Differential effects of quercetin glycosides on GABAC receptor channel activity

다국어 초록 (Multilingual Abstract)

Quercetin, a representative flavonoid, is acompound of low molecular weight found in various coloredplants and vegetables. Quercetin shows a wide rangeof neuropharmacological activities. In fact, quercetin naturallyexists as monomer-(quercetin-3-O-rhamnoside)(Rham1), dimer-(Rutin), or trimer-glycosides [quercetin-3-(2G-rhamnosylrutinoside)] (Rham2) at carbon-3 in fruitsand vegetables. The carbohydrate components are removedafter ingestion into gastrointestinal systems. The role of theglycosides attached to quercetin in the regulation of caminobutyricacid class C (GABAC) receptor channelactivity has not been determined. In the present study, we examined the effects of quercetin glycosides on GABACreceptor channel activity by expressing human GABACalone in Xenopus oocytes using a two-electrode voltageclamp technique and also compared the effects of quercetinglycosides with quercetin. We found that GABA-inducedinward current (IGABA) was inhibited by quercetin orquercetin glycosides. The inhibitory effects of quercetinand its glycosides on IGABA were concentration-dependentand reversible in the order of Rutin & quercetin & Rham1[Rham 2. The inhibitory effects of quercetin and itsglycosides on IGABA were noncompetitive and membranevoltage-insensitive. These results indicate that quercetinand its glycosides regulate GABAC receptor channelactivity through interaction with a different site from thatof GABA, and that the number of carbohydrate attached toquercetin might play an important role in the regulation ofGABAC receptor channel activity.

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