Influences of Fructus evodiae pretreatment on the pharmacokinetics of Rhizoma coptidis alkaloids

• Published in: Journal of ethnopharmacology 2011-10, Vol.137 (3), p.1395-1401
• Main Authors: Ma, Bing-Liang, Yao, Meng-Kan, Han, Xiang-Hui, Ma, Yue-Ming, Wu, Jia-Sheng, Wang, Chang-Hong
• Format: Article
• Language: English
• Subjects: Administration, Oral; Alkaloids - administration & dosage; Alkaloids - pharmacokinetics; Animals; Berberine; Drug Interactions; Drugs, Chinese Herbal - administration & dosage; Drugs, Chinese Herbal - pharmacokinetics; Evodia - chemistry; Female; Fructus evodiae; Fruit; Glucuronosyltransferase - genetics; Glucuronosyltransferase - metabolism; Herb–herb interactions; In Vitro Techniques; Intestinal Absorption; Intestines - metabolism; Liver - drug effects; Liver - metabolism; Male; Microsomes, Liver - metabolism; Pharmacokinetics; Plants, Medicinal; Ranunculaceae - chemistry; Rats; Rats, Sprague-Dawley; Rhizoma coptidis; Rhizome; UGT1A1; Up-Regulation
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2011.08.002

Rhizoma coptidis is a traditional Chinese medicine with pharmacological properties. It is usually prescribed with Fructus evodiae as traditional Chinese medicine (TCM) formulas. Here we report the influences of Fructus evodiae on the pharmacokinetics of the Rhizoma coptidis alkaloids and propose possible mechanisms. Rhizoma coptidis is a traditional Chinese medicine with pharmacological properties. It is usually prescribed with Fructus evodiae as traditional Chinese medicine (TCM) formulas. Here we report the influences of Fructus evodiae on the pharmacokinetics of the Rhizoma coptidis alkaloids and propose possible mechanisms. Pharmacokinetic experiments were performed in rats. In vitro absorption experiments were performed in everted rat gut sacs, while in vitro metabolism experiments and determination of hepatic UDP-glucuronosyltransferase (UGT) 1A1 mRNA expression were performed in rat liver microsomes. Pretreatment with Fructus evodiae extract for two weeks decreased the systemic exposure of the Rhizoma coptidis alkaloids. This effect was not due to inhibition of absorption or enhanced hepatic phase I metabolism of the Rhizoma coptidis alkaloids. However, Fructus evodiae pretreatment enhanced both the activity and expression of hepatic UGT1A1. The results showed that Fructus evodiae pretreatment decreased the systemic exposure of the Rhizoma coptidis alkaloids by inducing hepatic UGT1A1.