Korean J Physiol Pharmacol.  2011 Feb;15(1):17-22.

Quercetin Inhibits alpha3beta4 Nicotinic Acetylcholine Receptor-Mediated Ion Currents Expressed in Xenopus Oocytes

Affiliations
  • 1Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University, Seoul 143-701, Korea. synah@konkuk.ac.kr

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-HT3A 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 (IACh) in oocytes expressing alpha3beta4 nicotinic acetylcholine receptor. Co-treatment with quercetin and acetylcholine inhibited IACh in oocytes expressing alpha3beta4 nicotinic acetylcholine receptors. The inhibition of IACh by quercetin was reversible and concentration-dependent. The half-inhibitory concentration (IC50) of quercetin was 14.9+/-0.8 microM in oocytes expressing alpha3beta4 nicotinic acetylcholine receptor. The inhibition of IACh 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.

Keyword

Flavonoids; Quercetin; alpha3beta4 nicotinic acetylcholine receptor; Xenopus oocyte

MeSH Terms

Acetylcholine
Flavonoids
Fruit
Glycine
Ligand-Gated Ion Channels
Nervous System
Neurons
Oocytes
Quercetin
Receptors, Nicotinic
RNA, Complementary
Skin
Social Control, Formal
Vegetables
Xenopus
Acetylcholine
Flavonoids
Glycine
Ligand-Gated Ion Channels
Quercetin
RNA, Complementary
Receptors, Nicotinic
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