吴茱萸次碱对5种黄连生物碱大鼠体外肝代谢的抑制作用

Inhibition of rutaecarpine on in vitro hepatic metabolism of five Coptis alkaloids in rats

目的考察吴茱萸主要成分吴茱萸次碱对黄连中5种生物碱肝代谢的抑制作用,为深入研究黄连吴茱萸药对配伍机制提供依据。方法采用大鼠体外肝微粒体温孵法,考察吴茱萸次碱对黄连中5种生物碱(黄连碱、表小檗碱、小檗碱、巴马汀和药根碱)肝代谢的抑制作用。结果吴茱萸次碱对黄连碱、表小檗碱、小檗碱、巴马汀、药根碱均存在体外肝代谢抑制作用,半数抑制浓度(IC50)均大于50μmol/L,表现为体外弱抑制作用;抑制常数(Ki)的差异性具有统计学意义(P<0.05),抑制作用强弱程度顺序为小檗碱>药根碱>巴马汀>表小檗碱>黄连碱。结论为了解吴茱萸对黄连生物碱主要作用环节和揭示黄连吴茱萸药对配伍机制提供依据。

To investigate the inhibition of rutaecarpine, a main component in Evodiae Fructus, on the hepatic metabolism of five Coptis alkaloids, and to provide the basis for further study of compatibility mechanism between Coptidis Rhizoma and Evodiae Fructus. Methods Using rat liver microsome incubation method, the inhibition ofrutaecarpine on hepatic metabolism of five Coptis alkaloids in vitro was investigated. Results Rutaecarpine could inhibit the in vitro hepatic metabolisms of coptisine, epiberberine, berberine, palmatine, and jatrorrhizine. The half inhibitory concentration （IC_50） was all greater than 50 μmol/L which showed rutaecarpine had a weak inhibition on Coptis alkaloids. The differences of inhibition constant （Ki） were statistically significant （P 〈 0.05）. The order of inhibited extent was as follows： berberine 〉 jatrorrhizine 〉 palmatine 〉 epiberberine 〉 coptisine. Conclusion The results could provide the basis to learn the major role on the links that Evodiae Fructus acted on Coptis alkaloids and reveal the compatibility mechanism between Coptidis Rhizoma and Evodiae Fructus.