Abstract
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.
MeSH terms
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Animals
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Cells, Cultured
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Dose-Response Relationship, Drug
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Humans
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Hydroxybenzoates / chemistry
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Hydroxybenzoates / isolation & purification
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Hydroxybenzoates / pharmacology*
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Membrane Potentials / drug effects*
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Molecular Structure
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Nelumbo / chemistry*
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Oocytes / metabolism
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Receptors, Serotonin, 5-HT3 / genetics
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Receptors, Serotonin, 5-HT3 / metabolism*
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Seeds / chemistry
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Serotonin 5-HT3 Receptor Agonists / chemistry
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Serotonin 5-HT3 Receptor Agonists / isolation & purification
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Serotonin 5-HT3 Receptor Agonists / pharmacology*
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Serotonin 5-HT3 Receptor Antagonists / chemistry
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Serotonin 5-HT3 Receptor Antagonists / isolation & purification
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Serotonin 5-HT3 Receptor Antagonists / pharmacology*
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Structure-Activity Relationship
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Transfection
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Xenopus laevis
Substances
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Hydroxybenzoates
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Receptors, Serotonin, 5-HT3
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Serotonin 5-HT3 Receptor Agonists
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Serotonin 5-HT3 Receptor Antagonists