首页> 美国卫生研究院文献>Biomolecules >Inhibitory Activity of Flavonoids Chrysoeriol and Luteolin-7-O-Glucopyranoside on Soluble Epoxide Hydrolase from Capsicum chinense
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Inhibitory Activity of Flavonoids Chrysoeriol and Luteolin-7-O-Glucopyranoside on Soluble Epoxide Hydrolase from Capsicum chinense

机译:黄酮类绿松酚和木犀草素-7-O-葡萄糖苷对辣椒中可溶性环氧水解酶的抑制作用

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摘要

Three flavonoids derived from the leaves of Jacq. were identified as chrysoeriol ( ), luteolin-7- -glucopyranoside ( ), and isorhamnetin-7- -glucopyranoside ( ). They had IC values of 11.6±2.9, 14.4±1.5, and 42.7±3.5 µg/mL against soluble epoxide hydrolase (sEH), respectively. The three inhibitors ( – ) were found to non-competitively bind into the allosteric site of the enzyme with values of 10.5 ± 3.2, 11.9 ± 2.8 and 38.0 ± 4.1 µg/mL, respectively. The potential inhibitors and 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, and , could be complexed with sEH by the “induced fit” and “lock-and-key” models.
机译:雅克叶中的三种黄酮。被鉴定为chrysoeriol(),木犀草素7--吡喃葡萄糖苷()和异鼠李素7--吡喃葡萄糖苷()。它们对可溶性环氧化物水解酶(sEH)的IC值分别为11.6±2.9、14.4±1.5和42.7±3.5 µg / mL。发现这三种抑制剂(-)分别以10.5±3.2、11.9±2.8和38.0±4.1 µg / mL的值非竞争性结合到酶的变构位点。潜在的抑制剂位于含有酶活性位点的U形管的左边缘。此外,我们观察到了在300 K和1 bar下与这些复合物结合所涉及的几个因素的变化。最后,通过“诱导拟合”和“锁钥”模型,可以确定每种抑制剂和均可与sEH混合。

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