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Research ArticleArticle

Modulation of (–)-Epicatechin Metabolism by Coadministration with Other Polyphenols in Caco-2 Cell Model

Belén Sanchez-Bridge, Antoine Lévèques, Hequn Li, Emmanuelle Bertschy, Amaury Patin and Lucas Actis-Goretta
Drug Metabolism and Disposition January 2015, 43 (1) 9-16; DOI: https://doi.org/10.1124/dmd.114.060590
Belén Sanchez-Bridge
Nestlé Research Center, Nestec Ltd., Lausanne, Switzerland (B.S.B., A.L., E.B., A.P., L.A.G.); Division of Toxicology, Wageningen University, Tuinlaan, Wageningen, The Netherlands (H.L.)
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Antoine Lévèques
Nestlé Research Center, Nestec Ltd., Lausanne, Switzerland (B.S.B., A.L., E.B., A.P., L.A.G.); Division of Toxicology, Wageningen University, Tuinlaan, Wageningen, The Netherlands (H.L.)
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Hequn Li
Nestlé Research Center, Nestec Ltd., Lausanne, Switzerland (B.S.B., A.L., E.B., A.P., L.A.G.); Division of Toxicology, Wageningen University, Tuinlaan, Wageningen, The Netherlands (H.L.)
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Emmanuelle Bertschy
Nestlé Research Center, Nestec Ltd., Lausanne, Switzerland (B.S.B., A.L., E.B., A.P., L.A.G.); Division of Toxicology, Wageningen University, Tuinlaan, Wageningen, The Netherlands (H.L.)
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Amaury Patin
Nestlé Research Center, Nestec Ltd., Lausanne, Switzerland (B.S.B., A.L., E.B., A.P., L.A.G.); Division of Toxicology, Wageningen University, Tuinlaan, Wageningen, The Netherlands (H.L.)
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Lucas Actis-Goretta
Nestlé Research Center, Nestec Ltd., Lausanne, Switzerland (B.S.B., A.L., E.B., A.P., L.A.G.); Division of Toxicology, Wageningen University, Tuinlaan, Wageningen, The Netherlands (H.L.)
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Abstract

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.

Footnotes

    • Received August 12, 2014.
    • Accepted October 9, 2014.
  • The authors are (LAG, AL, MR) or were (HL) employees of Nestec Ltd., a subsidiary of Nestlé Ltd. that provides professional assistance, research, and consulting services for food, dietary, dietetic, and pharmaceutical products of interest to Nestlé Ltd. No other authors declare conflicts of interest. All authors read and approved the final manuscript.

  • dx.doi.org/10.1124/dmd.114.060590.

  • ↵Embedded ImageThis article has supplemental material available at dmd.aspetjournals.org.

  • Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 43 (1)
Drug Metabolism and Disposition
Vol. 43, Issue 1
1 Jan 2015
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Research ArticleArticle

Modulation of (–)-Epicatechin Metabolism

Belén Sanchez-Bridge, Antoine Lévèques, Hequn Li, Emmanuelle Bertschy, Amaury Patin and Lucas Actis-Goretta
Drug Metabolism and Disposition January 1, 2015, 43 (1) 9-16; DOI: https://doi.org/10.1124/dmd.114.060590

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Research ArticleArticle

Modulation of (–)-Epicatechin Metabolism

Belén Sanchez-Bridge, Antoine Lévèques, Hequn Li, Emmanuelle Bertschy, Amaury Patin and Lucas Actis-Goretta
Drug Metabolism and Disposition January 1, 2015, 43 (1) 9-16; DOI: https://doi.org/10.1124/dmd.114.060590
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