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齐墩果酸通过抑制组织因子表达发挥抗凝活性。

Anticoagulant activities of oleanolic acid via inhibition of tissue factor expressions.

机构信息

College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Korea.

出版信息

BMB Rep. 2012 Jul;45(7):390-5. doi: 10.5483/bmbrep.2012.45.7.065.

Abstract

Oleanolic acid (OA), a triterpenoid known for its anti-inflammatory and anti-cancer properties, is commonly present in several medicinal plants but its anticoagulant activities have not been studied. Here, the anticoagulant properties of OA were determined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), fibrin polymerization as well as cell-based thrombin and activated factor X (FXa) generation activities. Data showed OA prolonged aPTT and PT significantly and inhibited thrombin catalyzed fibrin polymerization. In addition, OA inhibited the activities of thrombin and FXa and inhibited the generation of thrombin or FXa in human endothelial cells. OA also inhibited TNF-α-induced tissue factor expression on human endothelial cells. In accordance with these anticoagulant activities, OA showed an anticoagulant effect in vivo. These results indicate that OA possesses antithrombotic activities and suggest that daily consumption of a herb containing OA may be preventing thrombosis in pathological states.

摘要

齐墩果酸(OA)是一种具有抗炎和抗癌特性的三萜类化合物,存在于几种药用植物中,但它的抗凝活性尚未得到研究。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)、纤维蛋白聚合以及基于细胞的凝血酶和活化因子 X(FXa)生成活性来确定 OA 的抗凝特性。数据显示,OA 显著延长 aPTT 和 PT,并抑制凝血酶催化的纤维蛋白聚合。此外,OA 抑制凝血酶和 FXa 的活性,并抑制人内皮细胞中凝血酶或 FXa 的生成。OA 还抑制 TNF-α诱导的人内皮细胞组织因子表达。根据这些抗凝活性,OA 在体内表现出抗凝作用。这些结果表明 OA 具有抗血栓形成活性,并提示日常食用含有 OA 的草药可能有助于预防病理状态下的血栓形成。

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