Antiinflammatory effects of genipin, an active principle of gardenia

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 homogen...

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Bibliographic Details
Published in:European journal of pharmacology 2004-07, Vol.495 (2), p.201-208
Main Authors: Koo, Hye-Jin, Song, Yun Seon, Kim, Hee-Jeong, Lee, Yong-Ha, Hong, Sung-Min, Kim, Su-Jung, Kim, Byung-Chul, Jin, Changbae, Lim, Chang-Jin, Park, Eun-Hee
Format: Article
Language:English
Subjects:
Angiogenesis
Angiogenesis Inhibitors - pharmacology
Animals
Anti-Inflammatory Agents - pharmacology
Antiinflammatory
Antioxidants - pharmacology
Biological and medical sciences
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
Genipin
Immunoblotting
Inducible nitric oxide synthase
Interferon-gamma - pharmacology
Iridoid Glycosides
Iridoids
Lipid peroxidation
Lipid Peroxidation - drug effects
Lipopolysaccharides - pharmacology
Macrophages - cytology
Macrophages - drug effects
Macrophages - metabolism
Male
Medical sciences
Mice
Mice, Inbred ICR
Nitric Oxide - metabolism
Nitric Oxide Synthase - biosynthesis
Nitric Oxide Synthase Type II
NO (Nitric oxide)
Pharmacology. Drug treatments
Pyrans - pharmacology
Rats
Rats, Sprague-Dawley
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Summary: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 μM) inhibited NO production and iNOS expression upon stimulation by lipopolysaccharide/interferon-γ (IFN-γ) in RAW 264.7, a murine macrophage cell line. Genipin markedly blocked lipopolysaccharide-evoked degradation of inhibitor-κB-β (IκB-β), indicating that it exhibits inhibitory effect on NO production through the inhibition of nuclear factor-κB (NF-κB) 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.
ISSN:0014-2999
1879-0712
DOI:10.1016/j.ejphar.2004.05.031