AI Article Synopsis
- * 3,5,2',4'-Tetramethoxystilbene (TMS), a compound similar to resveratrol, has shown potential in inhibiting platelet aggregation and thrombus formation by targeting PAR4.
- * The study indicates that the fully methylated structure of TMS is crucial for its effectiveness against PAR4, suggesting that similar compounds may be developed as new antiplatelet treatments.
Article Abstract
Thrombin is a potent platelet activator and a key mediator of blood coagulation, thereby playing a crucial role in cardiovascular disease. Recently, protease-activated receptor 4 (PAR4), one of thrombin receptors in human platelets, is emerging as a promising target for antiplatelet therapy. 3,5,2',4'-Tetramethoxystilbene (TMS), a resveratrol analog, have demonstrated promising effects on preventing atherosclerosis and hypertension, whereas its antiplatelet effect has never been investigated. Herein we show that TMS at concentrations of a few micromolar selectively inhibits PAR4-mediated human platelet aggregation, ATP secretion, integrin αIIbβ3 activation, and signaling pathways. In a whole-blood model of arterial flow, TMS also significantly reduced in vitro thrombus formation. Analysis of the structure-activity relationships of TMS and a panel of stilbene analogs reveal that full methylation of hydroxy groups of the stilbenes is the critical structural determinant for the anti-PAR4 activity. Our results suggest that fully methylated resveratrol analogs with anti-PAR4 activity are potential candidates for development of novel antiplatelet agents.
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| http://dx.doi.org/10.1016/j.cbi.2022.109889 | DOI Listing |
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