Inhibition of mannose receptor-mediated clearance of tissue-type plasminogen activator (t-PA) by dextran: a new explanation for its antithrombotic effect

Thromb Haemost. 1997 Oct;78(4):1249-54.

Abstract

Dextran is used during surgery as a prophylactic agent to prevent deep venous thrombosis. Recently it has been shown that dextran increases t-PA plasma concentrations in patients. As dextran is a potential ligand for the mannose receptor, we studied whether this glucose-polymer would be able to inhibit mannose receptor-mediated clearance of t-PA. In this report we show that dextran 40 and dextran 70 were able to inhibit t-PA binding to the isolated human mannose receptor (IC50 14 and 4 mg/ml, respectively). Both glucose-polymers inhibited mannose receptor-mediated t-PA degradation by human monocyte-derived macrophages in vitro (IC50 7 and 2 mg/ml, respectively). The alpha2-macroglobulin receptor/low density lipoprotein receptor-related protein (LRP)-mediated t-PA degradation by the macrophages was not affected by dextran. During and after a 45 min infusion of dextran 70 (Macrodex) in rats, in plasma endogenous t-PA concentrations increased to 162 +/- 33% and 122 +/- 35% respectively. The plasma clearance of a bolus injection of exogenous t-PA was decreased by 33 +/- 9% in the same rats. We conclude that dextran inhibits mannose receptor-mediated t-PA clearance. The inhibition of t-PA clearance during dextran infusion results in increased endogenous t-PA plasma concentrations. Increased t-PA concentrations present during thrombus formation are known to increase thrombus lysability. Thus the inhibition of t-PA clearance can contribute to the antithrombotic effect of dextran.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylgalactosamine / pharmacology
  • Animals
  • Cells, Cultured
  • Depression, Chemical
  • Dextrans / pharmacology*
  • Fibrinolytic Agents / pharmacology*
  • Glucose / pharmacology
  • Humans
  • Lectins, C-Type*
  • Macrophages / metabolism
  • Male
  • Mannose / pharmacology
  • Mannose Receptor
  • Mannose-Binding Lectins*
  • Metabolic Clearance Rate / drug effects
  • Protein Binding / drug effects
  • Rats
  • Rats, Wistar
  • Receptors, Cell Surface / drug effects*
  • Receptors, Cell Surface / metabolism
  • Receptors, LDL / drug effects
  • Receptors, LDL / metabolism
  • Recombinant Proteins / metabolism
  • Tissue Plasminogen Activator / metabolism*
  • Tissue Plasminogen Activator / pharmacokinetics

Substances

  • Dextrans
  • Fibrinolytic Agents
  • Lectins, C-Type
  • Mannose Receptor
  • Mannose-Binding Lectins
  • Receptors, Cell Surface
  • Receptors, LDL
  • Recombinant Proteins
  • Tissue Plasminogen Activator
  • Glucose
  • Acetylgalactosamine
  • Mannose