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Antibacterial activity of ofloxacin and its mode of action

Antibakterielle Aktivität und Wirkungsmechanismus von Ofloxacin

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Summary

The antibacterial activity of ofloxacin against Enterobacteriaceae,Pseudomonas aeruginosa, Haemophilus influenzae, Branhamella catarrhalis, andNeisseria gonorrhoeae was comparable to norfloxacin and enoxacin, and far exceeded the activity of pipemidic acid and nalidixic acid. The activity of ofloxacin was two to eight times less than that of ciprofloxacin. Ofloxacin was more active againstStaphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Acinetobacter spp.,Legionella spp., andBacteroides fragilis, than norfloxacin, enoxacin, pipemidic acid and nalidixic acid, and the activity of ofloxacin was comparable to that of ciprofloxacin. Ofloxacin was two to seven times more effective than norfloxacin in systemic infections in mice withS. aureus, Escherichia coli, Serratia marcescens andP. aeruginosa. Ofloxacin strongly inhibited DNA supercoiling activity of DNA gyrase purified fromE. coli KL-16. There is a parallel relationship between antibacterial activity of ofloxacin and its inhibitory action against DNA gyrases from ofloxacin-susceptible and ofloxacin-resistant clinical isolates ofE. coli. These results indicate that the high bactericidal action of ofloxacin and the related new quinolone agents can be explained by their potent inhibitory activities against DNA gyrase in bacterial cells.

Zusammenfassung

Ofloxacin war in seiner antibakteriellen Aktivität gegen Enterobacteriaceae,Pseudomonas aeruginosa, Haemophilus influenzae, Branhamella catarrhalis undNeisseria gonorrhoeae mit Norfloxacin und Enoxacin vergleichbar und weit wirksamer als Pipemidsäure und Nalidixinsäure. Die Aktivität von Ofloxacin war zwei- bis achtfach geringer als die von Ciprofloxacin. GegenStaphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Acinetobacter spp.,Legionella spp. undBacteroides fragilis besaß Ofloxacin größere Wirksamkeit als Norfloxacin, Enoxacin, Pipemidsäure und Nalidixinsäure und war mit Ciprofloxacin vergleichbar. Die Wirksamkeit von Ofloxacin bei systemischen Infektionen in Mäusen, verursacht durchS. aureus, Escherichia coli, Serratia marcescens undP. aeruginosa, war zwei- bis siebenmal stärker als die von Norfloxacin. Ofloxacin besaß starke Hemmwirkung gegen das durch die (ausE. coli Kl-16 rein gewonnene) DNA-Gyrase vermittelte Supercoiling der DNA. Zwischen antibakterieller Aktivität von Ofloxacin und seiner Hemmwirkung gegen DNA-Gyrasen Ofloxacinempfindlicher und Ofloxacin-resistenter klinischer Isolate vonE. coli besteht eine parallele Beziehung. Daraus kann man schließen, daß sich die hohe bakterizide Wirksamkeit von Ofloxacin und verwandten neuen Chinolonen durch ihre starke Hemmwirkung gegen DNA-Gyrasen in Bakterienzellen erklären läßt.

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Authors and Affiliations

  1. Episome Institute, 2220, Kogure, Fujimi-mura, Setagun, Gunma, Japan

    K. Sato Ph.D., Y. Inoue Ph.D., T. Fujii Ph.D., H. Aoyama Ph.D. & S. Mitsuhashi M. D.

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  1. K. Sato Ph.D.
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  2. Y. Inoue Ph.D.
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  3. T. Fujii Ph.D.
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  4. H. Aoyama Ph.D.
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  5. S. Mitsuhashi M. D.
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Sato, K., Inoue, Y., Fujii, T. et al. Antibacterial activity of ofloxacin and its mode of action. Infection 14 (Suppl 4), S226–S230 (1986). https://doi.org/10.1007/BF01661277

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