Inhibitory effects of quercetin on muscle-type of nicotinic acetylcholine receptor-mediated ion currents expressed in Xenopus oocytes

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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 α 3 β 4, α 7 and α 9 α 10. 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 μM 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.

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Lee, B. H., Shin, T. J., Hwang, S. H., Choi, S. H., Kang, J., Kim, H. J., … Nah, S. Y. (2011). Inhibitory effects of quercetin on muscle-type of nicotinic acetylcholine receptor-mediated ion currents expressed in Xenopus oocytes. Korean Journal of Physiology and Pharmacology, 15(4), 195–201. https://doi.org/10.4196/kjpp.2011.15.4.195

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