Structural effects of phenolic acids on the transepithelial transport of fluorescein in caco-2 cell monolayers.
The structural specificity of the monocarboxylic acid transporter (MCT) for the transport of phenolic acids was investigated by measuring the inhibitory effect on the fluorescein transport in Caco-2 cell monolayers. Although most of the monohydroxylated derivatives had an inhibitory effect, the di- and tri-hydroxylated ones did not. The methoxylated derivatives were more inhibitory than the hydroxylated ones in all the meta-substituted derivatives, suggesting that meta-hydroxylation of the substrate would decrease the affinity for MCT.
Konishi
Yutaka
Y
Applied Bioresearch Center, Research & Development Department, Kirin Brewery Co., Ltd., Gunma, Japan. konishiy@kirin.co.jp
Kubo
Kazuo
K
Shimizu
Makoto
M
D018938:Caco-2 Cells; D002463:Cell Membrane Permeability / Q000187:drug effects; D003373:Coumaric Acids / Q000737:chemistry / Q000494:pharmacology; D004847:Epithelial Cells / Q000378:metabolism*; D019793:Fluorescein / Q000493:pharmacokinetics*; D006801:Humans; D062385:Hydroxybenzoates / Q000737:chemistry* / Q000494:pharmacology*; D006900:Hydroxylation; D027501:Monocarboxylic Acid Transporters / Q000378:metabolism; D013329:Structure-Activity Relationship
D003373:Coumaric Acids; D062385:Hydroxybenzoates; D027501:Monocarboxylic Acid Transporters; C017616:phenolic acid; D019793:Fluorescein