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标题：Effects of Quercetin on Human α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid Receptor-Mediated Ion Currents
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作者：Tae-Joon Shin ; Sun-Hye Choi ; Byung-Hwan Lee 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2010
卷号：33
期号：9
页码：1615-1619
DOI：10.1248/bpb.33.1615
出版社：The Pharmaceutical Society of Japan
摘要：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 α-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 in a reversible and concentration-dependent manner. The IC₅₀ was 84.9±15.0 μ 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.
关键词：flavonoid;quercetin;α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid