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目的:研究戊己丸不同配比方对大鼠体外肝微粒体CYP3A1/3A2酶活性的影响,从“中药配伍-代谢”关系探讨戊己丸的配伍机制。方法:按L9(34)正交表,戊己丸的配比设计为9个受试复方,以睾丸酮为探针药,HPLC检测戊己丸对大鼠体外肝微粒体CYP3A1/3A2酶活性的影响。结果:黄连、吴茱萸、白芍各提取物及戊己丸1号～9号方抑制CYP3A1/3A2的IC50分别为38.96,871.96,15519.17,43.17,60.47,276.12,133.40,118.08,88.47,64.36,35.13,39.91mg.L-1;黄连及戊己丸均可显著抑制CYP3A1/3A2酶活性,不同配比戊己丸抑制CYP3A1/3A2酶活性作用不同,有统计学差异;随着黄连在戊己丸方中剂量水平的增高,戊己丸组方抑制CYP3A1/3A2酶活性的能力增强,且戊己丸组方中吴茱萸和白芍配比不同可以影响方中黄连抑制CYP3A1/3A2酶活性的程度。结论:戊己丸配比不同,对CYP3A1/3A2酶活性的抑制作用不同,这种差异可能是不同配比戊己丸药效学、药动学差异的原因所在。
OBJECTIVE: To study the effects of different formulations of Wuji Pills on the activity of CYP3A1 / 3A2 in vitro of rat microsomes, and to explore the compatibility mechanism of “Wuji Pills” from the relationship of “compatibility of traditional Chinese medicine with metabolism”. Methods: According to the orthogonal test of L9 (34) and the ratio of Wuji Pills, nine test compounds were designed. Testosterone was used as test substance to test the effect of Wuji Pill on rat liver microsomal CYP3A1 / 3A2 activity influences. Results: The IC50 of inhibition of CYP3A1 / 3A2 of Coptis chinensis Franch, Evodia rutaecarpa, Radix Paeoniae Alba and Radix et Rhizoma pestis No.1-9 were 38.96,871.96,15519.17,43.17,60.47,276.12,133.40,118.08,88.47,64.36,35.13 respectively , 39.91mg.L-1; Coptis chinensis and Wuji pills can significantly inhibit the CYP3A1 / 3A2 enzyme activity, different proportions of the pentamine pills inhibit CYP3A1 / 3A2 enzyme activity has a statistically significant difference; with the Coptis The middle dose level increased, the ability of Wuji pill group to inhibit CYP3A1 / 3A2 enzyme activity was enhanced, and Wujiuyu group and Radix Paeoniae radii different ratio can affect the degree of inhibition of CYP3A1 / 3A2 activity. Conclusion: The different ratios of Wuji Pills have different inhibitory effects on CYP3A1 / 3A2 enzyme activity, which may be the reason of different pharmacodynamics and pharmacokinetics of different proportions of Wuji Pills.