Posted by admin on Nov 1, 2012 in |
Quantitative structure activity relationship (QSAR) studies ware performed on series of structurally similar heterocyclic sulfonamide with enzyme gamma secretase inhibitor activity. The compounds were divided into training and test set and generated different QSAR models using V-Life MDS 3.5 software multiple linear regression (MLR) method. Best QSAR models were selected on the basis of various statistical parameters like square correlation coefficient (r2), cross validated square correlation coefficient (q2), pred_r2, standard error of estimation (SE) and sequential Failure test (F). 2D QSAR study reveals that gamma secretase inhibitor activity is governed by physicochemical Alignment Independent (AI) descriptors and design new compounds, with more potent activity. The best models were found to be Model–I model-II and model-III. Model-I having 5 descriptors, r2 = 0.8582, q2 = 0.5701, Failure test = 22.9812 and predicted r2 = 0.7513. Model-II having 4 descriptors, r2 = 0.8170, q2 = 0.6780, Failure test = 18.9765 and predicted r2 = 0.6193. Model-III having 4 descriptors, r2 = 0.8248, q2 = 0.7006, Failure test = 20.0027 and predicted...
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Posted by admin on Nov 1, 2012 in |
The aim of this research was to investigate cytotoxic effects of crude extracts of Caesalpinia pulcherrima (Family: Fabaceae). The flower of Caesalpinia pulcherrima was extracted with methanol and methanolic extract was fractionated into three fractions like n-Hexane, ethyl acetate and chloroform. The methanolic crude extracts were screened for cytotoxic properties using brine shrimp lethality bioassay. A reputed cytotoxic agent vincristine sulphate was used as a positive control. From the results of the brine shrimp lethality bioassay it can be well predicted that n-hexane, ethyl acetate, chloroform soluble fractions of Caesalpinia pulcherrima flower possess cytotoxic principles (LC50 1.940mg/mL, 2.704mg/mL and 8.359mg/mL respectively) comparison with positive control vincristine sulphate (LC50 0.563...
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Posted by admin on Nov 1, 2012 in |
In the present study, the endophytic actinomycetes were collected from three medicinal plants Azadiracta indica, Ocimum sanctum and Phyllanthus amarus. Endophytic actinomycetes were isolated using different media like Starch casein agar, Starch casein nitrate agar, Actinomycetes isolation agar and Soyabean agar, while it showed more colonies in Starch casein agar. The endophytic actinomycetes were stained and biochemical tests were performed. Antimicrobial compound was purified from the filtrate by ethanol extraction method. Antagonistic activities of endophytic actinomycetes isolates were tested against bacterial pathogens (Staphylococcus aureus, Streptococcus pyogenes, Klebsiella pneumoniae and Pseudomonas aeruginosa) and the fungi Rhizopus. For the selected isolates antibiotic resistance was checked using various antibiotic discs like Amoxycillin, Penicillin, Rifampicin and Ampicillin. The strains which showed efficient antibacterial activity were selected to study the effect of mutation by physical and chemical method. In this study, UV mutated endophytic actinomycetes increase antibiotic production than non-mutated endophytic Actinomycetes, whereas in chemical mutation it does not increase the antibiotic...
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Posted by admin on Oct 1, 2012 in |
Cancer is a group of disease characterized by unregulated cell growth and spread of cells from site of origin to other sites in body. Two main genetic changes lead to cancer they are inactivation of tumour suppressor gene and activation of proto-oncogene. Ras gene is a proto-oncogene, when this gene activated it stimulates signalling pathway and that causes unregulated proliferation of cells. Ras family is a group of three precursors H-Ras, K-Ras and N-Ras. It was analyzed that more than 30% of cancers occurs due to Ras gene. But most of the Ras related cancers are occur due to mutations in H-Ras gene. In H-Ras gene codons 12, 13 and 61 are hotspots. Bioinformatics tools are help to find out the amino acid sequence from which got the gene sequence of H-Ras. Using the H-Ras gene sequence, six primer pairs were designed to amplify the DNA of patients with the potential mutations. Designed primers can be used for the diagnosis of H-Ras related...
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Posted by admin on Oct 1, 2012 in |
FDTs are designed to disintegrate rapidly on contact with saliva and enables oral administration without water or chewing, these formulations offer increased convenience and ease of administration with the potential to improve patient compliance, particularly in certain populations, where swallowing of conventional solid oral dosage forms presents difficulties. In the present study, the effect of a natural superdisintegrant Fenugreek and synthetic superdisintegrants sodium starch glycolate (SSG) was compared in the formulations of fast dissolving tablets (FDT). FDTs of Diclofenac (model drug) were prepared by direct compression method. These tablets were evaluated for weight variation, hardness, thickness, disintegration time, water absorption ratio, friability and dissolution. Swelling index was also investigated with an aim to compare the swelling property of Fenugreek with Sodium starch glycolate (SSG). Fenugreek showed higher swelling index than SSG. Hence, the present study revealed that this natural superdisintegrants showed better disintegrating property than the most widely used synthetic superdisintegrants like...
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