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Inhibitory Effects of Quercetin on Muscle-type of Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes
The Korean Journal of Physiology and Pharmacology ; : 195-201, 2011.
Artigo em Inglês | WPRIM | ID: wpr-727882
ABSTRACT
The flavonoid quercetin is a low molecular weight compound generally found in apple, gingko, tomato, onion and other red-colored fruits and vegetables. Like other flavonoids, quercetin has diverse pharmacological actions. However, relatively little is known about the influence of quercetin effects in the regulation of ligand-gated ion channels. Previously, we reported that quercetin regulates subsets of nicotinic acetylcholine receptors such as alpha3beta4, alpha7 and alpha9alpha10. Presently, we investigated the effects of quercetin on muscle-type of nicotinic acetylcholine receptor channel activity expressed in Xenopus oocytes after injection of cRNA encoding human fetal or adult muscle-type of nicotinic acetylcholine receptor subunits. Acetylcholine treatment elicited an inward peak current (IACh) in oocytes expressing both muscle-type of nicotinic acetylcholine receptors and co-treatment of quercetin with acetylcholine inhibited IACh. Pre-treatment of quercetin further inhibited IACh in oocytes expressing adult and fetal muscle-type nicotinic acetylcholine receptors. The inhibition of IACh by quercetin was reversible and concentration-dependent. The IC50 of quercetin was 18.9+/-1.2 microM in oocytes expressing adult muscle-type nicotinic acetylcholine receptor. The inhibition of IACh by quercetin was voltage-independent and non-competitive. These results indicate that quercetin might regulate human muscle-type nicotinic acetylcholine receptor channel activity and that quercetin-mediated regulation of muscle-type nicotinic acetylcholine receptor might be coupled to regulation of neuromuscular junction activity.
Assuntos

Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Oócitos / Quercetina / Verduras / Xenopus / Flavonoides / Acetilcolina / Receptores Nicotínicos / RNA Complementar / Solanum lycopersicum / Cebolas Limite: Adulto / Humanos Idioma: Inglês Revista: The Korean Journal of Physiology and Pharmacology Ano de publicação: 2011 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Oócitos / Quercetina / Verduras / Xenopus / Flavonoides / Acetilcolina / Receptores Nicotínicos / RNA Complementar / Solanum lycopersicum / Cebolas Limite: Adulto / Humanos Idioma: Inglês Revista: The Korean Journal of Physiology and Pharmacology Ano de publicação: 2011 Tipo de documento: Artigo