Cargando…

Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.

Multidrug resistance (MDR), caused by overexpression of either P-glycoprotein or the multidrug resistance protein (MRP), is characterised by a decreased cellular drug accumulation due to an enhanced drug efflux. In this study, we examined the effects of genistein and structurally related (iso)flavon...

Descripción completa

Detalles Bibliográficos
Autores principales: Versantvoort, C. H., Rhodes, T., Twentyman, P. R.
Formato: Texto
Lenguaje:English
Publicado: Nature Publishing Group 1996
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2074826/
https://www.ncbi.nlm.nih.gov/pubmed/8980395
_version_ 1782138050947579904
author Versantvoort, C. H.
Rhodes, T.
Twentyman, P. R.
author_facet Versantvoort, C. H.
Rhodes, T.
Twentyman, P. R.
author_sort Versantvoort, C. H.
collection PubMed
description Multidrug resistance (MDR), caused by overexpression of either P-glycoprotein or the multidrug resistance protein (MRP), is characterised by a decreased cellular drug accumulation due to an enhanced drug efflux. In this study, we examined the effects of genistein and structurally related (iso)flavonoids on the transport of rhodamine 123 (Rh123) and daunorubicin in the MRP-overexpressing MDR lung cancer cell lines COR-L23/R and MOR/R. Genistein, genistin, daidzein and quercetin showed major differences in effects on Rh123 vs daunorubicin transport in the MRP-mediated MDR cell lines: the accumulation of daunorubicin was increased, whereas the accumulation of Rh123 was decreased by the flavonoids. The depolarisation of the membrane potential caused by genistein might be involved in the acceleration of the efflux of Rh123 measured in the MRP-overexpressing cell lines. These observations should be taken into account when using fluorescent dyes as probes for determination of transporter activity as a measure of MDR.
format Text
id pubmed-2074826
institution National Center for Biotechnology Information
language English
publishDate 1996
publisher Nature Publishing Group
record_format MEDLINE/PubMed
spelling pubmed-20748262009-09-10 Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds. Versantvoort, C. H. Rhodes, T. Twentyman, P. R. Br J Cancer Research Article Multidrug resistance (MDR), caused by overexpression of either P-glycoprotein or the multidrug resistance protein (MRP), is characterised by a decreased cellular drug accumulation due to an enhanced drug efflux. In this study, we examined the effects of genistein and structurally related (iso)flavonoids on the transport of rhodamine 123 (Rh123) and daunorubicin in the MRP-overexpressing MDR lung cancer cell lines COR-L23/R and MOR/R. Genistein, genistin, daidzein and quercetin showed major differences in effects on Rh123 vs daunorubicin transport in the MRP-mediated MDR cell lines: the accumulation of daunorubicin was increased, whereas the accumulation of Rh123 was decreased by the flavonoids. The depolarisation of the membrane potential caused by genistein might be involved in the acceleration of the efflux of Rh123 measured in the MRP-overexpressing cell lines. These observations should be taken into account when using fluorescent dyes as probes for determination of transporter activity as a measure of MDR. Nature Publishing Group 1996-12 /pmc/articles/PMC2074826/ /pubmed/8980395 Text en https://creativecommons.org/licenses/by/4.0/This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/.
spellingShingle Research Article
Versantvoort, C. H.
Rhodes, T.
Twentyman, P. R.
Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.
title Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.
title_full Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.
title_fullStr Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.
title_full_unstemmed Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.
title_short Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.
title_sort acceleration of mrp-associated efflux of rhodamine 123 by genistein and related compounds.
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2074826/
https://www.ncbi.nlm.nih.gov/pubmed/8980395
work_keys_str_mv AT versantvoortch accelerationofmrpassociatedeffluxofrhodamine123bygenisteinandrelatedcompounds
AT rhodest accelerationofmrpassociatedeffluxofrhodamine123bygenisteinandrelatedcompounds
AT twentymanpr accelerationofmrpassociatedeffluxofrhodamine123bygenisteinandrelatedcompounds