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目的:分析活血化瘀药物有效成分对生物转化酶的影响。方法:选取16只雄性SD大鼠,随机分为4组,每组4只,分别给予DEX色拉油混悬液、PB生理盐水溶液、β-NF色拉油混悬液、色拉油。分析大鼠血浆及肝微粒体温孵液中川芎嗪及其代谢产物的相关性。结果:在大鼠肝微粒体中诱导后的川芎嗪代谢较快,且川芎嗪在DEX、PB、DEX及对照组中的平均代谢消失率分别为(76.25±10.23)%、(19.26±7.13)%、(14.96±1.26)%、(13.49±1.34)%。强效的CYP3A抑制剂Ket能够抑制川芎嗪的代谢,其代谢率与CYP3A的特征性有着相关性。结论:川芎嗪生物转化的CYP450亚酶是CYP3A,且两者抑制或者诱导在药物中可能存在相互作用。
Objective: To analyze the influence of the active ingredients of drugs for promoting blood circulation and removing blood on bioconverting enzymes. Methods: Sixteen male Sprague-Dawley rats were randomly divided into 4 groups with 4 rats in each group. DEX salad oil suspension, PB physiological saline solution, β-NF salad oil suspension and salad oil were given respectively. The correlation between ligustrazine and its metabolites in rat plasma and liver microsomal incubation was analyzed. Results: Ligustrazine was rapidly metabolized in rat liver microsomes, and the average rate of disappearance of ligustrazine in DEX, PB, DEX and control groups was (76.25 ± 10.23)% and (19.26 ± 7.13)%, respectively %, (14.96 ± 1.26)%, (13.49 ± 1.34)%. Potent CYP3A inhibitor Ket can inhibit the metabolism of tetramethylpyrazine, its metabolic rate CYP3A has a characteristic correlation. CONCLUSION: Tetramethylpyrazine (CYP450) CYP450 is a CYP3A biotransducer that inhibits or induces the possible interaction of the two drugs in the drug.