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J Antimicrob Chemother. 2001 Apr;47(4):447-50.

Inhibitory activity of quinolones against DNA gyrase of Mycobacterium tuberculosis.

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New Product Research Laboratories I, Daiichi Pharmaceutical Co. Ltd, 16-13 Kitakasai 1-chome, Edogawa-ku, Tokyo 134-8630, Japan.


The in vitro inhibitory activities of quinolones against Mycobacterium tuberculosis DNA gyrase were measured. The 50% inhibitory concentrations (IC(50)s) of sitafloxacin (DU-6859a), sparfloxacin, ciprofloxacin and levofloxacin against supercoiling activity of DNA gyrase were 1.67, 4.80, 12.2 and 13.9 mg/L, respectively, and correlated well with their MICs. Two altered proteins of GyrA containing Ala-90Val, or Ala-90Val and Asp-94Gly were also purified and the inhibitory activities of the quinolones ranged from 12 to >83 times weaker than those against the wild-type enzyme. These results suggest that mutations in the corresponding genes confer quinolone resistance.

[Indexed for MEDLINE]

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