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目的:用Cocktail探针药物法研究制首乌对大鼠肝细胞色素P450(CYP450)的影响。方法:12只雄性SD大鼠随机分为制首乌组和空白对照组,每组6只,分别灌胃给予制首乌12 g·kg~(-1)或等量的生理盐水,连续7 d。尾iv给予“Cocktail”混合探针药物(咖啡因、氯唑沙宗、氨苯砜剂量分别为10,20,10 mg·kg~(-1))5 ml·kg~(-1),于给药后0.167,0.333,0.667,1,1.5,2,3,5,8,12,24 h从大鼠眼眶取血,HPLC检测探针药物在大鼠体内的代谢情况,以评价制首乌对肝细胞色素P450酶的影响。结果:制首乌组中咖啡因、氨苯砜和氯唑沙宗的代谢情况与空白对照组相比,t_(1/2)、AUC_((0–t))明显减小,CL明显升高(P<0.05或P<0.01)。结论:制首乌对代谢酶CYPl A2、CYP3A4和CYP2E1具有诱导作用。
Objective: To study the effect of Radix Polygoni multiflori on hepatocyte cytochrome P450 (CYP450) in rats by using Cocktail probe drug method. Methods: Twelve male Sprague Dawley rats were randomly divided into Shouwu group and blank control group, with 6 rats in each group. The rats were given gavage with 12 g · kg -1 or equivalent of normal saline for 7 d. The mice were anesthetized with 5 mL · kg -1 of “Cocktail” mixed-probe drugs (caffeine, chlorzoxazone, dapsone, respectively) Blood samples were taken from orbital of rats at 0.167, 0.333, 0.667, 1, 1.5, 2, 3, 5, 8, 12 and 24 h after drug administration. The metabolism of probe drugs in rats was detected by HPLC. Effect of Radix Polygoni Multiflori on Hepatic Cytochrome P450 Enzymes. Results: The metabolic rate of caffeine, dapsone and chlorzoxazone in Shouwu group was significantly lower than that in the blank control group (P <0.05), while the AUC (0-t) High (P <0.05 or P <0.01). Conclusion: Radix Polygoni multiflori induces the metabolic enzymes CYP1 A2, CYP3A4 and CYP2E1.