Posted by admin on Jul 31, 2022 in |
Introduction: The seeds of Aegle marmelos (bael) are less explored for their therapeutic activity; cytotoxic activity of bael seeds was yet to be studied. The present study aims at finding the cytotoxic activity of the successive extracts and the flavonoid fraction from the methanolic extract of the seeds. Methods: The extracts were prepared using solvents (petroleum ether, chloroform, ethyl acetate, methanol, and water) in increasing order of their polarity. Anti-oxidant activity of the extracts was evaluated using DPPH radical scavenging assay, nitric oxide scavenging assay, and hydrogen peroxide scavenging assay. Flavonoid fractions were obtained by thin-layer chromatography of the flavonoid-rich fraction prepared from the total methanolic extract. Human colon cancer cell line (HT 29), human breast cancer cell line (MCF-7), human lung cancer cell line (A-549) were used to evaluate the cytotoxicity of the extracts and the flavonoid fractions. Results: Various phytochemicals like alkaloids, flavonoids, tannins and phenols, steroids, and saponins were detected in phytochemical investigation of the extract. Ethyl acetate fraction showed comparable DPPH radical scavenging activity and...
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Posted by admin on Jul 31, 2022 in |
As per the ICH guidelines and regulatory authorities’ worldwide, it has become mandatory to establish a stability-indicating assay method (SIAM) for the drug substance (DS) and drug product (DP) to generate the stability data. It was undertaken to develop a precise, accurate, reliable, rapid, simple and specific method for estimating Teneligliptin free of interference from its probable degradation products. The present investigation has exploited the high-performance liquid chromatography (HPLC) technique. The retention time of Teneligliptin under optimized chromatographic conditions was found to be 5.71 ±0.02 min with a sharp, symmetrical peak (asymmetry of 0.66 ± 0.02). In the system suitability, the drug was found to adequately retain at 5.71 ±0.02 min with a sharp, symmetrical peak and high theoretical plate value of 4808, indicating high column efficiency. The solutions were observed to undergo hydrolysis in 0.1 N HCl and 0.1 N NaOH at room temperature and reflux. Teneligliptin was also found to be susceptible to rapid oxidation. Photolytic stress study indicates that drug in solid-state upon exposure to sunlight...
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Posted by admin on Jul 31, 2022 in |
Background: The current study used computational approaches to investigate the molecular, physicochemical and drug-like properties of some 4-(10-acetyl-10H-phenothiazines-3-yl)-1-phenylazetidin-2-one derivatives. Methods: The structures of the compounds were drawn using Chemdraw ultra12 and smiles were generated using ACD chem sketch software. The physicochemical and molecular properties were calculated using the OSIRIS data warrior, and Toxicity potential, pharmacokinetic profile and medicinal chemistry aspects were determined by Swiss ADME tools. The docking analysis was carried out by mCule for the antimicrobial and anti-inflammatory profiles. The compounds were targeted for beta-lactamase, peptidoglycan hydroxylase, Cyclo-oxygenase-1 and 2 inhibitions. Result: All the compounds exhibited moderate to good drug likeliness and pharmacokinetic potential. The molecules showed good bioactivity scores against enzyme receptors. The ADMET prediction showed PGP and CYP-inhibitory effects with the least toxic profile. The docking analysis showed good binding affinity toward beta-lactamase, peptidoglycan hydroxylase and cycloxygenase-1 enzymes. Conclusion: The compounds showed good drug likeliness properties along with good toxicity potential and pharmacokinetic profiles. From docking analysis, it was found that all the molecules had a good...
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Posted by admin on Jul 31, 2022 in |
Background: In the Unani System of Medicine, Sandal safed (Sandalwood) is used in many cardiac problems as it possesses Mufarreh (exhilarant) and Muqawwi Qalb (cardiotonic) activities. The present study was designed to evaluate the cardioprotective effect of Sandal safed in Isoproterenol-induced Myocardial Infarction. Methods: Male Wistar rats, weighing 150-200gm, divided into five groups of ten in each. Group I and III rats were given 5% gum acacia (vehicle) and Sandalwood powder in the dose of 800 mg/kg body weight, orally once daily for seven days, followed by subcutaneous administration of normal saline on the 8th and 9th day. Group II, IV & V were administered 5% gum acacia, test drug in the dose of 600 & 800mg/kg body weight, orally once daily for seven days, respectively, followed by isoproterenol hydrochloride (50 mg/ kg body weight) subcutaneously, twice at an interval of 24 h on 8th and 9th day. On 10th day, animals were sacrificed, heart and adrenal glands were weighed, and serum cardiac enzymes and lipid profile were analysed....
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Posted by admin on Jun 30, 2022 in |
A series of novel N10 -substituted 2,4-Dimethoxy acridones were synthesized as potent cytotoxic agents. DNA-binding studies of the synthesized compounds were carried out by the HPLC method using Calf thymus DNA (CT – DNA) based on their affinity or intercalation with CT-DNA, measured by binding percentage. The compound 12 bearing planar dimethoxy tricyclic ring linked with butyl pyrazole side chain showed the highest percentage of binding (90.78%) with CT-DNA and showed binding affinity of -6.08 Kcal/mol with the lipophilicity value of 3.33. Compound 8 showed the highest lipophilicity value of 5.09 with a binding affinity of -6.04 Kcal/mol and a percentage of drug binding (80.93%). Compound 5 showed high binding affinity of 7.01 Kcal/mol with percentage of drug binding (66.94%) and lipophilicity value of 3.72. The Binding affinity and percentage of drug binding showed favorable results. The docking outcome was in good agreement with DNA-binding results confirming the DNA binding activity of compounds. The lipophilicity and binding ability of the acridones with CT-DNA showed poor...
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