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- Analytical Profiling of Sofosbuvir as NS5B Protein Inhibitor for Oral Drug
Delivery: Method development and Validation
Authors: Shyam W. Rangari et al.
Abstract: Hepatitis C virus (HCV) non-structural protein 5B (NS5B), which is being studied for its RNA-dependent RNA polymerase (RDRP). It has been demonstrated that the RDRP is highly mobile and that it is crucial for viral replication. NS5B protein inhibition, which restricts viral RNA polymerase activity, is how sofosbuvir (SFV) stops viral replication. All first-line treatments for HCV genotypes 1-6 and a few second-line treatments need the use of sofosbuvir in conjunction with additional medications. For genotypes with a fixed speed of more than 90%, and typically around 100%, the combination of SFV and VLE is successful and advised. Infected patients with the human immunodeficiency virus (HIV) use it to increase endurance and prevent forced contaminations. This research offers a concurrent and comparative evaluation of the analytical studies reported in the literature for pharmacological estimation as a look ahead. More than 150 papers from eminent institutions doing scientific, technological, and medical research are currently available. A thorough description of the conventional, hyphenated, and distinctive SFV approaches has been successfully presented in the current review. Additionally, new NS5B inhibitor SFV has been considered to have therapeutic promise along with cutting-edge analytical research.
PubDate: Tue, 16 May 2023 00:15:39 PDT
- Caraway, peppermint and their essential oils in management of Irritable
Bowel Syndrome (IBS)
Authors: Mohaddese Mahboubi
Abstract: Irritable bowel syndrome (IBS) is known as functional gastrointestinal disorder with world prevalence of 9-23%. There is no effective treatment for management of IBS, so, research on effective treatments; especially among the medicinal plants is one interest of scientists. There are many clinical trials on efficacy of plant extracts and essential oils on patients with IBS, but the majority of clinical studies are focused on efficacy of combination of caraway and peppermint essential oils. The aim of this article was to evaluate the efficacy and safety of proprietary combination of peppermint oil and caraway oil for the treatment of IBS. The manuscript was prepared by searching in scientific resources, books, and thesis and documents. There are four clinical trials on oral use of a proprietary combination of peppermint oil and caraway oil in the form of enteric coated capsule was well tolerated by the patients and 4 weeks treatment by this preparation decreased the IBS-symptom severity score and improved the IBS-quality of life of patient with FD-concomitant IBS. Caraway oil, mainly d-carvone and l-limonene inhibits the intestinal fermentation processes by its antimicrobial effects, and inhibits the formation of foam in the stomach and intestinal juice. Peppermint oil, mainly menthol has similar properties and their combination of oils shows the synergistic effects. Although, there are some clinical studies on combination of peppermint and caraway oils in patients with IBS symptoms, but these clinical trials used the patients with FD-concomitant IBS, so, design a new large clinical study with IBS-patients from three types of IBS and evaluation of its efficacy and safety can be the subject of future clinical studies. However, the efficacy of topical combination of peppermint-caraway oils on abdominal skin of patients with IBS can be considered in future studies.
PubDate: Tue, 16 May 2023 00:15:32 PDT
- Selenium nanoparticles attenuate bleomycin-induced pulmonary oxidative
stress and fibrosis in rats
Authors: Azza M A. Abouelella et al.
Abstract: Pulmonary fibrosis is a fatal progressive lung disorder. Bleomycin (BLM) has been used for induction of experimental pulmonary fibrosis. Selenium nanoparticles (SeNPs) have been synthesized and investigated for their ability to ameliorate BLM-induced pulmonary fibrosis. SeNPs (0.5 mg⁄kg. ip) were administered for four weeks; two weeks pre and two weeks post BLM (2.5 U⁄kg. ip). BLM induced biochemical and histological deterioration of lungs. SeNPs induced significant histopathological and biochemical improvement of oxidative stress (MDA, SOD and GSH), inflammatory (IL6 and IL10) and fibrotic markers (hydroxyproline). In conclusion; SeNPs has potential therapeutic rather than protective effect on management of pulmonary damage.
PubDate: Wed, 22 Feb 2023 05:15:22 PST
- Modulation of TLR4/NF-κB, Nrf2/HO-1 and PI3K/Akt signaling by cilostazol
mitigates lipopolysaccharide-induced septic acute kidney injury
Authors: Ahmed F. Mohamed et al.
Abstract: Cilostazol was investigated as a protective agent against lipopolysaccharide (LPS)-associated acute kidney damage in mice. Cilostazol (50 mg/kg/day; p.o) administered for 7 consecutive days before a single LPS dose (2 mg/kg; i.p) hampered serum creatinine and cystatin C as well as renal KIM-1 and NGAL, repressed TLR4 and MYD88 transcription as well as NF-κB p65, IL-1β and MDA content, boosted Nrf-2 mRNA expression, HO-1 activity and GSH content. This was synchronous with an upregulation of p-PI3K and p-Akt expressions. Collectively, cilostazol prevented LPS renal injury which might correspond to modulation of TLR4/NF-κB, Nrf2/HO-1 and PI3K/Akt pathways.
PubDate: Wed, 15 Feb 2023 00:15:26 PST
- Morphological and Anatomical Characterization of Cymbopogon citratus (DC.)
Stapf Cultivated in Egypt
Authors: Yasmine F. Madi et al.
Abstract: Cymbopogon citratus (DC.) Stapf (family Poaceae) is a tropical lemon-scented perennial grass commonly used, fresh or dried, in food and herbal teas. This study revealed that C. citratus different organs are characterized by histological features distinctive to family Poaceae. Characteristic oil cells stained pink with Schiff′s reagent were noticed particularly in the leaf and culm. Scattered closed-type vascular bundles are observed in different organs. Graminaceous stomata and phytolith are restricted to the leaf blade, leaf sheath, and culm. C. citratus leaf is featured by its remarkable epidermal structure formed of long and short cells, bulliform cells, bundle sheath cells, as well, micro- and prickle-hairs that distinguished it from other organs. Sclerenchyma as a mechanical support is observed in all the organs apart from the root. Also, distinguishable non- glandular hairs are detected in the culm, rhizome, and constructs the epiblema structure in the root. The detailed morphological and anatomical study presented here is crucial to discriminate various Cymbopogon species, ensure proper identification of C. citratus (DC.) Stapf, and provide a valuable information for its herbal monograph.
PubDate: Fri, 16 Dec 2022 02:14:07 PST
- Microbial Contamination Of Non- Sterile Pharmaceutical Drops Produced In
Egypt
Authors: M. H. M. Hefny et al.
Abstract: This study is to assess the microbial quality of 360 of non-sterile pharmaceutical drops to note the microbial contamination. Quantitavely, there was no viable bacterial growth in (79.17%) of the tested samples. The samples were free from potentially bacterial pathogens. While, (87.22 %) were free from fungi. Qualitativley, showed that Staphylococcus epidermidis, Bacillus subtilis, and Micrococcus species at frequencies of (26.05 %), (20.17 %) and (15.97 %). Also, fungal contaminants were Aspergillus niger, Saccharomyces species, Penicillium species and Aspergillus flavus at frequencies of (17.65 %), (10.92 %), (7.56 %), (1.68 %) respectively. Egyptian pharmaceuticals should strictly deal with microbial stringency within the manufacturing, packaging, distribution and storage.
PubDate: Sat, 22 Oct 2022 06:10:25 PDT
- Effect of Selected Essential Oils Against Zoonoses and their
Epidemiological Survey Among Domestic Rodents in Egypt
Authors: Walaa S. Nasser et al.
Abstract: A cross-sectional seroprevalence survey of certain pathogenic zoonses in domestic rodents from Abou El Noumorus district, Egypt, was conducted. In addition, antimicrobial of selected essential oils (EOs) was performed and the Minimum Inhibitory Concentration (MIC) was measured. The overall prevalence of antibodies against tested organisms was determined. MIC of the tested EOs showed a promising result. This study provides a serological evidence about the occurrence of these bacteria among domestic rodents. This information is helpful for determining strategies for rat zoonotic diseases prevention and control. Also, it highlighted the effect of certain EOs against the isolated zoonotic pathogens.
PubDate: Fri, 16 Sep 2022 23:55:22 PDT
- Morpho-Anatomical Characters Of The Floral Structures Of Erythrina ×
Neillii Mabberley And Lorence (Fabaceae) And Their Importance To Species
Characterization
Authors: Salma Khaled Gabr et al.
Abstract: Erythrina (Coral tree, Family Fabaceae) is a genus of flowering plant worldwide cultivated for ornamental purposes. The flower of Erythrina species was widely used as a tranquilizer, sedative, and in dysentery and syphilis. Studies on the morphology of this genus are insufficient. This study aims to provide information on the morpho-anatomical characters of the E×neillii flowers and their usefulness in distinguishing this hybrid plant from other closely related species. Erythrina×neillii flower is characterized by a racemose compound panicle inflorescence, diadelphous androecium, superior gynoecium (monocarpellary) with marginal placentation, different type of stomata, rounded to triangular pollen grains with granular exine.
PubDate: Fri, 09 Sep 2022 18:10:23 PDT
- Genetic Diversity Of Cladosporium Species Isolated From Air Of Cairo,
Egypt Using Microsatellite Primed Pcr (Mp-pcr) And Universally Primed Pcr
(Up-pcr) Techniques
Authors: Mohammed Salah Abdulrahman et al.
Abstract: The samples were then identified by macroscopic and microscopical methods, Molecular fingerprinting, of Cladosporium strains populations depending on MP-PCR using Primers (AGG) 5 , (CAG) 5 , (GACA) 4 , and (AG) 8 C. In addition, we have applied the UP-PCR technique using L21 and Fok1 Genotyping patterns extracted by MP-PCR showed good discrimination with amplification of (AGG) 5 , (AG) 8 C and (CAG) 5 over (GACA) 4. In addition, L21 primer revealed variability over FOK1 primer. current work indicate that MP-PCR and UP-PCR fingerprinting method are appropriate for characterization of large groups of Cladosporium due to its simplicity
PubDate: Thu, 07 Jul 2022 21:35:27 PDT
- Phytochemicals, Acute Toxicity and Genotoxicity of Chewing Sticks from
Zanthoxylum zanthoxyloides Root and Distemonanthus benthamianus Stem
Authors: Chinwe S. Alaribe et al.
Abstract: Dental caries has been reported to touch almost half of the world’s population, making it one of the most prevalent disease conditions in the world. Studies have shown that chewing sticks could be useful in cleaning of teeth and could offer protection against dental conditions, including caries. Given the increasing usage of chewing sticks and their unstandardized nature, in this study we investigated the acute toxicity, genotoxic effects on liver and kidney, and phytochemical constituents of chewing sticks from Zanthoxylum zanthoxyloides root and Distemonanthus benthamianus stem, widely used in West Africa. Chemical tests showed the presence of saponins, alkaloids, flavonoids, tannins, terpenoids, steroids, and reducing sugars in ethanol extract of Z. zanthoxyloides root, while saponins, alkaloids, glycosides, and reducing sugars were detected in ethanol extract of D. benthamianus stem. The presence of these bioactive phytochemicals is indicative of the antimicrobial potentials of these plants and could support their usefulness as chewing sticks. Acute toxicity study revealed that the LD50 values of ethanol extracts of D. benthamianus stem and Z. zanthoxyloides root are greater than 2300 and 5000 mg/kg body weight, respectively. Genotoxicity assessment further revealed that D. benthamianus stem and Z. zanthoxyloides root ethanol extracts could induce genotoxic effect on liver and kidney at doses up to 2300 and 5000 mg/kg body weight, respectively. These findings indicate that despite the biochemical properties and medicinal importance of Z. zanthoxyloides root and D. benthamianus stem, their usage should be done with caution.
PubDate: Thu, 07 Jul 2022 21:35:22 PDT
- Antimicrobial and Cytotoxic activities of Ascidian Species Collected from
Egyptian Coasts
Authors: Amany Metwally et al.
Abstract: Discovering novel drugs for curing cancer and infectious diseases is the prime interest of several research areas now. Marine sessile invertebrates have produced secondary metabolites, a lot of which are utilized as novel pharmaceutical agents with diverse effects whether anti-cancer or anti-microbial. Ascidians are marine sessile animals (phylum: Chordata, class: Ascidiacea). Various anti-cancer, anti-viral, and anti-bacterial components are obtained from different bioactive compounds belonging to ascidian species and are in different stages of clinical trials. In this study, five ascidian species which are Polyclinum constellatum, Botryllus eilatensis, Didemnum sp., Symplegma rubra, and Styela canopus were collected from two coastal sites in Egypt. These specimens were utilized for preparing extracts using organic and inorganic solutions. Crystal violet assay using human breast cancer cell line was performed for evaluation cytotoxic activity of dried extracts, besides the diffusion agar technique to assess anti-microbial activity using 6-type fungi: Aspergillus fumigatus, Aspergillus flavus, Candida albicans, Syncephalastrum racemosum, Candida tropicalis, and Penicillium expansum, Gram-positive Bacteria: Staphylococcus aureus, Bacillus subtilis, and Streptococcus mutants, and Gram-negative bacteria: Enterobacter cloacae, Escherichia coli, and Proteus vulgaris. Two ascidian species, Didemnum sp. and S. rubra, showed significant cytotoxicity against human breast cancer cell line while other species showed moderate cytotoxicity. All investigated ascidian species have antibacterial compounds toward S. aureus and B. subtilis. The only species exhibited antibacterial activity against the fungus A. fumigatus was Botryllus eilatensis Didemnum sp. has exhibited activity against seven microbes, while S. canopus, Botryllus eilatensis, S. rubra, and P. constellatum have exhibited activities against 4,5,4, & 2 microbes from twelve used microbes, respectively. Therefore, ascidian species are excellent species for further studies to discover new pharmaceutical agents in Egypt.
PubDate: Thu, 03 Mar 2022 07:00:27 PST
- The beneficial effects of Ferula asafoetida oleo-gum resin in
gastrointestinal disorders
Authors: Mohaddese Mahboubi
Abstract: Ferula asafoetida is a plant from Umbelliferae Family, which its gum is traditionally used to treat the gastrointestinal disorders (parasite, bloating, digestion, cancer). According to its traditional applications, the subject of this review was to evaluate the efficacy of F. asafoetida in management of different gastrointestinal disorders in modern medicine. For this purpose, the scientific resources (PubMed, Web of Science, Scopus, Google Scholar, SpringerLink, SciFinder, ACS Publications, and Wiley), traditional books, and thesis were investigated by the word of Ferula asafoetida, Hing, and gastrointestinal tract and the results were evaluated. There was one clinical trial on the efficacy of F. asafoetida in treatment of functional dyspepsia, and the other pharmacological activities such as anti-parasite, anti-cancer, anti-diarrhea and liver protective effects were evaluated in preclinical studies. Although, F. asafoetida can be proposed as a good candidate for treatment of gastrointestinal disorders, but the majority of studies have been limited to the experimental investigations. Therefore, evaluation of its efficacy and safety in well-designed human clinical studies is required to use of this valuable oleo-gum resin.
PubDate: Thu, 24 Feb 2022 09:25:27 PST
- The Efficacy of Oral Ivabradine in Acute Phase in Non ST-segment Elevation
Myocardial Infarction (NSTEMI) Post PCI: A Pilot Study
Authors: Manar M. Ahmed et al.
Abstract: Background: An elevated heart rate is a major risk factor for cardiovascular mortality and morbidity. This study aims to evaluate the beneficial effect of heart rate reduction of oral ivabradine in patients presenting with non ST-segment elevation myocardial infarction (NSTEMI) during acute stage post percutaneous coronary intervention. Results: A total of 100 patients admitted to the emergency department, National Heart Institute, Cairo, Egypt, were randomized into two groups as follows: Group A: 50 patients with NSTEMI treated with ivabradine (5 mg twice daily) in addition to the conventional treatment; Group B: 50 patients with NSTEMI treated with the conventional treatment only. Demographic data, detailed history, clinical examination, chest pain onset, blood pressure, heart rate (HR), temperature and respiratory rate, electrocardiogram (ECG) as well as echocardiography and laboratory investigations were recorded. Patients were monitored for a period of 3e5 days (acute stage). There was a significant difference between both groups regarding reduction of heart rate on discharge in patients presenting with NSTEMI (P < 0.05). However, there was no significant differences in mortality, heart failure (HF), cardiogenic shock, arrhythmia and any mechanical complications in the acute stage. Conclusion: Ivabradine significantly reduced heart rate in patients with NSTEMI without affecting blood pressure or hemodynamics; however, this did not show a significant impact on major adverse cardiac events (MACE) during shortterm follow up in the Coronary Care Unit (CCU) (Clinicaltrials.gov NCT04285736).
PubDate: Thu, 30 Dec 2021 13:35:23 PST
- Knowledge, Attitude, Practices, and Barriers of Pharmacovigilance among
Healthcare Workers: A Cross-sectional Survey from Lahore, Pakistan
Authors: Zia U. Mustafa et al.
Abstract: Background: Adverse drug reactions (ADRs) are associated with increased length of hospital stay, permanent disability and even death. Objectives: The purpose of this study was to assess knowledge, attitude, practice (KAP), and barriers related to Pharmacovigilance (PV) among Pakistani healthcare workers (HCWs). Methods: A cross-sectional study was conducted in the second largest metropolitan city (Lahore) of Pakistan during a period of 4 months (JuneeSeptember 2018). A self-administered questionnaire was used to collect data from the doctors, pharmacists, and nurses from 8 tertiary care hospitals, recruited via convenient sampling. All data were analyzed in SPSS version 21. Results: A total of 363 participants (125 doctors, 83 pharmacists and 155 nurses) were recruited. The median [interquartile range (IQR)] knowledge score was 6 (3), with 44.6, 41.9, and 13.5% of participants having poor (score < 6), moderate (score 6e9), and good (score ≥ 10) PV related knowledge, respectively. Additionally, the median (IQR) attitude and practice score were 7 (3) and 4 (2), respectively [good attitudes 24.8% (score ≥ 8); good practices 33.9% (score ≥ 5)]. Pharmacist were found to have significantly better KAP related to PV than others (p < 0.001). Moreover, male HCWs had substantially better KAP than females. Conclusion: Although pharmacist have better KAP scores than other HCWs, yet overall KAP of PV among study participants were inadequate. Thus, continuous training and teaching programs should be conducted to improve awareness and to promote ADR reporting.
PubDate: Thu, 30 Dec 2021 13:35:18 PST
- Study the Effects of Taurine Oral Supplement used for Type 2 Diabetic
Patients on Body Weight; Glycemic Control and Some Bone Mineralization
Biochemical Markers
Authors: Falah Hassan Sheri et al.
Abstract: Background: Taurine is sulfur containing semi-essential amino acid that has important roles in many biological processes, but; its effects on glucose homeostasis, weight; growth and bone mineralization were not well defined in human. Objectives: evaluation the effects of oral taurine used for 3 months on bone mineralization biomarker; glycemic control and body weight in type II diabetic patients. Methods: interventional double-blind placebo-controlled study in which 80 patients with type2 diabetes mellitus (age range 45e55) assigned in either control (n ¼ 40) or study (n ¼ 40) group. The last group received 1000 mg capsule of taurine once a -d for three months. Parameters measured were serum calcium, 25(OH) vitamin D and osteocalcin, NTX-1; HbA1C% and Fasting blood glucose before and after 3 months. Results: Taurine led to significant (p < 0.05) rise in osteocalcin and significant lowering in Body weight and BMI and there were no significant changes in Serum Calcium; NTX-1; Vitamin D; HbA1C% and fasting blood glucose; all as compared with control values. Conclusion: 3 months of oral Taurine used in type II diabetic patients may modulate bone mineralization represented by elevation of osteocalcin; and reduction of body weight, but has no significant effect on glycemic control and did not reduce HbA1C%
PubDate: Thu, 30 Dec 2021 13:35:15 PST
- QBD based Design and Characterization of Proniosomal Transdermal Delivery
of Atenolol and Glibenclamide Combination: An Innovative Approach
Authors: P Anitha et al.
Abstract: There are numerous circumstances where chronic disease is associated with other disorders, especially in diseases like diabetes with noncommunicable disease risk factors, such as hypertension. This study shows a novel and innovative combinational proniosomal delivery of combination to beat the reactions by complex therapeutic regimen, and to improve patient compliance after controlling combinational transdermal delivery of Glibenclamide (GLB) and Atenolol (ATN) which have not been tried actually. To achieve the above reason, proniosomes were prepared and optimized utilizing Box-Behnken design. The ideal formulation was chosen by a point prediction method and formulation showed vesicle size of 562 ± 1.223 nm, entrapment efficiency of GLB & ATN 97.037 ± 1.43% and 96.230 ± 1.62% respectively which were found in concurrence with the predicted value. The optimized combinational proniosomal gel (OCPG) formulation was additionally assessed for in vitro drug release, In vitro drug permeation, and in vivo pharmacokinetic study. The OCPG formulation shows the greatest flux over the rabbit skin (128.609 ± 2.24 mg/cm2/h and 322.054 ± 1.53 mg/ cm2/h) of GLB and ATN respectively. The results indicated desired release and permeation profiles. OCPG showed significantly (p < 0.001) pharmacokinetic contemplate exhibited that transdermal proniosomal formulation demonstrated improvement in bioavailability of two drugs 129.30 and 174.62 times respectively as that of the oral formulation. Overall the results show that controlled release GLB and ATN provesicles offer a useful and promising transdermal delivery system for the treatment of type II diabetes and hypertension by using design. Henceforth this may be an achievement in treating diabetic hypertensive patient.
PubDate: Thu, 30 Dec 2021 13:30:20 PST
- The Use of Natural Polymers in Formation of Polyelectrolyte Complexation
Authors: Niharika Lal et al.
Abstract: In recent years, great advances have been made towards the development of various techniques for novel drug delivery systems. These techniques focus on the rate of drug delivery, duration of action and site of action. One of such technique in fabricating novel drug delivery system is the use of polymers in development of in-situ drug delivery systems. Polymers used as carriers have revolutionized over the years. The formation of a polymer complex with other oppositely charged polymers resulted in the formation of polyelectrolyte complexes, which possess unique physicochemical properties with high biocompatibility. The polyelectrolyte's themselves are characterized as cationic, anionic and non-ionic according to the nature of the functional group present at the polymer chain, type of macromolecules formed and interaction forces existing between the complex formed. Additionally, these natural complexes avoid the use of chemical agents for cross linking of polymeric chains, thereby limiting toxicity. Due to their sustain and convenient way to deliver highly water soluble drugs they could target therapeutically active moiety to the site of action, and for these reasons they have led to various applications in the biomedical sector, in pharmaceutical and nano biotechnology industries. Thereby the use of polymers in in-situ drug delivery offers many benefits because of their sustained and prolonged drug delivery action when compared with other conventional drug delivery systems. The present review focuses on the use of natural Polymers in polyelectrolyte complexes as a drug delivery technology.
PubDate: Thu, 30 Dec 2021 13:30:16 PST
- Determination of Spiramycin and Oxytetracycline in binary mixtures by
novel spectrophotometric methods with and without regression equation
Authors: Afaf Abou El Khaira et al.
Abstract: Spiramycin (SPI) and oxytetracycline (OTC) are widely used antibacterial drugs. Thus, a great attention has been focusing on the development of a simple and selective analytical procedure for fast analysis of these compounds in a binary pharmaceutical mixture. Herein, we report four simple and reproducible spectrophotometric methods for determination of SPI and OTC in a binary mixture and in veterinary pharmaceutical formulations. A ratio difference (RD) based on the difference in the amplitude of the ratio spectra and dual wavelength methods were proposed for sensitive and selective determination of SPI in presence of OTC. Furthermore, Constant Value and Concentration Value based spectrophotometric methods were suggested for simultaneous determination of SPI and OTC in a binary mixture. The methods were successfully applied for the determination of SPI and OTC over the concentration range from 4.0 to 36.0 µg mL-1 and from 2.0 to 32.0 µg mL-1, respectively. The proposed methods were validated according to the International Conference on Harmonization (ICH) guidelines. The methods are accurate (100±1%), precise (%RSD ≤1.5) and cost-effective for determination of SPI and OTC in binary mixtures.
PubDate: Wed, 18 Aug 2021 14:25:25 PDT
- A critical review on the plants used for the treatment of ulcer in Kerala
Authors: Jincy Jacob et al.
Abstract: Peptic ulcer disease and its complications remain the cause of significant morbidity worldwide, representing a major burden for health care resources. Although potent anti-ulcer drugs are available, most of them produce several side effects, thus emphasizing the need to search for new alternatives. As high as 80% of the world population depends on plant- derived medicines for the first line of primary health care, reinforcing the theory that plant extracts can be good sources of new drugs. This review focuses to consolidate the evidence-based information on antiulcer plants used in Kerala accumulated in databases (Google Scholar, PubMed, Scopus, Science Direct and Web of Science) upto January 2019. Plants like Acacia nilotica L., Achyranthes aspera Linn., Aegle marmelos L., Allium sativum L., Aloe barbadensis Miller, Annona muricata Linn., Bacopa monnieri Linn., Carica papaya Linn., Centella asiatica Linn., Curcuma longa Linn., Elettaria cardamomum Linn., Hibiscus rosa-sinensis Linn., Mangifera indica Linn., Mimosa pudica L., Moringa oleifera Linn., Ocimum sanctum Linn., Piper nigrum Linn., Phyllanthus emblica Linn., Terminalia chebula Retz., and Zingiber officinale Roscoe. are available in Kerala, reported with antiulcer activity. The secondary metabolites present in the plants like alkaloids, flavonoids, terpenoids, tannins, glycosides, terpines, and resins also have an important role in reliving ulcers due to its antisecretory, antioxidant, and cytoprotective properties. This review summarizes the botany, ethnopharmacology, phytochemistry and mechanism of action of antiulcer plants.
PubDate: Wed, 18 Aug 2021 14:25:24 PDT
- Design, Synthesis and Antibacterial Studies of Some New Pyridopyrimidine
Derivatives as Biotin Carboxylase Inhibitors
Authors: Vivek B. Panchabhai et al.
Abstract: Present study reports the development of novel pyridopyrimidine derivatives as biotin carboxylase inhibitors with potent antibacterial activity. These compounds were designed to avoid possibility of resistance development. Accordingly eighteen compounds were synthesised and characterized on the basis of spectral data. These compounds were tested for their antibacterial potential by the enzyme kinetic assay against the biotin carboxylase. The minimum inhibitory concentration (MIC) and single step resistance studies were also performed. Compound 2-((2-Phenylpyrido[2,3-d]pyrimidin-4-yl)amino)phenol (6o) showed promising activity in biotin carboxylase inhibition with low MIC. It showed molecular docking score of -7.96, this compound showed formation of hydrogen bonds with the active site residues and van Der Walls intractions. The MIC of compounds under investigation was in the rage of 2-5µg/mL over most of the strains studied. It also showed the mutant selection windows of around five which is better than the reference compound rifampin. This compound 6o can be studied further and developed into a potential antibacterial lead molecule.
PubDate: Wed, 18 Aug 2021 14:25:24 PDT
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