In vitro and in vivo effects of the anti-inflammatory peptides, antiflammins

Abstract

The anti-inflammatory synthetic polypeptides referred to as antiflammins are thought to be inhibitors of phospholipase A 2 (PLA 2) (EC 3.1.1.4). These peptides are from the sequence of amino acids of greatest similarity between uteroglobin and lipocortin I. The effect of these peptides was studied on PLA 2 activation in rat platelets and on acute inflammatory models after local or parenteral administration of drug. We found that antiflammins decreased collagen-induced platelet activation, but had no effect when arachidonic acid was used as activator. The peptides were able to inhibit acute inflammatory processes induced by carrageenan or phorbol esters when administered locally or parenterally. However, antiflammins had no effect on inflammation induced by exogenous PLA 2 administration. These results indicate that the antiflammins may have a direct inhibitory effect on PLA 2 activation but not on the enzyme or enzyme-substrate interaction.