罗布麻茶黄酮提取物对小鼠CYP2E1的影响

Effect of flavonoids extract from apocynum venetum tea on CYP2E1 in mice

中文关键词:  罗布麻茶  黄酮提取物  肝脏微粒体  CYP2E1  半数抑制浓度(IC50)

英文关键词:apocynum venetum tea  flavonoids extract  liver microsome  CYP2E1  half maximal inhibitory concentration (IC50)

中文摘要:

      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128.4 μg/mL。结论 罗布麻茶黄酮提取物对小鼠CYP2E1有抑制作用。

英文摘要:

      Objective CYP2E1 is one of the major drug metabolic enzymes in the liver. The effect of flavonoids extract from apocynum venetum tea (AVE) on CYP2E1 activity and expression in mice were investigated 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 microsome 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.