Dioscin from smilax china rhizomes inhibits platelet activation and thrombus formation via up-regulating cyclic

Ga Hee Lee1, Jin Pyo Lee1, Na Yoon Heo1

  • 1Department of Biomedical Laboratory Science, Namseoul University, Cheonan, 31020, Republic of Korea.

Scientific Reports
|July 15, 2025
PubMed

Insights

Dioscin, found in Smilax china rhizomes, inhibits platelet activation and thrombus formation by regulating key signaling pathways. This natural compound shows potential as a novel antithrombotic agent for cardiovascular disease prevention.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Cardiovascular Research

Background:

  • Cardiovascular disease is a leading cause of mortality, driven by abnormal platelet aggregation and coagulation.
  • Dioscin, a compound from Smilax china rhizomes, is known for anti-tumor properties, but its antiplatelet mechanism is unconfirmed.
  • Understanding dioscin's role in platelet function is crucial for developing new antithrombotic therapies.

Purpose of the Study:

  • To investigate the antithrombotic effects of dioscin on human platelets.
  • To elucidate the underlying molecular mechanisms by which dioscin inhibits platelet activation.
  • To assess the in vivo efficacy of dioscin in preventing thrombus formation.

Main Methods:

  • Assessed dioscin's impact on cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) levels in platelets.
  • Investigated dioscin's effects on the phosphorylation of inositol 1,4,5-triphosphate receptor (IP3R) and vasodilator-stimulated phosphoprotein (VASP).
  • Analyzed dioscin's regulation of phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt), mitogen-activated protein kinase (MAPK), and cytosolic phospholipase A2 (cPLA2) signaling pathways.
  • Evaluated dioscin's antithrombotic activity in a FeCl3-induced thrombosis model in vivo.

Main Results:

  • Dioscin significantly increased cAMP and cGMP production, leading to IP3R and VASP phosphorylation.
  • Inhibition of Ca2+ mobilization and suppression of integrin αIIbβ3 and fibrinogen binding were observed.
  • Dioscin modulated the phosphorylation of PI3K/Akt, MAPK, and cPLA2, impacting platelet granule release.
  • Administration of S. china rhizomes containing dioscin markedly reduced thrombus formation in vivo.

Conclusions:

  • Dioscin exhibits significant antiplatelet activity by modulating intracellular signaling pathways and protein phosphorylation.
  • The compound effectively inhibits platelet activation and thrombus formation, suggesting its therapeutic potential.
  • Dioscin from S. china rhizomes represents a promising candidate for the development of novel antithrombotic agents.

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