槲皮素及其糖苷类化合物对P450酶活性的体外抑制作用

被引：8

作者：

叶林虎 ^{[1
,2
]}

闫明珠 ^{[1
]}

孔令提 ^{[1
]}

贺梅 ^{[2
]}

常琪 ^{[1
]}

机构：

[1] 中国医学科学院北京协和医学院药用植物研究所

[2] 贵州省毕节市第一人民医院药剂科

来源：

中国药学杂志 | 2014年 / 49卷 / 12期

关键词：

槲皮素; 糖苷类化合物; 异槲皮苷; 金丝桃苷; 黄酮; 细胞色素P450; 药物相互作用;

D O I：

暂无

中图分类号：

R285 [中药药理学];

学科分类号：

摘要：

目的研究槲皮素、槲皮素-3-O-葡萄糖醛酸苷、异槲皮苷、金丝桃苷和芦丁对人肝微粒体CYP2C19、CYP2D6、CYP3A4、CYP2E1和CYP2C9的体外抑制作用,并比较槲皮素及其糖苷化合物对CYP酶的抑制程度。方法采用人肝微粒体、受试黄酮与5种探针底物在还原系统NADPH的作用下,于37℃水浴条件下共同孵育。通过液相色谱-质谱联用分析方法,测定探针底物的代谢产物生成量,评价受试化合物对CYP同工酶活性的影响。结果在人肝微粒体体外孵育反应体系中,槲皮素对CYP3A4和CYP2C9亚型活性抑制的IC50值分别为13.14和23.09μmol·L-1,其他亚型的IC50值均大于100μmol·L-1。槲皮素-3-O-葡萄糖醛酸苷、异槲皮苷、金丝桃苷和芦丁对这5种酶亚型的IC50值也均大于100μmol·L-1。结论槲皮素对CYP3A4和CYP2C9的活性有一定的抑制作用,而其糖苷类化合物则对这5种酶亚型的活性几乎均没有抑制作用,槲皮素糖苷化合物发生药物相互作用的可能性较其苷元小。

引用

页码：1051 / 1055

页数：5

共 11 条

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