PMID- 21461236 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20110714 LR - 20211020 IS - 2093-3827 (Electronic) IS - 1226-4512 (Print) IS - 1226-4512 (Linking) VI - 15 IP - 1 DP - 2011 Feb TI - Quercetin Inhibits alpha3beta4 Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes. PG - 17-22 LID - 10.4196/kjpp.2011.15.1.17 [doi] AB - Quercetin mainly exists in the skin of colored fruits and vegetables as one of flavonoids. Recent studies show that quercetin, like other flavonoids, has diverse pharmacological actions. However, relatively little is known about quercetin effects in the regulations of ligand-gated ion channels. In the previous reports, we have shown that quercetin regulates subsets of homomeric ligand-gated ion channels such as glycine, 5-HT(3A) and alpha7 nicotinic acetylcholine receptors. In the present study, we examined quercetin effects on heteromeric neuronal alpha3beta4 nicotinic acetylcholine receptor channel activity expressed in Xenopus oocytes after injection of cRNA encoding bovine neuronal alpha3 and beta4 subunits. Treatment with acetylcholine elicited an inward peak current (I(ACh)) in oocytes expressing alpha3beta4 nicotinic acetylcholine receptor. Co-treatment with quercetin and acetylcholine inhibited I(ACh) in oocytes expressing alpha3beta4 nicotinic acetylcholine receptors. The inhibition of I(ACh) by quercetin was reversible and concentration-dependent. The half-inhibitory concentration (IC(50)) of quercetin was 14.9+/-0.8 microM in oocytes expressing alpha3beta4 nicotinic acetylcholine receptor. The inhibition of I(ACh) by quercetin was voltage-independent and non-competitive. These results indicate that quercetin might regulate alpha3beta4 nicotinic acetylcholine receptor and this regulation might be one of the pharmacological actions of quercetin in nervous systems. 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 - Hwang, Sung-Hee AU - Hwang SH FAU - Choi, Sun-Hye AU - Choi SH FAU - Shin, Tae-Joon AU - Shin TJ FAU - Kang, Jiyeon AU - Kang J FAU - Lee, Sang-Mok AU - Lee SM FAU - Nah, Seung-Yeol AU - Nah SY LA - eng PT - Journal Article DEP - 20110228 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 - PMC3062079 OTO - NOTNLM OT - Flavonoids OT - Quercetin OT - Xenopus oocyte OT - alpha3beta4 nicotinic acetylcholine receptor EDAT- 2011/04/05 06:00 MHDA- 2011/04/05 06:01 PMCR- 2011/02/01 CRDT- 2011/04/05 06:00 PHST- 2010/12/27 00:00 [received] PHST- 2011/01/17 00:00 [revised] PHST- 2011/01/18 00:00 [accepted] PHST- 2011/04/05 06:00 [entrez] PHST- 2011/04/05 06:00 [pubmed] PHST- 2011/04/05 06:01 [medline] PHST- 2011/02/01 00:00 [pmc-release] AID - 10.4196/kjpp.2011.15.1.17 [doi] PST - ppublish SO - Korean J Physiol Pharmacol. 2011 Feb;15(1):17-22. doi: 10.4196/kjpp.2011.15.1.17. Epub 2011 Feb 28.