Skip Navigation


JAC Advance Access originally published online on February 24, 2005
Journal of Antimicrobial Chemotherapy 2005 55(4):511-517; doi:10.1093/jac/dki059
This Article
Right arrow Full Text Freely available
Right arrow FREE Full Text (PDF) Freely available
Right arrow All Versions of this Article:
55/4/511    most recent
dki059v1
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in ISI Web of Science
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrow Search for citing articles in:
ISI Web of Science (21)
Right arrowRequest Permissions
Right arrow Disclaimer
Google Scholar
Right arrow Articles by Seral, C.
Right arrow Articles by Van Bambeke, F.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Seral, C.
Right arrow Articles by Van Bambeke, F.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

© The Author 2005. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions{at}oupjournals.org

Comparative activity of quinolones (ciprofloxacin, levofloxacin, moxifloxacin and garenoxacin) against extracellular and intracellular infection by Listeria monocytogenes and Staphylococcus aureus in J774 macrophages

C. Seral{dagger}, M. Barcia-Macay, M. P. Mingeot-Leclercq, P. M. Tulkens and F. Van Bambeke*

Unité de pharmacologie cellulaire et moléculaire, Université catholique de Louvain, Brussels, Belgium

* Corresponding author. Tel: +32-2-764-73-78; Fax: +32-2-764-73-73; Email: vanbambeke{at}facm.ucl.ac.be

Objectives: Quinolones accumulate in eukaryotic cells and show activity against a large array of intracellular organisms, but systematic studies aimed at examining their pharmacodynamic profile against intracellular bacteria are scarce. The present work aims at comparing intracellular-to-extracellular activities in this context.

Methods: We assessed the activities of ciprofloxacin, levofloxacin, moxifloxacin and garenoxacin against the extracellular (broth) and intracellular (infected J774 macrophages) forms of Listeria monocytogenes (cytosolic infection) and Staphylococcus aureus (phagolysosomal infection) using a range of clinically meaningful extracellular concentrations (0.06–4 mg/L).

Results: All four quinolones displayed concentration-dependent bactericidal activity against extracellular and intracellular L. monocytogenes and S. aureus for extracellular concentrations in the range 1–4-fold their MIC. Compared at equipotent extracellular concentrations, intracellular activities against L. monocytogenes were roughly equal to those that were extracellular, but were 50–100 times lower against S. aureus. Because quinolones accumulate in cells (ciprofloxacin, ~3 times; levofloxacin, ~5 times; garenoxacin, ~10 times, moxifloxacin, ~13 times), these data show that, intracellularly, quinolones are 5–10 times less potent against L. monocytogenes (P=0.065 [ANCOVA]), and at least 100 times less potent (P < 0.0001) against S. aureus. Because of their lower MICs and higher accumulation levels, garenoxacin and moxifloxacin were, however, more active than ciprofloxacin and levofloxacin when compared at similar extracellular concentrations.

Conclusions: Quinolone activity is reduced intracellulary. This suggests that either only a fraction of cell-associated quinolones exert an antibacterial effect, or that intracellular activity is defeated by the local environment, or that intracellular bacteria only poorly respond to the action of quinolones.

Keywords: cellular pharmacodynamics , cellular pharmacokinetics , bactericidal activity , accumulation


Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?


This article has been cited by other articles:


Home page
 J Antimicrob ChemotherHome page
S. Lemaire, F. Van Bambeke, P. C. Appelbaum, and P. M. Tulkens
Cellular pharmacokinetics and intracellular activity of torezolid (TR-700): studies with human macrophage (THP-1) and endothelial (HUVEC) cell lines
J. Antimicrob. Chemother., November 1, 2009; 64(5): 1035 - 1043.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
B. Marquez, N. E. Caceres, M.-P. Mingeot-Leclercq, P. M. Tulkens, and F. Van Bambeke
Identification of the Efflux Transporter of the Fluoroquinolone Antibiotic Ciprofloxacin in Murine Macrophages: Studies with Ciprofloxacin-Resistant Cells
Antimicrob. Agents Chemother., June 1, 2009; 53(6): 2410 - 2416.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
S. Van de Velde, H. A. Nguyen, F. Van Bambeke, P. M. Tulkens, J. Grellet, V. Dubois, C. Quentin, and M.-C. Saux
Contrasting effects of human THP-1 cell differentiation on levofloxacin and moxifloxacin intracellular accumulation and activity against Staphylococcus aureus and Listeria monocytogenes
J. Antimicrob. Chemother., September 1, 2008; 62(3): 518 - 521.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
A. Lismond, P. M. Tulkens, M.-P. Mingeot-Leclercq, P. Courvalin, and F. Van Bambeke
Cooperation between Prokaryotic (Lde) and Eukaryotic (MRP) Efflux Transporters in J774 Macrophages Infected with Listeria monocytogenes: Studies with Ciprofloxacin and Moxifloxacin
Antimicrob. Agents Chemother., September 1, 2008; 52(9): 3040 - 3046.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
S. Grayo, M.-C. Lott-Desroches, O. Dussurget, R. Respaud, A. Fontanet, O. Join-Lambert, E. Singlas, and A. Le Monnier
Rapid Eradication of Listeria monocytogenes by Moxifloxacin in a Murine Model of Central Nervous System Listeriosis
Antimicrob. Agents Chemother., September 1, 2008; 52(9): 3210 - 3215.
[Abstract] [Full Text] [PDF]

Home page
 The Annals of PharmacotherapyHome page
C. McPherson, P. Gal, and J L. Ransom
Treatment of Citrobacter koseri Infection with Ciprofloxacin and Cefotaxime in a Preterm Infant
Ann. Pharmacother., July 1, 2008; 42(7): 1134 - 1138.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
S. Grayo, O. Join-Lambert, M. C. Desroches, and A. Le Monnier
Comparison of the In Vitro Efficacies of Moxifloxacin and Amoxicillin against Listeria monocytogenes
Antimicrob. Agents Chemother., May 1, 2008; 52(5): 1697 - 1702.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
O. R. Sipahi, T. Turhan, H. Pullukcu, S. Calik, M. Tasbakan, H. Sipahi, B. Arda, T. Yamazhan, and S. Ulusoy
Moxifloxacin versus ampicillin + gentamicin in the therapy of experimental Listeria monocytogenes meningitis
J. Antimicrob. Chemother., March 1, 2008; 61(3): 670 - 673.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
S. J. Dancer
The effect of antibiotics on methicillin-resistant Staphylococcus aureus
J. Antimicrob. Chemother., February 1, 2008; 61(2): 246 - 253.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
M. W. Valderas and W. W. Barrow
Establishment of a method for evaluating intracellular antibiotic efficacy in Brucella abortus-infected Mono Mac 6 monocytes
J. Antimicrob. Chemother., January 1, 2008; 61(1): 128 - 134.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
S. Lemaire, F. Van Bambeke, M.-P. Mingeot-Leclercq, and P. M. Tulkens
Modulation of the Cellular Accumulation and Intracellular Activity of Daptomycin towards Phagocytized Staphylococcus aureus by the P-Glycoprotein (MDR1) Efflux Transporter in Human THP-1 Macrophages and Madin-Darby Canine Kidney Cells
Antimicrob. Agents Chemother., August 1, 2007; 51(8): 2748 - 2757.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
H. A. Nguyen, J. Grellet, V. Dubois, M.-C. Saux, and C. Quentin
Factors compromising the activity of moxifloxacin against intracellular Staphylococcus aureus
J. Antimicrob. Chemother., April 1, 2007; 59(4): 755 - 758.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
J. Le Carrou, M. Laurentie, M. Kobisch, and A. V. Gautier-Bouchardon
Persistence of Mycoplasma hyopneumoniae in Experimentally Infected Pigs after Marbofloxacin Treatment and Detection of Mutations in the parC Gene.
Antimicrob. Agents Chemother., June 1, 2006; 50(6): 1959 - 1966.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
H. A. Nguyen, J. Grellet, D. Paillard, V. Dubois, C. Quentin, and M.-C. Saux
Factors influencing the intracellular activity of fluoroquinolones: a study using levofloxacin in a Staphylococcus aureus THP-1 monocyte model
J. Antimicrob. Chemother., May 1, 2006; 57(5): 883 - 890.
[Abstract] [Full Text] [PDF]

Home page
 Antimicrob. Agents Chemother.Home page
M. Barcia-Macay, C. Seral, M.-P. Mingeot-Leclercq, P. M. Tulkens, and F. Van Bambeke
Pharmacodynamic Evaluation of the Intracellular Activities of Antibiotics against Staphylococcus aureus in a Model of THP-1 Macrophages
Antimicrob. Agents Chemother., March 1, 2006; 50(3): 841 - 851.
[Abstract] [Full Text] [PDF]


Disclaimer: Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.