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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2001-2-9
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pubmed:abstractText |
We studied the effect of the antimalarial drug mefloquine on the resistance of K562 cells to doxorubicin. Mefloquine synergistically potentiated the cytotoxicity of doxorubicin for doxorubicin-resistant K562 cells (K562/DXR) at a concentration of 0.5-3 microM, but had hardly any synergistic effect in the parental cell line (K562) at the same concentration. Mefloquine was more potent than verapamil, a known modulator of multidrug-resistance. Since doxorubicin resistance in these cells is associated with the expression of high levels of P-glycoprotein, we evaluated the effect of mefloquine and of P-glycoprotein activity in cytofluorographic efflux experiments with the fluorescent dye rhodamine 123. Our results indicate that mefloquine inhibits the P-glycoprotein pump-efflux activity in a dose-related manner. Moreover, mefloquine reduces the expression of the immunoreactive P-glycoprotein in K562/DXR cells as evaluated by cytofluorimetric assay. Taken together, the results indicate that mefloquine reverses the multidrug-resistance phenotype through direct interaction with P-glycoprotein.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Affinity Labels,
http://linkedlifedata.com/resource/pubmed/chemical/Antibiotics, Antineoplastic,
http://linkedlifedata.com/resource/pubmed/chemical/Antimalarials,
http://linkedlifedata.com/resource/pubmed/chemical/Azides,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Coloring Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Dihydropyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Doxorubicin,
http://linkedlifedata.com/resource/pubmed/chemical/Mefloquine,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/Rhodamine 123,
http://linkedlifedata.com/resource/pubmed/chemical/Verapamil,
http://linkedlifedata.com/resource/pubmed/chemical/azidopine
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0379-0355
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
22
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
281-4
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:11031728-Affinity Labels,
pubmed-meshheading:11031728-Antibiotics, Antineoplastic,
pubmed-meshheading:11031728-Antimalarials,
pubmed-meshheading:11031728-Azides,
pubmed-meshheading:11031728-Binding, Competitive,
pubmed-meshheading:11031728-Calcium Channel Blockers,
pubmed-meshheading:11031728-Coloring Agents,
pubmed-meshheading:11031728-Dihydropyridines,
pubmed-meshheading:11031728-Doxorubicin,
pubmed-meshheading:11031728-Drug Resistance, Multiple,
pubmed-meshheading:11031728-Drug Resistance, Neoplasm,
pubmed-meshheading:11031728-Drug Synergism,
pubmed-meshheading:11031728-Humans,
pubmed-meshheading:11031728-Mefloquine,
pubmed-meshheading:11031728-P-Glycoprotein,
pubmed-meshheading:11031728-Phenotype,
pubmed-meshheading:11031728-Rhodamine 123,
pubmed-meshheading:11031728-Tumor Cells, Cultured,
pubmed-meshheading:11031728-Verapamil
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pubmed:year |
2000
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pubmed:articleTitle |
Enhancement of doxorubicin activity in multidrug-resistant cells by mefloquine.
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pubmed:affiliation |
Department of Pharmacology and Toxicology, Cancer Research Institute, Tohoku Pharmaceutical University, Sendai, Japan.
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pubmed:publicationType |
Journal Article
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