title: Antithrombotic activities of oroxylin A in vitro and in vivo.
abstract: Here, the anticoagulant activities of oroxylin A (OroA), a major component of Scutellaria baicalensis Georgi, were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of cell-based thrombin and activated factor X (FXa). Furthermore, the effects of OroA on the expressions of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were tested in tumor necrosis factor (TNF)-α activated human umbilical vein endothelial cells (HUVECs). Treatment with OroA resulted in prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and OroA inhibited production of thrombin and FXa in HUVECs. And OroA inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. In accordance with these anticoagulant activities, OroA elicited anticoagulant effects in mouse. In addition, treatment of OroA resulted in the inhibition of TNF-α-induced production of PAI-1, and treatment with OroA resulted in the significant reduction of the PAI-1 to t-PA ratio. Collectively, OroA possess antithrombotic activities and offer bases for development of a novel anticoagulant.
authors: Department of Anatomy and Histology, College of Oriental Medicine, Daegu Haany University, Gyeongsan, 712-715, Republic of Korea.
authors: Sae-Kwang
authors: SK
authors: Ku
authors: In-Chul
authors: IC
authors: Lee
authors: Jong-Sup
authors: JS
authors: Bae
mesh_terms: D000328:Adult; D000818:Animals; D000925:Anticoagulants / Q000494:pharmacology*; D000991:Antithrombins / Q000494:pharmacology*; D001760:Bleeding Time; D001777:Blood Coagulation / Q000187:drug effects*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D065427:Factor Xa Inhibitors / Q000494:pharmacology*; D005260:Female; D005337:Fibrin / Q000378:metabolism; D005419:Flavonoids / Q000494:pharmacology*; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D008297:Male; D008813:Mice, Inbred ICR; D010314:Partial Thromboplastin Time; D008517:Phytotherapy; D010946:Plants, Medicinal; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011517:Prothrombin Time; D031364:Scutellaria baicalensis; D010959:Tissue Plasminogen Activator / Q000378:metabolism; D055815:Young Adult
chemical_list: D000925:Anticoagulants; D000991:Antithrombins; D065427:Factor Xa Inhibitors; D005419:Flavonoids; D017395:Plasminogen Activator Inhibitor 1; D010975:Platelet Aggregation Inhibitors; C051321:SERPINE1 protein, human; C080669:5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one; D005337:Fibrin; D010959:Tissue Plasminogen Activator