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KMID : 1134820200490010011
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Journal of the Korean Society of Food Science and Nutrition
2020 Volume.49 No. 1 p.11 ~ p.18
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Inhibitory Effects of Scoparone on Thrombus Formation via Regulation of Cyclic Nucleotides in Collagen-Induced Platelets
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Lee Dong-Ha
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Abstract
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Platelet activation is essential for the hemostatic process for vascular damage. Excessive platelet activation, however, can lead to several cardiovascular diseases, including atherosclerosis, thrombosis, and myocardial infarction. Scoparone is found in the roots of the genus Artemisia or Scopolia. The pharmacological properties of this compound, including immunosuppression and vascular relaxation, have been studied, but no antiplatelet effects have been reported. This study examined the activities of scoparone on collagen-induced human platelet activation. Scoparone increased the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in a concentration-dependent manner. In addition, scoparone phosphorylated the inositol 1,4,5-triphosphate receptor (IP3R) and vasodilator-stimulated phosphoprotein (VASP) that act as substrates for cAMP-dependent kinase (PKA) and cGMP-dependent kinase (PKG). The phosphorylation of IP3R by scoparone-inhibited the Ca2+ mobilized from the Ca2+ channel of the dense tubular system. Moreover, the phosphorylation of VASP was involved in the inhibition of fibrinogen binding by inactivating αIIb/β3 in the platelet membrane. Scoparone finally reduced the level of thrombin-induced fibrin clot production and reduced thrombus formation. Therefore, scoparone has strong antiplatelet activity and is a potential prophylactic and therapeutic agent for thrombotic diseases from which platelets are derived.
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KEYWORD
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scoparone, cyclic nucleotide, inositol 1, 4, 5-triphosphate receptor, intracellular Ca2+, vasodilator-stimulated phosphoprotein
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