大黄酸对大鼠肝细胞色素P_(450)3A酶活性的抑制  

Inhibitory Effect of Rhein on Cytochrome P_(450) Activity of Rat Liver Microsomes

作　　者：李丹[1,2] 韩永龙[1,2,3] 孟祥乐[1,2] 孙习鹏[1] 余奇[1] 郭澄[1,2] 

机构地区：[1]上海市第六人民医院药剂科,200233 [2]上海中医药大学,201203 [3]大庆油田总医院临床药学科,黑龙江163001

出　　处：《医药导报》2010年第3期282-285,共4页Herald of Medicine

基　　金：上海市药学会上海医院药学科研基金资助项目(基金编号:2008-YY-0227)

摘　　要：目的研究大黄酸对大鼠肝微粒体细胞色素P4503A(CYP3A)酶活性的影响。方法在体外大鼠肝微粒体孵育体系中加入底物睾酮和不同浓度的大黄酸,采用高效液相色谱仪测定睾酮的羟基化代谢产物6β羟基睾酮的含量,计算CYP3A酶活性来反映大黄酸对CYP3A酶的抑制效果。结果大鼠肝微粒体孵育体系中,大黄酸对CYP3A酶活性有抑制作用,其半数抑制浓度(IC50)和Ki值分别为36.74,20.73μmol·L-1。结论在大鼠肝微粒体体外孵育系统中,大黄酸对CYP3A酶具有抑制作用。Objective To evaluate the effects of rhein on the activity of cytochrome P450 3A（CYP3A） enzyme of rat liver microsomes. Methods Rat liver microsomes were incubated with various concentrations of rhein and testosterone in vitro. The inhibition of CYP3A activity by rhein was evaluated by the amount of 6β-hydroxytestosterone which was determined by HPLC. Results Rhein suppressed the CYP3A activity in rat liver microsomes, with IC50= 36.74μmol·L^-1 and Ki = 20.73μmol·L^-1 , respectively. Conclusion Rhein could decrease the enzyme activity of rat liver CYP3A in vitro.

关 键 词：大黄酸 肝微粒体 CYP3A酶 抑制作用 

分 类 号：R282.7[医药卫生—中药学] R285.5[医药卫生—中医学]