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Effects of the Anti-inflammatory Serine Esterase Inhibitor, FOY, on Phospholipase A2 (EC 3.1.1.4) Activity in Rabbit Polymorphonuclear Leukocytes

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Specialty Pharmacology
Date 1983 Oct 1
PMID 6417683
Citations 2
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Abstract

Phospholipase A2 activity of polymorphonuclear leukocytes (PMNLs) towards radioactively labelled phosphatidylethanolamine is inhibited by FOY (ethyl 4-(6-guanidinohexanoyloxy)-benzoate methanesulfonate) in concentrations above 10(-4)M. The inhibition is noncompetitive with respect to the substrate employed and depends on the pH. Impairment of PMNL phospholipase A2 activity could play a role in the anti-inflammatory effect of FOY: the release of fatty acids from membrane phospholipids is reduced and consequently also the biosynthesis of bioactive oxygenated arachidonate metabolites, among them inflammatory mediators.

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