Anti-Thrombotic Activity of 3-Deoxysappanchalcone via Inhibiting Platelet Aggregation and Thrombin (FIIa)/Activated Factor X (FXa) Activity
Naturally occurring plant-based compounds are increasingly being explored for their therapeutic potential in treating a wide range of conditions, particularly those related to vascular health. The compound 3-deoxysappanchalcone (3-DSC), derived from <i>Caesalpinia sappan</i> L., has been proven to exhibit anti-inflammatory, anti-influenza, and anti-allergic properties, though its role in thrombosis and haemostasis remains unexplored. This study aimed to evaluate the anti-thrombotic potential of 3-DSC in both in vitro and in vivo models. The anticoagulant activities of 3-DSC were assessed using activated partial thromboplastin time (aPTT), prothrombin time (PT), and thrombin (FIIa) and activated factor X (FXa) activity assays, as well as fibrin polymerization and platelet aggregation tests. Its effects on plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) expression were evaluated in TNF-α-stimulated human umbilical vein endothelial cells (HUVECs). The results demonstrated that 3-DSC extended aPTT and PT, suppressed thrombin and FXa activities, reduced their production in HUVECs, inhibited thrombin-induced fibrin polymerization and platelet aggregation, and exerted anticoagulant effects in mice. Furthermore, 3-DSC significantly decreased the PAI-1 to t-PA ratio. These findings suggest that 3-DSC possesses potent anti-thrombotic properties by modulating coagulation pathways and fibrinolysis. Its therapeutic potential warrants further investigation for the development of novel anticoagulant agents.
Authors
- Gye Won Han (ORCID: https://orcid.org/0000-0003-4107-835X)
- Jong‐Sup Bae (ORCID: https://orcid.org/0000-0002-5756-9367)
- Jinhee Lee (ORCID: https://orcid.org/0000-0001-7172-0409)
Institutions
- Kyungpook National University (KR)
Publication Details
- Journal
- Molecules
- Published
- 2025-06-13
- DOI
- https://doi.org/10.3390/molecules30122580
- Citations
- 3
- Primary Topic
- Biological Stains and Phytochemicals
- Type
- article
- Field-Weighted Citation Impact
- 4.18
Funders
- National Research Foundation
- National Research Foundation of Korea
- Ministry of Science and ICT, South Korea