title: 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (THSG) attenuates human platelet aggregation, secretion and spreading in vitro.
abstract: BACKGROUND
  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.
  
  
  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.
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Ke
authors: K
authors: Xiang
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Gang
authors: G
authors: Liu
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Ya-Jun
authors: YJ
authors: Zhou
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Hong-Zhen
authors: HZ
authors: Hao
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Zhao
authors: Z
authors: Yin
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Ao-Di
authors: AD
authors: He
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Xing-Wen
authors: XW
authors: Da
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Ji-Zhou
authors: JZ
authors: Xiang
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China.
authors: Jia-Ling
authors: JL
authors: Wang
authors: Department of Pharmacology, Tongji Medical College of Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan 430030, China; The Key Laboratory for Drug Target Researches and Pharmacodynamic Evaluation of Hubei Province, Wuhan 430030, China. Electronic address: zyming@hust.edu.cn.
authors: Zhang-Yin
authors: ZY
authors: Ming
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism; D001792:Blood Platelets / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D005340:Fibrinogen / Q000378:metabolism; D005960:Glucosides / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D019007:P-Selectin / Q000378:metabolism; D010973:Platelet Adhesiveness / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D010979:Platelet Function Tests; D028502:Polygonum / Q000737:chemistry; D013267:Stilbenes / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D005960:Glucosides; D019007:P-Selectin; D010975:Platelet Aggregation Inhibitors; D013267:Stilbenes; C093026:2,3,5,4'-tetrahydroxystilbene 2-O-glucopyranoside; D000255:Adenosine Triphosphate; D005340:Fibrinogen
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