PT  - JOURNAL ARTICLE
AU  - Belén Sanchez-Bridge
AU  - Antoine Lévèques
AU  - Hequn Li
AU  - Emmanuelle Bertschy
AU  - Amaury Patin
AU  - Lucas Actis-Goretta
TI  - Modulation of (–)-Epicatechin Metabolism by Coadministration with Other Polyphenols in Caco-2 Cell Model
AID  - 10.1124/dmd.114.060590
DP  - 2015 Jan 01
TA  - Drug Metabolism and Disposition
PG  - 9--16
VI  - 43
IP  - 1
4099  - http://dmd.aspetjournals.org/content/43/1/9.short
4100  - http://dmd.aspetjournals.org/content/43/1/9.full
SO  - Drug Metab Dispos2015 Jan 01; 43
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.