Anti-inflammatory and platelet anti-aggregant activity of phospholipase-A2 inhibitors

Abstract

Mepacrine, papaverine, p‐bromophenacyl bromide and 2,3‐dibromo(4′‐cyclohexyl‐3′‐chloro)‐phenyl‐4‐oxo‐butyric acid (CB 874) inhibit the hydrolysis of phospholipids induced by thrombin in dog platelets. They also exhibit anti‐inflammatory and anti‐aggregant properties. These biological activities may be explained by a direct or indirect inhibitory action on phospholipase A₂. Phospholipase A₂ inhibitors may block not only the release of arachidonic acid and its subsequent conversion into prostaglandins but also the formation of lysophospholipids involved in inflammation and/or platelet aggregation.