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PMID: 17923487 Published · ppublish English Journal Article

Bactericidal action of daptomycin against stationary-phase and nondividing Staphylococcus aureus cells.

Antimicrobial agents and chemotherapy ·Vol. 51 ·No. 12 ·2007-12-00 ·Pages 4255-60

Mascio CT, Alder JD, Silverman JA

Abstract

Most antibiotics with bactericidal activity require that the bacteria be actively dividing to produce rapid killing. However, in many infections, such as endocarditis, prosthetic joint infections, and infected embedded catheters, the bacteria divide slowly or not at all. Daptomycin is a lipopeptide antibiotic with a distinct mechanism of action that targets the cytoplasmic membrane of gram-positive organisms, including Staphylococcus aureus. Daptomycin is rapidly bactericidal against exponentially growing bacteria (a 3-log reduction in 60 min). The objectives of this study were to determine if daptomycin is bactericidal against nondividing S. aureus and to quantify the extent of the bactericidal activity. In high-inoculum methicillin-sensitive S. aureus cultures in stationary phase (10(10) CFU/ml), daptomycin displayed concentration-dependent bactericidal activity, requiring 32 micro/ml to achieve a 3-log reduction. In a study comparing several antibiotics at 100 microg/ml, daptomycin demonstrated faster bactericidal activity than nafcillin, ciprofloxacin, gentamicin, and vancomycin. In experiments where bacterial cell growth was halted by the metabolic inhibitor carbonyl cyanide m-chlorophenylhydrazone or erythromycin, daptomycin (10 microg/ml) achieved the bactericidal end point (a 3-log reduction) within 2 h. In contrast, ciprofloxacin (10 microg/ml) did not produce bactericidal activity. Daptomycin (2 microg/ml) remained bactericidal against cold-arrested S. aureus, which was protected from the actions of ciprofloxacin and nafcillin. The data presented here suggest that, in contrast to that of other classes of antibiotics, the bactericidal activity of daptomycin does not require cell division or active metabolism, most likely as a consequence of its direct action on the bacterial membrane.

MeSH Terms
Anti-Bacterial Agents/pharmacology Cell Division/drug effects Ciprofloxacin/pharmacology Daptomycin/pharmacology Erythromycin/pharmacology Gentamicins/pharmacology Hydrazones/pharmacology Microbial Sensitivity Tests Nafcillin/pharmacology Staphylococcus aureus/drug effects,growth & development,metabolism Vancomycin/pharmacology
Chemicals
Anti-Bacterial Agents Gentamicins Hydrazones carbonyl 3-chlorophenylhydrazone Nafcillin Ciprofloxacin Erythromycin Vancomycin Daptomycin
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Mascio Carmela T M
Cubist Pharmaceuticals, Inc., 65 Hayden Avenue, Lexington, MA 02421,USA. carmela.mascio@cubist.com
Alder Jeff D
Silverman Jared A
References (30)
30 references, click to expand
  1. Bactericidal action of ofloxacin, sulbactam-ampicillin, rifampin, and isoniazid on logarithmic- and stationary-phase cultures of Mycobacterium tuberculosis.
    Antimicrob Agents Chemother. 1996 Oct;40(10):2296-9 PMID: 8891133
  2. Detachment characteristics and oxacillin resistance of Staphyloccocus aureus biofilm emboli in an in vitro catheter infection model.
    J Bacteriol. 2004 Jul;186(14):4486-91 PMID: 15231780
  3. Differential antibiotic susceptibilities of starved Mycobacterium tuberculosis isolates.
    Antimicrob Agents Chemother. 2005 Nov;49(11):4778-80 PMID: 16251329
  4. Bacterial biofilms: from the natural environment to infectious diseases.
    Nat Rev Microbiol. 2004 Feb;2(2):95-108 PMID: 15040259
  5. Inhibition of membrane potential-dependent amino acid transport by daptomycin.
    Antimicrob Agents Chemother. 1991 Dec;35(12):2639-42 PMID: 1687346
  6. In vitro pharmacodynamic effects of concentration, pH, and growth phase on serum bactericidal activities of daptomycin and vancomycin.
    Antimicrob Agents Chemother. 1992 Dec;36(12):2709-14 PMID: 1336344
  7. Growth cycle-induced changes in sensitivity of Staphylococcus aureus to bactericidal lipids from abscesses.
    J Med Microbiol. 1993 Jul;39(1):58-63 PMID: 8326513
  8. Mechanisms of antimicrobial resistance in bacteria.
    Am J Med. 2006 Jun;119(6 Suppl 1):S3-10; discussion S62-70 PMID: 16735149
  9. In vitro bactericidal activities of daptomycin against Staphylococcus aureus and Enterococcus faecalis are not mediated by inhibition of lipoteichoic acid biosynthesis.
    Antimicrob Agents Chemother. 2003 Aug;47(8):2682-4 PMID: 12878541
  10. Daptomycin versus standard therapy for bacteremia and endocarditis caused by Staphylococcus aureus.
    N Engl J Med. 2006 Aug 17;355(7):653-65 PMID: 16914701
  11. Daptomycin disrupts membrane potential in growing Staphylococcus aureus.
    Antimicrob Agents Chemother. 1991 Nov;35(11):2282-7 PMID: 1666494
  12. Lipoteichoic acid as a new target for activity of antibiotics: mode of action of daptomycin (LY146032).
    Antimicrob Agents Chemother. 1990 Jun;34(6):1220-6 PMID: 2168145
  13. In vitro bactericidal activity of daptomycin against staphylococci.
    J Antimicrob Chemother. 2002 Mar;49(3):467-70 PMID: 11864946
  14. In vitro activity of tigecycline against Staphylococcus epidermidis growing in an adherent-cell biofilm model.
    Antimicrob Agents Chemother. 2003 Dec;47(12):3967-9 PMID: 14638511
  15. Staphylococcus aureus aconitase inactivation unexpectedly inhibits post-exponential-phase growth and enhances stationary-phase survival.
    Infect Immun. 2002 Nov;70(11):6373-82 PMID: 12379717
  16. Structural transitions as determinants of the action of the calcium-dependent antibiotic daptomycin.
    Chem Biol. 2004 Jul;11(7):949-57 PMID: 15271353
  17. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032.
    Antimicrob Agents Chemother. 1987 Jul;31(7):1093-9 PMID: 2821889
  18. In vitro activities of daptomycin against 2,789 clinical isolates from 11 North American medical centers.
    Antimicrob Agents Chemother. 2001 Jun;45(6):1919-22 PMID: 11353654
  19. Fluorescence indicates a calcium-dependent interaction between the lipopeptide antibiotic LY146032 and phospholipid membranes.
    Biochemistry. 1988 Jun 28;27(13):4639-45 PMID: 2844233
  20. Bactericidal mechanism of gatifloxacin compared with other quinolones.
    J Antimicrob Chemother. 2002 Jan;49(1):185-8 PMID: 11751786
  21. The role of acyl chain character and other determinants on the bilayer activity of A21978C an acidic lipopeptide antibiotic.
    Biochim Biophys Acta. 1986 Jul 24;859(2):219-26 PMID: 3730378
  22. Activity of daptomycin against Gram-positive pathogens: a comparison with other agents and the determination of a tentative breakpoint.
    J Antimicrob Chemother. 2001 Oct;48(4):563-7 PMID: 11581239
  23. Roles of ribosomal binding, membrane potential, and electron transport in bacterial uptake of streptomycin and gentamicin.
    Antimicrob Agents Chemother. 1983 Jun;23(6):835-45 PMID: 6351731
  24. Mode of action of the new antibiotic for Gram-positive pathogens daptomycin: comparison with cationic antimicrobial peptides and lipopeptides.
    Biochim Biophys Acta. 2006 Sep;1758(9):1215-23 PMID: 16615993
  25. Role of nutrient limitation and stationary-phase existence in Klebsiella pneumoniae biofilm resistance to ampicillin and ciprofloxacin.
    Antimicrob Agents Chemother. 2003 Apr;47(4):1251-6 PMID: 12654654
  26. Increased killing of staphylococci and streptococci by daptomycin compared with cefazolin and vancomycin in an in vitro peritoneal dialysate model.
    Antimicrob Agents Chemother. 2003 Dec;47(12):3764-7 PMID: 14638479
  27. Correlation of daptomycin bactericidal activity and membrane depolarization in Staphylococcus aureus.
    Antimicrob Agents Chemother. 2003 Aug;47(8):2538-44 PMID: 12878516
  28. The stationary phase of the bacterial life cycle.
    Annu Rev Microbiol. 1993;47:855-74 PMID: 8257118
  29. Staphylococcus aureus ClpC is required for stress resistance, aconitase activity, growth recovery, and death.
    J Bacteriol. 2005 Jul;187(13):4488-96 PMID: 15968059
  30. Biofilms: survival mechanisms of clinically relevant microorganisms.
    Clin Microbiol Rev. 2002 Apr;15(2):167-93 PMID: 11932229
Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
Published
2007-12-00
Epub
2007-00-08
Pages
4255-60
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC2167999
Subset
IM
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