Suppression of Inflammatory Responses by Surfactin, 11Surfactin was formerly referred to as PI-003. a Selective Inhibitor of Platelet Cytosolic Phospholipase A2

摘要: Surfactin inhibits platelet and spleen cytosolic 100 kDa phospholipase A2 (PLA2). In contrast, this same compound enhances rat group II PLA2 activity by approximately 2-fold slightly increases I from porcine pancreas Naja naja venom in vitro. does not affect a Ca2+ -independent partially purified bovine brain. Thus, selectively the form of PLA2. Based on vitro studies utilizing preincubation surfactin with enzyme, dialysis, increased concentrations substrates, inhibitory effect appears to be due direct interaction enzyme. Linear regression analysis linear portion concentration-response curve reveals an IC50 8.5 microM. To further determine pattern, Dixon plot was constructed show that inhibition is competitive, but uncompetitive, constant Ki = 4.7 microM 50 mM Tris-HCl buffer, pH 8.0, at 37 degrees. blocked non-stimulated calcium ionophore A23187-stimulated release arachidonic acid monkey kidney CV-1 cells, which contain as major activity, shown anionic exchange DEAE-5PW high performance liquid chromatography profile western blotting analysis. ameliorated inflammation induced several chemicals. That is, it exhibited vivo anti-inflammatory tested inflammatory reactions including 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema, carrageenan-induced paw acetic acid-induced writhing. These results demonstrate selective inhibitor for putative agent through produced PLA2, may suppress responses.