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目的:揭示金合欢素预防雌激素依赖性肿瘤发生的一种机制。方法:通过建立体外代谢模型,采用高效液相色谱-电化学检测器法,分析金合欢素对雌二醇经人细胞色素酶CYP1B1亚酶途径代谢生成致癌产物4-羟基雌二醇的抑制作用。结果:金合欢素对以雌二醇为底物的CYP1B1酶活性的半抑制浓度为(1.43±0.27)μmol·L~(-1),具有较强的抑制雌激素致癌代谢产物生成的活性。结论:金合欢素可以有效地抑制人CYP1B1酶的活性,阻碍雌激素致癌代谢产物的生成,从而预防肿瘤的发生。
Aims: To reveal a mechanism by which acacia prevents estrogen-dependent tumors. Methods: The inhibitory effect of acacetin on 4-hydroxyestradiol, an oncogenic metabolite of estradiol metabolized by the human cytochrome CYP1B1 subunit, was analyzed by establishing an in vitro metabolic model and using high performance liquid chromatography-electrochemical detector effect. Results: The semi-inhibitory concentration of acacetin on the enzyme activity of estradiol-based CYP1B1 was (1.43 ± 0.27) μmol·L -1, which showed a strong inhibitory effect on the production of estrogen-induced oncogenic metabolites. Conclusion: Acacsin can effectively inhibit the activity of human CYP1B1 enzyme and hinder the formation of estrogen carcinogenic metabolites, thereby preventing the occurrence of tumors.