Molecular mechanisms of the naringin low uptake by intestinal Caco-2 cells

✍ Scribed by Franck Tourniaire; Meryl Hassan; Marc André; Odette Ghiringhelli; Christian Alquier; Marie-Josèphe Amiot

• Publisher: John Wiley and Sons
• Year: 2005
• Tongue: English
• Weight: 107 KB
• Volume: 49
• Category: Article
• ISSN: 1613-4125
• DOI: 10.1002/mnfr.200500088

✦ Synopsis

Naringin, the main flavanone of grapefruit, was reported to display numerous biological effects: antioxidant, hypocholesteremic, anti-atherogenic and favoring drug absorption. Naringin absorption mechanisms were studied in Caco-2 cells (TC7 clone). We investigated the possible involvement of several membrane transporters implicated in polyphenolic compounds intestinal transport (sodium-dependent glucose transporter 1, monocarboxylate transporter, multidrug-associated resistance proteins 1 and 2, and P-glycoprotein). Naringin was poorly absorbed by Caco-2 cells, according to its low value of apparent permeability coefficient (P(app) = 8.1 +/- 0.9 x 10(-8) cm/s). In the presence of verapamil, a specific inhibitor of P-glycoprotein, cellular uptake was increased by almost threefold after 5 min, and P(app) was doubled after 30 min. Our results indicated the involvement of P-glycoprotein, an ATP-driven efflux pump, capable of transporting naringin from the Caco-2 cell to the apical side. This phenomenon could explain, at least in part, the low absorption of this flavanone at the upper intestinal level.