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目的研究喜炎平注射液对人肝微粒体P450酶亚型的体外抑制作用。方法人肝微粒体、喜炎平注射液与5种探针底物(奥美拉唑、右美沙芬、睾酮、氯唑沙宗和甲苯磺丁脲)在还原系统烟酰胺腺嘌呤二核苷酸磷酸还原酶(NADPH)的作用下,于37℃水浴下共同孵育。用液相色谱-质谱联用法,测定探针底物的代谢产物生成量,评价喜炎平注射液对P450酶活性的影响。结果在人肝微粒体体外孵育反应体系中,喜炎平注射液对CYP2C19、CYP2D6、CYP3A4、CYP2E1和CYP2C9酶亚型活性抑制的IC50值分别为1.89,4.10,0.13,0.09,1.44 mg·mL-1。结论喜炎平注射液对CYP3A4和CYP2E1有较强的抑制作用,临床使用时应注意其潜在的药物相互作用。
Objective To study the inhibitory effect of Xiyanping injection on human liver microsomal P450 enzyme subtype in vitro. Methods Human liver microsomes, xiyanping injection and five probe substrates (omeprazole, dextromethorphan, testosterone, chlorzoxazone and tolbutamide) were used in the reduction system nicotinamide adenine dinucleotide Acid phosphate reductase (NADPH), co-incubated at 37 ℃ water bath. The amount of metabolites produced by the probe substrate was determined by liquid chromatography-mass spectrometry, and the effect of Xiyanping injection on P450 enzyme activity was evaluated. Results The IC50 values of Xiyanping injection in inhibiting the activity of CYP2C19, CYP2D6, CYP3A4, CYP2E1 and CYP2C9 subtypes were 1.89, 4.10, 0.13, 0.09 and 1.44 mg · mL- 1. Conclusion Xiyanping Injection has a strong inhibitory effect on CYP3A4 and CYP2E1, and its potential drug interactions should be noticed when used clinically.