Ku Sae-Kwang, Lee Wonhwa, Kang Min, Bae Jong-Sup
Department of Anatomy and Histology, College of Korean Medicine, Daegu Haany University, Gyeongsan, 712-715, Republic of Korea.
Arch Pharm Res. 2015 Jun;38(6):1080-9. doi: 10.1007/s12272-014-0501-7. Epub 2014 Oct 18.
Aspalathin (Asp) and nothofagin (Not) are two major active dihydrochalcones found in green rooibos tea (Aspalathus linearis; family, Fabaceae; tribe, Crotalarieae), which have been reported for their anti-oxidant activity. Here, the anticoagulant activities of Asp and Not were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of thrombin (Factor IIa, FIIa) and activated factor X (FXa). And, the effects of Asp and Not 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 Asp and Not 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, Asp and Not inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. Asp and Not also elicited anticoagulant effects in mice. In addition, treatment with Asp and Not resulted in significant reduction of the PAI-1 to t-PA ratio. Collectively, Asp and Not possesses antithrombotic activities and offers a basis for development of a novel anticoagulant.
白杨素（Asp）而非诺托番（Not）是绿路易波士茶（线叶金雀花；豆科；猪屎豆族）中发现的两种主要活性二氢查耳酮，它们已被报道具有抗氧化活性。在此，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（因子IIa，FIIa）和活化因子X（FXa）的活性，检测了Asp和Not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（HUVECs）中评估了Asp和Not对纤溶酶原激活物抑制剂1型（PAI-1）和组织型纤溶酶原激活物（t-PA）表达的影响。用Asp和Not处理导致aPTT和PT延长，凝血酶和FXa的活性受到抑制，以及HUVECs中凝血酶和FXa的产生受到抑制。此外，Asp和Not抑制凝血酶催化的纤维蛋白聚合和血小板聚集。Asp和Not在小鼠中也引发了抗凝作用。此外，用Asp和Not处理导致PAI-1与t-PA的比率显著降低。总体而言，Asp和Not具有抗血栓形成活性，并为开发新型抗凝剂提供了依据。
