JJK694, a Synthesized Obovatol Derivative, Inhibits Platelet Activation by Suppressing Cyclooxygenase and Lipoxygenase Activities

DOI Web Site Web Site PubMed 参考文献72件
  • YU Ji-Yeon
    Laboratory for Chemical Genomics, Korea Research Institute of Chemical Technology Laboratory for Chemical Genomics, Korea Research Institute of Chemical Technology
  • LEE Jung-Jin
    Korean Medicine (KM)-Based Herbal Drug Research Group, Korea Institute of Oriental Medicine Korean Medicine (KM)-Based Herbal Drug Research Group, Korea Institute of Oriental Medicine
  • JUNG Jae-Kyung
    College of Pharmacy, Research Center for Bioresource and Health, Chungbuk National University College of Pharmacy, Research Center for Bioresource and Health, Chungbuk National University
  • MIN Yong-Ki
    Laboratory for Chemical Genomics, Korea Research Institute of Chemical Technology Laboratory for Chemical Genomics, Korea Research Institute of Chemical Technology
  • KIM Tack-Joong
    Division of Biological Science and Technology, College of Science and Technology, Yonsei University Division of Biological Science and Technology, College of Science and Technology, Yonsei University
  • MA Jin Yeul
    Korean Medicine (KM)-Based Herbal Drug Research Group, Korea Institute of Oriental Medicine Korean Medicine (KM)-Based Herbal Drug Research Group, Korea Institute of Oriental Medicine
  • LEE Mi-Yea
    Department of Nursing, Kyungbok University Department of Nursing, Kyungbok University
  • YUN Yeo-Pyo
    College of Pharmacy, Research Center for Bioresource and Health, Chungbuk National University College of Pharmacy, Research Center for Bioresource and Health, Chungbuk National University

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Obovatol has various biological activities, including anti-proliferative, neurotrophic, anti-fibrillogenic, anti-platelet, anti-fungal and anti-inflammatory activities. In this study, we investigated the effects of JJK694, a synthesized obovatol derivative, on rabbit platelet activation and its molecular mechanisms. JJK694 significantly inhibited washed rabbit platelet aggregation and serotonin secretion induced by collagen and arachidonic acid, but had little effect on thrombin- or U46619-induced aggregation. These results suggest that JJK694 selectively inhibits collagen- and arachidonic acid-mediated signaling. JJK694 also showed a concentration-dependent decrease in cytosolic Ca2+ mobilization, but it had no effect on arachidonic acid liberation. On the other hand, it significantly inhibited the formation of arachidonic acid metabolites, including thromboxane A2 (TXA2), prostaglandin D2, and 12-hydroxy-5,8,10,14-eicosatetraenoic acid (12-HETE), by suppression of cyclooxygenase (COX)-1 and lipoxygenase (LOX) activities. These results indicate that JJK694 hasanti-platelet activities through inhibition of arachidonic acid metabolite production by suppression of COX-1 and LOX activities.

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