[The action of benzydamine on phospholipase activation].
The effects of the antiinflammatory drug benzydamine (Tantum) on phospholipase activities were determined in vitro, employing various enzyme preparations (rat liver plasma membranes, endoplasmic reticulum, lysosomes; human seminal plasma) and stereospecifically radiolabeled phosphatidylethanolamines as substrates. Fatty acid release from the sn-2 position was inhibited at drug concentrations above 10(-5) mol/l. Concerning the mode of inhibition, a mixed type was found for the soluble phospholipase A2. Impaired fatty acid release from the sn-2 position might contribute to the mechanism of antiinflammatory action of benzydamine by rendering less free precursor acid available for the synthesis of eicosanoids. Fatty acid release from the sn-1 position was inhibited at benzydamine concentrations from 10(-6)-10(-2) mol/l only in lysosomes, whereas in plasma membranes and endoplasmic reticulum it was stimulated, maximally (at 10(-3) mol/l) about 25% and 50%, respectively.
D000818:Animals; D001591:Benzydamine / Q000494:pharmacology*; D004721:Endoplasmic Reticulum / Q000201:enzymology; D004789:Enzyme Activation / Q000187:drug effects; D066298:In Vitro Techniques; D008099:Liver / Q000201:enzymology; D008247:Lysosomes / Q000201:enzymology; D008297:Male; D010740:Phospholipases / Q000378:metabolism*; D010741:Phospholipases A / Q000037:antagonists & inhibitors / Q000378:metabolism*; D054467:Phospholipases A2; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D013094:Spermatozoa / Q000201:enzymology
D011720:Pyrazoles; D001591:Benzydamine; D010740:Phospholipases; D010741:Phospholipases A; D054467:Phospholipases A2
Wirkung von Benzydamin auf Phospholipase-Aktivitäten.