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Free Radic Biol Med ; 49(5): 738-47, 2010 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-20554019

RESUMEN

In this work we describe the protective effects of quercetin against H(2)O(2) in 24-h-pretreated neuronal cultures. We explored quercetin availability and subcellular fate through the use of HPLC-Diode Array Detection (DAD), epifluorescence, and confocal microscopy. We focused on quercetin modulation of thiol-redox systems by evaluating changes in mitochondrial thioredoxin Trx2, the levels of total glutathione (GSH), and the expression of the gamma-glutamate-cysteine ligase catalytic subunit (GCLC), the rate-limiting enzyme of GSH synthesis, by the use of Western blot, HPLC, and real-time PCR techniques, respectively. We further explored the activation of the protective NF-E2-related factor 2 (Nrf2)-dependent signaling pathway by quercetin using immunocytochemistry techniques. Our results showed rapid quercetin internalization into neurons, reaching the nucleus after its addition to the culture. Quercetin pretreatment increased total GSH levels, but did not increase Trx2. Interestingly it caused Nrf2 nuclear translocation and significantly increased GCLC gene expression. At the moment of H(2)O(2) addition, intracellular quercetin or related metabolites were undetectable in the cultures although quercetin pretreatment prevented neuronal death from the oxidant exposure. Our findings suggest alternative mechanisms of quercetin neuroprotection beyond its long-established ROS scavenging properties, involving Nrf2-dependent modulation of the GSH redox system.


Asunto(s)
Núcleo Celular/efectos de los fármacos , Citoprotección/efectos de los fármacos , Glutatión/metabolismo , Factor 2 Relacionado con NF-E2/metabolismo , Neuronas/efectos de los fármacos , Quercetina/farmacología , Transporte Activo de Núcleo Celular/efectos de los fármacos , Animales , Antioxidantes/farmacocinética , Antioxidantes/farmacología , Muerte Celular/efectos de los fármacos , Núcleo Celular/metabolismo , Evaluación Preclínica de Medicamentos , Peróxido de Hidrógeno/toxicidad , Neuronas/metabolismo , Fármacos Neuroprotectores/farmacocinética , Fármacos Neuroprotectores/farmacología , Estrés Oxidativo/efectos de los fármacos , Estrés Oxidativo/fisiología , Transporte de Proteínas/efectos de los fármacos , Quercetina/farmacocinética , Ratas , Ratas Sprague-Dawley , Regulación hacia Arriba/efectos de los fármacos
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