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Vol. 294, Issue 3, 830-836, September 2000
-Glucoside across
Human Intestinal Caco-2 Cell Monolayers by Apical Multidrug
Resistance-Associated Protein-21
Department of Cell and Molecular Pharmacology and Experimental
Therapeutics (R.A.W., G.E.L., T.W.) and Department of Cell Biology and
Anatomy (K.J.K.), Medical University of South Carolina, Charleston,
South Carolina
Although there is strong evidence to suggest that flavonoid consumption
is beneficial to human health, the extent to which flavonoids are
absorbed and the mechanisms involved are controversial. Contrary to
common dogma, we previously demonstrated that quercetin 4'-
-glucoside, the predominant form of the most abundant dietary flavonoid, quercetin, was not absorbed across Caco-2 cell monolayers. The aim of this study was to test the hypothesis that a specific efflux
transporter is responsible for this lack of absorption. Transport of
quercetin 4'--glucoside, alone or with inhibitors, was examined with
Caco-2 cell monolayers. In addition, subcellular localization of the
multidrug resistance-associated proteins MRP1 and MRP2 was examined by
immunofluorescent confocal microscopy. Efflux of quercetin
4'--glucoside, a saturable process, was not altered by verapamil, a
P-glycoprotein inhibitor, but was competitively inhibited by MK-571, an
MRP inhibitor. These data in combination with immunofluorescent
localization of MRP2 to the apical membrane support a role for MRP2 in
the intestinal transcellular efflux of quercetin 4'--glucoside.
These results suggest a role for MRP2 in the transport of a new class
of agents, dietary glucosides.
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