Posted by admin on Apr 30, 2015 in |
Matrix metalloproteinase 12 (MMP-12) inhibitions is an important research topic because of its wide range of associated health implications. The interaction mode of a series of pyridinone compounds with MMP-12 has been studied using molecular docking and 3D-QSAR approaches. Flexible docking was used for the determination of active conformation and molecular alignment. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used to develop 3D-QSAR models of 64 pyridinone-based compounds. The q2 values were 0.552and 0.542 for both CoMFA and CoMSIA models, respectively. The ability of these models was validated by 16 compounds of the test set. The resulting contour maps produced by the best CoMFA and CoMSIA models were used to identify the structural features relevant to the biological activity in this series of compounds. FlexX were employed to dock the inhibitors into the active site of the MMP-12 and these docking studies revealed the vital interactions and binding conformation of the inhibitors. The results demonstrate that combination of ligand-based and receptor-based modeling is...
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Posted by admin on Apr 30, 2015 in |
Ficus cyathistipula Warb. growing in Egypt is an evergreen tree, reaching up to six meters high. The macro- and micromorphological characters of the stem, leaf and fruit of the plant have been studied with the aim to find the diagnostic features and pointed towards their identification in both entire and powdered forms: partly united, leafy and conspicuous stipules, numerous ca-oxalate crystals, collateral vascular bundles with group of intraxylary phloem, mucilage and tannin cells, laticiferous vessels were the most significant. A total of 60 RAPD fragments have been recorded when DNA of the plant under investigation was amplified using eleven decamer primers designed for the genetic characterization. Furthermore, proximate analysis for the leaves was carried out to facilitate the detection of the quality and uniformity of the plant where the results (g %) showed a total ash (13.06), acid insoluble ash (0.58), water soluble ash (12.39), crude fiber (38) and moisture content...
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Posted by admin on Apr 30, 2015 in |
Epsilon poly-L-lysine (ε-PL) is a nontoxic biopolymer widely used in food and pharmaceutical industry. The present work reports the nutritional requirements for submerged fermentation of Streptomyces noursei NRRL 5126 using a combination of one factor at a time and statistical orthogonal array method. Two-fold increase in ε-PL productivity (74 mg/L) was observed using optimized medium containing glycerol as carbon source along with proteose peptone and ammonium sulphate as nitrogen source. Various metabolic precursors such as amino acids, tricarboxylic acid cycle intermediates were investigated for improved production of ε-PL. Four fold increase (74 mg/L to 310 mg/L) in ε-PL production was achieved by incorporation of L-aspartate (2mM) and citric acid (5mM). Fed batch fermentation for ε-PL production with intermittent feeding with glycerol and in combination with metabolic precursors was studied. Fed batch fermentation with intermittent feeding of glycerol gave a maximum yield of 233 mg/L. Productivity was further enhanced and reached a maximum of 408 mg/L by addition of glycerol along with 5 mM citric acid after 24 h and...
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Posted by admin on Apr 30, 2015 in |
The objective of the present work is to develop simple, precise and accurate colorimetric methods for the estimation of aripiprazole (ARP), tapentadol (TAP) using chloranilic acid reagent. ARP belongs to the class of antipsychotics. TAP is centrally acting analgesic drug. The methods are based mainly on charge transfer complexation of these drugs with p-chloranilic acid to give magenta purple colored products which were extracted into chloroform. The products were quantified at 543 nm for both ARP and TAP. The linearity of the methods was assessed in the range of 80-400 µg/ml for ARP and 200-1000µg/ml for TAP, respectively. The LOD and LOQ are 5.17 and 15.66; 82.5 and 250 for ARP and TAP, respectively. The colorimetric methods were extensively validated as per ICH guidelines and all the parameters were within the acceptance criteria with a correlation of 0.9999 and the % RSD less than 2. The results of the accuracy studies were nearer to 100%. The methods were proven to be more accurate, simple, precise and rapid by statistical...
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Posted by admin on Apr 30, 2015 in |
Objective: The present study was an effort to evaluate the effect of Ocimum sanctum on plasma concentration of metformin HCl and investigating its pharmacokinetic parameters using bioanalytical method. Methods: Seven groups comprising of six rats were used. Group I served as normal control and Group II was negative control of Streptozotocin induced Diabetic rats. Group III received 100mg/kg p.o. Metformin alone while Group IV and V were administered with 100mg/kg and 150mg/kg p.o. extract respectively. Group VI and VII were given metformin and extract in combination. Blood glucose level was determined in treated rats for 0.5, 2, 4, 8, 12 and 24hr as part of protocol I and directly on 2nd, 4th and 7th day as part of protocol II. RP-HPLC method was developed and validated for estimation of plasma levels of metformin HCl in plasma. With the help of above developed method, pharmacokinetic parameters were evaluated in plasma for metformin alone and combination with Ocimum sanctum. Results: RP-HPLC method was developed successfully for determination of plasma concentration of...
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