Posted by admin on Jun 30, 2019 in |
Deoxyelephantopin and isodeoxyelephantopin are member of a group of compounds, sesquiterpene lactones, that include proven anticancer agents against many types of cancer cells. Many sesquiterpene lactones suppress cancers by inhibiting NFκβ. This study explores the inhibitory interaction between deoxyelephantopin and isodeoxyelephantopin on NFκB using QSAR and molecular docking. Physicochemical properties and NFκβ (pIC50) inhibition values of a number of sesquiterpene lactone compounds from in–vitro studies were used as reference data in constructing the QSAR model equation. This model was used to predict the inhibition potential of deoxyelephantopin and isodeoxyelephantopin on NFκβ. This result was confirmed with molecular docking. The potential NFκβ inhibition of deoxyelephantopin and isodeoxyelephantopin obtained were 59.1037 μM and 62.0321 μM, respectively, with RMSE = 0.07831 R2 = 0.95465 and Q2 = 0.67719. Both test compounds showed affinity for the Lys 122 receptor residue (PDB ID: 1NF1) with a docking score of -9.5318 kcal/mol and -8.4429 kcal/mol,...
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Posted by admin on Jun 30, 2019 in |
In an attempt to reveal the medicinal values of Orthosiphon glabratus Benth leaf, which claims to have traditional use for the management of diabetes. In-vitro antioxidant and antidiabetic potentials of Orthosiphon glabratus leaf in different solvent fractions were studied by utilizing DPPH, ABTS, and α-amylase, α-glucosidase inhibitory methods respectively. A preliminary phytochemical study shows the presence of important constituents such as alkaloids, flavonoids, phenols, cardiac glycosides and terpenoids in all the solvent fractions. The ethyl acetate fraction exhibits the best inhibition activity against DPPH and ABTS, and its IC50 was found to be 2.28 and 1.68 µg/mL respectively, which is significantly lower (P<0.05) than reference. In case of antidiabetic activity, ethyl acetate fraction shows the highest enzyme inhibitory action against α-amylase and α-glucosidase and IC50 value was found to be 2.09 and 4.66 µg/mL respectively than (P<0.05) acarbose. The results of in-vitro antioxidant and antidiabetic assays on different solvent fractions of Orthosiphon glabratus leaf, it is evident that the ethyl acetate fraction could be potential candidature, which possessing the...
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Posted by admin on Jun 30, 2019 in |
A new precise, selective, accurate and rapid Ultra Performance Liquid Chromatographic stability indicating method has been developed and validated for simultaneous quantitative determination of Dapagliflozin and Saxagliptin in bulk and pharmaceutical dosage form. The chromatographic separation was achieved with HSS 100 × 2.1 mm, 1.8 m size column. The optimized mobile phase consisting of Phosphate buffer: acetonitrile in the ratio of 50:50 v/v. The flow rate was 0.3 mL/min, and eluents were detected at 260 nm using a PDA detector. The retention time of Dapagliflozin and Saxagliptin were found to be 0.900 and 1.119 min respectively. The percentage recoveries for both the molecules were found to be in the range of 98.61 -100.5%. The calibration curve was constructed between peak areas vs. concentration and demonstrated good linearity in the range of (2.5-15 µg/ml Dapagliflozin and 1.25-7.5 µg/ml Saxagliptin). Degradation studies were carried for Dapagliflozin and Saxagliptin under various stress conditions such as acid, base, oxidation, thermal, photochemical and UV degradation peaks were resolved...
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Posted by admin on Jun 30, 2019 in |
Acanthophora Spicifera is a species of marine red seaweed and in the family Rhodomelaceae. They were freshly collected from Mandapam Coastal Area, Rameswaram Tamil Nadu, India and rinsed in seawater and packed in aseptic bags for further proceedings to the laboratory. Seaweeds are potential renewable resources in the marine environment. It has been used as antioxidant and antimutagen. The results of the present study revealed the reduction of cell viability after the treatment of methanolic extract of Acanthophora spicifera (10-200 µg/mL). In DNA Fragmentation by comet assay showed the methanolic extract of Acanthophora spicifera, the presence of the tail reflect the DNA damage and the potent cell mortality was shown at the concentration 200 µg/ml then decreased significantly with the decreased concentration of extract. Our study also demonstrated the revealed the protective effect of Acanthophora spicifera in HT-29 cell line treated with the methanolic extract of Acanthophora spicifera. Therefore, we concluded that Acanthophora spicifera might be used as a rich source of phytoconstituents and natural...
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Posted by admin on Jun 30, 2019 in |
The present study was designed to assess the pharmacokinetics of drug metabolized by hepatic cytochrome 3A4 (CYP3A4) in human volunteers with physical activity at the high altitude hypobaric hypoxic environment. The International Physical Activity Questionnaire short form 7 (IPAQ SF-7) was used to measure the physical activity. The total of 24 healthy male volunteers participated in this study; for them, the intensity of physical activity was measured in terms of metabolic equivalence of tasks (METs). The pharmacokinetic study was conducted using an oral dose of Alprazolam. The blood samples were collected at fixed intervals up to 24 h. The pharmacokinetic variables were found to be changed with increased intensity of physical activity. The metabolism phase was significantly decreased in vigorous and walking physical activity groups. The area under the curve (AUC) and half-life were also decreased. The pharmacokinetics of drug was found to be decreased with increased intensity of vigorous and walking physical activity in humans working at high altitude hypobaric hypoxia environment. It was assumed that oxygenation of...
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