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目的:考察川楝子对大鼠肝细胞色素P450 1A2、2E1、3A1活性的影响。方法:大鼠分组,连续灌胃给予150g生药/kg的川楝子7天;苯巴比妥组腹腔注射0.08g/kg的苯巴比妥3次。高效液相色谱法对肝细胞色素P450 1A2、2E1、3A1代谢能力进行测定。结果:连续给予川楝子7天后,对肝细胞色素P450 1A2代谢能力影响不明显,但可使大鼠肝微粒体酶蛋白含量增加,使肝细胞色素P450 1A2总代谢能力增强;对大鼠大鼠肝细胞色素P450 2E1活性及代谢能力均无明显影响;川楝子可诱导雌性大鼠大鼠肝细胞色素P450 3A1,使6-OH睾酮代谢生成速率及肝脏总代谢睾酮的能力增强;对雄性大鼠肝细胞色素P450 3A1有诱导的趋势,使6-OH睾酮代谢生成速率及肝脏总代谢睾酮的能力有增强的趋势,但与对照组比较差异无显著意义。结论:川楝子对大鼠肝细胞色素P450 3A1活性具有诱导作用。
Objective: To investigate the effects of Toosendan on the activities of hepatocyte cytochrome P450 1A2, 2E1 and 3A1 in rats. Methods: The rats were divided into groups and were given 150g crude drug / kg toosendanin orally for 7 days. Phenobarbital group was injected intraperitoneally with 0.08g / kg phenobarbital three times. High performance liquid chromatography (HPLC) was used to determine the metabolism of hepatocyte cytochrome P450 1A2, 2E1 and 3A1. Results: Toosendanin administered continuously for 7 days had no obvious effect on the metabolism of hepatocyte cytochrome P450 1A2, but increased the content of hepatic microsomal enzyme protein and enhanced the total metabolism of hepatocyte cytochrome P450 1A2. Toosendanin can induce hepatocyte cytochrome P450 3A1 in rats, and enhance the metabolic rate of 6-OH testosterone and liver’s total metabolic testosterone; Rat liver cytochrome P450 3A1 induced trend, the 6-OH testosterone metabolic rate and liver metabolic activity of testosterone increased trend, but compared with the control group no significant difference. CONCLUSION: Toosendanin can induce the activity of hepatocyte cytochrome P450 3A1 in rats.