Posted by admin on Aug 31, 2016 in |
Docking and site directed mutagenesis approach was used to explore mode of binding and inhibition for human acetylcholinesterase (hAChE) and organophosphates (OPs). More than 200 OP molecules were investigated using Glide docking module of Schrodinger suit as co-crystal structure between two are not available in Protein Data Bank. In initial screening Trp86 was found to be involved in maximum Pi-Cation interaction on anionic subsite of hAChE other than Ser203 (Catalytic site). With extra precision glide docking Phoxim Ethyl Phosphonate (PEP) tops among 200 OPs based on glide docking score and interacted with Trp86, Gly121 and Ser203 whereas MM-GBSA score shows less binding affinity than heptenophos and dichlorovos. Trp86 preferred Pi interaction with ring bearing OPs and hydrophobic interactions with smaller OPs without ring bearing structures. Site directed mutagenesis at Trp86 (Trp86 to Ala86) shown the deterioration of the binding site in terms of size reduction, loss of electrostatic and geometric stabilization in binding cavity and significant reduction in binding of OPs in preferred orientation. Dock score of both wild...
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Posted by admin on Aug 31, 2016 in |
Present study was conducted to know the antifertility potential of Achyranthus aspera leaves in female mice and has shown promising results of antiovulatory activity, estrogenic and constant teratogenic activities. Administrations of A. aspera leaves methanolic extract at the dosage 25 mg/kg and 50 mg/kg body weight were subjected for testing their antiovulatory, estrogenic and teratogenic activity in female mice by applying statistical analysis in gravimetric, biochemical and histopathological parameters of ovary and uterus. At autopsy on day 31st, both the dose treated mice revealed increase in ovarian weight, histological changes like increasing number of atretic follicle and decreases in healthy developing follicles, Graafian follicles and corpora lutea. Total cholesterol content and alkaline phosphatase of the ovary were increased and protein, glycogen, acid phosphatase content were decreased. Teratogenic activity did not alter any changes in the morphological and physiological behavior of experimental period. Results suggested that, methanolic extract of A. aspera leaves are more active at low dose compared to high dose and might be used as an herbal contraceptive...
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Posted by admin on Aug 31, 2016 in |
Background: Venous thromboembolism (VTE) is a common complication during and after hospitalization for medical patients. Previous studies have shown that only about one third of high risk medical patients receives VTE prophylaxis. Guidelines such as the one produced by the American college of Chest Physicians (ACCP) are aimed at reducing hospital associated VTE. The objective of this study was to determine the appropriateness of VTE prophylaxis in medical inpatients at a large teaching hospital. Methods: In a prospective cross-sectional study, VTE prophylaxis were evaluated and the data were recorded during October 2014 to March 2015 in medical wards of “Alzahra” hospital, Isfahan, Iran. A caprini score, a VTE risk factor assessment tool was calculated for each patient based on data collected. Appropriate prophylaxis was determined after examining data, caprini score and prophylaxis regimen according to the ACCP 9th edition guideline. Results: A total of 100 patients met the inclusion criteria and were reviewed. According to the risk stratification, 18 patients classified as low risk, 30 as moderate and 47...
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Posted by admin on Aug 31, 2016 in |
Simple, specific, accurate and cost economic UV spectrophotometric methods were developed and validated for determination of Celiprolol Hydrochloride. Instead of using organic solvents, mixture of dilute hydrochloric acid and water was used during method development and validation. The drug was extracted from tablet formulation with a mixture of water and hydrochloric acid. Stability of drug solution and formulation was established throughout the analysis time. Zero Order Derivative and Area Under Curve methods were developed for estimation of drug and both the methods were validated as per ICH guidelines. The linearity of drug was established by performing calibration curve. The analytical range of drug was established from linearity study. Precision of the method was established with Intraday and interday analysis. Accuracy was established by conducting recovery study. Robustness of both the methods was confirmed by conducting analysis with different...
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Posted by admin on Aug 31, 2016 in |
This project involves in the development of sustained release matrix tablets of Gemigliptin. Which is an oral anti-hyperglycemic agent designed for the management of non insulin dependent diabetes mellitus (NIDDM). The basic goal of therapy is to achieve a steady sate blood level that is therapeutically effective and non toxic for an extended period of time. The objective in dosage form design is to optimise the delivery of medication to achieve the control of therapeutic effect in the face of uncertain fluctuation in the in-vivo environment in which drug release takes place. Eight formulations of Gemigliptin 50mg were formulated by admixing with HPMC K4M, Carbopol were used as rate controlling polymers in different concentrations, Micro crystalline cellulose, Lactose, Talc, Magnesium stearate. Pre-formulation and post-formulation studies were carried out and the values obtained, satisfies the pharmacopoeial specifications. Several kinetic models were applied to the dissolution profiles to determine the drug release kinetics. Of all the formulations F5 exhibited gradual and completion extended release for Gemigliptin. The F5 (carbopol) with 1:1...
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