Antiinflammatory effects of genipin, an active principle of gardenia

Eur J Pharmacol. 2004 Jul 14;495(2-3):201-8. doi: 10.1016/j.ejphar.2004.05.031.


Genipin, the aglycone of geniposide, is metabolically produced from the geniposide in body tissues. The purpose of this study is to clarify some pharmacological actions of genipin. Genipin showed concentration-dependent inhibition on lipid peroxidation induced by Fe++/ascorbate in rat brain homogenate. Genipin exhibited significant topical antiinflammatory effect shown as an inhibition of croton oil-induced ear edema in mice. Nitric oxide (NO) synthesis by inducible nitric oxide synthase (iNOS) is increased in inflammatory diseases and leads to cellular injury. Genipin concentration-dependently (50-300 microM) inhibited NO production and iNOS expression upon stimulation by lipopolysaccharide/interferon-gamma (IFN-gamma) in RAW 264.7, a murine macrophage cell line. Genipin markedly blocked lipopolysaccharide-evoked degradation of inhibitor-kappaB-beta (IkappaB-beta), indicating that it exhibits inhibitory effect on NO production through the inhibition of nuclear factor-kappaB (NF-kappaB) activation. It was also shown to contain potent antiangiogenic activity in a dose-dependent manner, which was detected by chick embryo chorioallantoic membrane assay. In summary, we demonstrate that genipin possesses antiinflammatory and is a specific hydroxyl radical scavenger. Its antiangiogenic and NO production-inhibitory properties are also presented.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / pharmacology
  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Antioxidants / pharmacology
  • Brain / drug effects
  • Brain / metabolism
  • Cell Line
  • Cell Survival / drug effects
  • Chorioallantoic Membrane / blood supply
  • Chorioallantoic Membrane / drug effects
  • Dose-Response Relationship, Drug
  • Ear / pathology
  • Edema / prevention & control
  • Female
  • Gardenia / chemistry*
  • Immunoblotting
  • Interferon-gamma / pharmacology
  • Iridoid Glycosides
  • Iridoids
  • Lipid Peroxidation / drug effects
  • Lipopolysaccharides / pharmacology
  • Macrophages / cytology
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Male
  • Mice
  • Mice, Inbred ICR
  • Nitric Oxide / metabolism
  • Nitric Oxide Synthase / biosynthesis
  • Nitric Oxide Synthase Type II
  • Pyrans / pharmacology*
  • Rats
  • Rats, Sprague-Dawley


  • Angiogenesis Inhibitors
  • Anti-Inflammatory Agents
  • Antioxidants
  • Iridoid Glycosides
  • Iridoids
  • Lipopolysaccharides
  • Pyrans
  • Nitric Oxide
  • Interferon-gamma
  • genipin
  • Nitric Oxide Synthase
  • Nitric Oxide Synthase Type II
  • Nos2 protein, mouse
  • Nos2 protein, rat