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Flavonoid dimers are highly potent killers of multidrug resistant cancer cells overexpressing MRP1.

Abstract：

:MRP1 overexpression in multidrug-resistant cancer cells has been shown to be responsible for collateral sensitivity to some flavonoids that stimulate a huge MRP1-mediated GSH efflux. This massive GSH depletion triggers the death of these cancer cells. We describe here that bivalent flavonoid dimers strikingly stimulate such MRP1-mediated GSH efflux and trigger a 50-100 fold more potent cell death than their corresponding monomers. This selective and massive cell death of MRP1-overexpressing cells (both transfected and drug-selected cell lines) is no longer observed either upon catalytic inactivation of MRP1 or its knockdown by siRNA. The best flavonoid dimer, 4e, kills MRP1-overexpressing cells with a selective ratio higher than 1000 compared to control cells and an EC50 value of 0.1 μM, so far unequaled as a collateral sensitivity agent targeting ABC transporters. This result portends the flavonoid dimer 4e as a very promising compound to appraise in vivo the therapeutic potential of collateral sensitivity for eradication of MRP1-overexpressing chemoresistant cancer cells in tumors.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Dury L,Nasr R,Lorendeau D,Comsa E,Wong I,Zhu X,Chan KF,Chan TH,Chow L,Falson P,Di Pietro A,Baubichon-Cortay H

doi

10.1016/j.bcp.2016.10.013

subject

Has Abstract

pub_date

2017-01-15 00:00:00

pages

10-18

eissn

0006-2952

issn

1873-2968

pii

S0006-2952(16)30382-3

journal_volume

124

pub_type

杂志文章

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