Antiplatelet and antithrombotic activities of purpurogallin in vitro and in vivo
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Enzymatic oxidation of pyrogallol was efficiently transformed toan oxidative product, purpurogallin (PPG). Here, the anticoagulantactivities of PPG were examined by monitoring activatedpartial thromboplastin time (aPTT), prothrombin time (PT), andthe activities of thrombin and activated factor X (FXa). And, theeffects of PPG on expression of plasminogen activator inhibitortype 1 (PAI-1) and tissue-type plasminogen activator (t-PA) wereevaluated in tumor necrosis factor (TNF)-α activated humanumbilical vein endothelial cells (HUVECs). Treatment with PPGresulted in prolonged aPTT and PT and inhibition of theactivities of thrombin and FXa, as well as inhibited productionof thrombin and FXa in HUVECs. In addition, PPG inhibitedthrombin-catalyzed fibrin polymerization and platelet aggregation. PPG also elicited anticoagulant effects in mice. Inaddition, treatment with PPG resulted in significant reduction ofthe PAI-1 to t-PA ratio. Collectively, PPG possesses antithromboticactivities and offers a basis for development of a novel anticoagulant.
Abstract
Enzymatic oxidation of pyrogallol was efficiently transformed toan oxidative product, purpurogallin (PPG). Here, the anticoagulantactivities of PPG were examined by monitoring activatedpartial thromboplastin time (aPTT), prothrombin time (PT), andthe activities of thrombin and activated factor X (FXa). And, theeffects of PPG on expression of plasminogen activator inhibitortype 1 (PAI-1) and tissue-type plasminogen activator (t-PA) wereevaluated in tumor necrosis factor (TNF)-α activated humanumbilical vein endothelial cells (HUVECs). Treatment with PPGresulted in prolonged aPTT and PT and inhibition of theactivities of thrombin and FXa, as well as inhibited productionof thrombin and FXa in HUVECs. In addition, PPG inhibitedthrombin-catalyzed fibrin polymerization and platelet aggregation. PPG also elicited anticoagulant effects in mice. Inaddition, treatment with PPG resulted in significant reduction ofthe PAI-1 to t-PA ratio. Collectively, PPG possesses antithromboticactivities and offers a basis for development of a novel anticoagulant.
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