Anticoagulant and antiprotease activities of a heparinoid sulfated glucoside-bearing polymer

J Biomater Sci Polym Ed. 1998;9(9):973-84. doi: 10.1163/156856298x00280.

Abstract

We studied anticoagulant and antiprotease activities of the poly(glucosyloxyethyl methacrylate) sulfate [poly(GEMA)-sulfate] in plasma and purified enzyme systems in order to evaluate the anticoagulant behavior of a heparin-like sulfated glucoside-bearing polymer. As a result, we found that poly(GEMA)-sulfate can inhibit some coagulation proteases, although its antiprotease behavior differed from those of heparin and dextran sulfate. Poly(GEMA)-sulfate could not enhance antithrombin activity; therefore, we did not observe any significant inhibition of Factor Xa via antithrombin. However, we found that poly(GEMA)-sulfate was able to inhibit thrombin through the activation of heparin cofactor II. In addition, poly(GEMA)-sulfate was able to inhibit Tenase. In our previous research. we found that the anticoagulant activity of poly(GEMA)-sulfate is due primarily to the formation of an insoluble complex with fibrinogen. This paper showed that the antiprotease activities of poly(GEMA)-sulfate contribute to some extent to its anticoagulant activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticoagulants / chemistry
  • Anticoagulants / pharmacology*
  • Antithrombin III / chemistry
  • Antithrombin III / pharmacology
  • Blood Coagulation / drug effects*
  • Blood Coagulation / physiology
  • Dextrans / chemistry
  • Dextrans / pharmacology
  • Dipeptides / chemistry
  • Factor Xa / chemistry
  • Factor Xa / pharmacology
  • Glucosides / chemistry
  • Glucosides / pharmacology*
  • Heparin / chemistry
  • Heparin / pharmacology
  • Heparin Cofactor II / chemistry
  • Heparin Cofactor II / pharmacology
  • Heparinoids / chemistry
  • Heparinoids / pharmacology*
  • Humans
  • Oligopeptides / chemistry
  • Partial Thromboplastin Time
  • Polymethacrylic Acids / chemistry
  • Polymethacrylic Acids / pharmacology*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology*
  • Serine Proteinase Inhibitors / chemistry
  • Serine Proteinase Inhibitors / pharmacology
  • Spectrophotometry

Substances

  • Anticoagulants
  • Dextrans
  • Dipeptides
  • Glucosides
  • Heparinoids
  • Oligopeptides
  • Polymethacrylic Acids
  • Protease Inhibitors
  • Serine Proteinase Inhibitors
  • poly(glucosyloxyethyl methacrylate) sulfate
  • benzoyl-Ile-Glu-Gly-Arg-p-nitroanilide
  • S 2238
  • Heparin Cofactor II
  • Antithrombin III
  • Heparin
  • Factor Xa