Pharmacological influence on polymorphonuclear granulocytes elastase under various test conditions.
The effect of diclofenac-Na, glycosaminoglycanpolysulfate (GAGPS), eglin C and alpha 1-proteinase inhibitor on the activity of elastase from polymorphonuclear granulocytes (PMN-elastase) was tested under various conditions. The synthetic substrate methoxysuccinyl-1-ala-1-pro-1-val-p-nitroaniline was used to measure the activity of the enzyme. The inhibition or activation of PMN-elastase by the test substances was dependent on the type and concentration of buffer, the pH, the presence of a tenside and most notably, the presence of electrolytes. Components of the synovial fluid changed the effects of these electrolytes. Therefore, it is as yet unclear, to what degree the inhibition of PMN-elastase contributes to the therapeutical effects of non-steroidal anti-inflammatory drugs and anti-osteoarthritic drugs.
Steinmeyer
J
J
Institut für Pharmakologie und Toxikologie, Universität Bonn, Fed. Rep. of Germany.
Kalbhen
D A
DA
D004008:Diclofenac / Q000494:pharmacology; D006025:Glycosaminoglycans / Q000494:pharmacology; D006801:Humans; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D009504:Neutrophils / Q000201:enzymology*; D010196:Pancreatic Elastase / Q000378:metabolism*; D011506:Proteins; D015842:Serine Proteinase Inhibitors / Q000494:pharmacology; D015843:Serpins; D000515:alpha 1-Antitrypsin / Q000494:pharmacology
D006025:Glycosaminoglycans; D011506:Proteins; D015842:Serine Proteinase Inhibitors; D015843:Serpins; D000515:alpha 1-Antitrypsin; C028656:eglin proteinase inhibitors; D004008:Diclofenac; C013786:A73025; D010196:Pancreatic Elastase