Journal of Antimicrobial Chemotherapy (1999) 43, 61-70
© 1999 The British Society for Antimicrobial Chemotherapy
Quinolone accumulation by Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coli
Antimicrobial Agents Research Group, Department of Infection, University of Birmingham, Edgbaston, Birmingham B15 2TT, UK
The accumulation of nalidixic acid and 14 fluoroquinolones over a range of external drug
concentrations (10–100 mg/L; c. 25–231 µM) into intact cells of Escherichia coli KL-16, Staphylococcus aureus NCTC 8532, Pseudomonas aeruginosa NCTC 10662 and spheroplasts of E. coli was
investigated. The effect of 100 µM carbonyl cyanide m-chlorophenyl hydrazone
(CCCP) upon the concentration of quinolone accumulated by intact cells and spheroplasts of E. coli was also determined. Except for pefloxacin, there was an increase in the
concentration of the six quinolones examined accumulated by E. coli, despite a
reduction in fluorescence at alkaline pH. For ciprofloxacin the partition coefficient (Papp) was constant despite an increase in the pH; however, the Papp for nalidixic acid decreased significantly with an increase in pH. The concentration of
nalidixic acid, ciprofloxacin and enrofloxacin accumulated by E. coli and S. aureus increased with an increase in temperature up to 40°C and 50°C, respectively.
Above these temperatures the cell viability decreased. With an increase in drug concentration
there was, for intact E. coli and 12/15 agents, and for S. aureus and 10/15
agents, a linear increase in the concentration of drug accumulated. However, for P.
aeruginosa and 13/15 agents there was apparent saturation of an accumulation pathway.
Assuming 100% accumulation into intact cells of E. coli, for 10/14
fluoroquinolones 
40% was accumulated by spheroplasts. CCCP increased the
concentration of quinolone accumulated but the increase varied with the agent and the bacterial
species. The variation in the effect of CCCP upon accumulation of the different quinolones into E. coli could result from chemical interactions or from different affinities of the
proposed efflux transporter for each quinolone. Overall, these data suggest that accumulation of
most quinolones into E. coli and S. aureus proceeds by simple diffusion, but
that P. aeruginosa behaves differently.
* Tel: +44-(0)21-414-6969; Fax: +44-(0)21-414-6966; E-mail: l.j.v.piddock{at}bham.ac.uk
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