三七总皂苷对CYP450的影响及药物相互作用预测  

Effects of Panaxnotoginoside on CYP450 Subtype Enzymes

作　　者：石杰[1] 陈安进[1] 张芳[1] 王本坚[1] 

机构地区：[1]青岛市立医院药物研究室,山东青岛266071

出　　处：《药物流行病学杂志》2008年第5期281-284,共4页Chinese Journal of Pharmacoepidemiology

基　　金：青岛市科技局计划项目(kzd-26)。

摘　　要：目的:研究三七总皂苷(血塞通)对肝微粒体CYP450酶不同亚型的影响,进一步了解其在肝脏的代谢特点并据此对该药与其他药物相互作用的安全性进行预测,为临床合理应用提供依据。方法:检测肝药酶CYP1A2和CYP3A4的专属探针药物咖啡因、氨苯砜的原型浓度,采用原型药物减少初始速率测定法考察其体外代谢变化情况,从而评价三七总皂苷对CYP1A2、CYP3A4的诱导或抑制作用。结果:三七总皂苷对肝药酶CYP1A2有诱导作用,而对CYP3A4无影响。结论:三七总皂苷对CYP450。不同亚型酶的影响不同。在临床应用时,尤其是与CYP1A2代谢有关的药物合用时,应充分考虑到这种影响,以避免潜在的毒性或不良反应。Objective： To study the effects of panaxnotoginoside（PNS）on CYP1A2 and CYP3A4 and estimate the safety of this drug. Method ： The concentrations of caffeine and dapsone were determined, and then their metabolic changes in vitro were studied; thus the inhibition or induction of PNS would be estimated. Result： PNS could induce CYPIA2 but had no effect on CYP3A4. Conclusion： PNS had different effects on difference subtype enzymes. When PNS are used with other drugs, which are related with CYP1A2 enzyme, some potential adverse reactions are needed considering.

关 键 词：三七总皂苷 CYP1A2 CYP3A4 咖啡因 氨苯砜 

分 类 号：R969.2[医药卫生—药理学]