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KMID : 0811720110150040195
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Korean Journal of Physiology & Pharmacology
2011 Volume.15 No. 4 p.195 ~ p.201
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Inhibitory Effects of Quercetin on Muscle-type of Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes
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Lee Byung-Hwan
Shin Tae-Joon
Hwang Sung-Hee
Choi Sun-Hye
Kang Ji-Yeon
Kim Hyeon-Joong
Park Chan-Woo
Lee Soo-Han
Nah Seung-Yeol
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Abstract
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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 ?3?4, ?7 and ?9?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?M 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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KEYWORD
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Flavonoids, Quercetin, Muscle-type nicotinic acetylcholine receptors, Xenopus oocyte
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