Effect of Achyranthes Aspera Linn. Leaves Extract on Reactive Oxygen Species (ROS) in Diabetes-induced Rats by Flow cytometry and Possible Molecular Mechanism through Molecular Docking
{"title":"Effect of Achyranthes Aspera Linn. Leaves Extract on Reactive Oxygen Species (ROS) in Diabetes-induced Rats by Flow cytometry and Possible Molecular Mechanism through Molecular Docking","authors":"T. Deshpande, H. Une","doi":"10.2174/1573408016999201228193350","DOIUrl":null,"url":null,"abstract":"\n\nOxidative stress is caused due to the overproduction of the reactive oxygen\nspecies (ROS) and the disturbance developed in the antioxidant potential of biochemical processes.\nROS mostly form in the brain due to the high consumption of oxygen and the insufficiency of endogenous\nantioxidant resistance mechanisms. Cytochrome P450 2E1 has an excessive percentage of\nNADPH oxidase activity, which causes the production of ROS and increases oxidative stress.\n\n\n\nWe have studied the effect of ethyl acetate extract of Achyranthes Aspera (EAAA) on ROS\nin the brain of diabetes-induced rats. We have also investigated the possible molecular mechanism of\nreduction in ROS through molecular docking.\n\n\n\nTo study the oxidative stress induced by ROS in diabetic rats, we estimated the ROS in rat\nbrain through flow cytometry. The oral dose of EAAA 50mg/kg and 100 mg/kg was given to diabetesinduced\nrats. Results were articulated as mean ± standard deviation (SD). Data were analyzed using\nanalysis of variance (ANOVA) followed by Bonferroni as a post hoc test. We performed molecular\ndocking of flavonoids on CYP2E1 to study the inhibitory potential.\n\n\n\nThe results have shown that EAAA reduces the generation of ROS in the diabetes-induced rat\nin a dose-dependent manner. The oral dose of EAAA 50mg/kg and 100 mg/kg was given to the rats\nand the ROS generation got affected accordingly. Luteolin, quercetin, and apigenin inhibited the\nCYP2E1 very effectively. Luteolin formed 4 hydrogen bonds with CYP2E1, which indicated its potential\ninhibition. Although, luteolin and apigenin showed a very good binding affinity with the enzyme.\n\n\n\n From the present work, we have concluded that the ethyl acetate extract of achyrantesaspera\ncan effectively inhibit the ROS generation in the diabetes-induced rats by inhibiting the activity\nof CYP2E1.\n","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2021-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Enzyme Inhibition","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1573408016999201228193350","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 0
Abstract
Oxidative stress is caused due to the overproduction of the reactive oxygen
species (ROS) and the disturbance developed in the antioxidant potential of biochemical processes.
ROS mostly form in the brain due to the high consumption of oxygen and the insufficiency of endogenous
antioxidant resistance mechanisms. Cytochrome P450 2E1 has an excessive percentage of
NADPH oxidase activity, which causes the production of ROS and increases oxidative stress.
We have studied the effect of ethyl acetate extract of Achyranthes Aspera (EAAA) on ROS
in the brain of diabetes-induced rats. We have also investigated the possible molecular mechanism of
reduction in ROS through molecular docking.
To study the oxidative stress induced by ROS in diabetic rats, we estimated the ROS in rat
brain through flow cytometry. The oral dose of EAAA 50mg/kg and 100 mg/kg was given to diabetesinduced
rats. Results were articulated as mean ± standard deviation (SD). Data were analyzed using
analysis of variance (ANOVA) followed by Bonferroni as a post hoc test. We performed molecular
docking of flavonoids on CYP2E1 to study the inhibitory potential.
The results have shown that EAAA reduces the generation of ROS in the diabetes-induced rat
in a dose-dependent manner. The oral dose of EAAA 50mg/kg and 100 mg/kg was given to the rats
and the ROS generation got affected accordingly. Luteolin, quercetin, and apigenin inhibited the
CYP2E1 very effectively. Luteolin formed 4 hydrogen bonds with CYP2E1, which indicated its potential
inhibition. Although, luteolin and apigenin showed a very good binding affinity with the enzyme.
From the present work, we have concluded that the ethyl acetate extract of achyrantesaspera
can effectively inhibit the ROS generation in the diabetes-induced rats by inhibiting the activity
of CYP2E1.
期刊介绍:
Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.