Differential inhibition of human secretory and cytosolic phospholipase A2.

The roles and relative contributions of secretory and cytosolic phospholipases A2 in physiology and pathology are not precisely known. In a search for differential inhibitors of these enzymes, which could serve as tools to clarify this issue, we evaluated the potencies of reference compounds and three series of new compounds, viz. substrate analogues, 1,2-amino alcohols and enolized beta-tricarbonyl derivatives, as inhibitors of secretory phospholipase A2 from human polymorphonuclear leukocytes (sPLA2) and of cytosolic phospholipase A2 from human U937 cells (cPLA2).