黄酮类化合物对人肝微粒体中甲氧基试卤灵脱甲基酶活性的抑制作用。

Inhibition of methoxyresorufin demethylase activity by flavonoids in human liver microsomes.

作者信息

Zhai S, Dai R, Wei X, Friedman F K, Vestal R E

机构信息

Clinical Pharmacology and Gerontology Research Unit, Department of Veterans Affairs Medical Center, Mountain State Medical Research Institute, Boise, Idaho 83702, USA.

出版信息

Life Sci. 1998;63(8):PL119-23. doi: 10.1016/s0024-3205(98)00323-3.

DOI:10.1016/s0024-3205(98)00323-3

PMID:9718089

Abstract

Flavonoids are a class of dietary phytochemicals with anticarcinogenic properties. A series of ten structurally related flavonoids were evaluated for their effect on methoxyresorufin O-demethylase (MROD) activity in human liver microsomes. All compounds inhibited this cytochrome P450 1A2 (CYP1A2) mediated activity. 3,5,7-Trihydoxyflavone (galangin) was the most potent inhibitor, followed by 3-hydroxyflavone and flavone. The relative inhibitory potency of flavonoids is related to their structures. The results suggest that flavonoids may modulate pharmacological and toxicological effects mediated by CYP1A2.

摘要

黄酮类化合物是一类具有抗癌特性的膳食植物化学物质。对一系列十种结构相关的黄酮类化合物对人肝微粒体中甲氧基试卤灵O - 脱甲基酶（MROD）活性的影响进行了评估。所有化合物均抑制这种细胞色素P450 1A2（CYP1A2）介导的活性。3,5,7 - 三羟基黄酮（高良姜素）是最有效的抑制剂，其次是3 - 羟基黄酮和黄酮。黄酮类化合物的相对抑制效力与其结构有关。结果表明，黄酮类化合物可能调节由CYP1A2介导的药理和毒理作用。