Source:http://linkedlifedata.com/resource/pubmed/id/12532374
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2003-1-17
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pubmed:abstractText |
The purpose of this study was to identify the effects of dietary flavonoids, which are present in fruits, vegetables, and plant-derived beverages, on the transport of daunomycin (DNM) and vinblastine (VBL) in Panc-1 cells. Panc-1 is a human pancreatic adenocarcinoma cell line, which expresses Multidrug Resistance-Associated Protein1 (MRP1). The 2-h accumulation of (3)H-DNM and (3)H-VBL was determined in the presence and absence of 22 flavonoids. Biochanin-A, genistein, quercetin, chalcone, silymarin, phloretin, morin, and kaempferol, at 100 microM concentrations, all significantly increased the accumulation of both DNM and VBL in Panc-1 cells, with morin increasing DNM and VBL accumulation by 546 +/- 50% (mean +/- SE, n = 9) and 553 +/- 37% (n = 9), respectively. Fisetin treatment significantly decreased the accumulation of both DNM and VBL. Concentration-dependent studies demonstrated significant effects on VBL accumulation at 50 microM, but not at 10 microM concentrations, except for chalcone that was effective at a 10 microM concentration. Following a 24-h incubation, there were no changes in MRP1 membrane expression or glutathione-S-transferase activity in cells. Cellular glutathione (GSH) concentrations were significantly decreased following a 2-h incubation with biochanin A, chalcone, genistein, phloretin, quercetin, and silymarin, and following a 24-h incubation with biochanin A, chalcone, genistein, and phloretin. These results therefore indicate that the flavonoids morin, chalcone, silymarin, phloretin, genistein, quercetin, biochanin A, and kaempferol can inhibit MRP1-mediated drug transport, effects that may involve binding interactions with MRP1, as well as modulation of GSH concentrations.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antibiotics, Antineoplastic,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents, Phytogenic,
http://linkedlifedata.com/resource/pubmed/chemical/Ccl6 protein, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/Chemokines, CC,
http://linkedlifedata.com/resource/pubmed/chemical/Daunorubicin,
http://linkedlifedata.com/resource/pubmed/chemical/Flavonoids,
http://linkedlifedata.com/resource/pubmed/chemical/Glutathione,
http://linkedlifedata.com/resource/pubmed/chemical/Glutathione Transferase,
http://linkedlifedata.com/resource/pubmed/chemical/Neoplasm Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/Vinblastine
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-3549
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2003 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 92:250-257, 2003
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pubmed:issnType |
Print
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pubmed:volume |
92
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
250-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12532374-Antibiotics, Antineoplastic,
pubmed-meshheading:12532374-Antineoplastic Agents, Phytogenic,
pubmed-meshheading:12532374-Biological Transport, Active,
pubmed-meshheading:12532374-Blotting, Western,
pubmed-meshheading:12532374-Chemokines, CC,
pubmed-meshheading:12532374-Daunorubicin,
pubmed-meshheading:12532374-Flavonoids,
pubmed-meshheading:12532374-Glutathione,
pubmed-meshheading:12532374-Glutathione Transferase,
pubmed-meshheading:12532374-Humans,
pubmed-meshheading:12532374-Neoplasm Proteins,
pubmed-meshheading:12532374-P-Glycoprotein,
pubmed-meshheading:12532374-Tumor Cells, Cultured,
pubmed-meshheading:12532374-Vinblastine
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pubmed:year |
2003
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pubmed:articleTitle |
Effect of flavonoids on MRP1-mediated transport in Panc-1 cells.
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pubmed:affiliation |
Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, University at Buffalo, The State University of New York, 517 Hochstetter Hall, Amherst, New York 14260-1200, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, Non-U.S. Gov't
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