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

Introduction: 2,3,5,4'-tetrahydroxystilbene-2-O-beta-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 mu g/mL), thrombin(0.04U/mL), U46619 (3 mu M) and ADP (2 mu M). ATP secretion induced by collagen (2 mu g/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 gamma RIIa, Akt(Ser473) and GSK3 beta(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. (C) 2013 Elsevier Ltd. All rights reserved.