisates with Different Methods
Authors: Venera R. Timergalieva, Chiara G. M. Gennari, Francesco Cilurzo, Francesca Selmin, Rouslan I. Moustafine
First page: 23
Abstract: The aim of this study is to compare three different dissolution methods to assess the drug release from oral lyophilisates, based on interpolyelectrolyte complexes (IPECs). IPECs were prepared by mixing solutions of a linear polymer, Eudragit® EPO, with a polymer with a cross-linked structure, Noveon® AA-1 or Carbopol® 10 Ultrez (in ratios of 1:2 and 1:1, respectively). Metformin or metronidazole were used as model drugs to achieve a systemic or local effect. A comparative assessment of the drug release kinetics was carried out using artificial saliva and three different set-ups: a paddle stirrer (USP apparatus 2), a flow cell (USP apparatus 4) and a Franz diffusion cell. The results demonstrated that oral lyophilisates disintegrated within 1 min. In the case of metformin, the drug release was completed in about 90 min independently of the set-up. The static conditions in the Franz diffusion cell and USP apparatus 2 permitted the aggregation of the IPEC; therefore, the release profiles show a significant difference compared to the USP apparatus 4.
Citation: Scientia Pharmaceutica
PubDate: 2023-04-25
DOI: 10.3390/scipharm91020023
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 24: Effectiveness of Zingiber montanum Herbal
Compress Remedy for Pain Management: An Updated Systematic Review and
Meta-Analysis
Authors: Kanjana Worasing, Bunleu Sungthong, Wiraphol Phimarn
First page: 24
Abstract: The Zingiber montanum herbal compress remedy is a type of herbal medicine that can be used as an alternative treatment for improving pain symptoms. This study aimed to evaluate the clinical efficacy of a Z. montanum herbal compress remedy for pain relief. PubMed, Scopus, ScienceDirect, and Thai databases were systematically searched for relevant articles published from inception to December 2022. Only randomized clinical trials (RCTs) wherein the efficacy of the Z. montanum remedy was compared to that of a placebo or non-steroidal anti-inflammatory drugs (NSAIDs) were included. Six RCTs with a total of 812 patients were included in the analysis. The efficacy of the Z. montanum remedy had a significantly decreased pain score compared to the placebo (SMD = −0.63; 95% CI = −1.20, −0.06; I2 = 90%), but there was no significant difference when compared to NSAIDs (SMD = −0.61; 95% CI = −1.41, 0.81; I2 = 73%). Moreover, the efficacy of the Z. montanum remedy in terms of the flexibility score (SMD = 0.59; 95% CI −0.56, 1.74; I2 = 86.0%) and quality of life (SMD = 0.34; 95% CI −0.38, 1.05; I2 = 81.0%) was similar to that of the placebo. This meta-analysis demonstrates that the use of the Z. montanum herbal compress remedy significantly reduces the pain scores reported by patients.
Citation: Scientia Pharmaceutica
PubDate: 2023-05-03
DOI: 10.3390/scipharm91020024
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 25: Effect of Etifoxine on Locomotor Activity
and Passive Learning in Rats with Diazepam-Induced Cognitive Deficit
Authors: Vesela Kokova, Elisaveta Apostolova
First page: 25
Abstract: Etifoxine is an anxiolytic drug with a dual mechanism of action. In contrast to conventional benzodiazepine anxiolytics, which induce cognitive dysfunction and myorelaxation, no memory impairment nor a decrease in motor activity is observed with etifoxine. This study aims to evaluate the effects of etifoxine on locomotor activity and passive learning in rats with diazepam-induced memory deficit. Male Wistar rats were treated intraperitoneally for 7 days with: (1) saline; (2) diazepam 2.5 mg/kg bw or (3) diazepam 2.5 mg/kg bw and etifoxine in a dose of 50 mg/kg bw. Activity cage test was used for evaluation of locomotor activity, and step-through and step-down tests were performed to study the passive learning. Etifoxine increased the number of horizontal movements on the 7th and 14th days of the experiment. The drug exhibits anti-amnesic effect in a model of diazepam-induced anterograde amnesia by enhancing long-term memory in passive learning tests. The data obtained suggest that etifoxine can reduce the benzodiazepine-induced cognitive deficit. Moreover, such a combination can alleviate the negative influence of benzodiazepines on locomotor activity. However, additional studies are necessary to translate these results into clinical practice.
Citation: Scientia Pharmaceutica
PubDate: 2023-05-04
DOI: 10.3390/scipharm91020025
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 26: Fused Triazole-Azepine Hybrids as
Potential Non-Steroidal Antiinflammatory Agents
Authors: Sergii Demchenko, Roman Lesyk, Oleh Yadlovskyi, Serhii Holota, Sergii Yarmoluk, Sergii Tsyhankov, Anatolii Demchenko
First page: 26
Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the oldest and most widely used groups of drugs nowadays. However, the problem of searching for and creating new NSAIDs remains open, primarily due to the risks owing to their short- and long-term use. In this context, triazole-azepine hybrid molecules are attractive and prospective objects for the rational design of novel potential NSAIDs. In the present work studies of 3-aryl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepines as potential non-steroidal anti-inflammatory agents are reported. Evaluation of drug-like properties for all tested triazole-azepine hybrids was performed in silico using SwissADME. The screening of analgesic and anti-inflammatory activities was performed in vivo using acid-induced writhing and carrageenin-induced hind paw oedema models in mice. Derivatives with activity levels more potent compared with reference drugs ketorolac and diclofenac sodium were identified. Preliminary SAR was performed based on the screening results.
Citation: Scientia Pharmaceutica
PubDate: 2023-05-16
DOI: 10.3390/scipharm91020026
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 27: Polymeric Microneedles: An Emerging
Paradigm for Advanced Biomedical Applications
Authors: Deepak Kulkarni, Dipak Gadade, Nutan Chapaitkar, Santosh Shelke, Sanjay Pekamwar, Rushikesh Aher, Ankita Ahire, Manjusha Avhale, Rupali Badgule, Radhika Bansode, Bhujang Bobade
First page: 27
Abstract: Microneedles are gaining popularity as a new paradigm in the area of transdermal drug delivery for biomedical and healthcare applications. Efficient drug delivery with minimal invasion is the prime advantage of microneedles. The concept of the microneedle array provides an extensive surface area for efficient drug delivery. Various types of inorganics (silicon, ceramic, metal, etc.) and polymeric materials are used for the fabrication of microneedles. The polymeric microneedles have various advantages over other microneedles fabricated using inorganic material, such as biocompatibility, biodegradation, and non-toxicity. The wide variety of polymers used in microneedle fabrication can provide a broad scope for drug delivery and other biomedical applications. Multiple metallic and polymeric microneedles can be functionalized by polymer coatings for various biomedical applications. The fabrication of polymeric microneedles is shifting from conventional to advanced 3D and 4D printing technology. The multifaceted biomedical applications of polymeric microneedles include drug delivery, vaccine delivery, biosensing, and diagnostic applications. Here, we provide the overview of the current and advanced information on polymers used for fabrication, the selection criteria for polymers, biomedical applications, and the regulatory perspective of polymer-based and polymer-coated microneedles, along with a patent scenario.
Citation: Scientia Pharmaceutica
PubDate: 2023-05-31
DOI: 10.3390/scipharm91020027
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 28: New Advances and Perspectives of Influenza
Prevention: Current State of the Art
Authors: Volodymyr Oberemok, Oksana Andreeva, Edie Alieva, Anastasiya Bilyk
First page: 28
Abstract: The modern world, swaddled in the benefits of civilization, has fostered the development of science and the introduction of products of technological progress. This has allowed serious individual health problems, including those associated with viral diseases, to become targets for prophylaxis, treatment, and even cure. Human immunodeficiency viruses, hepatitis viruses, coronaviruses, and influenza viruses are among the most disturbing infectious agents in the human experience. Influenza appears to be one of the oldest viruses known to man; these viruses were among the first to cause major epidemics and pandemics in human history, collectively causing up to 0.5 million deaths worldwide each year. The main problem in the fight against influenza viruses is that they mutate constantly, which leads to molecular changes in antigens, including outer membrane glycoproteins, which play a critical role in the creation of modern vaccines. Due to the constant microevolution of the virus, influenza vaccine formulas have to be reviewed and improved every year. Today, flu vaccines represent an eternal molecular race between a person and a virus, which neither entity seems likely to win.
Citation: Scientia Pharmaceutica
PubDate: 2023-06-14
DOI: 10.3390/scipharm91020028
Issue No: Vol. 91, No. 2 (2023)
- Sci. Pharm., Vol. 91, Pages 5: Detailing the Ten Main Professional Roles
of a Pharmacist to Provide the Scope of Professional Functions
Authors: Yuliia Kremin, Lilia Lesyk, Roman Lesyk, Oksana Levytska, Bohdan Hromovyk
First page: 5
Abstract: As members of a public trust profession, pharmacists are the most accessible medical team members. Therefore, every pharmacist must know the scope of their professional roles (PR) and professional functions (PF). The study aimed to detail the major PR into a pooled set of PF. The research materials were the provisions of the World Health Organization, the International Pharmaceutical Federation, and scientific works on the PR of pharmacists. Methods of critical analysis, concretization, functional decomposition, and scientific generalization were used. As a result of detailing the 10 main PR according to the “ten-star pharmacist” concept for each, a combined set of partial PFs of the pharmacist was obtained. The decomposition takes into account the principle of complexity limitation, which allowed three to six partial PF for the respective PR to be obtained, namely: three PFs for a life-long-learner, five PFs for a caregiver, a decision-maker, a teacher, a leader, a researcher, an entrepreneur, and an agent of positive change, six PFs for a communicator and a manager. Thus, due to the decomposition of each of the 10 main PR of the pharmacist into three or six corresponding partial PFs, we received a multifunctional verbal model of difficult to organize, professional activities, which is identified by a total of 50 PFs. The importance of using this model in formulating professional competencies and learning outcomes of educational programs for pharmacists is emphasized.
Citation: Scientia Pharmaceutica
PubDate: 2023-01-13
DOI: 10.3390/scipharm91010005
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 6: A Review of the Biological Properties of
Purple Corn (Zea mays L.)
Authors: Kim, Lee, Kim, Hong, Deepa, Kim
First page: 6
Abstract: In the food and beverage industries, replacing synthetic colorants with plant-based colorants has become popular in recent times. Purple corn (Zea mays L.) is an important source of natural colorants due to its range in color from orange to purple. The whole plant of purple corn has a high amount of anthocyanin content. Anthocyanin is the water-soluble pigment found in various fruits and vegetables. The color pigments are chiefly found in the pericarp or kernels, in addition to corn cobs. Purple corn is rich in various health-promoting compounds, mainly anthocyanins such as cyanidin-3-O-glucoside, perlagonidin-3-O-glucoside, peonidin 3-O-glucoside, and their malonylated forms. This review emphasized recent updates regarding the in vitro and in vivo biological properties of extracts and compounds from purple corn. Purple corn color extracts possess a variety of biological properties, including antioxidant, anti-inflammatory, anticancer, anti-diabetic, anti-obesity, etc. The results of in vitro and in vivo studies of the biological properties of purple corn could lead to the development of different health-promoting products in the near future.
Citation: Scientia Pharmaceutica
PubDate: 2023-01-19
DOI: 10.3390/scipharm91010006
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 7: Phytochemical Characterization of
Pterocephalus frutescens with In-Silico Evaluation as Chemotherapeutic
Medicine and Oral Pharmacokinetics Prediction Study
Authors: Atef A. El-Hela, Marwa S. Abu Bakr, Mostafa M. Hegazy, Mohammed A. Dahab, Ayman Abo Elmaaty, Adel Ehab Ibrahim, Sami El Deeb, Hatem S. Abbass
First page: 7
Abstract: Virtual screening of the potential lead chemotherapeutic phytochemicals from medicinal plants has useful application in the field of in-silico modelling and computer-based drug design by orienting and scoring ligands in the active binding site of a target protein. The phytochemical investigation of the Pterocephalus frutescens extract in n-butanol resulted in the isolation and structure elucidation of three iridoids and four flavonoids which were identified as Geniposide (1), Geniposidic acid (2), Nepetanudoside C (3), Isovitexin (4), Luteolin-7-O-glucoside (5) Isoorientin (6) and Orientin (7), respectively. Molecular docking studies were used to compare the binding energies of the isolated phytochemicals at four biological cancer-relevant targets; namely, aromatase, carbonic anhydrase IX, fatty acid synthase, and topoisomerase II-DNA complex. The docking study concluded that the isolated compounds have promising cytotoxic activities, in particular, Luteolin-7-O-glucoside (5) and Orientin (7) which exhibited high binding affinities among the isolated compounds at the active sites of the target enzymes; Aromatase (−8.73 Kcal/mol), and Carbonic anhydrase IX (−8.92 Kcal/mol), respectively, surpassing the corresponding binding scores of the co-crystallized ligands and the reference drugs at these target enzymes. Additionally, among the isolated compounds, Luteolin-7-O-glucoside (5) showed the most outstanding binding affinities at the active sites of the target enzymes; Fatty acid synthase, and Topisomerase II-DNA complex with binding scores of −6.82, and −7.99 Kcal/mol, respectively. Finally, the SwissADME online web tool predicted that most of these compounds possessed acceptable oral bioavailability and drug likeness characteristics.
Citation: Scientia Pharmaceutica
PubDate: 2023-01-28
DOI: 10.3390/scipharm91010007
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 8: Acknowledgment to the Reviewers of Scientia
Pharmaceutica in 2022
Authors: Scientia Pharmaceutica Editorial Office Scientia Pharmaceutica Editorial Office
First page: 8
Abstract: High-quality academic publishing is built on rigorous peer review [...]
Citation: Scientia Pharmaceutica
PubDate: 2023-01-29
DOI: 10.3390/scipharm91010008
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 9: Antimicrobial Activity of Novel Deep
Eutectic Solvents
Authors: Noor Akbar, Naveed Ahmed Khan, Taleb Ibrahim, Mustafa Khamis, Amir Sada Khan, Ahmad M. Alharbi, Hasan Alfahemi, Ruqaiyyah Siddiqui
First page: 9
Abstract: Herein, we utilized several deep eutectic solvents (DES) that were based on hydrogen donors and hydrogen acceptors for their antibacterial application. These DES were tested for their bactericidal activities against Gram-positive (Streptococcus pyogenes, Bacillus cereus, Streptococcus pneumoniae, and methicillin-resistant Staphylococcus aureus) and Gram-negative (Escherichia coli K1, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Serratia marcescens) bacteria. Using lactate dehydrogenase assays, DES were evaluated for their cytopathic effects towards human cells. Results from antibacterial tests revealed that DES prepared from the combination of methyl-trioctylammonium chloride and glycerol (DES-4) and DES prepared form methyl-trioctylammonium chloride and fructose (DES-11) at a 2 µL dose showed broad-spectrum antibacterial behavior and had the highest bactericidal activity. Moreover, DES-4 showed 40% and 68% antibacterial activity against P. aeruginosa and E. coli K1, respectively. Similarly, DES-11 eliminated 65% and 61% E. coli K1 and P. aeruginosa, respectively. Among Gram-positive bacteria, DES-4 showed important antibacterial activity, inhibiting 75% of B. cereus and 51% of S. pneumoniae. Likewise, DES-11 depicted 70% B. cereus and 50% S. pneumoniae bactericidal effects. Finally, the DES showed limited cytotoxic properties against human cell lines with the exception of the DES prepared from Methyltrioctylammonium chloride and Citric acid (DES-10), which had 88% cytotoxic effects. These findings suggest that DES depict potent antibacterial efficacies and cause minimal damage to human cells. It can be concluded that the selected DES in this study could be utilized as valuable and novel antibacterial drugs against bacterial infections. In future work, the mechanisms for bactericides and the cytotoxicity effects of these DES will be investigated.
Citation: Scientia Pharmaceutica
PubDate: 2023-02-08
DOI: 10.3390/scipharm91010009
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 10: Comparison of Substance Sources in
Experimental Antimicrobial Susceptibility Testing
Authors: Filip Bielec, Małgorzata Brauncajs, Dorota Pastuszak-Lewandoska
First page: 10
Abstract: Funding is often a constraint when planning research, especially in countries where basic research is underfunded. Researchers must take into account these limitations, e.g., in relation to the selection of appropriate reagents, the source of which may affect the study’s final results. The aim of this article was to compare the results of bacteria susceptibility testing using three different sources of antimicrobial: the pure powder available from the supplier and two tablet formulations with different excipients. The chosen substance was furazidin (nitrofuran derivative). The susceptibility was tested on a group of 45 uropathogenic Enterobacterales using both microdilution and disk diffusion methods. The obtained results indicated that despite the relatively higher price, the powder appeared to be the best substance for scientific purposes, especially for quantitative determinations.
Citation: Scientia Pharmaceutica
PubDate: 2023-02-09
DOI: 10.3390/scipharm91010010
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 11: Long-Term Paracetamol Treatment Impairs
Cognitive Function and Brain-Derived Neurotrophic Factor in Adult Rat
Brain
Authors: Laddawan Lalert, Nutnicha Tantarungsee, Tipthanan Chotipinit, Wilawan Ji-au, Anan Srikiatkhachorn, Supang Maneesri-le Grand
First page: 11
Abstract: Paracetamol (acetaminophen, APAP) is known as a safe pain reliever; however, its negative effects on the central nervous system have gradually been reported. We examined alterations in learning and memory, and brain-derived neurotrophic factor (BDNF) expression in the frontal cortex and hippocampus at different durations of APAP treatment in rats. Novel object recognition (NOR) and Morris water maze (MWM) paradigms were used to assess learning and memory in rats fed with 200 mg/kg APAP at single-dose, 15-day or 30-day treatments. BDNF expression was evaluated through immunohistochemistry and Western blotting. The single-dose APAP treatment did not alter the NOR performance. However, deficits in the NOR and MWM capacities were detected in the rats with longer durations of APAP treatment. An analysis of BDNF expression revealed no significant change in BDNF expression in the single-dose APAP treatment, while rats given APAP for extended periods as treatment showed a significant decrement in this protein in the frontal cortex and hippocampus. Short-term APAP treatment has no effect on learning and memory, or BDNF expression; however, long-term APAP exposure causes cognitive impairment. The diminishment of the BDNF level in the frontal cortex and hippocampus due to the long period of treatment with APAP may at least in part be involved in altered learning and memory in rats.
Citation: Scientia Pharmaceutica
PubDate: 2023-02-13
DOI: 10.3390/scipharm91010011
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 12: Preclinical In Vitro Investigation of MDM2
Inhibition in Combination with Antiangiogenic Therapy for Breast Cancer
Treatment
Authors: Ali M. Alaseem, Khalid Alhazzani, Ahmed Zuwaiel Alanazi, Yasser Alqarni, Mohammad M. Algahtani, Abdullah S. Alhamed, Glowi Alasiri, Fahad T. Alotaibi, Talha Jawaid, Jehad A. Aldali
First page: 12
Abstract: Background: Combining antiangiogenic drugs with other chemotherapeutic drugs has been found to produce superior therapeutic outcomes and prevent drug resistance in a variety of cancers. Methods: Experimental assays such as the MTT assay, flow cytometry, western blotting, and qPCR have been used to evaluate the efficacy of combination therapy. Results: When compared to controls and monotherapies, the combination treatment of axitinib and idasanutlin demonstrated a substantial decrease in cell viability at lower doses, a significant decrease in migration, and a shift toward early and late apoptosis. This study examined major apoptotic, metastatic, and angiogenic factors, including MDM2, p21, BCL-2, BCL-XL, and MMP9, which have showed differential expressions at the protein and mRNA levels after combination. Axitinib and idasanutlin decreased tumorigenesis and migration in vitro in the MCF-7 cell line when compared to other chemotherapeutic medications. The suggested mechanisms of the antitumorigenic effect of the combination therapy may depend on its capacity to promote the production of apoptotic markers and reduce antiapoptotic markers. Conclusions: Treatments with axitinib and idasanutlin demonstrated effective therapeutic targeting of the primary angiogenic growth factor and, consequently, the pro-metastatic arbitrators. This will not only eliminate cancer cells but also stop other malignant processes and ultimately reduce the metastatic cascade.
Citation: Scientia Pharmaceutica
PubDate: 2023-02-20
DOI: 10.3390/scipharm91010012
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 13:
3-[5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl]-propionic
Acid as a Potential Polypharmacological Agent
Authors: Yulian Konechnyi, Andrii Lozynskyi, Iryna Ivasechko, Tetiana Dumych, Solomiya Paryzhak, Oksana Hrushka, Ulyana Partyka, Iryna Pasichnyuk, Dmytro Khylyuk, Roman Lesyk
First page: 13
Abstract: Searching for new types of biological activities among preliminarily identified hit compounds is a key challenge in modern medicinal chemistry. In our study, a previously studied 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl]-propionic acid (Les-6614) was screened for antimicrobial, antifungal, anti-allergic, and antitumor activities. Moreover, cytotoxicity, molecular docking, and SwissAdme online target screening were accomplished. It was determined that the Les-6614 has slight antimicrobial and antitumor activity. However, the studied compound decreased IgE levels in sensitized guinea pigs by 33–86% and reduced IgA, IgM, IL-2, and TNF-α, indicating anti-inflammatory and anti-allergic aactivities. According to the SwissADME web tool, target predictions for Les-6614 potentially have an affinity for lysosomal protective protein, Thromboxane-A synthase, and PPARγ. The molecular docking confirmed that the studied 2-thioxo-4-thiazolidinone derivative showed good bonding with LLP and TXAS, leading to stable protein–ligand complexes. Additionally, Les-6614 is a potential PPARγ modulator, which is important in the pathogenesis of allergy, cancer, and cardiovascular diseases.
Citation: Scientia Pharmaceutica
PubDate: 2023-03-02
DOI: 10.3390/scipharm91010013
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 14: Carthamus tinctorius Suppresses
LPS-Induced Anti-Inflammatory Responses by Inhibiting the
MAPKs/NF-κB Signaling Pathway in HaCaT Cells
Authors: So-Yeon Kim, Minji Hong, Ponnuvel Deepa, Kandhasamy Sowndhararajan, Se Jin Park, SeonJu Park, Songmun Kim
First page: 14
Abstract: This study aimed to elucidate the anti-inflammatory activity of C. tinctorius leaves by measuring inflammatory parameters such as nitric oxide (NO) production and mRNA expression of iNOS, interleukin-6 (IL-6), and IL-1β in lipopolysaccharide (LPS)-induced HaCaT cells. Further, the effect of C. tinctorius ethanol extract on the MAPKs/NF-κB signaling pathway was examined in HaCaT cells. The phytochemical profile of the ethanol extract of C. tinctorius leaves was determined using UPLC-QTOF-MS/MS. The results indicated that the ethanol extract of C. tinctorius effectively attenuated LPS-induced secretion of NO, IL-6, and IL-1β in HaCaT cells. Further, LPS-stimulated mRNA and protein expressions of iNOS were decreased by pre-treatment with C. tinctorius ethanol extract at the transcriptional level in HaCaT cells. Moreover, the ethanol extract of C. tinctorius suppressed NF-κB signaling in LPS-induced HaCaT cells. This suppression was mediated by MAPKs/NF-κB signaling, inhibiting the phosphorylation of p38 and p65 in HaCaT cells. However, there is no significant effect on the phosphorylation of JNK by the ethanol extract. The QTOF-MS/MS analysis revealed the identification of 27 components in the ethanol extract of C. tinctorius leaves. The data demonstrate that the ethanol extract of C. tinctorius leaves protects the LPS-induced HaCaT cells by inhibiting the expression of iNOS, IL-6, and IL-1β and suppressing the phosphorylation of the p38, p65, p-JNK via inactivation of MAPKs/NF-κB signaling pathway. These results demonstrate that C. tinctorius leaves may serve as a potential candidate to prevent inflammation-related diseases.
Citation: Scientia Pharmaceutica
PubDate: 2023-03-06
DOI: 10.3390/scipharm91010014
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 15: Antiviral Molecular Targets of Essential
Oils against SARS-CoV-2: A Systematic Review
Authors: Muhammad Iqhrammullah, Diva Rayyan Rizki, Agnia Purnama, Teuku Fais Duta, Harapan Harapan, Rinaldi Idroes, Binawati Ginting
First page: 15
Abstract: Essential oils are potential therapeutics for coronavirus disease 2019 (COVID-19), in which some of the volatile compounds of essential oils have been well known for their broad antiviral activities. These therapeutic candidates have been shown to regulate the excessive secretion of pro-inflammatory cytokines, which underlies the pathogenesis of severe COVID-19. We aimed to identify molecular targets of essential oils in disrupting the cell entry and replication of SARS-CoV-2, hence being active as antivirals. Literature searches were performed on PubMed, Scopus, Scillit, and CaPlus/SciFinder (7 December 2022) with a truncated title implying the anti-SARS-CoV-2 activity of essential oil. Data were collected from the eligible studies and described narratively. Quality appraisal was performed on the included studies. A total of eight studies were included in this review; four of which used enzyme inhibition assay, one—pseudo-SARS-CoV-2 culture; two—whole SARS-CoV-2 culture; and one—ACE2-expressing cancer cells. Essential oils may prevent the SARS-CoV-2 infection by targeting its receptors on the cells (ACE2 and TMPRSS2). Menthol, 1,8-cineole, and camphor are among the volatile compounds which serve as potential ACE2 blockers. β-caryophyllene may selectively target the SARS-CoV-2 spike protein and inhibit viral entry. Other interactions with SARS-CoV-2 proteases and RdRp are observed based on molecular docking. In conclusion, essential oils could target proteins related to the SARS-CoV-2 entry and replication. Further studies with improved and uniform study designs should be carried out to optimize essential oils as COVID-19 therapies.
Citation: Scientia Pharmaceutica
PubDate: 2023-03-06
DOI: 10.3390/scipharm91010015
Issue No: Vol. 91, No. 1 (2023)
- Sci. Pharm., Vol. 91, Pages 16: Evaluation of the Wound Healing Potential
of Hypericum triquetrifolium Turra: An Experimental Animal Study and
Histopathological Examination
Authors: Tamam El-Elimat, Haya S. El-Qaderi, Wael M. Hananeh, Mahmoud M. Abu AlSamen, Ahmed H. Al Sharie, Musa A. Alshehabat, Mohammad Al-Gharaibeh, Feras Q. Alali
First page: 16
Abstract: The wound healing potential of the aerial parts of Hypericum triquetrifolium Turra (Hypericaceae) was evaluated using an in vivo excision wound model in rats. Adult male Sprague Dawley rats were randomly assigned into seven groups; blank vehicles (olive oil and petroleum jelly), negative control, treatments [H. triquetrifolium ethanolic extract in petroleum jelly (5% and 10%) and H. triquetrifolium olive oil macerate (100 and 200 g/L)], and positive control (MEBO). Treatments were applied topically once daily until the wounds had completely healed. Wound areas and contraction rates were calculated, and full-thickness samples of the healed skin were collected for histopathological examination. H. triquetrifolium ointment (5%) showed the best wound healing activity with statistically significant differences when compared with the MEBO, petroleum jelly, and the negative control groups. Tissue sections were histopathologically examined in terms of re-epithelialization, granulation tissue development, collagen deposition, inflammatory cell infiltration, angiogenesis, and ulcer formation to support the in vivo excision wound model findings. H. triquetrifolium ointment (5%) showed the best histopathological scores in both re-epithelialization and ulcer formation. For quality control purposes, a high-performance liquid chromatography (HPLC) method was used to quantify key marker compounds in the extract, namely hypericin and rutin which showed a content of 0.64% and 4.46% (w/w), respectively. Based on the experimental results, H. triquetrifolium ointment (5%) exhibits remarkable wound healing properties at various stages of the wound healing process. Further investigations to prove its safety and efficacy in different types of wounds and to uncover its cellular mechanisms are warranted.
Citation: Scientia Pharmaceutica
PubDate: 2023-03-20
DOI: 10.3390/scipharm91010016
Issue No: Vol. 91, No. 1 (2023)
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