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Eur J Pharmacol ; 746: 63-9, 2015 Jan 05.
Artículo en Inglés | MEDLINE | ID: mdl-25445049

RESUMEN

Loureirin A is a flavonoid extracted from Dragon׳s Blood that has been used to promote blood circulation and remove stasis in Chinese traditional medicine. However, the mechanisms of these effects are not fully understood. We explored the anti-platelet activity and underlying mechanism of loureirin A in vitro. Our results indicated that loureirin A negatively affected agonist-induced platelet aggregation such as collagen, collagen-related peptide (CRP), ADP and thrombin. Loureirin A inhibited collagen-induced platelet ATP secretion and thrombin-stimulated P-selectin expression in a dose-dependent manner. Platelet spreading on immobilized fibrinogen was significantly impaired in the presence of loureirin A. Immunoblotting analysis indicated that 100µM of loureirin A almost completely eliminated collagen-induced Akt phosphorylation at Ser473. Interestingly, a submaximal dose (50µM) of loureirin A had an additive inhibitory effect with the phosphoinositide 3-kinase (PI3K) inhibitor Ly294002 on collage-induced Akt phosphorylation in platelets. Taken together, loureirin A had an inhibitory effect on platelet activation, perhaps through an impairment of PI3K/Akt signaling.


Asunto(s)
Chalconas/farmacología , Inhibidores de Agregación Plaquetaria/farmacología , Proteínas Proto-Oncogénicas c-akt/metabolismo , Adenosina Trifosfato/metabolismo , Animales , Plaquetas/efectos de los fármacos , Plaquetas/fisiología , Fibrinógeno/química , Fibrinógeno/metabolismo , Regulación de la Expresión Génica/efectos de los fármacos , Humanos , Proteínas Inmovilizadas/química , Proteínas Inmovilizadas/metabolismo , Masculino , Ratones , Selectina-P/metabolismo , Fosforilación/efectos de los fármacos , Extractos Vegetales/química , Agregación Plaquetaria/efectos de los fármacos , Trombina/farmacología
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