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

Q4 Pharmacology, Toxicology and Pharmaceutics
T. Deshpande, H. Une
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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.
牛膝草的药理作用。流式细胞术研究叶片提取物对糖尿病大鼠活性氧(ROS)的影响及分子对接可能的分子机制
氧化应激是由于活性氧(ROS)的过量产生和生化过程中抗氧化潜能的紊乱引起的。活性氧主要在大脑中形成,由于高氧消耗和内源性抗氧化抵抗机制的不足。细胞色素P450 2E1具有过高百分比的nadph氧化酶活性,导致ROS的产生,增加氧化应激。研究牛膝乙酸乙酯提取物(EAAA)对糖尿病大鼠脑内松香的影响。我们还通过分子对接研究了ROS减少的可能分子机制。为了研究ROS对糖尿病大鼠氧化应激的诱导作用,我们采用流式细胞术测定了大鼠脑中的ROS水平。糖尿病大鼠口服EAAA 50mg/kg和100mg /kg。结果以均数±标准差(SD)表示。采用方差分析(ANOVA)对数据进行分析,随后采用Bonferroni作为事后检验。我们通过类黄酮对CYP2E1的分子对接来研究其抑制潜能。结果表明,EAAA在糖尿病诱导的大鼠中以剂量依赖的方式减少ROS的产生。给大鼠口服EAAA 50mg/kg和100mg /kg,对ROS生成有一定影响。木犀草素、槲皮素和芹菜素非常有效地抑制了cyp2e1。木犀草素与CYP2E1形成4个氢键,表明其具有潜在的抑制作用。木犀草素和芹菜素均与该酶具有良好的结合亲和力。从目前的工作来看,我们认为牛膝草乙酸乙酯提取物通过抑制CYP2E1的活性,有效地抑制了糖尿病大鼠体内ROS的产生。
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来源期刊
Current Enzyme Inhibition
Current Enzyme Inhibition Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
1.30
自引率
0.00%
发文量
30
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.
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