Akhtarnoer6646
Acacia jacquemontii Benth. is used traditionally to treat hypertension but no scientific literature supports this claim. So, this study was aimed at validating this claim. This was done by injecting various doses of crude extract of Acacia jacquemontii, AJC (5, 10, 20, 30mg/kg) and all fractions (hexane, ethyl acetate, n-butanol and aqueous) (3, 5, 10, 20mg/kg) intravenously in anaesthetized rat. Based on the results, butanol fraction (AJB) at 20mg/kg was found to be the most potent, so it was selected for exploring mechanisms of action. For this purpose, different groups were injected with various pharmacological inhibitors (L-NAME, atropine, captopril, propranolol and hexamethonium) prior to AJB administration. Also, AJB at 20mg/kg was evaluated for prolonged hypotensive effect for the period of 40 min. Results showed a significant dose dependent reduction in BP in normotensive and in hypertensive rats. AJC and AJB produced a decline in SBP, DBP and MAP with p less then 0.05 - p less then 0.001 and p less then 0.001 respectively in normotensive animals. Whereas in hypertensive animals, AJC showed significant reduction at 5mg/kg with p less then 0.01 and at 10, 20 and 30 mg/kg with p less then 0.001. AJB produced a decline in hypertensive animals at all tested doses with p less then 0.001. AJB resulted in hypotensive effect mediated by β receptors, ganglionic block operating central sympathetic neural responses and renin angiotensin aldosterone system (RAAS). This study supports the ethnomedicinal claim of Acacia jacquemontii Benth. in treating hypertension.Emergence and spread of multidrug resistant (MDR) Staphylococcus aureus strains is becoming major challenge in treatment of soft tissue infections. This study aimed to explore antimicrobial and synergistic antimicrobial potential of three commercially available thiazoline derivatives (2-amino-2-thiazoline, 2-thiazoline-2-thiol and 2-acetyl-2-thiazoline) against MDR Staphylococcus aureus strains isolated from abscess drainage samples (n=20). MDR Staphylococcus aureus isolates were identified by Kirby-Bauer disk diffusion assay and were further subjected to molecular identification by 16srRNA amplification and DNA sequencing. Minimum Inhibitory Concentration (MIC) values of test compounds and antibiotics (0.25-512μg/mL) were measured and subsequently, synergism assay was performed to calculate Fractional Inhibitory Concentration (FIC) index. Out of twenty Staphylococcus aureus isolates, sixteen (80%) were found to be MDR whereas four (20%) were Non-MDR. Moxifloxacin and vancomycine were found most effective antibiotics, inhibiting 100% (n=20) and 95% (n=19) strains respectively. Antimicrobial activity of 2-amino-2-thiazoline (MIC 32μg/mL), 2-thiazoline-2-thiol (MIC 64μg/mL) and 2-acetyl-2-thiazoline (MIC 32μg/mL) was found significant against all ten tested MDR strains. Synergistic combinations of thiazoline derivatives with test antibiotics reduced MIC values significantly. Therefore, combination of tested thiazoline derivatives with antibiotics could be used as alternative therapeutic approach to treat soft tissue infections caused by MDR Staphylococcus aureus after further pre-clinical and clinical studies.Numerous ailments have been effectively treated with natural plants for long time all over the world. Plants provided a back bone for the exploration of novel medicinal compounds. Therefore, chief focus of our study was to isolate the biologically active compounds from the plant source and evaluate their antidiarrheal potentials, as diarrhea is still the most dominant disease in developing countries. The isolation and structure elucidation of two new compounds were identified from methanolic and chloroform extracts of Psidium guajava (guava) leaves. Extracts of plants were acquired by successive maceration from dried powder. Castor oil induced diarrheal-model was used to evaluate the antidiarrheal activity and therapeutic response was endorsed to the suppression of normal and wet stools in Spraug Dawley rats. Through the series of fractionations, compound-A was obtained from methanolic extract and named 3-(4-amino 1,3,8-tri-OH 5,6-di-CH3 7-propyl 1,2,3,4,4a,5,8,8a-octahydronaphthalen 2-yl) propanoic3-(4-NH3 7-butyl 1,3,8-tri-OH 5,6-di-CH3 1,2,3,4,4a,5,8,8a-octahydronaphthalen 2-yl)propanoic anhydride. Compound-B was entitled 5-(3-hydroxy-1,4-di-CH3-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-yl)pent-3-enoic acid was acquired from the chloroform extract. The structure elucidations of both compounds were interpreted through spectroscopic data, including EI-MS, FTIR, 1HNMR and 13C-NMR. Selleck PARP/HDAC-IN-1 The significant antidiarrheal activities were determined with crude extracts and isolated compounds. In inference, present study revealed that substantial antidiarrheal feature of guava is confined to the identified compounds.Hepatitis C virus (HCV) has major role in spreading of liver diseases worldwide. The HCV nonstructural NS5B is a polymerase (RdRp) that is present at the carboxylic-end of the polyprotein chain. It is essential and most important for the replication cycle. In current study, the potential of 100 phytochemicals against HCV NS5B polymerase was determined. Phytochemical structures were retrieved from PubChem database. The phytochemicals were docked with the NS5B active site amino acids, in order to discover their attractions as inhibitors. After docking, molecules with top five conformations were selected from 100 molecules by docking scores and RMSD values. The results demonstrated strong interactions of phytochemicals with the NS5B. The selected compounds with best docking scores and RMSD were found to be glycitein, ferulic acid, eugenol, 1-octanol and sebacic acid. These were further evaluated through Lipinski's rule of five to explore their molecular properties and drug-likeliness characteristics and all five selected phytochemicals were found to have drug-likeliness characteristics. Further, according to ADME analysis, the ferulic acid, 1-octanol and eugenol were found to be nontoxic, non-carcinogenic and have the ability to cross the blood brain barriers. Therefore, these phytochemicals could be strong drug candidates for HCV NS5B.