Coffee induces breast cancer resistance protein expression in Caco-2 cells

Marina Isshiki, Kazuo Umezawa, Hiroomi Tamura

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)


Coffee is a beverage that is consumed world-wide on a daily basis and is known to induce a series of metabolic and pharmacological effects, especially in the digestive tract. However, little is known concerning the effects of coffee on transporters in the gastrointestinal tract. To elucidate the effect of coffee on intestinal transporters, we investigated its effect on expression of the breast cancer resistance protein (BCRP/ABCG2) in a human colorectal cancer cell line, Caco-2. Coffee induced BCRP gene expression in Caco-2 cells in a coffee-dose dependent manner. Coffee treatment of Caco-2 cells also increased the level of BCRP protein, which corresponded to induction of gene expression, and also increased cellular efflux activity, as judged by Hoechst33342 accumulation. None of the major constituents of coffee tested could induce BCRP gene expression. The constituent of coffee that mediated this induction was extractable with ethyl acetate and was produced during the roasting process. Dehydromethylepoxyquinomicin (DHMEQ), an inhibitor of nuclear factor (NF)-κB, inhibited coffee-mediated induction of BCRP gene expression, suggesting involvement of NF-κB in this induction. Our data suggest that daily consumption of coffee might induce BCRP expression in the gastrointestinal tract and may affect the bioavailability of BCRP substrates.

Original languageEnglish
Pages (from-to)1624-1627
Number of pages4
JournalBiological and Pharmaceutical Bulletin
Issue number10
Publication statusPublished - 2011 Oct


  • Breast cancer resistance protein
  • Caco-2
  • Coffee
  • Nuclear factor κB

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science


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