Staff Publications

Staff Publications

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    'Staff publications' is the digital repository of Wageningen University & Research

    'Staff publications' contains references to publications authored by Wageningen University staff from 1976 onward.

    Publications authored by the staff of the Research Institutes are available from 1995 onwards.

    Full text documents are added when available. The database is updated daily and currently holds about 240,000 items, of which 72,000 in open access.

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Record number 370256
Title The effect of quercetin phase II metabolism on its MRP1 and MRP2 inhibiting potential
Author(s) Zanden, J.J. van; Woude, H. van der; Vaessen, J.; Usta, M.; Wortelboer, H.M.; Cnubben, N.H.P.; Rietjens, I.M.C.M.
Source Biochemical Pharmacology 74 (2007)2. - ISSN 0006-2952 - p. 345 - 351.
DOI https://doi.org/10.1016/j.bcp.2007.04.002
Department(s) Sub-department of Toxicology
VLAG
Publication type Refereed Article in a scientific journal
Publication year 2007
Keyword(s) multidrug-resistance protein - glycoprotein-mediated transport - dietary flavonoids - abc transporters - p-glycoprotein - drug-resistance - cell-line - modulation - plant - identification
Abstract The present study characterises the effect of phase II metabolism, especially methylation and glucuronidation, of the model flavonoid quercetin on its capacity to inhibit human MRP1 and MRP2 activity in Sf9 inside-out vesicles. The results obtained reveal that 3¿-O-methylation does not affect the MRP inhibitory potential of quercetin. However, 4¿-O-methylation appeared to reduce the potential to inhibit both MRP1 and MRP2. In contrast, glucuronidation in general, and especially glucuronidation at the 7-hydroxylmoiety, resulting in 7-O-glucuronosyl quercetin, significantly increased the potential of quercetin to inhibit MRP1 and MRP2 mediated calcein transport with inhibition of MRP1 being generally more effective than that of MRP2. Overall, the results of this study reveal that the major phase II metabolites of quercetin are equally potent or even better inhibitors of human MRP1 and MRP2 than quercetin itself. This finding indicates that phase II metabolism of quercetin could enhance the potential use of quercetin- or flavonoids in general¿as an inhibitor to overcome MRP-mediated multidrug resistance.
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