Anticoagulant activities of piperlonguminine in vitro and in vivo

Abstract

Piperlonguminine (PL), an important component of Piperlongum fruits, is known to exhibit anti-hyperlipidemic, antiplateletand anti-melanogenic activities. Here, the anticoagulantactivities of PL were examined by monitoring activatedpartial-thromboplastin-time (aPTT), prothrombin-time (PT), andthe activities of thrombin and activated factor X (FXa). Theeffects of PL on the expressions of plasminogen activatorinhibitor type 1 (PAI-1) and tissue-type plasminogen activator(t-PA) were also tested in tumor necrosis factor-α (TNF-α)activated HUVECs. The results showed that PL prolonged aPTTand PT significantly and inhibited the activities of thrombin andFXa. PL inhibited the generation of thrombin and FXa inHUVECs. In accordance with these anticoagulant activities, PLprolonged in vivo bleeding time and inhibited TNF-α inducedPAI-1 production. Furthermore, PAI-1/t-PA ratio was significantlydecreased by PL. Collectively, our results suggest that PLpossesses antithrombotic activities and that the current studycould provide bases for the development of new anticoagulantagents. [BMB Reports 2013; 46(10): 484-489]

Keywords

• Coagulation cascade
• Endothelium
• Fibrinolysis
• Piperlonguminine