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- Title
Inhibitory Effects of Quercetin on Muscle-type of Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes.
- Authors
Byung-Hwan Lee; Tae-Joon Shin; Sung-Hee Hwang; Sun-Hye Choi; Jiyeon Kang; Hyeon-Joong Kim; Chan-Woo Park; Soo-Han Lee; Seung-Yeol Nah
- 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 α3β 4, α7 and α9α10. 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±1.2μM in oocytes expressing adult muscle-type nicotinic acetylcholine receptor. The inhibition of IACh by quercetin was voltageindependent and non-competitive. These results indicate that quercetin might regulate human muscletype 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.
- Subjects
XENOPUS eggs; OVUM; FLAVONOIDS; ACETYLCHOLINE; XENOPUS; NICOTINIC receptors
- Publication
Korean Journal of Physiology & Pharmacology, 2011, Vol 15, Issue 4, p195
- ISSN
1226-4512
- Publication type
Article
- DOI
10.4196/kjpp.2011.15.4.195