Department of Anatomy and Histology, College of Korean Medicine, Daegu Haany University, Gyeongsan 712-715, Korea.
College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 702-701, Korea.
BMB Rep. 2014 Jul;47(7):376-81. doi: 10.5483/bmbrep.2014.47.7.195.
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)-α 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.
没食子酸的酶促氧化被有效地转化为氧化产物棓酸（PPG）。在这里，通过监测活化部分凝血活酶时间（aPTT）、凝血酶原时间（PT）以及凝血酶和活化因子 X（FXa）的活性来检查 PPG 的抗凝活性。并且，在肿瘤坏死因子（TNF）-α激活的人脐静脉内皮细胞（HUVEC）中评估了 PPG 对纤溶酶原激活物抑制剂 1（PAI-1）和组织型纤溶酶原激活物（t-PA）表达的影响。PPG 的处理导致 aPTT 和 PT 延长，以及凝血酶和 FXa 活性受到抑制，并抑制 HUVEC 中凝血酶和 FXa 的产生。此外，PPG 抑制凝血酶催化的纤维蛋白聚合和血小板聚集。PPG 还在小鼠中表现出抗凝作用。此外，PPG 的处理导致 PAI-1 与 t-PA 的比值显著降低。总之，PPG 具有抗血栓形成活性，为开发新型抗凝剂提供了依据。
