title: Antiinflammatory effects of genipin, an active principle of gardenia.
abstract: 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.
authors.affiliation: College of Pharmacy, Sookmyung Women's University, Cheongpa-dong, Yongsan, Seoul 140-742, Republic of Korea.
authors.forename: Hye-Jin
authors.initials: HJ
authors.lastname: Koo
authors.forename: Yun Seon
authors.initials: YS
authors.lastname: Song
authors.forename: Hee-Jeong
authors.initials: HJ
authors.lastname: Kim
authors.forename: Yong-Ha
authors.initials: YH
authors.lastname: Lee
authors.forename: Sung-Min
authors.initials: SM
authors.lastname: Hong
authors.forename: Su-Jung
authors.initials: SJ
authors.lastname: Kim
authors.forename: Byung-Chul
authors.initials: BC
authors.lastname: Kim
authors.forename: Changbae
authors.initials: C
authors.lastname: Jin
authors.forename: Chang-Jin
authors.initials: CJ
authors.lastname: Lim
authors.forename: Eun-Hee
authors.initials: EH
authors.lastname: Park
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D000975:Antioxidants / Q000494:pharmacology; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D049033:Chorioallantoic Membrane / Q000098:blood supply / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004423:Ear / Q000473:pathology; D004487:Edema / Q000517:prevention & control; D005260:Female; D032062:Gardenia / Q000737:chemistry*; D015151:Immunoblotting; D007371:Interferon-gamma / Q000494:pharmacology; D057889:Iridoid Glycosides; D039823:Iridoids; D015227:Lipid Peroxidation / Q000187:drug effects; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009569:Nitric Oxide / Q000378:metabolism; D019001:Nitric Oxide Synthase / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II; D011714:Pyrans / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D020533:Angiogenesis Inhibitors; D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D057889:Iridoid Glycosides; D039823:Iridoids; D008070:Lipopolysaccharides; D011714:Pyrans; D009569:Nitric Oxide; D007371:Interferon-gamma; C007834:genipin; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse; C496318:Nos2 protein, rat