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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...
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Formato: | Texto |
Lenguaje: | English |
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Nature Publishing Group
1996
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2074826/ https://www.ncbi.nlm.nih.gov/pubmed/8980395 |
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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 |
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