Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Korean J Physiol Pharmacol
2011 Feb 01;151:17-22. doi: 10.4196/kjpp.2011.15.1.17.
Show Gene links
Show Anatomy links
Quercetin Inhibits α3β4 Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes.
Lee BH
,
Hwang SH
,
Choi SH
,
Shin TJ
,
Kang J
,
Lee SM
,
Nah SY
.
???displayArticle.abstract???
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 α7 nicotinic acetylcholine receptors. In the present study, we examined quercetin effects on heteromeric neuronal α3β4 nicotinic acetylcholine receptor channel activity expressed in Xenopus oocytes after injection of cRNA encoding bovine neuronal α3 and β4 subunits. Treatment with acetylcholine elicited an inward peak current (I(ACh)) in oocytes expressing α3β4 nicotinic acetylcholine receptor. Co-treatment with quercetin and acetylcholine inhibited I(ACh) in oocytes expressing α3β4 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 µM in oocytes expressing α3β4 nicotinic acetylcholine receptor. The inhibition of I(ACh) by quercetin was voltage-independent and non-competitive. These results indicate that quercetin might regulate α3β4 nicotinic acetylcholine receptor and this regulation might be one of the pharmacological actions of quercetin in nervous systems.
Arias,
Luminal and non-luminal non-competitive inhibitor binding sites on the nicotinic acetylcholine receptor.
1996, Pubmed
Arias,
Luminal and non-luminal non-competitive inhibitor binding sites on the nicotinic acetylcholine receptor.
1996,
Pubmed
Boorman,
Stoichiometry of human recombinant neuronal nicotinic receptors containing the b3 subunit expressed in Xenopus oocytes.
2000,
Pubmed
,
Xenbase
Boulter,
Functional expression of two neuronal nicotinic acetylcholine receptors from cDNA clones identifies a gene family.
1987,
Pubmed
,
Xenbase
Boulter,
Isolation of a cDNA clone coding for a possible neural nicotinic acetylcholine receptor alpha-subunit.
,
Pubmed
Campos-Caro,
Neuronal nicotinic acetylcholine receptors on bovine chromaffin cells: cloning, expression, and genomic organization of receptor subunits.
1997,
Pubmed
,
Xenbase
Cardoso,
Effects of ethanol on recombinant human neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes.
1999,
Pubmed
,
Xenbase
Dani,
Nicotinic acetylcholine receptors and nicotinic cholinergic mechanisms of the central nervous system.
2007,
Pubmed
Di Angelantonio,
Molecular biology and electrophysiology of neuronal nicotinic receptors of rat chromaffin cells.
2003,
Pubmed
Free,
Evidence for constitutive expression of bovine adrenal a3beta4* nicotinic acetylcholine receptors.
2002,
Pubmed
García-Colunga,
Modulation of nicotinic acetylcholine receptors by strychnine.
1999,
Pubmed
,
Xenbase
García-Colunga,
Effects of serotonergic agents on neuronal nicotinic acetylcholine receptors.
1995,
Pubmed
,
Xenbase
Gotti,
Neuronal nicotinic receptors: from structure to pathology.
2004,
Pubmed
Grønlien,
Importance of M2-M3 loop in governing properties of genistein at the α7 nicotinic acetylcholine receptor inferred from α7/5-HT3A chimera.
2010,
Pubmed
,
Xenbase
Haghighi,
A molecular link between inward rectification and calcium permeability of neuronal nicotinic acetylcholine alpha3beta4 and alpha4beta2 receptors.
2000,
Pubmed
,
Xenbase
Harborne,
Advances in flavonoid research since 1992.
2000,
Pubmed
Havsteen,
The biochemistry and medical significance of the flavonoids.
2002,
Pubmed
Heidmann,
Multiple sites of action for noncompetitive blockers on acetylcholine receptor rich membrane fragments from torpedo marmorata.
1983,
Pubmed
Herrero,
Differential blockade of rat alpha3beta4 and alpha7 neuronal nicotinic receptors by omega-conotoxin MVIIC, omega-conotoxin GVIA and diltiazem.
1999,
Pubmed
,
Xenbase
Jensen,
Charge selectivity of the Cys-loop family of ligand-gated ion channels.
2005,
Pubmed
Kandaswami,
Free radical scavenging and antioxidant activity of plant flavonoids.
1994,
Pubmed
Karlin,
Emerging structure of the nicotinic acetylcholine receptors.
2002,
Pubmed
Kindler,
Additive inhibition of nicotinic acetylcholine receptors by corticosteroids and the neuromuscular blocking drug vecuronium.
2000,
Pubmed
,
Xenbase
Lee,
Human glycine alpha1 receptor inhibition by quercetin is abolished or inversed by alpha267 mutations in transmembrane domain 2.
2007,
Pubmed
,
Xenbase
Lee,
Quercetin enhances human α7 nicotinic acetylcholine receptor-mediated ion current through interactions with Ca(2+) binding sites.
2010,
Pubmed
,
Xenbase
Lee,
Effects of quercetin on α9α10 nicotinic acetylcholine receptor-mediated ion currents.
2011,
Pubmed
Lee,
Quercetin inhibits the 5-hydroxytryptamine type 3 receptor-mediated ion current by interacting with pre-transmembrane domain I.
2005,
Pubmed
,
Xenbase
Oyama,
Myricetin and quercetin, the flavonoid constituents of Ginkgo biloba extract, greatly reduce oxidative metabolism in both resting and Ca(2+)-loaded brain neurons.
1994,
Pubmed
Palma,
Effects of Zn2+ on wild and mutant neuronal alpha7 nicotinic receptors.
1998,
Pubmed
,
Xenbase
Picq,
Effect of two flavonoid compounds on central nervous system. Analgesic activity.
1991,
Pubmed
Shinohara,
Effects of resveratrol, a grape polyphenol, on catecholamine secretion and synthesis in cultured bovine adrenal medullary cells.
2007,
Pubmed
,
Xenbase
Sine,
Local anesthetics and histrionicotoxin are allosteric inhibitors of the acetylcholine receptor. Studies of clonal muscle cells.
1982,
Pubmed
Speroni,
Neuropharmacological activity of extracts from Passiflora incarnata.
1988,
Pubmed
Valera,
Progesterone modulates a neuronal nicotinic acetylcholine receptor.
1992,
Pubmed
,
Xenbase
Yu,
Polyphenols of Rubus coreanum Inhibit Catecholamine Secretion from the Perfused Adrenal Medulla of SHRs.
2009,
Pubmed
Zhang,
Dual effects of nobiletin, a citrus polymethoxy flavone, on catecholamine secretion in cultured bovine adrenal medullary cells.
2010,
Pubmed
,
Xenbase
