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目的:考察注射用丹参总酚酸(TSAI)对大鼠肝微粒体CYP1A2和CYP3A的诱导作用。方法:健康Wistar大鼠随机分为空白对照组、苯巴比妥钠诱导组和给药组,每组6只,雌雄各半,连续给药7 d,处死,制备肝微粒体;将特异性探针底物非那西丁、睾酮与肝微粒体共孵育,高效液相色谱测定孵育所得代谢产物对乙酰氨基酚和6β-羟基睾酮的生成速率,评价TSAI对CYP1A2和CYP3A的诱导作用。结果:空白对照组、诱导组和给药组的对乙酰氨基酚的生成速率分别为(18.04±1.00),(43.07±2.90)和(16.03±2.41)ng.mg-1.min-1,6β-羟基睾酮的生成速率分别为(15.79±1.43),(40.86±3.32)和(17.12±2.65)ng.mg-1.min-1。结论:TSAI对大鼠肝微粒体CYP1A2和CYP3A无诱导作用。
OBJECTIVE: To investigate the induction of CYP1A2 and CYP3A in liver microsomes of rat by TSAI injection. Methods: Healthy Wistar rats were randomly divided into blank control group, phenobarbital sodium induction group and administration group, 6 in each group, male and female, continuous administration for 7 days, sacrificed to prepare liver microsomes; Probe substrate phenacetin and testosterone were incubated with liver microsomes. The formation rates of acetaminophen and 6β-hydroxytestosterone were determined by high performance liquid chromatography (HPLC), and the induction of CYP1A2 and CYP3A by TSAI was evaluated. Results: The formation rates of acetaminophen in the blank control group, the induction group and the administration group were (18.04 ± 1.00), (43.07 ± 2.90) and (16.03 ± 2.41) ng.mg-1.min-1,6β - Hydroxytestosterone was (15.79 ± 1.43), (40.86 ± 3.32) and (17.12 ± 2.65) ng.mg-1.min-1, respectively. Conclusion: TSAI has no effect on the liver microsomal CYP1A2 and CYP3A in rats.