Differential Regulations of Quercetin and Its Glycosides on Ligand-Gated Ion Channels(Pharmacology)

概要

論文の詳細を見る
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) (Rhaml), 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.
社団法人日本薬学会の論文
2008-04-01

Differential Regulations of Quercetin and Its Glycosides on Ligand-Gated Ion Channels(Pharmacology)

スポンサーリンク

概要

著者

関連論文

スポンサーリンク