Regulation of the 5-HT3A receptor-mediated current by alkyl 4-hydroxybenzoates isolated from the seeds of Nelumbo nucifera.
Four known alkyl 4-hydroxybenzoates, i.e., methyl 4-hydroxybenzoate (1), ethyl 4-hydroxybenzoate (2), propyl 4-hydroxybenzoate (3), and butyl 4-hydroxybenzoate (4), were isolated from the seeds of Nelumbo nucifera Gaertner (Nymphaeaceae) for the first time. The structures of the isolates were identified by 1D- and 2D-NMR spectroscopy and comparison with published values. The compounds were evaluated for their effects on the 5-HT-stimulated inward current (I(5-HT)) mediated by the human 5-HT(3)A receptors expressed in Xenopus oocytes. Compounds 1 and 2 enhanced the I(5-HT), but 4 reduced it. These results indicate that 4 is an inhibitor of the 5-HT(3)A receptors expressed in Xenopus oocytes.
Youn
Ui Joung
UJ
The Center for Cell Signaling & Drug Discovery Research, College of Pharmacy, Ewha Womans University, Seoul, Korea. yuny@ewha.ac.kr
Lee
Jun-Ho
JH
Lee
Yoo Jin
YJ
Nam
Joo Won
JW
Bae
Hyunsu
H
Seo
Eun-Kyoung
EK
D000818:Animals; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D006801:Humans; D062385:Hydroxybenzoates / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects*; D015394:Molecular Structure; D031653:Nelumbo / Q000737:chemistry*; D009865:Oocytes / Q000378:metabolism; D044406:Receptors, Serotonin, 5-HT3 / Q000235:genetics / Q000378:metabolism*; D012639:Seeds / Q000737:chemistry; D058827:Serotonin 5-HT3 Receptor Agonists / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D058831:Serotonin 5-HT3 Receptor Antagonists / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014162:Transfection; D014982:Xenopus laevis
D062385:Hydroxybenzoates; D044406:Receptors, Serotonin, 5-HT3; D058827:Serotonin 5-HT3 Receptor Agonists; D058831:Serotonin 5-HT3 Receptor Antagonists