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Flavonoid-mediated inhibition of intestinal ABC transporters may affect the oral bioavailability of drugs, food-borne toxic compounds and bioactive ingredients

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Author: Brand, W. · Schutte, M.E. · Williamson, G. · Zanden, J.J. van · Cnubben, N.H.P. · Groten, J.P. · Bladeren, P.J. van · Rietjens, I.M.C.M.
Institution: TNO Kwaliteit van Leven
Source:Biomedicine and Pharmacotherapy, 9, 60, 508-519
Identifier: 239576
doi: doi:10.1016/j.biopha.2006.07.081
Keywords: Biology · Biomedical Research · ATP binding cassette (ABC) transport proteins · Flavonoids · Intestinal transcellular transport · Animals · ATP-Binding Cassette Transporters · Biological Availability · Biological Transport · Drug Resistance, Multiple · Flavonoids · Humans · Intestines


The transcellular transport of ingested food ingredients across the intestinal epithelial barrier is an important factor determining bioavailability upon oral intake. This transcellular transport of many chemicals, food ingredients, drugs or toxic compounds over the intestinal epithelium can be highly dependent on the activity of membrane bound ATP binding cassette (ABC) transport proteins, able to export the compounds from the intestinal cells. The present review describes the ABC transporters involved in the efflux of bioactive compounds from the intestinal cells, either to the basolateral blood side, facilitating absorption, or back into the intestinal lumen, reducing bioavailability. The role of the ABC transporters in intestinal transcellular uptake also implies a role for inhibitors of these transporters in modulation of the bioavailability upon oral uptake. The present paper focuses on the role of flavonoids as important modulators or substrates of intestinal ABC transport proteins. Several examples of such an effect of flavonoids are presented. It can be concluded that flavonoid-mediated inhibition of ABC transporters may affect the bioavailability of drugs, bioactive food ingredients and/or food-borne toxic compounds upon oral uptake. All together it appears that the flavonoid-mediated interactions at the level of the intestinal ABC transport proteins may be an important mechanism for unexpected food-drug, food-toxin or food-food interactions. The overview also indicates that future studies should focus on i) in vivo validation of the flavonoid-mediated effects on bioavailability of drugs, toxins and beneficial bioactive food ingredients detected in in vitro models, and on ii) the role of flavonoid phase II metabolism in modulating the activity of the flavonoids to act as ABC transporter inhibitors and/or substrates. © 2006 Elsevier Masson SAS. All rights reserved.