약학회지 (YAKHAK HOEJI)

  • 제57권2호
  • /
  • Pages.95-100
  • /
  • 2013
  • /
  • 0377-9556(pISSN)
  • /
  • 2383-9457(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

새로운 옥사졸리디논계 항균제 LCB01-0183의 항균 활성

Antimicrobial Activities of LCB01-0183, a New Oxazolidinone

  • 투고 : 2013.02.05
  • 심사 : 2013.04.01
  • 발행 : 2013.04.30
PDF 다운로드
⟨ 이전 논문 다음 논문 ⟩

초록

This study was performed to analyze in vitro and in vivo activities of LCB01-0183, a new oxazolidinone, against clinical isolates of bacteria. In vitro antibacterial activity of LCB01-0183 was tested by the two fold agar dilution method. In vivo activity of LCB01-0183 was determined against systemic infections in mice. LCB01-0183 showed most potent activity among the test compounds against clinical isolates of Gram-positive bacteria. Furthermore, the protective activity of LCB01-0183 was very effective against systemic infections in mice by oral or subcutaneous administration. In time kill study, LCB01-0183 showed a bacteriostatic activity during 24 hours. LCB01-0183 had potent in vitro and in vivo activity against Gram-positive bacteria including drug-resistant strains.

키워드

참고문헌

  1. Michael, A. F. and Christopher, T. W. : Antibiotics for emerging pathogens. Science 325, 1089 (2009). https://doi.org/10.1126/science.1176667
  2. Sreenivas, K., Amarnath, P. V. S., Mallik, A., Sarnaik, H., Selva Kumar, N., Takhi, M., Trehan, S., Sitaram Kumar, M., Iqbal, J., Rajagopalan, R. and Chakrabarti, R. : In vitro and in vivo antibacterial evaluation of DRF 8417, a new oxazolidinone. J. Antimicrob. Chemother. 60, 159 (2007). https://doi.org/10.1093/jac/dkm116
  3. Levy, S. B. and Marshall, B. : Antibacterial resistance worldwide: causes, challenges and responses. Nature. Med. 10, s122 (2004). https://doi.org/10.1038/nm1145
  4. Noskin, G. A., Siddiqui, F., Stosor, V., Hacek, D. and Peterson, L. R. : In vitro activities of linezolid against important Grampositive bacterial pathogens including vancomycin-resistant Enterococci. Antibicrob. Agents. Chemother. 43, 2059 (1999).
  5. Vara Prasad, J. V. : New oxazolidinones. Curr. Opin. Microbiol. 10, 454 (2007). https://doi.org/10.1016/j.mib.2007.08.001
  6. Swaney, S. M., Aoki, H., Ganoza, M. C. and Shinabarger, D. L. : The oxazolidinone linezollid inhibits initiation of protein synthesis in bacteria. Antimicrob. Agents. Chemother. 42, 3251 (1998).
  7. Gill, C. J., Abruzzo, G. K., Flattery, A. M., Misura, A. S., Bartizal, K. and Hickey, E. J. : In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection. Antimicrob. Agents. Chemother. 51, 3434 (2007). https://doi.org/10.1128/AAC.01567-06
  8. Lin, A. H., Murray, R. W., Vidamar, T. J. and Marotti, K. R. : The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob. Agents. Chemother. 41, 2127 (1997).
  9. Shaw, K. J., Poppe, S., Schaadt, R., Brown-Driver, V., Finn, J., Pillar, C. M., Shinabarger, D. and Zurenko, G. : In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains. Antimicrob. Agents. Chemother. 52, 4442 (2008). https://doi.org/10.1128/AAC.00859-08
  10. Leach, K. L., Swaney, S. M., Colca, J. R., McDonald, W. G., Blinn, J. R., Thomasco, L. M., Gadwood, R. C., Shinabarger, D., Xiong, L. and Mankin, A. S. : The site of action of oxazolidinone antibiotics in living bacteria and in human mitochondria. Mol. Cell. 26, 393 (2007). https://doi.org/10.1016/j.molcel.2007.04.005
  11. Moise, P. A., Forrest, A., Birmingham, M. C. and Schentag, J. J. : The efficacy and safety of linezolid as treatment for Staphylococcus aureus infections in compassionate use patients who are intolerant of, or who have failed to respond to vancomycin. J. Antimicrob. Chemother. 50, 1017 (2002). https://doi.org/10.1093/jac/dkf215
  12. Jones, R. N., Ross, J. E., Castanheira, M. and Mendes, R. E. : United States resistance surveillance results for linezolid (LEADER Program for 2007). Diagn. Microbiol. Infect. Dis. 62, 416 (2008). https://doi.org/10.1016/j.diagmicrobio.2008.10.010
  13. Meka, V. G. and Gold, H. S. : Antimicrobial resistance to linezolid. Clin. Infect. Dis. 39, 1010 (2004). https://doi.org/10.1086/423841
  14. Clinical and Laboratory Standards Institute (CLSI) : Performance Standards for Antimicrobial Susceptibility Testing; 21th Informational Supplement. CLSI Document M100-S22. CLSI, Wayne, PA (2012).
  15. Clinical and Laboratory Standards Institute (CLSI) : Methods for Determining Bactericidal Activity of Antimicrobial Agents. CLSI document M26-A. CLSI, Wayne, PA (1999).
  16. Bliss, C. I. : Statistics in bioassay. Academic Press, Inc., New York (1985).
  17. Spellberg, B., Powers, J. H., Brass, E. P., Miller, L. G. and Edwards, J. E. Jr. : Trends in antimicrobial drug development implications for the future. Clin. Infect. Dis. 38, 1279 (2004). https://doi.org/10.1086/420937
  18. Luh, K. T., Hsueh, P. R., Teng, L. J., Pan, H. J., Chen, Y. C., Lu, J. J., Wu, J. J. and Ho, S. W. : Quinupristin-dalfopristin resistance among Gram-positive bacteria in Taiwan. Antimicrob. Agents. Chemother. 44, 3374 (2004).
  19. Lobritz, M., Hutton-Thomas, R., Marshall, S. and Rice, L. B. : Recombination proficiency influences frequency and locus of mutational resistance to linezolid in Enterococcus faecalis. Antimicrob. Agents. Chemother. 47, 3318 (2003). https://doi.org/10.1128/AAC.47.10.3318-3320.2003
  20. Mendes, R. E., Deshpande, L. M., Castanheira, M., DiPersio, J., Saubolle, M. A. and Jones, R. N. : First report of cfrmediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States. Antimicrob. Agents. Chemother. 52, 2244 (2008). https://doi.org/10.1128/AAC.00231-08
  21. Diekema, D. J. and Jones, R. N. : Oxazolidinone antibiotics. Lancet 358, 1975 (2001). https://doi.org/10.1016/S0140-6736(01)06964-1