Posted by admin on Nov 30, 2019 in |
Allium cepa L. has known potent antidiabetic effects due to several of its constituents, including kaempferol -3-O-β-D-6”-(p-coumaroyl) glucopyranoside (kaempferol). This preliminary work was aimed at preparing oral hard gelatin capsules of kaempferol obtained from Allium cepa L. In order to obtain more potent hypoglycemic activities, lower side effects with good patient compliance over the crude extract kaempferol were isolated from Allium cepa L. and formulated into capsule dosage form. The capsules were prepared by filling hard gelatin capsule shells with blends of kaempferol with excipients which included Avicel® PH102, agglomerated lactose®, Primogel®, Ac-Di-Sol®, maize starch, stearic acid, and talc. The blends were evaluated for their micrometric properties such as bulk densities, tapped densities, Hausner’s quotients, compressibility indices, true densities, flow rate and angle of repose. Prepared capsules were evaluated for weight variation, disintegration time, content uniformity, dissolution profiles and antidiabetic properties in alloxan-induced diabetic rats with distilled water and glibenclamide respectively as negative and positive controls. The capsules were of good properties with disintegration time (2.75 ± 0.22 –...
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Posted by admin on Nov 30, 2019 in |
Purpose: Helicobacter pylori (H-pylori) infection has been commonly associated with gastric ulcers. Lepidium sativum (L. Sativum) is an herbaceous edible plant, botanically related to mustard and watercress with remarkable pharmacological features. In this study, we investigate the anti-microbial and anti-oxidant effect of L. sativum seed methanolic extract in-vitro and correlate this with the gastroprotective potential of this extract against H-pylori–induced gastric ulcer in an in-vivo model. Methods: L. sativum extract was quantified for phenolic compounds using high-performance liquid chromatography, and the anti-microbial and anti-oxidant activities of the extract were evaluated in-vitro. Furthermore, an in-vivo rat model was assessed in order to explore the effect of L. sativum extract against H. pylori-induced gastric ulcer in-vitro. Results: The L. sativum extract exhibited significant antioxidant and anti-microbial activities against different pathogenic organisms. In vivo, L. sativum extract reduced the ulcer index, increased the percentage of ulcer inhibition, halted lipid peroxide and triggered anti-oxidant markers. Moreover, it suppressed inflammatory and apoptotic markers. The histopathological results for L. sativum treated rats showed the amelioration...
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Posted by admin on Nov 30, 2019 in |
A simple, accurate and precise UPLC method was developed and validated for dissolution testing of Lamivudine, Tenofovir disoproxil fumarate and Efavirenz in tablet dosage form. The separation was achieved under optimized chromatographic condition on an Acquity UPLC BEH (50 mm × 2.1 mm, 1.7 μm) column with mobile phase consist of 20 mM potassium dihydrogen phosphate buffer pH 2.5: acetonitrile with gradient elution at a flow rate of 0.37 mL/min using 35 °C column oven temperature with UV detection at 260 nm. The method was validated as per ICH and USP guideline and the values were found to be within the limits. So, the proposed method was found to be simple, linear, accurate, precise, robust and...
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Posted by admin on Nov 30, 2019 in |
A new series of hydroxamic (5a-5j) and carboxylic acid analogs (4a-4j) based on the 1, 3, 4-thiadiazole scaffold was designed and synthesized to explore its potential as new antitumor agents. The chemical structures of the compounds were confirmed based on TLC, IR, 1H NMR, and 13C NMR analysis. Molecular docking studies showed that the target compounds correctly dock into the binding pocket of histone deacetylase inhibitor (PDB Code 1w22 reference compound), while their bioavailability / drug-likeness was predicted to be acceptable. The predicted physicochemical were compared with those of a reference compound. Biological results revealed that the structural modifications proposed significantly affected inhibitory potency as well as selectivity for HDAC inhibitors. Most target compounds were significantly more active specifically 5a, 5b, 5e with IC50 values in the low micromolar or, the most active compounds in the series. Selected compounds were tested on the viability of MDA-MB-231 (breast cancer cell) and K562 (chronic myelogenous leukemia cell), A549 (human lung cancer), PC3 (Prostate cancer cell lines) using MTT...
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Posted by admin on Nov 30, 2019 in |
Type 2 diabetes mellitus poses an important health care problem because of its associated two to threefold increased risk of cardiovascular disease and its high prevalence and incidence worldwide. Dyslipidemia is an independent risk factor for severe morbidity and mortality in terms of cardiovascular risk in type-2 DM patients. Studies have shown an association between metformin and lipid profile changes although results are inconclusive. Thus, this study was done to evaluate the changes in serum lipid profiles in patients who are newly started on metformin. It was a prospective, observational and non-interventional study. 50 newly diagnosed patients of type 2 DM were enrolled and started on metformin. Lipid profile was assessed before starting treatment and then after 12 weeks. Statistical analysis was done using paired t-test. In results serum total cholesterol, triglyceride and VLDL were significantly decreased after 12 weeks of metformin therapy. The apparent change was also observed in serum LDL and HDL, but it was not statistically significant. Thus, it may be speculated that metformin has beneficial...
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