Biomol Ther.  2016 Jul;24(4):410-417. 10.4062/biomolther.2015.153.

Differential Effects of Quercetin and Quercetin Glycosides on Human α7 Nicotinic Acetylcholine Receptor-Mediated Ion Currents

Affiliations
  • 1Department of Physiology, College of Veterinary Medicine and BioMolecular Informatics Center, Konkuk University, Seoul 05029, Republic of Korea. synah@konkuk.ac.kr
  • 2Department of Pharmaceutical Engineering, Sangji University, Wonju 26339, Republic of Korea.
  • 3International Ginseng and Herb Research Institute, Geumsan 32724, Republic of Korea.
  • 4Life Science Division, Korea Institute of Science and Technology, Seoul 02792, Republic of Korea.
  • 5Neuropsychopharmacology and Toxicology Program, College of Pharmacy, Kangwon National University, Chunchon 24341, Republic of Korea.
  • 6Mibyeong Research Center, Korea Institute of Oriental Medicine, Daejeon 34054, Republic of Korea.

Abstract

Quercetin is a flavonoid usually found in fruits and vegetables. Aside from its antioxidative effects, quercetin, like other flavonoids, has a various neuropharmacological actions. Quercetin-3-O-rhamnoside (Rham1), quercetin-3-O-rutinoside (Rutin), and quercetin-3-(2(G)-rhamnosylrutinoside (Rham2) are mono-, di-, and tri-glycosylated forms of quercetin, respectively. In a previous study, we showed that quercetin can enhance α7 nicotinic acetylcholine receptor (α7 nAChR)-mediated ion currents. However, the role of the carbohydrates attached to quercetin in the regulation of α7 nAChR channel activity has not been determined. In the present study, we investigated the effects of quercetin glycosides on the acetylcholine induced peak inward current (I(ACh)) in Xenopus oocytes expressing the α7 nAChR. I(ACh) was measured with a two-electrode voltage clamp technique. In oocytes injected with α7 nAChR copy RNA, quercetin enhanced I(ACh), whereas quercetin glycosides inhibited I(ACh). Quercetin glycosides mediated an inhibition of I(ACh), which increased when they were pre-applied and the inhibitory effects were concentration dependent. The order of I(ACh) inhibition by quercetin glycosides was Rutin≥Rham1>Rham2. Quercetin glycosides-mediated I(ACh) enhancement was not affected by ACh concentration and appeared voltage-independent. Furthermore, quercetin-mediated I(ACh) inhibition can be attenuated when quercetin is co-applied with Rham1 and Rutin, indicating that quercetin glycosides could interfere with quercetin-mediated α7 nAChR regulation and that the number of carbohydrates in the quercetin glycoside plays a key role in the interruption of quercetin action. These results show that quercetin and quercetin glycosides regulate the α7 nAChR in a differential manner.

Keyword

Flavonoids; Quercetin; Quercetin glycosides; α7 nAChR

MeSH Terms

Acetylcholine*
Carbohydrates
Flavonoids
Fruit
Glycosides*
Humans*
Oocytes
Quercetin*
Receptors, Nicotinic
RNA
Rutin
Vegetables
Xenopus
Acetylcholine
Carbohydrates
Flavonoids
Glycosides
Quercetin
RNA
Receptors, Nicotinic
Rutin
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