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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.

Citation

K Terashi, M Oka, H Soda, M Fukuda, S Kawabata, K Nakatomi, K Shiozawa, T Nakamura, K Tsukamoto, Y Noguchi, M Suenaga, C Tei, S Kohno. Interactions of ofloxacin and erythromycin with the multidrug resistance protein (MRP) in MRP-overexpressing human leukemia cells. Antimicrobial agents and chemotherapy. 2000 Jun;44(6):1697-700

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PMID: 10817732

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