PMID- 21994477 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20111110 LR - 20211020 IS - 2093-3827 (Electronic) IS - 1226-4512 (Print) IS - 1226-4512 (Linking) VI - 15 IP - 4 DP - 2011 Aug TI - Inhibitory Effects of Quercetin on Muscle-type of Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes. PG - 195-201 LID - 10.4196/kjpp.2011.15.4.195 [doi] AB - 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 (I(ACh)) in oocytes expressing both muscle-type of nicotinic acetylcholine receptors and co-treatment of quercetin with acetylcholine inhibited I(ACh). Pre-treatment of quercetin further inhibited I(ACh) in oocytes expressing adult and fetal muscle-type nicotinic acetylcholine receptors. The inhibition of I(ACh) by quercetin was reversible and concentration-dependent. The IC(50) of quercetin was 18.9+/-1.2 microM in oocytes expressing adult muscle-type nicotinic acetylcholine receptor. The inhibition of I(ACh) 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. FAU - Lee, Byung-Hwan AU - Lee BH AD - Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University, Seoul 143-701, Korea. FAU - Shin, Tae-Joon AU - Shin TJ FAU - Hwang, Sung-Hee AU - Hwang SH FAU - Choi, Sun-Hye AU - Choi SH FAU - Kang, Jiyeon AU - Kang J FAU - Kim, Hyeon-Joong AU - Kim HJ FAU - Park, Chan-Woo AU - Park CW FAU - Lee, Soo-Han AU - Lee SH FAU - Nah, Seung-Yeol AU - Nah SY LA - eng PT - Journal Article DEP - 20110831 PL - Korea (South) TA - Korean J Physiol Pharmacol JT - The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology JID - 9709505 PMC - PMC3186920 OTO - NOTNLM OT - Flavonoids OT - Muscle-type nicotinic acetylcholine receptors OT - Quercetin OT - Xenopus oocyte EDAT- 2011/10/14 06:00 MHDA- 2011/10/14 06:01 PMCR- 2011/08/01 CRDT- 2011/10/14 06:00 PHST- 2011/06/03 00:00 [received] PHST- 2011/07/20 00:00 [revised] PHST- 2011/08/02 00:00 [accepted] PHST- 2011/10/14 06:00 [entrez] PHST- 2011/10/14 06:00 [pubmed] PHST- 2011/10/14 06:01 [medline] PHST- 2011/08/01 00:00 [pmc-release] AID - 10.4196/kjpp.2011.15.4.195 [doi] PST - ppublish SO - Korean J Physiol Pharmacol. 2011 Aug;15(4):195-201. doi: 10.4196/kjpp.2011.15.4.195. Epub 2011 Aug 31.