This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Right arrowReprints and Permissions
Right arrow Copyright Information
Right arrow Books from ASM Press
Right arrow MicrobeWorld
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Takei, M.
Right arrow Articles by Oomori, Y.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Takei, M.
Right arrow Articles by Oomori, Y.

 Previous Article  |  Next Article 

Antimicrobial Agents and Chemotherapy, October 1998, p. 2678-2681, Vol. 42, No. 10
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.

Inhibitory Activities of Gatifloxacin (AM-1155), a Newly Developed Fluoroquinolone, against Bacterial and Mammalian Type II Topoisomerases

Masaya Takei,* Hideyuki Fukuda, Tokutaro Yasue, Masaki Hosaka, and Yasuo Oomori

Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd., Nogi, Tochigi 329-0114, Japan

Received 18 March 1998/Returned for modification 10 June 1998/Accepted 7 August 1998

We determined the inhibitory activities of gatifloxacin against Staphylococcus aureus topoisomerase IV, Escherichia coli DNA gyrase, and HeLa cell topoisomerase II and compared them with those of several quinolones. The inhibitory activities of quinolones against these type II topoisomerases significantly correlated with their antibacterial activities or cytotoxicities (correlation coefficient [r] = 0.926 for S. aureus, r = 0.972 for E. coli, and r = 0.648 for HeLa cells). Gatifloxacin possessed potent inhibitory activities against bacterial type II topoisomerases (50% inhibitory concentration [IC50] = 13.8 µg/ml for S. aureus topoisomerase IV; IC50 = 0.109 µg/ml for E. coli DNA gyrase) but the lowest activity against HeLa cell topoisomerase II (IC50 = 265 µg/ml) among the quinolones tested. There was also a significant correlation between the inhibitory activities of quinolones against S. aureus topoisomerase IV and those against E. coli DNA gyrase (r = 0.969). However, the inhibitory activity against HeLa cell topoisomerase II did not correlate with that against either bacterial enzyme. The IC50 of gatifloxacin for HeLa cell topoisomerase II was 19 and was more than 2,400 times higher than that for S. aureus topoisomerase IV and that for E. coli DNA gyrase. These ratios were higher than those for other quinolones, indicating that gatifloxacin possesses a higher selectivity for bacterial type II topoisomerases.

* Corresponding author. Mailing address: Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd., 2399-1, Mitarai, Nogi, Shimotsuga, Tochigi 329-0114, Japan. Phone: 81-280-562201. Fax: 81-280-571293. E-mail: fvbb0984{at}mb.infoweb.ne.jp.

Antimicrobial Agents and Chemotherapy, October 1998, p. 2678-2681, Vol. 42, No. 10
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.


This article has been cited by other articles:

  • Dawis, M. A., Isenberg, H. D., France, K. A., Jenkins, S. G. (2003). In vitro activity of gatifloxacin alone and in combination with cefepime, meropenem, piperacillin and gentamicin against multidrug-resistant organisms. J Antimicrob Chemother 51: 1203-1211 [Abstract] [Full Text]  
  • Takei, M., Fukuda, H., Kishii, R., Kadowaki, Y., Atobe, Y., Hosaka, M. (2002). Contribution of the C-8-Methoxy Group of Gatifloxacin to Inhibition of Type II Topoisomerases of Staphylococcus aureus. Antimicrob. Agents Chemother. 46: 3337-3338 [Full Text]  
  • Shalit, I., Horev-Azaria, L., Fabian, I., Blau, H., Kariv, N., Shechtman, I., Alteraz, H., Kletter, Y. (2002). Immunomodulatory and Protective Effects of Moxifloxacin against Candida albicans-Induced Bronchopneumonia in Mice Injected with Cyclophosphamide. Antimicrob. Agents Chemother. 46: 2442-2449 [Abstract] [Full Text]  
  • Takei, M., Fukuda, H., Kishii, R., Hosaka, M. (2001). Target Preference of 15 Quinolones against Staphylococcus aureus, Based on Antibacterial Activities and Target Inhibition. Antimicrob. Agents Chemother. 45: 3544-3547 [Abstract] [Full Text]  
  • Roychoudhury, S., Catrenich, C. E., McIntosh, E. J., McKeever, H. D., Makin, K. M., Koenigs, P. M., Ledoussal, B. (2001). Quinolone Resistance in Staphylococci: Activities of New Nonfluorinated Quinolones against Molecular Targets in Whole Cells and Clinical Isolates. Antimicrob. Agents Chemother. 45: 1115-1120 [Abstract] [Full Text]  
  • Purswani, M., Eckert, S., Arora, H., Johann-Liang, R., Noel, G. J. (2000). The effect of three broad-spectrum antimicrobials on mononuclear cell responses to encapsulated bacteria: evidence for down-regulation of cytokine mRNA transcription by trovafloxacin. J Antimicrob Chemother 46: 921-929 [Abstract] [Full Text]  
  • Lu, T., Zhao, X., Drlica, K. (1999). Gatifloxacin Activity against Quinolone-Resistant Gyrase: Allele-Specific Enhancement of Bacteriostatic and Bactericidal Activities by the C-8-Methoxy Group. Antimicrob. Agents Chemother. 43: 2969-2974 [Abstract] [Full Text]  


Copyright © 2009 by the American Society for Microbiology.   For an alternate route to Journals.ASM.org, visit: http://intl-journals.asm.org | More Info»