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目的研究半枝莲水相和乙醇相提取物对人细胞色素P450主要酶活性的影响,为半枝莲的开发和合理地临床应用提供参考。方法以咪哒唑仑、甲苯磺丁脲、咖啡因、氯唑沙完、异喹呱和试卤灵为探针药,用高效液相色谱法分别测定不同提取溶质的半枝莲粗提物对人细胞色素P450主要酶活性的影响。结果①半枝莲粗提物对CYP3A4、CYP2C9、CYP1A2、CYP1A1酶的活性呈现出剂量依赖性抑制作用。②半枝莲水相粗提物比乙醇相粗提物对CYP1A1和CYP1A2酶的体外抑制作用强。结论半枝莲水相提取物和乙醇相提取物是CYP3A4、CYP2C9、CYP1A2、CYP1A1体外抑制剂。
OBJECTIVE: To study the effects of aqueous extracts and ethanol extracts of Scutellaria barbata on activities of human cytochrome P450 and to provide reference for the development and rational clinical application of Scutellaria barbata. Methods Mipazolam, tolbutamide, caffeine, chlorzoxa finished, disoquinolate and resorufin were used as probes to determine the crude extracts of Scutellaria barbatae with different extraction solutes by high performance liquid chromatography. Effects on human cytochrome P450 activity. Results 1The activity of CYP3A4, CYP2C9, CYP1A2 and CYP1A1 showed a dose-dependent inhibitory effect. 2 The crude extracts from the aqueous extract of Scutellaria barbata had a stronger inhibitory effect on the CYP1A1 and CYP1A2 enzymes than the crude ethanol extracts. Conclusion The aqueous extracts and ethanol extracts of Scutellaria barbata are inhibitors of CYP3A4, CYP2C9, CYP1A2, and CYP1A1 in vitro.