Antithrombotic and antiplatelet activities of vicenin-2

Cyclopia subternata is a medicinal plant commonly used in traditional medicine to relieve pain in physiological processes. However, there are limited modern data on its pharmacological effects and active components relating to its traditional use. Here, the anticoagulant and antiplatelet activities of vicenin-2 (VCN), an active compound in C. subternata, were determined. The anticoagulant activities were investigated by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of thrombin and activated factor X (FXa). The effects of VCN on the expression of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were evaluated in tumor necrosis factor (TNF)-α-activated human umbilical vein endothelial cells (HUVECs). Treatment with VCN resulted in prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, as well as inhibited production of thrombin and FXa in HUVECs. In addition, VCN inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. VCN also elicited anticoagulant effects in mice. In addition, treatment with VCN resulted in significant reduction of the PAI-1 to t-PA ratio. Collectively, VCN possesses antithrombotic activities and offers a basis for development of a novel anticoagulant.