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标题：Differential Regulations of Quercetin and Its Glycosides on Ligand-Gated Ion Channels
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作者：Byung-Hwan Lee ; Mi Kyung Pyo ; Jun-Ho 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：2008
卷号：31
期号：4
页码：611-617
DOI：10.1248/bpb.31.611
出版社：The Pharmaceutical Society of Japan
摘要：Quercetin, one of the flavonoids, is a compound of low molecular weight found in various plants and shows a wide range of diverse neuropharmacological actions. In fruits and vegetables, quercetin exists as monomer- (quercetin-3- O -rhamnoside) (Rham1), dimer- (Rutin), or trimer-glycosides [quercetin-3-(2^G-rhamnosylrutinoside)] (Rham2) at carbon-3. In the previous studies, we demonstrated that quercetin inhibits both glycine and 5-hydroxytryptamine type 3, (5-HT_3A) receptor channel activities expressed in Xenopus oocytes. However, the effects of quercetin glycosides on glycine and 5-HT_3A receptor channel activities are not well known. In the present study, we investigated the effects of quercetin glycosides on the human glycine α1 receptor and mouse 5-HT_3A receptor channel activities expressed in Xenopus oocytes using a two-electrode voltage clamp technique. In oocytes expressing glycine or 5-HT_3A receptors, quercetin- or its glycosides-induced inhibitions on glycine- ( I _Gly) and 5-HT-induced current ( I _5-HT) were dose-dependent and reversible. Applications of quercetin and its glycosides inhibited I _Gly in order of quercetin>Rutin≥Rham1>Rham2. Applications of quercetin and its glycosides inhibited I _5-HT in order of Rham2≥quercetin>Rutin=Rham1. The inhibitions of I _Gly by quercetin glycosides were non-competitive and voltage-sensitive, whereas the inhibitions of I _5-HT by quercetin glycosides were competitive and voltage-insensitive manners. These results also indicate that quercetin glycosides might regulate the human glycine α1 and mouse 5-HT_3A receptors with differential manners.
关键词：flavonoid;quercetin glycoside;ligand-gated ion channel;Xenopus oocyte