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Antithrombotic activities of oroxylin A in vitro and in vivo

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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.

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Acknowledgments

This study was supported by the National Research Foundation of Korea (NRF) funded by the Korean government [MEST] (Grant Nos. 2012-0009400) and by the Korean Health Technology R&D Project, Ministry of Health & Welfare, Republic of Korea (Grant No. A111305).

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The authors have no conflict of interest to declare.

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Authors and Affiliations

  1. Department of Anatomy and Histology, College of Oriental Medicine, Daegu Haany University, Gyeongsan, 712-715, Republic of Korea

    Sae-Kwang Ku

  2. Department of Cosmetic Science and Technology, Seowon University, Cheongju, 361-742, Republic of Korea

    In-Chul Lee

  3. College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, Kyungpook National University, 80 Daehak-ro, Buk-gu, Taegu, 702-701, Republic of Korea

    Jong-Sup Bae

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  1. Sae-Kwang Ku
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  2. In-Chul Lee
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Correspondence to Jong-Sup Bae.

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Ku, SK., Lee, IC. & Bae, JS. Antithrombotic activities of oroxylin A in vitro and in vivo. Arch. Pharm. Res. 37, 679–686 (2014). https://doi.org/10.1007/s12272-013-0233-0

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  • DOI: https://doi.org/10.1007/s12272-013-0233-0

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