Myricetin stimulates the absorption of the pro-carcinogen PhIP

The effect of the flavonoid myricetin on the transport of the pro-carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5- b]pyridine (PhIP) through differentiated Caco-2 monolayers, a model for the intestinal epithelium, is described. Myricetin causes an increase of the transport of PhIP from the apical to...

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Bibliographic Details
Published in:Cancer letters 2006-01, Vol.231 (1), p.36-42
Main Authors: Schutte, Maaike E., van de Sandt, Johannes J.M., Alink, Gerrit M., Groten, John P., Rietjens, Ivonne M.C.M.
Format: Article
Language:English
Subjects:
ABC transporter
ABC transporters
Absorption
apparent drug permeability
Apparent permeability
ATP-Binding Cassette Transporters - physiology
Caco-2
Caco-2 Cells
Carcinogens - pharmacokinetics
Cell culture
cells
Experiments
expression
Flavonoids - pharmacology
Humans
Imidazoles - pharmacokinetics
localization
Membrane Transport Proteins - metabolism
modulation
Multidrug Resistance-Associated Proteins - antagonists & inhibitors
Multidrug Resistance-Associated Proteins - metabolism
multidrug-resistance protein-1
mutagen
Myricetin
Permeability
PhIP
potentially anticarcinogenic flavonoids
Proteins
Studies
transport
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Summary:The effect of the flavonoid myricetin on the transport of the pro-carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5- b]pyridine (PhIP) through differentiated Caco-2 monolayers, a model for the intestinal epithelium, is described. Myricetin causes an increase of the transport of PhIP from the apical to the basolateral compartment. This effect was observed at physiologically relevant concentrations of PhIP and myricetin. Cyclosporin A (MRP2 inhibitor) but not PSC833 (P-gp inhibitor) showed a similar effect on PhIP transport. The results indicate that myricetin induces an increased basolateral uptake of the pro-carcinogen PhIP, in part through inhibition of the MRP2 mediated excretion of PhIP from the intestinal cells back to the lumen.
ISSN:0304-3835
1872-7980
DOI:10.1016/j.canlet.2005.01.020