Cellular Uptake and Efflux of trans-Piceid and Its Aglycone trans-Resveratrol on the Apical Membrane of Human Intestinal Caco-2 Cells
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文摘
Two stilbenes (trans-piceid and its aglycone trans-resveratrol) were investigated in the uptake acrossthe apical membrane of the human intestinal cell line Caco-2 in order to determine their mechanismsof transport. The uptake was quantified using a reverse phase high-performance liquid chromatographymethod with fluorescence detection. The rate of cellular accumulation in the cells was found to behigher for trans-resveratrol than for trans-piceid. In addition, trans-resveratrol uses passive transportto cross the apical membrane of the cells, whereas the transport of trans-piceid is likely active. Withregard to the mechanisms of transport, the involvement of the active transporter SGLT1 in theabsorption of trans-piceid was deduced using various inhibitors directly or indirectly exploiting theactivity of this transporter (glucose, phlorizin, and ouabain). Moreover, we investigated the involvementof the multidrug-related protein 2 (MRP2), an efflux pump present on the apical membrane, in stilbeneefflux by Caco-2 cells. The effect of MK-571 (an MRP inhibitor) seems to implicate MRP2 asresponsible for apical efflux of trans-piceid and trans-resveratrol.Keywords: Caco-2 cells; trans-piceid; trans-resveratrol; apical transporters; SGLT1; MRP2

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