5种黄连生物碱大鼠体外肝代谢特征比较  

Comparison on in vitro hepatic metabolic characteristics of five kinds of alkaloids from Coptis chinensis

作　　者：李志慧[1] 薛宝娟[1] 张玉杰[1] 苏瑾[1] 叶静[1] 魏宝红[1] 

机构地区：[1]北京中医药大学中药学院,北京100102

出　　处：《中草药》2014年第4期532-535,共4页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金面上项目(81073140);北京中医药大学自主选题项目(2011JYBZZ-XS050)

摘　　要：目的探讨黄连中5种结构相似异喹啉生物碱大鼠体外肝代谢的选择性。方法采用大鼠体外肝微粒体温孵方法,通过考察温孵时间、微粒体蛋白浓度以及底物浓度对小檗碱、巴马汀、黄连碱、表小檗碱和药根碱代谢的影响,求得代谢反应动力学参数Km、Vmax和CLint。结果 5种黄连生物碱成分的体外肝代谢动力学参数Km和CLint间差异明显(P<0.05)。结论黄连中5种异喹啉生物碱大鼠体外肝代谢存在显著选择性。Objective To explore the in vitro hepatic metabolic selectivity of five kinds of isoquinoline alkaloids （with the similar structures） from Coptis chinensis in rats. Methods Using the method of rat in vitro liver microsomes incubation model, the metabolic kinetics parameters Km, Vmax, and CLint for berberine, palmatine, coptisine, epiberberine, and jateorhizine were calculated by observing the influence of incubation time, protein concentration of liver microsomes, and substrate concentration on metabolic characteristics in liver. Results The difference of in vitro hepatic metabolic kinetics parameters Km and fLint among five kinds of alkaloids from C. chinensis is statistically significant （P 〈 0.05）. Conclusion There is a significant selectivity in in vitro hepatic metabolism of five kinds of isoquinoline alkaloids from C. chinensis in rats.

关 键 词：黄连生物碱 体外肝代谢 代谢选择性 肝线粒体 异喹啉生物碱 

分 类 号：R285.5[医药卫生—中药学]