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中华猕猴桃根的成分及其对细胞色素P450酶的抑制活性

Constituents from the Roots of Actinidia chinensis and Their Cytochrome P450 Enzyme Inhibitory Activities.

作者信息

Xu Yi-Xin, Xiang Zhao-Bao, Jin Yong-Sheng, Xu Wen, Sun Lian-Na, Chen Wan-Sheng, Chen Hai-Sheng

机构信息

School of Pharmacy, Second Military Medical University, No. 325 Guohe Road, Shanghai, 200433, P. R. China.

School of Pharmacy, Shanghai University of Medical & Health Sciences, Shanghai, 200237, P. R. China.

出版信息

Chem Biodivers. 2016 Nov;13(11):1454-1459. doi: 10.1002/cbdv.201500518. Epub 2016 Nov 10.

Abstract

A newly discovered triterpenoid, (2α,3β)-2,3,23-trihydroxyurs-13(18)-en-28-oic acid (1), along with twelve known compounds (2 - 13), were isolated from the roots of Actinidia chinensis Planch (Actinidiaceae). Their chemical structures were determined by 1D- and 2D-NMR spectra and mass spectrometry (MS). The crude extracts and six main constituents (8 - 13) were tested for cytochrome P450 (CYPs) enzyme inhibitory activity. The results showed that, except for compound 8, compounds 9 - 13 had different inhibitory effects on the cytochrome P450 (CYPs) enzyme, and compound 9 significantly inhibited the catalytic activities of CYP3A4 to < 10% of its control activities.

摘要

从中华猕猴桃(猕猴桃科)根部分离得到一种新发现的三萜类化合物,(2α,3β)-2,3,23-三羟基乌苏-13(18)-烯-28-酸(1),以及12种已知化合物(2 - 13)。通过一维和二维核磁共振光谱以及质谱(MS)确定了它们的化学结构。对粗提物和六种主要成分(8 - 13)进行了细胞色素P450(CYPs)酶抑制活性测试。结果表明,除化合物8外,化合物9 - 13对细胞色素P450(CYPs)酶有不同的抑制作用,化合物9显著抑制CYP3A4的催化活性,使其降至对照活性的<10%。

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