title: WA8242A1, A2 and B, novel secretory phospholipase A2 inhibitors produced by Streptomyces violaceusniger. II. Biological properties.
abstract: WA8242A1, A2 and B, novel inhibitors of secretory phospholipase A2 (PLA2), were obtained from Streptomyces violaceusniger No. 8242. WA8242B inhibited secretory group I and II PLA2s in a dose-dependent manner. The mode of inhibition of group II PLA2 by WA8242B was in competitive fashion. WA8242B inhibited group II PLA2-induced Prostaglandin I2 (PGI2) production by human umbilical vein endothelial cells. Furthermore, WA8242B was effective in mouse zymosan writhing model.
authors.affiliation: Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Yoshimura
authors.forename: T
authors.initials: T
authors.lastname: Otsuka
authors.forename: Y
authors.initials: Y
authors.lastname: Muramatsu
authors.forename: T
authors.initials: T
authors.lastname: Fujiwara
authors.forename: M
authors.initials: M
authors.lastname: Okamoto
authors.forename: S
authors.initials: S
authors.lastname: Hashimoto
authors.forename: M
authors.initials: M
authors.lastname: Okuhara
mesh_terms: D015074:2-Aminoadipic Acid / Q000737:chemistry / Q000302:isolation & purification; D000818:Animals; D004730:Endothelium, Vascular / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D054467:Phospholipases A2; D013302:Streptomyces / Q000737:chemistry*; D014471:Umbilical Veins / Q000187:drug effects; D015054:Zymosan / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D015074:2-Aminoadipic Acid; D015054:Zymosan; D010741:Phospholipases A; D054467:Phospholipases A2