title: The effect of herbal medicine danshensu and ursolic acid on pharmacokinetics of rosuvastatin in rats.
abstract: The aim of this study was to explore potential herb-drug interaction between danshensu or ursolic acid and rosuvastatin. Compared to the control group given rosuvastatin alone, the concurrent use of danshensu (46 mg/kg) or ursolic acid (80 mg/kg) prior to the oral administration of rosuvastatin (100 mg/kg) increased the systemic exposure of rosuvastatin more than twofold. The plasma clearance of rosuvastatin was reduced to more than 57% in the presence of danshensu or ursolic acid. Rosuvastatin is minimally metabolized in the CYP2C9 isoenzyme pathway and to an even lesser extent in the CYP2C19 isoenzyme pathway. Rosuvastatin is a substrate of drug transporters such as human OATP1B1, OATP 1B3, OATP 1A2, BCRP and NTCP. Therefore, the present results suggested that the potential drug interaction between danshensu or ursolic acid and rosuvastatin may be mediated by one or more transporters (OATP1B1, OATP 1B3, OATP 1A2, BCRP and NTCP) and/or CYPs.
authors: Department of Pharmacy, The First Affiliated Hospital of Nanchang University, Nanchang, People's Republic of China.
authors: Jin-Hua
authors: JH
authors: Wen
authors: Yu-Qing
authors: YQ
authors: Xiong
mesh_terms: D000818:Animals; D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D005464:Fluorobenzenes / Q000493:pharmacokinetics*; D041743:Herb-Drug Interactions; D007773:Lactates / Q000494:pharmacology*; D027381:Liver-Specific Organic Anion Transporter 1 / Q000502:physiology; D008297:Male; D011743:Pyrimidines / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides / Q000493:pharmacokinetics*; D014315:Triterpenes / Q000494:pharmacology*; D000097245:Ursolic Acid
chemical_list: D004365:Drugs, Chinese Herbal; D005464:Fluorobenzenes; D007773:Lactates; D027381:Liver-Specific Organic Anion Transporter 1; D011743:Pyrimidines; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides; D014315:Triterpenes; D000097245:Ursolic Acid; C035055:3,4-dihydroxyphenyllactic acid