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1.
Naunyn Schmiedebergs Arch Pharmacol ; 381(2): 137-45, 2010 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-20052460

RESUMEN

Scutellarin is a flavonoid extracted from a traditional Chinese herb, Erigeron breviscapus Hand Mazz, which has been broadly used in treating various cardiovascular diseases. In this study, we investigated its effect on cardiac hypertrophy and the underlying mechanism. Both in vitro and in vivo cardiac hypertrophy models were employed to explore the anti-hypertrophic action of scutellarin. We found that scutellarin significantly suppressed the hypertrophic growth of neonatal cardiac myocytes exposed to phenylephrine (PE) and mouse heart subjected to pressure overload induced by aortic banding, accompanied with the decreased expression of hypertrophic markers beta-myosin heavy chain and atrial natriuretic peptide. We then measured the change of free intracellular calcium using laser scanning confocal microscope. We found that scutellarin alleviated the increment of free intracellular calcium during cardiac hypertrophy either induced by PE or aortic banding. The expression of calcium downstream effectors calcineurin and phosphorylated calmodulin kinase II (CaMKII) were significantly suppressed by scutellarin. Our study indicated that scutellarin exerts its anti-hypertrophic activity via suppressing the Ca(2+)-mediated calcineurin and CaMKII pathways, which supports the observation that clinical application of scutellarin is beneficial for cardiovascular disease patients.


Asunto(s)
Apigenina/farmacología , Calcineurina/biosíntesis , Proteína Quinasa Tipo 2 Dependiente de Calcio Calmodulina/fisiología , Calcio/fisiología , Glucuronatos/farmacología , Vasodilatadores/farmacología , Animales , Animales Recién Nacidos , Apigenina/uso terapéutico , Señalización del Calcio , Proteína Quinasa Tipo 2 Dependiente de Calcio Calmodulina/biosíntesis , Proteínas Quinasas Dependientes de Calcio-Calmodulina/metabolismo , Cardiomegalia/tratamiento farmacológico , Cardiomegalia/metabolismo , Cardiomegalia/patología , Tamaño de la Célula/efectos de los fármacos , Células Cultivadas , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Glucuronatos/uso terapéutico , Ratones , Ratones Endogámicos C57BL , Miocitos Cardíacos/efectos de los fármacos , Miocitos Cardíacos/metabolismo , Miocitos Cardíacos/patología , Fenilefrina/farmacología , Ratas , Ratas Wistar , Transducción de Señal/efectos de los fármacos , Vasodilatadores/uso terapéutico
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