目的：研究甘草甜素(glycyr hizin)体外对细胞色素P450酶亚型CYP1A2活性的影响。方法：以咖啡因为探针药，采用高效液相色谱法测定探针药与相应代谢产物的浓度，研究甘草甜素在人肝微粒体孵化体系和重组酶体系中对CYP1A2活性的影响。结果：在人肝微粒体反应体系中，0.1，0.2，0.4，0.8mmol囯L-1甘草甜素使咖啡因的代谢产物的生成分别降低了31±15％(p=0.007)、43±8％(p=0.012)、48±6％(p=0.037)、49±4％(p=0.029)；在体外重组酶反应体系中，0.1，0.4mmol囯L-1甘草甜素使咖啡因的代谢产物的生成分别降低了48±9％( p=0.012)、82±8％( p=0.004)。结论：甘草甜素对C Y P1A2酶体外活性有较明显的抑制作用；随着甘草甜素浓度的增高，抑制作用也相应增强。
Objective: To investigate the effect of glycyrrhizin on CYP1A2activity in vitro.Method:Caffeine(a CYP1A2 substrate) was used as probe. The concentrations of the probe drug and its metabolite were determined by HPLC. The effect of glycyrrhizin on activity of CYP1A2 was detected through human microsomes and recombinant enzyme reaction system in vitro. Results:Glycyrrhizin inhibited the activity of CYP1A2in vitro. In human liver microsome, 0.1mM, 0.2mM, 0.4mM, 0.8mMglycyrrhizin decreased the activities of CYP1A2by 31±15%(p=0.007), 43±8%(p=0.012), 48±6%(p=0.037), 49±4%respectively. In recombinant enzyme reaction system, 0.1mM, 0.4mM,glycyrrhizin decreased the activities of CYP1A2by48±9%(p=0.012)、82±8%(p=0.004).Conclusion:Glycyrrhizin inhibited the activity of CYP1A2 in a dose-dependent fashion in vitro .
NETL
NSTL
万方数据
