【摘要】 目的:初步考察尿毒清颗粒(NDQ)对重组人CYP450(细胞色素P450)和P-gp(P糖蛋白)的体外影响。方法:①使用Promega P450-GloTMScreening System,通过荧光发光原理来检测NDQ组、抑制剂组对重组CYP450的IC50值,比较NDQ组与抑制剂组IC50来评价NDQ对重组人CYP1A2,CYP2D6,CYP3A4,CYP2C19,CYP2C9的抑制作用。②使用BD ATPase Assay Kit,通过发光法检测NDQ组、空白对照组P-gp ATP酶活性,比较NDQ组、空白对照组ATP酶活性来评价NDQ是否为重组人P-gp的底物或抑制剂。结果:①NDQ组与抑制剂组IC50值(mg/ml)如下,CYP1A2:17.47、3.37×10-6;CYP3A4:33、4.1813×10-5;CYP2C9:10.39、1.056×10-3;CYP2D6:13.98、2.2459×10-6;CYP2C19:9.251、1.442×10-3。②NDQ组的P-GP ATP酶的活性为16.39nmol/mg protein/min,空白对照组的ATP酶活性为4.72 nmol/mg protein/min。结论:①NDQ组与抑制剂组IC50值差异较大,不在一个数量级,NDQ对重组人CYP 1A2、CYP 2D6、CYP 3A4、CYP2C19、CYP2C9基本没有抑制作用。②NDQ组ATP酶活性高于空白组并具有显著性差异,因此,NDQ可能为重组人P-GP的抑制剂或底物。更多还原

【Abstract】 Objective: To investigate the effect of Niaoduqing(NDQ)Granule on recombinant CYP450s and P-gp in vitro.Methods: 1.Using P450-GloTM Screening System to detect the IC50 of sample group by the fluorescence light.NDQ group were compared with positive control to investigate the inhibition of NDQ to CYP1A2,CYP2C9,CYP3A4,CYP2D6,CYP2C19 in vitro.2.Using BD GentestTM ATPase Assay Kit to detect the activity of P-gp ATP enzyme of sample group by the fluorescence light.NDQ group were compared with the control to investigate whether NDQ is the potential substrate or inhibitor.Results: 1.The IC50 of NDQ and positive group(mg/ml): CYP1A2: 17.47、3.37×10-6;CYP3A4:33、4.1813×10-5;CYP2C9:10.39、1.056×10-3;CYP2D6:13.98、2.2459×10-6;CYP2C19:9.251、1.442×10-3.2.NDQ to P-GP ATP of the enzyme activity was 16.39 nmol/mg protein/min,the control group was 4.72 nmol/mg protein/min.Conclusion: 1.The study demonstrated that NDQ can not inhibit the five major human CYP450.2.NDQ is like to be the potential substrate or inhibitor for human P-GP.更多还原