Abstract
To investigate interactions between the multidrug resistance protein (MRP) and antimicrobial agents, we examined the effects of 12 agents on vincristine sensitivity and efflux of the calcein acetoxy-methyl ester (calcein-AM) of a MRP substrate in MRP-overexpressing cells. Only ofloxacin and erythromycin enhanced sensitivity with increased intracellular vincristine accumulation and inhibited the calcein-AM efflux. Our findings suggest that the two agents are possible MRP substrates and may competitively inhibit MRP function as a drug efflux pump.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
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Antineoplastic Agents, Phytogenic / pharmacology*
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Antineoplastic Agents, Phytogenic / therapeutic use
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Drug Interactions*
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Erythromycin / pharmacology*
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Erythromycin / therapeutic use
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Fluoresceins / metabolism
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Genes, MDR*
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Humans
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Leukemia / drug therapy*
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Leukemia / genetics
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Leukemia / metabolism
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Ofloxacin / pharmacology*
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Ofloxacin / therapeutic use
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Tumor Cells, Cultured
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Vincristine / pharmacology*
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Vincristine / therapeutic use
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antineoplastic Agents, Phytogenic
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Fluoresceins
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Vincristine
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Erythromycin
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Ofloxacin
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fluorexon