Key result
Purpurogallin prolonged aPTT and PT, inhibited thrombin and FXa activities, and reduced the PAI-1 to t-PA ratio in vitro and in vivo, demonstrating antithrombotic properties.
Why the study?
Does purpurogallin exhibit antithrombotic and anticoagulant activities in vitro and in vivo?
Does purpurogallin exhibit antithrombotic and anticoagulant activities in vitro and in vivo?
Purpurogallin demonstrates significant antithrombotic and anticoagulant activities in preclinical models, suggesting potential as a novel anticoagulant.
Should not change clinical practice; leaves open translation of antithrombotic effects from animal models to humans.
Enzymatic oxidation of pyrogallol was efficiently transformed to an oxidative product, purpurogallin (PPG). Here, the anticoagulant activities of PPG were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of thrombin and activated factor X (FXa). And, the effects of PPG on expression of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were evaluated in tumor necrosis factor (TNF)-<TEX>α</TEX> activated human umbilical vein endothelial cells (HUVECs). Treatment with PPG 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, PPG inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. PPG also elicited anticoagulant effects in mice. In addition, treatment with PPG resulted in significant reduction of the PAI-1 to t-PA ratio. Collectively, PPG possesses antithrombotic activities and offers a basis for development of a novel anticoagulant.
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Ku et al. (2014) studied Thrombosis. Purpurogallin (PPG) was evaluated on Anticoagulant activities (aPTT, PT, thrombin and FXa activities). Purpurogallin prolonged aPTT and PT, inhibited thrombin and FXa activities, and reduced the PAI-1 to t-PA ratio in vitro and in vivo, demonstrating antithrombotic properties.
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