Differential induction of the expression of GST subunits by geniposide in rat hepatocytes

Pharmacology. 2004 Jan;70(1):15-22. doi: 10.1159/000074238.

Abstract

Geniposide, an iridoid glycoside isolated from the fruit of Gardenia jasminoides Ellis, has the biological capabilities of detoxication, antioxidation, and anticarcinogenesis. In this study, the mechanism of geniposide affecting the GST (glutathione S-transferase) system was investigated. Primary cultured rat hepatocytes were treated with geniposide and examined for total GST activity and expression of GST subunits. The results showed that the geniposide-induced GST activity was dose and time dependent. Western blotting data demonstrated that geniposide induced increased protein levels of GSTM1 and GSTM2 (approximately 1.7- and 1.8-fold of control, respectively), but did not increase those of GSTA1. The corresponding transcripts levels were confirmed by RT-PCR. Using PD98059, the effect of geniposide was verified to be via the MEK pathway. The results suggest that geniposide possesses a potential for detoxication by inducing GST activity via increasing the transcription of GSTM1 and GSTM2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Drugs, Chinese Herbal
  • Enzyme Induction / drug effects*
  • Enzyme Induction / genetics
  • Flavonoids / pharmacology
  • Fruit
  • Glutathione Transferase / antagonists & inhibitors
  • Glutathione Transferase / biosynthesis*
  • Glutathione Transferase / genetics
  • Glycosides / administration & dosage
  • Glycosides / pharmacokinetics
  • Glycosides / therapeutic use
  • Hepatitis / drug therapy
  • Hepatocytes / drug effects*
  • Hepatocytes / enzymology*
  • Iridoids / administration & dosage
  • Iridoids / pharmacokinetics*
  • Iridoids / therapeutic use*
  • Isoenzymes / biosynthesis
  • Male
  • Plant Extracts
  • Pyrans
  • RNA, Messenger / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Rubiaceae
  • Time Factors

Substances

  • Drugs, Chinese Herbal
  • Flavonoids
  • Glycosides
  • Iridoids
  • Isoenzymes
  • Plant Extracts
  • Pyrans
  • RNA, Messenger
  • geniposide
  • Glutathione Transferase
  • glutathione S-transferase M1
  • glutathione S-transferase Mu 2
  • 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one