血塞通及川芎嗪对细胞色素P450不同亚型代谢酶影响的研究  

Effects of traditional Chinese medicine Panax notoginoside(血塞通) and Tetramethylpyrazine(川芎嗪)on cytochrome P450 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：《中国中西医结合急救杂志》2008年第6期342-345,共4页Chinese Journal of Integrated Traditional and Western Medicine in Intensive and Critical Care

基　　金：山东省青岛市科技局科技计划项目(K2-26)

摘　　要：目的研究血塞通和川芎秦对肝微粒体细胞色素P450(CYP450)酶系统不同亚型的影响,预测它们之间及与其他药物间的相互作用,并为临床合理用药提供参考。方法通过研究CYP450亚型CYP1A2、CYP3A4的专属探针药物咖啡因、氨苯砜的体外代谢变化,评价血塞通和川芎秦对这两个酶的诱导或抑制作用。结果对照组、血塞通组和川芎嗪组中咖啡因和氨苯砜的浓度均随时间延长而降低,3组间差异无统计学意义。血塞通组探针药物咖啡因体外半衰期明显短于对照组〔(19.24±2.37)min比(25.15±2.02)min,P<0.01〕,川芎嗪组咖啡因体外半衰期〔(27.67±4.64)min〕与对照组无明显差异,说明血塞通对肝药酶CYP1A2有诱导作用,而对CYP3A4无影响;血塞通组和川芎嗪组探针药物氨苯砜体外半衰期与对照组比较差异均无统计学意义〔(16.29±2.94)min、(15.16±1.67)min比(16.16±1.51)min,P均>0.05〕,说明川芎嗪对肝药酶CYP1A2和CYP3A4均无影响。结论药物对CYP450各亚型酶的影响不同。血塞通在同CYP1A2代谢相关的药物合用时,应充分考虑其对CYP1A2的影响,以避免可能出现的毒性反应或不良反应。Objective To study the effects of traditional Chinese medicine Panax notoginoside(PNS,血塞通) and Tetramethylpyrazine(TMPz,川芎嗪) on different subtypes of cytochrome P450(CYP450),based on that,to forecast the inter-reaction between these two drugs and between each one of them and another drug,and also to estimate the safety assessment of them.Methods The metabolic changes of caffeine and dapsone which are the specific probe drugs for subtypes of CYP450,CYP1A2 and CYP3A4,were studied in vitro to estimate the inhi...

关 键 词：细胞色素P450 肝微粒体 血塞通 川芎嗪 咖啡因 氨苯砜 

分 类 号：R285.5[医药卫生—中药学]