黄连解毒汤主要有效成分对人CYP450酶的体外抑制作用研究  

Rinhibition of Human CYP Enzymes in vitro by Active Component from Huanglian Jiedu Decoction

作　　者：刘柏东[1] 吴晓霞[1] 于友华[1] 

机构地区：[1]中国中医科学院医学实验中心,北京100700

出　　处：《中国实验方剂学杂志》2014年第12期115-118,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：中国中医科学院自主选题项目(2010zz003)

摘　　要：目的:体外评价黄连解毒汤主要有效成分对人肝细胞色素P450(CYP1A2,CYP2A6,CYP2B6,CYP2C9,CYP2D6,CYP3A4)活性的影响。方法:利用液质联用仪(LC-MS-MS)建立同时测定6种探针药物的分析方法,选择合适的孵育体系、孵育时间、蛋白浓度建立Cocktail模型,并通过工具药进行验证。利用Cocktail模型筛选黄芩苷、汉黄芩苷、黄芩素、汉黄芩素、小檗碱、药根碱、黄连碱、表小檗碱、巴马汀、兰花碱、栀子苷对6种酶活性抑制的体外评价。结果:黄芩素、汉黄芩素及黄芩苷对CYP1A2的IC50分别为37.7,46.3,49.9μmol·L-1,小檗碱、药根碱、黄连碱、表小檗碱对CYP2D6抑制作用的IC50分别为39.7,46.5,7.3,11.5μmol·L-1。结论:黄连解毒汤中黄芩及黄连的主要有效成分对细胞色素P450酶有不同程度的抑制,在临床联合用药时要注意代谢层面的相互作用,减少不良反应的发生。Objective： To study the inhibition of the human CYP enzymes in vitro by active components from Huanglian Jiedu decoction. Method： A LC-MS-MS method was used to simultaneously determine six probe metabolites from human liver microsome to optimize the incubation conditions such as incubation time, microsomal concentration, and probe concentration. A specific P4_50 inhibitor was as positive control. The inhibitory potential of baicalin, wogonoside, baicalein, wogonin, berberine, jateorhizine, coptisine, epiberberine, palmatine, magnoflorine, jasminoidin on six CYP enzymes was investigated. Result： The IC_50 of baicalein, wogonin, wogonoside to CYP1A2 was 37.7, 46.3, 49.9 μmol · L-1. The IC_50 of berberine, jateorhizine, coptisine, epiberberine to CYP2D6 was 39.7, 46.5, 7.3, 11.5 μmol · L-1. Conclusion： The active component of Scutellaria and coptis chinensis in the Huanglian Jiedu decoction show some inhibitory on some CYP enzymes.

关 键 词：黄连解毒汤 细胞色素P450 液质联用仪 

分 类 号：R284.1[医药卫生—中药学]