Abstract:
:Heparin is the most widely used anticoagulant drug for prevention and treatment of thrombosis. However, inhibition of blood coagulation might not fully explain the antithrombotic activity of this drug. The present study shows that different heparin preparations (50 nM) completely prevent human platelet aggregation, serotonin release and thromboxane B2 production induced by purified neutrophil-derived cathepsin G (E.C. No. 3.4.21.20). This inhibitory effect was not related to the anticoagulant property of the compounds, since a heparin preparation with an inactivated active for antithrombin III was also effective. Heparins inhibited the protease activity of the enzyme over the same range of concentrations. Since the effect of cathepsin G on platelets requires an intact proteolytic active site, the inhibitory effect of the drugs on cathepsin G-induced platelet activation may be explained by a blockade of protease activity. Heparins were also shown to reduce platelet activation induced by cathepsin G released from activated polymorphonuclear leucocytes in mixed cell suspensions. As polymorphonuclear leucocytes might contribute to both arterial and venous thrombosis through platelet activation induced by the release of cathepsin G, this novel property of heparin could be used to optimize its antithrombotic efficacy.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Evangelista V,Piccardoni P,Maugeri N,De Gaetano G,Cerletti Cdoi
10.1016/0014-2999(92)90437-9keywords:
subject
Has Abstractpub_date
1992-06-17 00:00:00pages
401-5issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(92)90437-9journal_volume
216pub_type
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