title: Cellular uptake and efflux of trans-piceid and its aglycone trans-resveratrol on the apical membrane of human intestinal Caco-2 cells.
abstract: Two stilbenes (trans-piceid and its aglycone trans-resveratrol) were investigated in the uptake across the apical membrane of the human intestinal cell line Caco-2 in order to determine their mechanisms of transport. The uptake was quantified using a reverse phase high-performance liquid chromatography method with fluorescence detection. The rate of cellular accumulation in the cells was found to be higher for trans-resveratrol than for trans-piceid. In addition, trans-resveratrol uses passive transport to cross the apical membrane of the cells, whereas the transport of trans-piceid is likely active. With regard to the mechanisms of transport, the involvement of the active transporter SGLT1 in the absorption of trans-piceid was deduced using various inhibitors directly or indirectly exploiting the activity of this transporter (glucose, phlorizin, and ouabain). Moreover, we investigated the involvement of the multidrug-related protein 2 (MRP2), an efflux pump present on the apical membrane, in stilbene efflux by Caco-2 cells. The effect of MK-571 (an MRP inhibitor) seems to implicate MRP2 as responsible for apical efflux of trans-piceid and trans-resveratrol.
authors.affiliation: Groupe d'Etude des Substances Végétales à Activités Biologiques, EA 3675, UFR des Sciences Pharmaceutiques, Université de Bordeaux II, 146 rue Léo Saignat, 33076 Bordeaux Cedex, France.
authors.forename: Caroline
authors.initials: C
authors.lastname: Henry
authors.forename: Xavier
authors.initials: X
authors.lastname: Vitrac
authors.forename: Alain
authors.initials: A
authors.lastname: Decendit
authors.forename: Rachid
authors.initials: R
authors.lastname: Ennamany
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Krisa
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Mérillon
mesh_terms: D001692:Biological Transport; D018938:Caco-2 Cells; D002462:Cell Membrane / Q000378:metabolism*; D005960:Glucosides / Q000378:metabolism*; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism*; D007700:Kinetics; D008562:Membrane Glycoproteins / Q000378:metabolism; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins / Q000037:antagonists & inhibitors / Q000502:physiology; D009004:Monosaccharide Transport Proteins / Q000378:metabolism; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000037:antagonists & inhibitors / Q000502:physiology; D011422:Propionates / Q000494:pharmacology; D011804:Quinolines / Q000494:pharmacology; D000077185:Resveratrol; D051269:Sodium-Glucose Transporter 1; D013267:Stilbenes / Q000378:metabolism*
chemical_list: D005960:Glucosides; D008562:Membrane Glycoproteins; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins; D009004:Monosaccharide Transport Proteins; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D011422:Propionates; D011804:Quinolines; D000077185:Resveratrol; D051269:Sodium-Glucose Transporter 1; D013267:Stilbenes; C000715087:ABCC2 protein, human; C495674:SLC5A1 protein, human; C059141:verlukast; C058229:polydatin