Posted by admin on Apr 30, 2018 in |
Spleen tyrosine kinase (Syk) is a member of tyrosine kinase family protein. Syk protein plays a vital role during intracellular signal transduction from high affinity IgE receptor (FcεRI) in allergic reaction. Flavonoids are well known compounds for their anti-allergic properties. In this present work, thirty-four structurally similar flavonoids are investigated as Syk inhibitors by using 3-dimensional quantitative structure-activity relationship (QSAR) models and molecular docking studies. By applying genetic algorithm (GA) method, different types of 3D-MoRSE descriptors are selected from various types of geometrical descriptors for model building. A Multiple Linear Regression is built up, considering the inhibitory effect of seventeen flavonoids on model mast cells by QSARINS software. The model is validated internally using the Q2 LOO criterion in leave-one-out method. William graph and Insubria graph are plotted to identify the application domain for that model. The same model is also externally validated for other seventeen flavonoid compounds. Docking studies of these thirty-four compounds are also performed using AutoDock to identify interacting amino acids of Syk protein. Docking analysis...
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Posted by admin on Apr 30, 2018 in |
A biofilm is a microbial determined sessile group portrayed by cells that are irreversibly appended to a substratum or interface or to each other. Biofilms are the main cause for increase in virulence and antibiotic resistance of microorganisms. Both gram positive and gram negative pathogens are known to produce biofilms. Due to the production of biofilm, the bacteria adhere to the surface strongly and are protected from any antibiotic agents. The present study is aimed at isolation and characterization of biofilm forming bacteria from UTI samples. Further, N-acylhomoserine lactone (AHL), an autoinducer responsible for the formation of biofilms in gram negative bacteria was characterized. The capacity of the UPEC isolates to form biofilms was analysed using biofilm assay. Further on, N-acylhomoserine lactone was extracted by liquid liquid extraction (LLE) and was estimated colorimetrically and spectroscopically by using fourier transform infrared spectroscopy (FT-IR). The UPEC isolates exhibited strong biofilm forming capacity. The AHL that was extracted showed a characteristic absorbance for C=O bond of lactone ring, and N=H and C-O...
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Posted by admin on Apr 30, 2018 in |
Inflammatory bowel disease (IBD) is a multifactorial process that causes ulcerative colitis and Crohn’s disease due to unknown mechanisms associated with release of proinflammatory mediators. Aim of the present study is to evaluate inhibitory activity by bark extract Tectona grandis Linn. (TGE) against experimental induced IBD. Two different models were used to induce IBD viz., Indomethacin-induced enterocolitis and acetic acid induced ulcerative colitis in rats. Male wistar rats were pretreated with TGE the dose of 10 and 25 mg/kg p.o. daily for a period of 7 days. On 8th and 9th day indomethacin was administered (7.5 mg/kg, s.c.) for to induce enterocolitis. In case of acetic acid induced ulcerative colitis model, two ml (3%, v/v) acetic acid in saline was instilled into the rectum of a rat. Quantification of inflammation was done using myeloperoxidase assay (MPO), lactate dehydrogenase (LDH), lipid peroxidase (LPO). All parameters were altered in ulcerated rats, and improved in animals receiving TGE an effect that was comparable to that of the standard sulfasalazine, especially at the...
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Posted by admin on Apr 30, 2018 in |
The aim of the present work is to develop and evaluate colon targeted drug delivery of satranidazole for an effective and safe therapy of amoebiasis. Amoebiasis is a parasitic disease caused by E. histolytica and it causes about 34 – 50 million symptomatic infections each year. The treatment of amoebiasis is effective with satranidazole. Therefore it was planned to develop a suitable dosage form, which can deliver maximum amount of the drug in the colonic environment such that there would be effective action on amoebiasis. This investigation was planned to characterize the satranidazole for their physico-chemical properties and to evaluate rheological and compressional characteristics of the tablets. It was planned to optimize the amount of PH dependent polymer eudragit L100 and eudragit S100 carriers for colonic delivery. The coating formulation consisted of Eudragit L100: Eudragit S100 in ratio of 6:4 at 10% coating level has potential for the required lag time of 5 hours. In-vitro release study was shown after effective lag...
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Posted by admin on Apr 30, 2018 in |
Bioactive compounds are the frontline potent agents in both nutraceutical and pharmaceutical industries. Recently, the bioactive compounds are gaining much importance for their ability in enhancing resistance to various diseases and to improve the health of people both by traditional and modern ways of administrations. Therefore, in the present investigation was undertaken to identify the compounds present in the leaf of Waltheria indica Linn. by Gas Chromatography-Mass Spectrometry (GC-MS) analysis by ethanol extract. The GC-MS analysis showed 27 bioactive compounds. The major compounds identified are 2,3-Dihydro-3,5-Dihydroxy-6-methyl-4h-pyran-4-one, tetradecane, nonadecane, tetracosane, phytol and squalene. In a mass spectrum, each compounds were identified based on their retention time and peak area. Pharmacological activities of these compounds indicated that the compounds present in the leaf of said plant can be used as a crude drug and can also be used to develop a novel...
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