期刊
BIOMOLECULES
卷 10, 期 2, 页码 -出版社
MDPI
DOI: 10.3390/biom10020180
关键词
flavonoids; soluble epoxide hydrolase; non-competitive mode; induced fit; lock-and-key
资金
- Korea Atomic Energy Research Institute (KAERI), Republic of Korea
Three flavonoids derived from the leaves of Capsicum chinense Jacq. were identified as chrysoeriol (1), luteolin-7-O-glucopyranoside (2), and isorhamnetin-7-O-glucopyranoside (3). They had IC50 values of 11.6 +/- 2.9, 14.4 +/- 1.5, and 42.7 +/- 3.5 mu g/mL against soluble epoxide hydrolase (sEH), respectively. The three inhibitors (1-3) were found to non-competitively bind into the allosteric site of the enzyme with K-i values of 10.5 +/- 3.2, 11.9 +/- 2.8 and 38.0 +/- 4.1 mu g/mL, respectively. The potential inhibitors 1 and 2 were located at the left edge ofa U-tube shape that contained the enzyme active site. Additionally, we observed changes in several factors involved in the binding of these complexes under 300 K and 1 bar. Finally, it was confirmed that each inhibitor, 1 and 2, could be complexed with sEH by the induced fit and lock-and-key models.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据