黄连配伍肉桂对小檗碱大鼠肝代谢的影响及其机制探讨  

Study on the effect of coptis coadministrated with cassia on liver metabolic activities of berberine in rats and its mechanism

作　　者：叶静[1] 张瑞[1] 黄果[1] 魏宝红[1] 杨丽娟[1] 张玉杰[1] 

机构地区：[1]北京中医药大学中药学院,北京100102

出　　处：《药物分析杂志》2013年第10期1702-1705,共4页Chinese Journal of Pharmaceutical Analysis

基　　金：国家自然科学基金项目(30672585;81073140)

摘　　要：目的:考察大鼠经口给予黄连配伍肉桂的制剂后对小檗碱肝脏代谢的影响及其肝药酶的变化,探讨黄连-肉桂药对的配伍机制。方法:以HPLC法测定大鼠肝微粒体温孵体系中小檗碱的含量,考察小檗碱在肉桂、黄连和黄连-肉桂(10∶1)诱导组及溶媒对照组大鼠肝微粒体系中的代谢变化;采用Nash显色,分光光度法测定空白组、黄连组、肉桂组和黄连肉桂配伍(10∶1)组大鼠肝微粒体中红霉素N-脱甲基酶(ERD)活性。结果:与空白对照组相比,小檗碱在各给药组大鼠肝微粒体温孵液中的代谢速率均有显著下降(P<0.001),各组代谢速率从小到大的顺序为黄连-肉桂配伍组,肉桂组,黄连组,空白对照组。与空白组比较,肉桂组和黄连-肉桂配伍组ERD活性均明显受到抑制(P<0.01);黄连组对ERD活性作用不明显(P>0.05)。结论:黄连-肉桂配伍合用通过抑制大鼠肝药酶ERD活性降低黄连主要有效成分小檗碱的肝脏代谢,这可能是黄连-肉桂配伍相互作用的重要机制。Objective： To clarify the impact of the compatibility of coptis and cassia on the liver metabolism of berberine and changes of hepatic enzymes,and to explore the metabolic mechanism of this compatibility. Methods： RP-HPLC method was applied to determine the content of berberine in rat liver microsomal incubation system and investigate the metabotic changes of berberine in rat liver microsomal systems in coptis group,cassia group,coptis-cassia（10：1）induction group,and solvent control group.The activity of erythromycin-N-demethylase（ERD）in each group of rat liver microsomes was determined using spectrophotometry and Nash coloration. Results： Compared with blank control group,metabolic rates of berberine in all treatment groups were significantly lowered（P〈0.001）,and the order from low to high was coptis-cassia,cassia,coptis,blank group.Compared with black group,cassia and coptis-cassia groups showed significant inhibition for the ERD activity（P〈0.01）,while the effect on the ERD activity in coptis group was not significant（P〉0.05）. Conclusion： The liver metabolism of berberine in coptis significantly decreases in compatibility of coptis-cassia,which may result from inhibiting rat liver microsomal metabolic activity.This can be one significant mechanism of this compatibility.

关 键 词：黄连 肉桂 肝代谢 CYP3A4 小檗碱 

分 类 号：R917[医药卫生—药物分析学]