Lee, Byung-Hwan Pyo, Mi Kyung Lee, Jun-Ho Choi, Sun-Hye Shin, Tae-Joon Lee, Sang-Mok Lim, Yoongho Han, Ye Sun Paik, Hyun-Dong Cho, Ssang-Goo Yun-Choi, Hye Sook Rhim, Hyewhon Nah, Seung-Yeol 2024-01-20T23:32:13Z 2024-01-20T23:32:13Z 2021-09-03 2008-04 0918-6158 https://pubs.kist.re.kr/handle/201004/133585 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)vertical bar(Rham2) at carbon-3. In the previous studies, we demonstrated that quercetin inhibits both glycine and 5-hydroxytryptamine type 3, (5-HT3A) receptor channel activities expressed in Xenopus oocytes. However, the effects of quercetin glycosides on glycine and 5-HT3A receptor channel activities are not well known. In the present study, we investigated the effects of quercetin glycosides on the human glycine alpha 1 receptor and mouse 5-HT3A receptor channel activities expressed in Xenopus oocytes using a two-electrode voltage clamp technique. In oocytes and 5-expressing glycine or 5-HT3A receptors, quercetin- or its glycosides-induced inhibitions on glycine-(I-Gly) and 5-HT-induced current (I5-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 hibited I5-HT in order of Rham2 >= quercetin > Rutin=Rham1. The inhibitions of I-Gly by quercetin glycosides were noncompetitive and voltage-sensitive, whereas the inhibitions of I5-HT by quercetin glycosides were competitive and voltage-insensitive manners. These results also indicate that quercetin glycosides might regulate the human glycine alpha 1 and mouse 5-HT3A receptors with differential manners. English PHARMACEUTICAL SOC JAPAN ACETYLCHOLINE-RECEPTOR 5-HT3 RECEPTOR FLAVONOIDS INHIBITION METABOLISM ABSORPTION FAMILY SITES BRAIN Differential regulations of quercetin and its glycosides on ligand-gated ion channels Article 10.1248/bpb.31.611 1 BIOLOGICAL & PHARMACEUTICAL BULLETIN, v.31, no.4, pp.611 - 617 BIOLOGICAL & PHARMACEUTICAL BULLETIN 31 4 611 617 scie scopus 000255503700015 2-s2.0-41849137308 Pharmacology & Pharmacy Pharmacology & Pharmacy Article ACETYLCHOLINE-RECEPTOR 5-HT3 RECEPTOR FLAVONOIDS INHIBITION METABOLISM ABSORPTION FAMILY SITES BRAIN flavonoid quercetin glycoside ligand-gated ion channel Xenopus oocyte