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KMID : 1134820210500121292
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Journal of the Korean Society of Food Science and Nutrition
2021 Volume.50 No. 12 p.1292 ~ p.1298
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Esculetin Can Attenuate Thrombosis through Inhibition of U46619-Induced Platelet Activation
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Park Chang-Eun
Lee Dong-Ha
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Abstract
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Esculetin, a bioactive 6,7-dihydroxy derivative of coumarin, displays pharmacological activity against obesity, diabetes, renal failure, and cardiovascular diseases (CVDs). It has been reported that esculetin inhibits collagen and arachidonic acid-induced platelet aggregation in washed human platelets. However, there are no effects on other agonists such as thrombin and U46619, and its mechanism of action has not been completely elucidated. This study investigated the effects of esculetin on the modulation of platelet function using human platelets induced by the agonist U46619 (9,11-dideoxy 9a,11a-methanoepoxy prostaglandin F2a), which is one of the analogues of thromboxane A2. U46619 activates platelets, and increases intracellular calcium mobilization and fibrinogen binding. However, esculetin upregulated the cyclic nucleotides and downregulated intracellular calcium mobilization, glycoprotein Ⅱb/Ⅲa (αⅡb/β3)-mediated fibrinogen binding, and clot retraction, dose-dependently. In conclusion, esculetin has demonstrated potent antiplatelet and antithrombotic properties, making it a potential therapeutic drug candidate to prevent platelet-related thrombosis and cardiovascular disease.
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KEYWORD
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esculetin, cAMP/cGMP, intracellular Ca2+, fibrinogen binding, fibrin clot
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