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槲皮素和香豆素抑制二肽基肽酶-IV 并具有抗氧化特性:计算、体外、离体。

Quercetin and Coumarin Inhibit Dipeptidyl Peptidase-IV and Exhibits Antioxidant Properties: In Silico, In Vitro, Ex Vivo.

机构信息

Institute of Life Science, Shri Vaishnav Vidyapeeth Vishwavidyalaya, Indore 452111, India.

School of Life Sciences, Devi Ahilya University, Indore, Madhya Pradesh 452001, India.

出版信息

Biomolecules. 2020 Jan 31;10(2):207. doi: 10.3390/biom10020207.

Abstract

Quercetin and coumarin, two naturally occurring phytochemicals of plant origin, are known to regulate hyperglycemia and oxidative stress. The present study was designed to evaluate the inhibitory activity of quercetin and coumarin on dipeptidyl peptidase-IV (DPP-IV) and their antioxidant potential. DPP-IV inhibition assays were performed, and evaluated IC values of diprotin A, quercetin, coumarin, and sitagliptin were found to be 0.653, 4.02, 54.83, and 5.49 nmol/mL, respectively. Furthermore, in silico studies such as the drug-likeliness and docking efficiency of quercetin and coumarin to the DPP-IV protein were performed; the ex vivo antiperoxidative potential of quercetin and coumarin were also evaluated. The results of the present study showed that the DPP-IV inhibitory potential of quercetin was slightly higher than that of sitagliptin. Virtual docking revealed the tight binding of quercetin with DPP-IV protein. Quercetin and coumarin reduced oxidative stress in vitro and ex vivo systems. We report for the first time that both compounds inhibited the DPP-IV along with antioxidant activity and thus may be use as function food ingredients in the prevention of diabetes.

摘要

槲皮素和香豆素是两种天然存在于植物中的植物化学物质,已知它们可以调节高血糖和氧化应激。本研究旨在评估槲皮素和香豆素对二肽基肽酶-IV(DPP-IV)的抑制活性及其抗氧化潜力。进行了 DPP-IV 抑制试验,并评估了二肽基肽酶-IV 的抑制活性,发现二肽基肽酶-IV 的抑制活性为 0.653、4.02、54.83 和 5.49 nmol/mL。此外,还进行了槲皮素和香豆素对 DPP-IV 蛋白的药物可能性和对接效率等体外研究;还评估了槲皮素和香豆素的体外抗过氧化潜力。本研究结果表明,槲皮素对 DPP-IV 的抑制作用略高于西他列汀。虚拟对接显示槲皮素与 DPP-IV 蛋白的紧密结合。槲皮素和香豆素在体外和体内系统中均能减轻氧化应激。我们首次报道这两种化合物均能抑制 DPP-IV 并具有抗氧化活性,因此可能可作为预防糖尿病的功能性食品成分。

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