EFFECT OF ANTIRHEUMATIC DRUGS ON NEUTRAL PROTEASE FROM HUMAN LEUKOCYTE GRANULES

  • 1 January 1976
    • journal article
    • research article
    • Vol. 35  (9-10) , 337-346
Abstract
The inhibitory effect of 38 antirheumatic and other agents on purified neutral protease from human polymorphonuclear leukocytes was studied by determining the decrease in enzyme activity on Z-Ala-NPH [N-tert-butyloxycarbonyl-alanine p-nitrophenyl ester] as substrate. Analgesics, salicylates, cytostatic agents and steroids, as well as D-penicillamine, colchicine, allopurinol, chlorzoxazone and chlorpromazine, either had no effect on neutral protease or inhibited it only to a very small extent. Typical antirheumatic agents like Au and pyrazolone derivatives suppressed the activity of the enzyme at a concentration of 10-5 M. The 2 sulfonated polysaccharides Arteparon and pentosan polysulfate (SP 54) were the most potent inhibitors of neutral protease (inhibition down to 10-8 M). Increasing concentrations of various inorganic salts gradually suppressed the effect of some otherwise effective drugs on neutral protease. The drugs were completely ineffective at a salt concentration of 0.5 M. At physiological concentrations, however, this effect was insignificant. Inhibition of neutral protease may be one way in which some antirheumatic drugs exert a therapeutic effect in rheumatic diseases.

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