Andrographis paniculata Extract and Andrographolide Modulate the Hepatic Drug Metabolism System and Plasma Tolbutamide Concentrations in Rats

被引：23

作者：

Chen, Haw-Wen ^{[1
]}

Huang, Chin-Shiu ^{[2
]}

Liu, Pei-Fen ^{[1
]}

Li, Chien-Chun ^{[3
]}

Chen, Chiung-Tong ^{[4
]}

Liu, Cheng-Tzu ^{[3
]}

Chiang, Jia-Rong ^{[1
]}

Yao, Hsien-Tsung ^{[1
]}

Lii, Chong-Kuei ^{[1
,2
]}

机构：

[1] China Med Univ, Dept Nutr, Taichung 404, Taiwan

[2] Asia Univ, Dept Hlth & Nutr Biotechnol, Taichung 413, Taiwan

[3] Chung Shan Med Univ, Dept Nutr, Taichung 408, Taiwan

[4] Natl Hlth Res Inst, Inst Biotechnol & Pharmaceut Res, Miaoli 350, Taiwan

来源：

EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE | 2013年 / 2013卷

关键词：

CONSTITUTIVE ANDROSTANE RECEPTOR; GLUTATHIONE-S-TRANSFERASE; MESSENGER-RNA EXPRESSION; PHASE-II ENZYMES; ACTIVE DITERPENOIDS; LIVER-MICROSOMES; PI-CLASS; INDUCTION; ACTIVATION; GENES;

D O I：

10.1155/2013/982689

中图分类号：

R [医药、卫生];

学科分类号：

100218 [急诊医学];

摘要：

Andrographolide is the most abundant terpenoid of A. paniculata which is used in the treatment of diabetes. In this study, we investigated the effects of A. paniculata extract ( APE) and andrographolide on the expression of drug-metabolizing enzymes in rat liver and determined whether modulation of these enzymes changed the pharmacokinetics of tolbutamide. Rats were intragastrically dosed with 2 g/kg/day APE or 50 mg/kg/day andrographolide for 5 days before a dose of 20 mg/kg tolbutamide was given. APE and andrographolide reduced the AUC(0-12h) of tolbutamide by 37% and 18%, respectively, compared with that in controls. The protein and mRNA levels and enzyme activities of CYP2C6/11, CYP1A1/2, and CYP3A1/2 were increased by APE and andrographolide. To evaluate whether APE or andrographolide affected the hypoglycemic action of tolbutamide, high-fat diet-induced obese mice were used and treated in the same manner as the rats. APE and andrographolide increased CYP2C6/11 expression and decreased plasma tolbutamide levels. In a glucose tolerance test, however, the hypoglycemic effect of tolbutamide was not changed by APE or andrographolide. These results suggest that APE and andrographolide accelerate the metabolism rate of tolbutamide through increased expression and activity of drug-metabolizing enzymes. APE and andrographolide, however, do not impair the hypoglycemic effect of tolbutamide.

引用

页数：11

共 59 条

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