WA8242A1, A2 and B, novel secretory phospholipase A2 inhibitors produced by Streptomyces violaceusniger. II. Biological properties.
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.
Yoshimura
S
S
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
Otsuka
T
T
Muramatsu
Y
Y
Fujiwara
T
T
Okamoto
M
M
Hashimoto
S
S
Okuhara
M
M
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
D004791:Enzyme Inhibitors; D015074:2-Aminoadipic Acid; D015054:Zymosan; D010741:Phospholipases A; D054467:Phospholipases A2