Transport of quercetin di-sodium salt in the human intestinal epithelial Caco-2 cell monolayer 139.
Quercetin di-sodium salt (QDS), a water-soluble derivative of quercetin (Q), is a potent free radical scavenger. The aim of this study was to examine the in vitro intestinal transport of QDS compared to that of Q using the Caco-2 human intestinal epithelial cell line. The apical (A) to basolateral (B) transport of QDS was found to be higher than the B to A transport of this compound. This polarized transport involved the presence of a carrier protein system. The involvement of the sodium/glucose transporter-1 (SGLT-1) was shown by using phloridzin, a selective inhibitor of this conveyor system. However, the transport of Q was not affected by this inhibitor. Moreover, the influx of QDS was pH-sensitive and decreased at pH 5.5 compared with that observed at pH 7.4 and 6.5. The permeability of QDS was 10-fold higher than that of Q. This could be explained by the involvement of SLGT-1 and the absence of an active efflux pump in the absorption of QDS in comparison with Q. This finding was supported by comparing the solubility of Q with that of QDS. This study indicates that both the higher solubility of QDS and its dependence on the SGLT-1 transport system resulted in more efficient permeability compared to Q.
UMR CNRS/ULP 7175, LC1, Biomolécules, Biotechnologie et Innovation Thérapeutique, Université Louis Pasteur, France.
H A
HA
Milane
A
A
Al Ahmad
M
M
Naitchabane
T F
TF
Vandamme
L
L
Jung
G
G
Ubeaud
D000975:Antioxidants / Q000378:metabolism*; D001692:Biological Transport; D018938:Caco-2 Cells; D002414:Cations, Monovalent; D002463:Cell Membrane Permeability; D004847:Epithelial Cells / Q000378:metabolism; D016166:Free Radical Scavengers / Q000378:metabolism*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism*; D011794:Quercetin / Q000378:metabolism*; D012492:Salts / Q000378:metabolism; D012964:Sodium / Q000378:metabolism; D051269:Sodium-Glucose Transporter 1 / Q000378:metabolism; D012995:Solubility
D000975:Antioxidants; D002414:Cations, Monovalent; D016166:Free Radical Scavengers; D012492:Salts; D051269:Sodium-Glucose Transporter 1; D011794:Quercetin; D012964:Sodium