巨角茶叶甲醇提取物对四氯化碳诱导大鼠肝损伤的分子对接、体外抗氧化及体内保肝活性

Q4 Pharmacology, Toxicology and Pharmaceutics
Shripad Bairagi, P. Ghule, R. Gilhotra
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引用次数: 1

摘要

巨角石是一种广泛生长的植物,据称有几种治疗特性,可以治疗牙痛、耳痛、扭伤、焦虑、疼痛、癫痫和精神障碍。本研究旨在探讨巨角甘油三酯(Calotropis gigantea leaves, CGL)甲醇提取物对四氯化碳诱导的大鼠肝损伤的体外抗氧化和体内肝保护作用。本研究采用Sprague - Dawley大鼠(180-250 g)。通过测定不同动物组中SGOT、SGPT、ALP、胆红素等不同生化参数和LPO、GSH、SOD、CAT等体内抗氧化参数来测定CGL的保肝活性。我们还通过分子对接研究了CGL的一些重要化学成分对CYP2E1的抑制潜力。体内肝保护研究表明,CGL提取物可显著降低[200 mg, SGOT (110.16 IU/L), SGPT (101.33 IU/L), ALP (186.66 IU/L),胆红素(1.1 mg/dl)和LPO (6.933 M/mg蛋白)],并以剂量依赖性方式提高[GSH (14.051 M/mg蛋白),SOD(257.5%)和CAT (15.975 μM)]的酶活性。不幸的是,CGL提取物并没有显示出比标准药物水飞蓟素更有效的活性。与天然配体相比,所有植物成分都显示出与CYP2E1的有效结合亲和力。在所有的植物成分中,中脂醇和CYP2E1发生了强烈的相互作用,是活性最强的分子。从自由基清除活性来看,CGL提取物比抗坏血酸具有更强的自由基清除活性,表明其含有较高的多酚和生育酚,并具有体内保护肝脏的活性。从分子对接来看,巨茶甘油三酯具有潜在的抑制CYP2E1和阻止自由基产生的作用,最终减少氧化应激及相关疾病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Molecular Docking, in vitro Antioxidant, and in vivo Hepatoprotective Activity of Methanolic extract of Calotropis gigantea leaves in Carbon Tetrachloride-induced Liver injury in Rats
Calotropis gigantea (Asclepiadaceae), a wildly growing plant, has several purported therapeutic characteristics and treats toothache and earache, sprains, anxiety, pain, epilepsy, and mental disorders. The purpose of this study was to determine the in vitro antioxidant and in vivo hepatoprotective capabilities of a methanolic extract of Calotropis gigantea leaves (CGL) against carbon tetrachloride-induced liver injury in rats. The Sprague Dawley rats (180-250 g) were used for the current study. The hepatoprotective activity of CGL was determined by estimating the different biochemical parameters like SGOT, SGPT, ALP, bilirubin, and in-vivo antioxidant parameters like LPO, GSH, SOD, and CAT in different animal groups. We have also investigated the inhibitory potential of some significant chemical constituents of CGL on CYP2E1 through molecular docking. In vivo hepatoprotective studies indicates the CGL extract administration caused a significant reduction [at 200 mg, SGOT (110.16 IU/L), SGPT (101.33 IU/L), ALP (186.66 IU/L), bilirubin (1.1 mg/dl), and LPO (6.933 M/mg protein)] and elevation [GSH (14.051 M/mg protein), SOD (257.5%), and CAT (15.975 μM)] in enzyme activity in a dose-dependent manner. Unfortunately, CGL extract has not shown a more potent activity than the standard drug Silymarin. All the phytoconstituents have shown potent binding affinity with CYP2E1 compared to the native ligand. Amongst all the phytoconstituents, Medioresinol was the most active and potent molecule that has developed compelling interactions with CYP2E1. From free radical scavenging activity, it was concluded that CGL extract exerts more scavenging activity than ascorbic acid, which indicates a high level of polyphenols and tocopherols and also exhibited in vivo hepatoprotective activity. From the molecular docking, it has been concluded that Calotropis gigantea can potentially inhibit CYP2E1 and prevent the generation of free radicals, which will ultimately reduce oxidative stress and associated diseases.
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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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