title: Influences of Fructus evodiae pretreatment on the pharmacokinetics of Rhizoma coptidis alkaloids.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  RESULTS
  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.
  
  
  CONCLUSIONS
  The results showed that Fructus evodiae pretreatment decreased the systemic exposure of the Rhizoma coptidis alkaloids by inducing hepatic UGT1A1.
authors.affiliation: Laboratory of Pharmacokinetics, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Bing-Liang
authors.initials: BL
authors.lastname: Ma
authors.forename: Meng-Kan
authors.initials: MK
authors.lastname: Yao
authors.forename: Xiang-Hui
authors.initials: XH
authors.lastname: Han
authors.forename: Yue-Ming
authors.initials: YM
authors.lastname: Ma
authors.forename: Jia-Sheng
authors.initials: JS
authors.lastname: Wu
authors.forename: Chang-Hong
authors.initials: CH
authors.lastname: Wang
mesh_terms: D000284:Administration, Oral; D000470:Alkaloids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D004347:Drug Interactions; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D032086:Evodia / Q000737:chemistry; D005260:Female; D005638:Fruit; D014453:Glucuronosyltransferase / Q000235:genetics / Q000378:metabolism; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism*; D008099:Liver / Q000187:drug effects / Q000378:metabolism*; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D010946:Plants, Medicinal; D029626:Ranunculaceae / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D027343:Rhizome; D015854:Up-Regulation; D000099148:UGT1A1 Enzyme
chemical_list: D000470:Alkaloids; D004365:Drugs, Chinese Herbal; D014453:Glucuronosyltransferase; C499946:Ugt1a1 protein, rat; D000099148:UGT1A1 Enzyme; C494417:huanglian