环孢素A与盐酸小檗碱合用对大鼠肝脏和小肠药物代谢酶的影响  

Effects of berberine chloride and coadministration with cyclo sporin on liver and small intestine microsomal cytochrome P450 isoenzyme in rat

作　　者：余爱荣[1] 辛华雯[1] 吴笑春[1] 李罄[1] 朱敏[1] 

机构地区：[1]广州军区武汉总医院,湖北武汉430070

出　　处：《中国医院药学杂志》2005年第2期104-106,共3页Chinese Journal of Hospital Pharmacy

基　　金：湖北省自然科学基金项目(编号:2002AB114)

摘　　要：　目的:研究盐酸小檗碱(berberine chloride,Ber)与环孢素 A(CsA)合用对大鼠肝脏和小肠药物代谢酶的影响。方法:采用分光光度法测定各给药组大鼠肝脏和小肠微粒体中红霉素 N- 脱甲基酶(ERD)、氨基比林 N 脱甲基酶(ADM)和谷胱甘肽转移酶(GST)的活性。结果:Ber组和Ber+CsA组能明显抑制肝微粒体中 ERD、ADM和 GST酶活性(P<0.05),而且 Ber+CsA组较CsA单用组有更明显的抑制作用(P<0.05)。Ber+CsA组还能明显抑制肠微粒体中 ERD、ADM和 GST酶活性(P<0.05)。结论:Ber与CsA合用时,能显著抑制大鼠肝脏和小肠药物代谢酶活性,这可能是Ber增加CsA血药浓度的一个重要机制。OBJECTIVE To study the effects of berberine chloride（Ber） and coadministration with cyclosporin （CsA） on liver and small intestine microsomal cytochrome P450 isoenzyme in rat. METHODS The activities of erythromycin demethylase（ERD） and aminopyrence N-demethylase（ADM） and Glutathione S transferees （GST） for each group were determined by spectrophotometry. RESULTS 200 mg·kg^-1 Ber group and 200 mg·kg^-1 Ber administrated with 10 mg·kg^-1 CsA group could markedly inhibite the activities of ERD and ADM and GST on liver microsomal in rat compared to the control group and the inhibition ratio was found reduced further in Ber plus CsA group compared to CsA group. In addition, 200 mg·kg^-1 Ber administrated with 10 mg·kg^-1 CsA had significant inhibitory effect on ERD and ADM and GST activities on small intestine microsomal in rat. CONCLUSION It may be an important mechanism on CsA concentration increase by Ber that Ber administrated with CsA decreases the activities of liver and small intestine microsomal cytochrome P450 isoenzyme.

关 键 词：盐酸小檗碱 环孢素A 药物代谢酶 

分 类 号：R965[医药卫生—药理学]