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目的:探讨仙茅体内代谢过程与药物代谢酶细胞色素P4503A(CYP3A)的相关性,为进一步研究机体CYP3A活性变化对仙茅性-效表达的影响奠定基础。方法:SD雄性大鼠随机分为2组,即正常组和利福平组。利福平组每天灌胃给予200mg/kg药物混悬液,正常组给予等体积蒸馏水,连续7d,第8天每组各取6只大鼠一次性灌胃仙茅水煎液(20g/kg)后,分别于20、50、90、180min时眼眶取血测仙茅入血成分苔黑酚葡萄糖苷血药浓度,其他大鼠断头处死,取肝、小肠、肾测定CYP3A活性。结果:利福平组大鼠肝微粒体CYP3A活性明显升高(P<0.05),小肠、肾微粒体CYP3A活性有升高趋势;利福平组大鼠各时间点血药浓度均低于正常组,且在20、50、90时差异有统计学意义(P<0.05,P<0.01)。结论:利福平诱导后大鼠肝微粒体CYP3A活性升高,而苔黑酚葡萄糖苷血药浓度明显降低,说明仙茅体内代谢过程与药物代谢酶CYP3A相关。
OBJECTIVE: To investigate the correlation between the metabolism of cimicifuga and cytochrome P450 3A (CYP3A) in vivo and to lay the foundation for the further study of the effect of CYP3A activity on the expression of sex-effective cimicifuga. Methods: SD male rats were randomly divided into two groups: normal group and rifampicin group. Rifampicin group was given intragastric administration of 200mg / kg drug suspension daily, and the normal group was given equal volume of distilled water for 7 days. On the 8th day, 6 rats in each group were given ginseng decoction (20g / kg ), Respectively, at 20,50,90,180 min orbital blood flow test Cortex anisopliae blood components orcinol glucoside blood concentration, other rats were decapitated, liver, small intestine and kidney were measured CYP3A activity. Results: The activity of CYP3A in the liver microsomes of rifampicin group was significantly increased (P <0.05), and the CYP3A activity of microsomes in small intestine and kidney was increased. The plasma concentrations of rifampicin group were lower than normal Group, and the difference was statistically significant at 20,50,90 (P <0.05, P <0.01). CONCLUSION: The activity of CYP3A in rat liver microsomes induced by rifampicin is increased, while the blood concentration of orcinol glucoside is significantly decreased, which indicates that the metabolism of cimicifuga is related to the enzyme CYP3A.