RT Journal Article
SR Electronic
T1 Modulation of (–)-Epicatechin Metabolism by Coadministration with Other Polyphenols in Caco-2 Cell Model
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 9
OP 16
DO 10.1124/dmd.114.060590
VO 43
IS 1
A1 Belén Sanchez-Bridge
A1 Antoine Lévèques
A1 Hequn Li
A1 Emmanuelle Bertschy
A1 Amaury Patin
A1 Lucas Actis-Goretta
YR 2015
UL http://dmd.aspetjournals.org/content/43/1/9.abstract
AB Widely consumed beverages such as red wine, tea, and cocoa-derived products are a great source of flavanols. Epidemiologic and interventional studies suggest that cocoa flavanols such as (–)-epicatechin may reduce the risk of cardiovascular diseases. The interaction of (–)-epicatechin with food components including other polyphenols could modify its absorption, metabolism, and finally its bioactivity. In the present study we investigate (–)-epicatechin absorption and metabolism when coexposed with other polyphenols in the intestinal absorptive Caco-2 cell model. Depending on the type of polyphenols coadministered, the total amount of 3′-O-methyl-epicatechin and 3′-O-sulfate-epicatechin conjugates found both in apical and basal compartments ranged from 19 to 801 nM and from 6 to 432 nM, respectively. The coincubation of (–)-epicatechin with flavanols, chlorogenic acid, and umbelliferone resulted in similar amounts of 3′-O-methyl-epicatechin effluxed into the apical compartment relative to control. Coincubation with isorhamnetin, kaempferol, diosmetin, nevadensin, chrysin, equol, genistein, and hesperitin promoted the transport of 3′-O-methyl-epicatechin toward the basolateral side and decreased the apical efflux. Quercetin and luteolin considerably inhibited the appearance of this (–)-epicatechin conjugate both in the apical and basolateral compartments. In conclusion, we could demonstrate that the efflux of (–)-epicatechin conjugates to the apical or basal compartments of Caco-2 cells is modulated by certain classes of polyphenols and their amount. Ingesting (–)-epicatechin with specific polyphenols could be a strategy to increase the bioavailability of (–)-epicatechin and to modulate its metabolic profile.