title: Antiallergic effect of ardisiaquinone A, a potent 5-lipoxygenase inhibitor.
abstract: The antiallergic effects of ardisiaquinone A, a potent 5-lipoxygenase inhibitor, were examined. Pretreatment with ardisiaquinone A (0.1-10 microM) significantly inhibited compound 48/80-induced production of cysteinyl-leukotrienes (cys-LTs; LTC4, LTD4 and LTE4) in rat peritoneal mast cells, but not histamine release. The IC50 value was 5.56 microM. Pre-administration with ardisiaquinone A (0.1-1 mg/kg, s.c.) dose-dependently inhibited rat homologous passive cutaneous anaphylaxis (PCA) and the maximal inhibitory ratio was 22.3 +/- 3.9% at the dose of 1 mg/kg. Ardisiaquinone A (1-5 mg/kg, s.c.) dose-dependently prevented the allergen-induced increase of tracheal pressure in ovalbumin-sensitized guinea pigs, especially during the late phase. In conclusion, the findings of this study show that 5-lipoxygenase inhibitor ardisiaquinone A partially attenuates the allergen-induced increases of vascular permeability and tracheal pressure via the inhibition of cys-LTs production in mast cells.
authors.affiliation: Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Fukuishi
authors.forename: T
authors.initials: T
authors.lastname: Takada
authors.forename: Y
authors.initials: Y
authors.lastname: Fukuyama
authors.forename: M
authors.initials: M
authors.lastname: Akagi
mesh_terms: D000818:Animals; D018926:Anti-Allergic Agents / Q000494:pharmacology*; D016227:Benzoquinones / Q000737:chemistry / Q000494:pharmacology*; D016084:Bronchoconstriction / Q000187:drug effects; D003545:Cysteine / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D005260:Female; D006168:Guinea Pigs; D006636:Histamine Release / Q000187:drug effects; D017997:Leukotriene C4 / Q000096:biosynthesis; D017998:Leukotriene D4 / Q000096:biosynthesis; D017999:Leukotriene E4 / Q000096:biosynthesis; D015289:Leukotrienes / Q000096:biosynthesis; D016859:Lipoxygenase Inhibitors; D008297:Male; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011914:Rats, Inbred BN; D017208:Rats, Wistar; D003189:p-Methoxy-N-methylphenethylamine / Q000494:pharmacology
chemical_list: D018926:Anti-Allergic Agents; D016227:Benzoquinones; D015289:Leukotrienes; D016859:Lipoxygenase Inhibitors; C112381:cysteinyl-leukotriene; C091304:ardisiaquinone A; D017997:Leukotriene C4; D003189:p-Methoxy-N-methylphenethylamine; D017998:Leukotriene D4; D017999:Leukotriene E4; D003545:Cysteine