The pharmacokinetics of a novel anti-tumor agent, beta-elemene, in Sprague-Dawley rats.
beta-Elemene, a natural sesquiterpene, is a novel anti-tumor agent. The pharmacokinetics of beta-elemene after single i.v. administration have been investigated in male SD rats. beta-Elemene was administered at three doses (50, 75 and 100 mg/kg) and a full pharmacokinetic profile was obtained. beta-Elemene was metabolized extensively and eliminated rapidly. High permeability of beta-elemene through the blood-brain barrier was found following i.v. administration based on the brain/plasma ratio. Following i.v. administration, the drug was eliminated primarily as metabolite and minimally as unchanged drug. Cumulative fecal, biliary and urinary excretion of beta-elemene in rats was 0.61%, 0.06% and 0.003% of the administered dose (75 mg/kg) at 32 h after administration, respectively. These results indicate that biotransformation may be the main elimination passage of beta-elemene. The metabolism of beta-elemene was extensive and the structure of the metabolite (M1) in rat bile was determined by GS/MS and NMR analysis.
Wang
Kun
K
Department of Pharmacology, Dalian Medical University, PR China.
Li
Zi
Z
Chen
Yuren
Y
Su
Chengye
C
D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001646:Bile / Q000378:metabolism; D001711:Biotransformation; D001798:Blood Proteins / Q000378:metabolism; D002849:Chromatography, Gas; D008297:Male; D011485:Protein Binding; D051381:Rats; D017207:Rats, Sprague-Dawley; D012717:Sesquiterpenes / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D001798:Blood Proteins; D012717:Sesquiterpenes; C445979:beta-elemene