CAJ | 학술논문

目的： CYP2E1是肝脏中主要的药物代谢酶，在肝脏疾病发生及发展中发挥重要的作用。本实验分别通过体内、体外实验，研究罗布麻茶黄酮提取物对小鼠CYP2E1活性和表达的影响，为评价罗布麻茶对肝脏的保护作用和药物的联合使用提供理论依据。方法将30只昆明小鼠随机分为空白对照组、黄酮提取物低剂量组和高剂量组(50和100 mg/kg)，连续灌胃给药10天。采用探针药物法测定小鼠肝脏微粒体中CYP2E1催化对硝基苯酚代谢的活力。采用Western Blot法检测肝脏微粒体中CYP2E1蛋白的表达情况。体外抑制实验中，考察不同浓度的黄酮提取物对 CYP2E1的抑制作用，计算半数抑制浓度(IC50)值。结果灌服高剂量黄酮提取物(100 mg/kg)后，小鼠体内 CYP2E1酶活性和表达量均显著降低，黄酮提取物对 CYP2E1的 IC50值为128.4μg/mL。结论罗布麻茶黄酮提取物对小鼠CYP2E1有抑制作用。
목적： CYP2E1시간장중주요적약물대사매，재간장질병발생급발전중발휘중요적작용。본실험분별통과체내、체외실험，연구라포마다황동제취물대소서CYP2E1활성화표체적영향，위평개라포마다대간장적보호작용화약물적연합사용제공이론의거。방법장30지곤명소서수궤분위공백대조조、황동제취물저제량조화고제량조(50화100 mg/kg)，련속관위급약10천。채용탐침약물법측정소서간장미립체중CYP2E1최화대초기분분대사적활력。채용Western Blot법검측간장미립체중CYP2E1단백적표체정황。체외억제실험중，고찰불동농도적황동제취물대 CYP2E1적억제작용，계산반수억제농도(IC50)치。결과관복고제량황동제취물(100 mg/kg)후，소서체내 CYP2E1매활성화표체량균현저강저，황동제취물대 CYP2E1적 IC50치위128.4μg/mL。결론라포마다황동제취물대소서CYP2E1유억제작용。
ABSTRACT:Objective CYP2E1 is one of the major drug metabolic enzymes in the liver. The effect of fla-vonoids extract from apocynum venetum tea (AVE) on CYP2E1 activity and expression in mice were investi-gated by in vitro and in vivo experiments. Methods The mice were randomly separated to 3 groups, control group, low dose-and high dose AVE (50 and 100 mg/kg, respectively), and the AVE were administered using an intragastric tube once daily for 10 days. Catalytic activity of CYP2E1 in liver microsome was measured by using probe drugs method, and nitrophenol was used as the probe substrate. The expression of CYP2E1 protein in liver microsome was detected using Western blot method. In the in vitro inhibition experiments, liver micro-some was incubated with different concentrations of flavonoids extract, and the 50% inhibitory concentration (IC50) value of AVE on CYP2E1 was calculated. Results After fed with high dose of AVE (100 mg/kg), CYP2E1 activity and expression in mice were significantly reduced comparing to the control group, and IC50 of AVE on CYP2E1 was 128.4 μg/mL. Conclusion Flavonoids extract from apocynum tea effectively inhibits CYP2E1 in mice.