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Quercetin increases the bioavailability of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in rats

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Author: Schutte, M.E. · Alink, G.M. · Freidig, A.P. · Spenkelink, B. · Vaessen, J.C.H. · Sandt, J.J.M. van de · Groten, J.P. · Rietjens, I.M.C.M.
Institution: TNO Kwaliteit van Leven · KvL
Source:Food and Chemical Toxicology, 11, 46, 3422-3428
Identifier: 241103
doi: doi:10.1016/j.fct.2008.08.015
Keywords: Biology · Biomedical Research · ABC transporters · Caco-2 monolayers · In silico modelling · PhIP · Quercetin · Rat · 2 amino 1 methyl 6 phenylimidazo[4,5 b]pyridine · quercetin · animal experiment · animal tissue · article · bioavailability · cell strain CACO 2 · computer model · controlled study · dietary intake · human · human cell · in vitro study · in vivo study · male · nonhuman · rat · Animals · Antioxidants · Area Under Curve · Biological Availability · Biological Transport, Active · Caco-2 Cells · Carcinogens · Humans · Imidazoles · Male · Models, Biological · Quercetin · Random Allocation · Rats · Rats, Wistar · Rattus


This study investigates whether the previous observation that quercetin increases the transport of PhIP through Caco-2 monolayers in vitro could be confirmed in an in vivo rat model. Co-administration of 1.45 μmol PhIP/kg bw and 30 μmol quercetin/kg bw significantly increased the blood AUC(0-8 h) of PhIP in rats to 131 ± 14% of the AUC(0-8 h) for rats dosed with PhIP alone. Significantly increased blood PhIP levels were detected at 15, 30, 45 and 180 min. At 4 and 8 h post-dosing a difference in the PhIP levels in the blood between the two treatment groups was no longer observed. In vitro and in silico modeling of PhIP transport using Caco-2 cells and a previously described kinetic model for PhIP transport revealed that the relative increase in PhIP transport caused by quercetin is dependent on the concentration of the two compounds. When substituting the PhIP and quercetin concentrations used in the in vivo experiment in the kinetic model, an effect of quercetin on PhIP transport was predicted that matches the actual effect of 131% observed in vivo. It is concluded that quercetin increases the bioavailability of the pro-carcinogen PhIP in rats pointing at a potential adverse effect of this supposed beneficial food ingredient. © 2008 Elsevier Ltd. All rights reserved. Chemicals / CAS: 2 amino 1 methyl 6 phenylimidazo[4,5 b]pyridine, 105650-23-5; quercetin, 117-39-5; 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine, 105650-23-5; Antioxidants; Carcinogens; Imidazoles; Quercetin, 117-39-5