Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Screening of an Inhibitor of the Tetracycline Efflux Pump is a Tetracycline-Resistant Clinical-Isolate of Staphylococcus aureus 743
Takahiro HIRATARumi WAKATABEJoergen NIELSENTomoko SATOHShin-ichi NIHIRAAkihito YAMAGUCHI
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1998 Volume 21 Issue 7 Pages 678-681

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Abstract

Clinically-isolated methicillin-resistant Staphylococcus aureus (MRSA) strain 743 exhibited resistance to tetracycline as judged from the active efflux of the drug. The efflux of tetracycline was inhibited by an uncoupler, carbonyl cyanide m-chlorophenylhydrazone (CCCP), and minocycline. Inhibitors of the efflux pump were examined in this strain to determine the cellular accumulation of tetracycline. Out of seven compounds examined, three caused a significant increase in the cellular concentration of tetracycline by inhibiting the efflux pump. Two of them seem to be energy inhibitors. Ro 07-3149 inhibited the efflux pump without affecting the energy state, and exhibited very low antibacterial activity but showed weak synergy with tetracycline.

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© The Pharmaceutical Society of Japan
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