Shin, Tae-Joon Choi, Sun-Hye Lee, Byung-Hwan Pyo, Mi Kyung Hwang, Sung-Hee Kim, Bo-Ra Lee, Sang-Mok Han, Ye Sun Lee, Jun-Ho Park, Ji-Ho Kim, Hyoung-Chun Rhim, Hyewhon Nah, Seung-Yeol 2024-01-20T18:33:54Z 2024-01-20T18:33:54Z 2021-09-05 2010-09 0918-6158 https://pubs.kist.re.kr/handle/201004/131130 Quercetin is a low molecular weight flavonoid found in dietary fruits and vegetables. Quercetin, like other flavonoids, has demonstrated neuroprotective effects in vitro and in vivo. However, relatively little is known about how quercetin achieves its neuroprotective abilities. The alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor is one of several excitatory receptors, which play an important role in postsynaptic neurotransmission. Over-stimulation of ionotropic glutamate receptor including AMPA receptors is closely associated with excitatory neurotoxicities. In the present study, we investigated the effects of quercetin on the glutamate-induced inward current (I-Glu) in Xenopus oocytes that heterologously express human AMPA receptor and stargazin, an auxiliary subunit of AMPA receptor. I-Glu was measured using the two-electrode voltage clamp technique. In oocytes injected with cRNAs coding AMPA receptor (GluR1) and stargazin, quercetin inhibited I-Glu reversible and concentration-dependent manner. The IC50 was 84.9 +/- 15.0 mu M. Quercetin action on I-Glu was attenuated by increasing glutamate concentration, and was membrane holding potential-dependent. These results show a possibility that quercetin interacts with AMPA receptor, which was heterologously expressed in Xenopus oocytes and that quercetin action on I-Glu of AMPA receptor could be one of contributions of quercetin-mediated neuroprotections. English PHARMACEUTICAL SOC JAPAN ACETYLCHOLINE-RECEPTOR GLUTAMATE RECEPTORS CHANNELS CELLS FLAVONOIDS SUBUNIT NEUROTOXICITY INHIBITION OOCYTES BINDING Effects of Quercetin on Human alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptor-Mediated Ion Currents Article 10.1248/bpb.33.1615 1 BIOLOGICAL & PHARMACEUTICAL BULLETIN, v.33, no.9, pp.1615 - 1619 BIOLOGICAL & PHARMACEUTICAL BULLETIN 33 9 1615 1619 scie scopus 000281427600028 2-s2.0-77957575181 Pharmacology & Pharmacy Pharmacology & Pharmacy Article ACETYLCHOLINE-RECEPTOR GLUTAMATE RECEPTORS CHANNELS CELLS FLAVONOIDS SUBUNIT NEUROTOXICITY INHIBITION OOCYTES BINDING flavonoid quercetin alpha-amino-3-hydroxy-5-methyl-4-isoxoazolepropionic acid