2. Academic Validation
  3. Celastrol inhibits platelet function and thrombus formation

Celastrol inhibits platelet function and thrombus formation

  • Biochem Biophys Res Commun. 2023 Dec 10:693:149366. doi: 10.1016/j.bbrc.2023.149366.
Xiaoqian Li 1,  Jie Zhang 1,  Yingying Li 1,  Yue Dai 1,  Hui Zhu 1,  Huimin Jiang 1,  Yiran Han 2,  Xiang Chu 1,  Yueyue Sun 1,  Wen Ju 1,  Zhenyu Li 1,  Lingyu Zeng 1,  Kailin Xu 1,  Jianlin Qiao 3
Affiliations

Affiliations

  • 1 Blood Diseases Institute, Xuzhou Medical University, Xuzhou, China; Department of Hematology, The Affiliated Hospital of Xuzhou Medical University, Xuzhou, China; Key Laboratory of Bone Marrow Stem Cell, Jiangsu Province, Xuzhou, China.
  • 2 The First Clinical School of Medicine, Xuzhou Medical University, Xuzhou, China.
  • 3 Blood Diseases Institute, Xuzhou Medical University, Xuzhou, China; Department of Hematology, The Affiliated Hospital of Xuzhou Medical University, Xuzhou, China; Key Laboratory of Bone Marrow Stem Cell, Jiangsu Province, Xuzhou, China. Electronic address: [email protected].
PMID: 38091842 DOI: 10.1016/j.bbrc.2023.149366
Abstract

Introduction: Celastrol is an active pentacyclic triterpenoid extracted from Tripterygium wilfordii and has anti-inflammatory and anti-tumor properties. Whether Celastrol modulates platelet function remains unknown. Our study investigated its role in platelet function and thrombosis.

Methods: Human platelets were isolated and incubated with Celastrol (0, 1, 3 and 5 μM) at 37 °C for 1 h to measure platelet aggregation, granules release, spreading, thrombin-induced clot retraction and intracellular calcium mobilization. Additionally, Celastrol (2 mg/kg) was intraperitoneally administrated into mice to evaluate hemostasis and thrombosis in vivo.

Results: Celastrol treatment significantly decreased platelet aggregation and secretion of dense or alpha granules induced by collagen-related peptide (CRP) or Thrombin in a dose-dependent manner. Additionally, Celastrol-treated platelets showed a dramatically reduced spreading activity and decreased clot retraction. Moreover, Celastrol administration prolonged tail bleeding time and inhibited formation of arterial/venous thrombosis. Furthermore, Celastrol significantly reduced calcium mobilization.

Conclusion: Celastrol inhibits platelet function and venous/arterial thrombosis, implying that it might be utilized for treating thrombotic diseases.

Keywords

Calcium mobilization; Celastrol; Hemostasis; Platelets; Thrombosis.

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