Scoparone demonstrates in vitro antiplatelet properties by inhibiting collagen-induced platelet aggregation, granule secretion, and TXA2 production via suppression of PI3K/Akt and MAPK phosphorylation.
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Substances regulating platelet activation warrant investigation; Level 5 evidence leaves open clinical translation for thrombosis prevention.
When blood vessels are damaged, a fast hemostatic response should occur to minimize blood loss and maintain normal circulation.Platelet activation and aggregation are essential in this process.However, excessive platelet aggregation or abnormal platelet aggregation may be the cause of cardiovascular diseases such as thrombosis, stroke, and atherosclerosis.Therefore, finding a substance capable of regulating platelet activation and suppressing agglutination reaction is important for the prevention and treatment of cardiovascular diseases.6,7-Dimethoxy-2Hchromen-2-one (Scoparone), found primarily in the roots of Artemisia or Scopolia plants, has been reported to have a pharmacological effect on immunosuppression and vasodilation, but studies of platelet aggregation and its mechanisms are still insufficient.This study confirmed the effect of scoparone on collagen-induced human platelet aggregation, TXA 2 production, and major regulation of intracellular granule secretion (ATP and serotonin release).In addition, the effect of scoparone on the phosphorylation of the phosphoproteins PI3K/Akt and mitogenactivated protein kinases (MAPK) involved in signal transduction in platelet aggregation was studied.As a result, scoparone significantly inhibited the phosphorylation of PI3K/Akt and MAPK, which significantly inhibited platelet aggregation through TXA 2 production and intracellular granule secretion (ATP and serotonin release).Therefore, we suggest that scoparone is an antiplatelet substance that regulates the phosphorylation of phosphoproteins such as PI3K/Akt and MAPK and is of value as a preventive and therapeutic agent for platelet-derived cardiovascular disease.
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Dong‐Ha Lee (2020) studied this question.
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