Metabolism and pharmacokinetics of genipin and geniposide in rats.
Geniposide, an iridoid glucoside, is a major constituent in the fruits of Gardenia jasminoides (Gardenia fruits), a popular Chinese herb. Genipin, the aglycone of geniposide, is used to prepare blue colorants in food industry and also a crosslinking reagent for biological tissue fixation. In this study, we investigated the metabolism and pharmacokinetics of genipin and geniposide in rats. Blood samples were withdrawn via cardiopuncture and the plasma samples were assayed by HPLC method before and after hydrolysis with sulfatase and beta-glucuronidase. The results indicated that after oral administration of genipin or Gardenia fruit decoction, genipin sulfate was a major metabolite in the bloodstream, whereas the parent forms of genipin and geniposide were not detected. Importantly, oral administration of 200mg/kg of genipin resulted in a mortality of 78% (7/9) in rats.
Hou
Y C
YC
School of Pharmacy, College of Pharmacy, China Medical University, 91 Hsueh Shih Road, Taichung 40421, Taiwan, ROC.
Tsai
S Y
SY
Lai
P Y
PY
Chen
Y S
YS
Chao
P D L
PD
D000818:Animals; D002138:Calibration; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002756:Cholagogues and Choleretics / Q000378:metabolism* / Q000493:pharmacokinetics* / Q000633:toxicity; D002851:Chromatography, High Pressure Liquid; D003627:Data Interpretation, Statistical; D032062:Gardenia / Q000737:chemistry; D006868:Hydrolysis; D007275:Injections, Intravenous; D057889:Iridoid Glycosides; D039823:Iridoids / Q000378:metabolism* / Q000493:pharmacokinetics* / Q000633:toxicity; D008297:Male; D010936:Plant Extracts / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results
D002756:Cholagogues and Choleretics; D057889:Iridoid Glycosides; D039823:Iridoids; D010936:Plant Extracts; C007835:geniposide; C007834:genipin