Key result
The isoflavonoids genistein and daidzein demonstrated marked cyclooxygenase-1 inhibitory activity and acted as antagonists on thromboxane receptors, suggesting a potential to inhibit platelet aggregation.
Dietary isoflavonoids such as genistein and daidzein exhibit antiplatelet effects by inhibiting COX-1 and antagonizing thromboxane A2 receptors in vitro.
Should not change clinical antiplatelet practice; leaves open translational research on isoflavonoid mechanisms.
Flavonoids, important components of human diet, have been claimed to possess a significant antiplatelet potential, in particular due to their effects on the arachidonic acid cascade. Due to variable and incomplete results, this study was aimed at delivering a detailed analysis of the effects of 29 structurally relevant, mainly natural flavonoids on three consecutive steps of the arachidonic acid cascade.Only the isoflavonoids genistein and daidzein were shown to possess a marked cyclooxygenase-1 inhibitory activity, which was higher than that of acetylsalicylic acid using the isolated ovine enzyme, and physiologically relevant, although lower than acetylsalicylic acid in human platelets. None of the tested flavonoids possesses an effect on thromboxane synthase in a clinically achievable concentration. Contrarily, many flavonoids, particularly those possessing an isolated 7-hydroxyl group and/or a 4'-hydroxyl group, acted as antagonists on thromboxane receptors. Interestingly, the substitution of the free 7-hydroxyl group by glucose might not abolish the activity.In conclusion, the consumption of few flavonoids in a diet, particularly of the isoflavonoids genistein and daidzein, may positively influence platelet aggregation.
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Karlíčková et al. (2015) studied Healthy volunteers (in vitro platelet study) (n=31). 29 flavonoids (including genistein and daidzein) vs. Acetylsalicylic acid (ASA) and 1-benzylimidazole was evaluated on Inhibition of cyclooxygenase-1, thromboxane synthase, and thromboxane A2 receptors. The isoflavonoids genistein and daidzein demonstrated marked cyclooxygenase-1 inhibitory activity and acted as antagonists on thromboxane receptors, suggesting a potential to inhibit platelet aggregation.
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