地奥司明
醛糖还原酶
化学
生物化学
药理学
IC50型
类黄酮
酶
传统医学
抗氧化剂
体外
医学
作者
Kushagra Dubey,Raghvendra Dubey,Revathi Gupta,Arun Kumar Gupta
出处
期刊:Current Computer - Aided Drug Design
[Bentham Science Publishers]
日期:2021-04-01
卷期号:17 (2): 307-313
被引量:3
标识
DOI:10.2174/1573409916666200324135734
摘要
Diosmin is a flavonoid obtained from the citrus fruits of the plants. Diosmin has blood lipid lowering activities, antioxidant activity, enhances venous tone and microcirculation, protects capillaries, mainly by reducing systemic oxidative stress.The present study demonstrates the potential of Diosmin against the enzymes aldose reductase, α-glucosidase, and α-amylase involved in diabetes and its complications by in vitro evaluation and reverse molecular docking studies.The assay of aldose reductase was performed by using NADPH as starting material and DL-Glyceraldehyde as a substrate. DNS method was used for alpha amylase inhibition and in alpha glucosidase inhibitory activity p-nitrophenyl glucopyranoside (pNPG) was used as substrate. The reverse molecular docking studies was performed by using Molegro software (MVD) with grid resolution of 30 Å.Diosmin shows potent inhibitory effect against aldose reductase (IC50:333.88±0.04 μg/mL), α-glucosidase (IC50:410.3±0.01 μg/mL) and α-amylase (IC50: 404.22±0.02 μg/mL) respectively. The standard drugs shows moderate inhibitory activity for enzymes. The MolDock Score of Diosmin was -224.127 against aldose reductase, -168.17 against α-glucosidase and - 176.013 against α-amylase respectively, which was much higher than standard drugs.From the result it was concluded that diosmin was a potentially inhibitor of aldose reductase, alpha amylase and alpha glucosidase enzymes then the standard drugs and it will be helpful in the management of diabetes and its complications. This will also be benevolent to decrease the socio economical burden on the middle class family of the society.
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