Han Gyuri, Lee Jinhee, Bae Jong-Sup
Research Institute of Pharmaceutical Sciences, CMRI, College of Pharmacy, Kyungpook National University, Daegu 41566, Republic of Korea.
Molecules. 2025 Jun 13;30(12):2580. doi: 10.3390/molecules30122580.
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 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.
天然存在的植物性化合物因其在治疗多种疾病,尤其是与血管健康相关疾病方面的治疗潜力而受到越来越多的探索。从[植物名称]中提取的化合物3-脱氧萨潘查尔酮(3-DSC)已被证明具有抗炎、抗流感和抗过敏特性,但其在血栓形成和止血中的作用仍未得到探索。本研究旨在评估3-DSC在体外和体内模型中的抗血栓形成潜力。使用活化部分凝血活酶时间(aPTT)、凝血酶原时间(PT)、凝血酶(FIIa)和活化因子X(FXa)活性测定,以及纤维蛋白聚合和血小板聚集试验来评估3-DSC的抗凝活性。在肿瘤坏死因子-α刺激的人脐静脉内皮细胞(HUVECs)中评估其对纤溶酶原激活物抑制剂1型(PAI-1)和组织型纤溶酶原激活物(t-PA)表达的影响。结果表明,3-DSC延长了aPTT和PT,抑制了凝血酶和FXa活性,减少了它们在HUVECs中的产生,抑制了凝血酶诱导的纤维蛋白聚合和血小板聚集,并在小鼠中发挥了抗凝作用。此外,3-DSC显著降低了PAI-1与t-PA的比值。这些发现表明,3-DSC通过调节凝血途径和纤维蛋白溶解具有强大的抗血栓形成特性。其治疗潜力值得进一步研究以开发新型抗凝剂。