摘要
目的:考察藏药余甘子鞣质部位对大鼠肝微粒体代谢酶P450活性的影响。方法:采用"Cocktail"探针底物与大鼠肝微粒体体外温孵法,通过HPLC同时测定6种探针药物氨苯砜、氢溴酸右美沙芬、香豆素、非那西丁、氯唑沙宗、甲苯磺丁脲的代谢消除率,评价余甘子鞣质部位对P450酶中CYP3A4、CYP2D6、CYP2A6、CYP1A2、CYP2E1、CYP2C9亚酶活性的影响。结果:余甘子鞣质部位对P450酶影响较小,CYP3A4,CYP1A2的IC50值超过200μg·m L-1,CYP2C9的IC50值超过500μg·m L-1。结论:藏药余甘子鞣质部位对肝P450酶活性影响较弱。
This study aimed to investigate the effects of tannins extracted from Tibetan medicine Phyllanthi Fructus on cytochrome P450 enzyme of liver microsomes in rats.Cocktail probe substrates were incubated with liver microsomes in vitro.Metabolic elimination percentages of the six probe substrates,including dapsone,dextromethorphan hydrobromide,coumarin,phenacetin,chlorzoxazone and tolbutamide,were determined by HPLC.The effects of tannins extracted from Tibetan medicine Phyllanthi Fructus on the enzymatic activity of rat liver microsomal P450 s was evaluated.It was found that tannins extracted from Phyllanthi Fructus did not impact P450 enzymes.The IC50 values of CYP3A4 and CYP1A2 were over 200 μg·m L-1,while the IC50 value of CYP2C9 was superior to 500 μg·m L-1.In conclusion,Tannins extracted from Tibetan medicine Phyllanthi Fructus did not significantly affect cytochrome P450 enzymes.
出处
《世界科学技术-中医药现代化》
2016年第7期1159-1165,共7页
Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology
基金
国家自然科学基金委面上项目(81274187):基于藏药余甘子酚酸类成分体内动态变化的抗癌药效物质与质量控制研究
负责人:张兰珍
关键词
余甘子鞣质部位
大鼠肝微粒体
代谢酶P450
活性
Tannins extracted from Phyllanthi Fructus
rat liver microsomes
metabolic enzyme P450
activity
