Ku Sae-Kwang, Bae Jong-Sup
Department of Anatomy and Histology, College of Korean Medicine, Daegu Haany University, Gyeongsan 712-715, Republic of Korea.
College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 702-701, Republic of Korea.
Fitoterapia. 2014 Oct;98:27-35. doi: 10.1016/j.fitote.2014.07.006. Epub 2014 Jul 11.
Wogonin (WGN), a flavonoid extracted from Scutellaria baicalensis Georgi, has several biological effects including antioxidant, anti-inflammatory, antiviral, neuroprotective, anxiolytic, and anticancer activities, and the flavonoid wogonoside (WGNS) can be derived from S. baicalensis, as it is a metabolite of wogonin. Here, the anticoagulant activities of WGN(S) 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 WGN(S) 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 WGN(S) 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, WGN(S) inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. WGN(S) also elicited anticoagulant effects in mice. In addition, treatment with WGN(S) resulted in significant reduction of the PAI-1 to t-PA ratio. Collectively, WGN(S) possesses antithrombotic activities and offers a basis for development of a novel anticoagulant.
汉黄芩素(WGN)是从黄芩中提取的一种黄酮类化合物,具有多种生物学效应,包括抗氧化、抗炎、抗病毒、神经保护、抗焦虑和抗癌活性,而黄酮类化合物汉黄芩苷(WGNS)可从黄芩中获得,因为它是汉黄芩素的一种代谢产物。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)的活性来检测WGN(S)的抗凝活性,并在肿瘤坏死因子(TNF)-α激活的人脐静脉内皮细胞(HUVECs)中评估WGN(S)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WGN(S)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,WGN(S)抑制凝血酶催化的纤维蛋白聚合和血小板聚集。WGN(S)在小鼠中也引发抗凝作用。此外,用WGN(S)处理导致PAI-1与t-PA的比率显著降低。总的来说,WGN(S)具有抗血栓形成活性,为开发新型抗凝剂提供了依据。