2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (THSG) attenuates human platelet aggregation, secretion and spreading in vitro

Thromb Res. 2014 Feb;133(2):211-7. doi: 10.1016/j.thromres.2013.11.006. Epub 2013 Nov 15.

Abstract

Introduction: 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside(THSG) is a water-soluble component of the rhizome extract from the traditional Chinese herb Polygonum multiflorum. Recent studies have demonstrated that THSG has potent anti-oxidative and anti-inflammatory effects. In this study, we investigated the anti-platelet aggregation, secretion and spreading of THSG with different methods. The purpose was to explore the anti-platelet effect of THSG and the underlying mechanism.

Materials and methods: We investigated the anti-platelet activity of THSG on platelet aggregation induced by collagen (2 μg/mL), thrombin(0.04U/mL), U46619 (3 μM) and ADP (2 μM). ATP secretion induced by collagen (2 μg/mL) was also investigated. P-selectin expression and PAC-1 binding were measured by flow cytometry. In addition, human platelet spreading on immobilized fibrinogen and immunoblotting were also tested.

Results: THSG dose-dependently inhibited platelet aggregation and ATP secretion induced by collagen. It inhibited platelet P-selectin expression and PAC-1 binding induced by thrombin(0.1U/mL). THSG also inhibited human platelet spreading on immobilized fibrinogen, a process mediated by platelet outside-in signaling. Western blot analysis showed that THSG could inhibit platelet Fc γ RIIa, Akt(Ser473)and GSK3β(Ser9) phosphorylation.

Conclusions: Our study indicates that THSG has potent anti-platelet activity to collagen induced aggregation. THSG is likely to exert protective effects in platelet-associated thromboembolic disorders by modulating human platelet.

Keywords: 2,3,5,4’-tetrahydroxystilbene-2-O-β-D glucoside; 9,11-Dideoxy-9a,11a-methanoepoxy prostaglandin F2a; ADP; ATP; Aggregation; EDTA; Fc γ RIIa; Granule release; MAPK; PGE1; PPP; PRP; Platelet; Prostaglandin E1; THSG; TxA2; U46619; adenosine diphosphate; adenosine triphosphate; ethyle nediaminetetraacetic acid; mitogen, activated protein kinase; platelet poor plasma; platelet rich plasma; thromboxaneA2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Blood Platelets / cytology
  • Blood Platelets / drug effects*
  • Blood Platelets / metabolism
  • Fibrinogen / metabolism
  • Glucosides / isolation & purification
  • Glucosides / pharmacology*
  • Humans
  • P-Selectin / metabolism
  • Platelet Adhesiveness / drug effects
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / isolation & purification
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Function Tests
  • Polygonum / chemistry
  • Stilbenes / isolation & purification
  • Stilbenes / pharmacology*

Substances

  • Glucosides
  • P-Selectin
  • Platelet Aggregation Inhibitors
  • Stilbenes
  • 2,3,5,4'-tetrahydroxystilbene 2-O-glucopyranoside
  • Adenosine Triphosphate
  • Fibrinogen