Inhibition of porcine pancreas phospholipase A2 activation by gabexate mesilate

Summary We investigated the effect of gabexate mesilate on the catalytic activity of phospholipase A₂ in homogenized porcine pancreatic tissue. Gabexate mesilate is a potent inhibitor of serine proteases. There is no direct inhibition of phospholipase A₂ catalytic activity in concentrations up to 6 mmol/l. Preincubation of homogenized pancreatic tissue with gabexate mesilate leads to a reduction of phospholipase A₂ activity even in concentrations as low as 6 µmol/l. The activation of purified porcine prophospholipase A₂ added to pancreatic tissue can be completely inhibited. Thus, gabexate mesilate might influence the activation of phospholipase A₂ administered in therapeutic concentrations in inflamed pancreatic tissue.Abbreviations PLA₂ Phospholipase A₂ - ProPLA₂ Prophospholipase A₂