环氧化物水解酶2
四肽
化学
IC50型
立体化学
肽
氢键
对接(动物)
动力学
圆二色性
酶
生物化学
体外
分子
有机化学
医学
物理
护理部
量子力学
作者
Joy I. Obeme-Nmom,Raliat O. Abioye,Toluwase Hezekiah Fatoki,Chibuike C. Udenigwe
出处
期刊:Journal of food bioactives
[International Society for Nutraceuticals & Functional Foods (ISNFF)]
日期:2023-03-31
卷期号:21
被引量:2
标识
DOI:10.31665/jfb.2023.18341
摘要
Soluble epoxide hydrolase (sEH) contributes to the pathophysiology of neurodegenerative diseases by decreasing the epoxyeicosatrienoic acids/dihydroeicosatrienoic acids ratio and influencing the anti-inflammatory system. Thus, sEH inhibition reduces systemic inflammation, particularly in the brain. This study investigated sEH inhibition by a tetrapeptide, YMSV, and its mechanism of action. Enzyme inhibition kinetics demonstrated that YMSV is a mixed-competitive inhibitor of sEH, with a half-maximal inhibitory concentration (IC50) of 179.5 ± 0.92 µM. Secondary structural analysis of sEH by circular dichroism showed that YMSV decreased the α-helices by 7.7% and increased the β-sheets and random coils by 11.4% and 22%, respectively. Molecular docking simulation indicated that YMSV formed a hydrogen bond with the Asp333 residue of the hydrolase pocket of sEH in addition to the binding of non-active site residues. The findings provide new insights into the mechanism of sEH inhibition by YMSV and its potential as a peptide-based anti-depressant nutraceutical.
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