Isolation of soluble epoxide hydrolase inhibitor of capsaicin analogs from Capsicum chinense Jacq. cv. Habanero

被引：15

作者：

Kim, Jang Hoon ^{[1
]}

Jo, Yeong Deuk ^{[1
]}

Jin, Chang Hyun ^{[1
]}

机构：

[1] Korea Atom Energy Res Inst, Adv Radiat Technol Inst, Jeongeup 56212, Jeollabuk Do, South Korea

来源：

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES | 2019年 / 135卷

关键词：

Capsicum chinense; Capsaicin analogs; sEH inhibitor; Molecular simulation; EPOXYEICOSATRIENOIC ACID; OPTIMIZATION; POTENCY; UREAS;

D O I：

10.1016/j.ijbiomac.2019.06.028

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Capsaicin (1) and dihydrocapsaicin (2) were isolated from the aerial parts of Capsicum chinense Jacq. cv. Habanero. In in vitro studies, the exhibited potent inhibitory activity against soluble epoxide hydrolase (sEH), with IC50 values of 5.6 +/- 1.2 and 7.3 +/- 0.7 mu M. Enzyme kinetics suggested that the two compounds (1 and 2) were competitive inhibitors with K-i values of 2.5 +/- 1.0 and 4.7 +/- 23 mu M, respectively. Molecular docking and molecular dynamic studies showed that capsaicin analogs (1 and 2) bound strongly with Asp335, Tyr383, and Tyr466 residues in the active site. These results suggest that the two inhibitors (1 and 2) represent potentially therapeutic inhibitors of sEH. (C) 2019 Elsevier B.V. All rights reserved.

引用

页码：1202 / 1207

页数：6

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