Print Email Facebook Twitter Quercetin increases the bioavailability of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in rats Title Quercetin increases the bioavailability of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in rats Author Schutte, M.E. Alink, G.M. Freidig, A.P. Spenkelink, B. Vaessen, J.C.H. van de Sandt, J.J.M. Groten, J.P. Rietjens, I.M.C.M. TNO Kwaliteit van Leven KvL Publication year 2008 Abstract 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 Subject BiologyBiomedical ResearchABC transportersCaco-2 monolayersIn silico modellingPhIPQuercetinRat2 amino 1 methyl 6 phenylimidazo[4,5 b]pyridinequercetinanimal experimentanimal tissuearticlebioavailabilitycell strain CACO 2computer modelcontrolled studydietary intakehumanhuman cellin vitro studyin vivo studymalenonhumanratAnimalsAntioxidantsArea Under CurveBiological AvailabilityBiological Transport, ActiveCaco-2 CellsCarcinogensHumansImidazolesMaleModels, BiologicalQuercetinRandom AllocationRatsRats, WistarRattus To reference this document use: http://resolver.tudelft.nl/uuid:cb55f0f3-31bf-4e4f-af43-64f4066e59a9 DOI https://doi.org/10.1016/j.fct.2008.08.015 TNO identifier 241103 ISSN 0278-6915 Source Food and Chemical Toxicology, 46 (11), 3422-3428 Document type article Files To receive the publication files, please send an e-mail request to TNO Library.