Inhibitory activity of quinolones against DNA gyrase of Mycobacterium tuberculosis | Zendy

Yoshikuni Onodera | Zendy

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Inhibitory activity of quinolones against DNA gyrase of Mycobacterium tuberculosis

Author(s) -

Yoshikuni Onodera

Publication year - 2001

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/47.4.447

Subject(s) - dna gyrase , sparfloxacin , quinolone , dna supercoil , mycobacterium tuberculosis , microbiology and biotechnology , ciprofloxacin , minimum inhibitory concentration , ofloxacin , levofloxacin , antibacterial agent , biology , dna , chemistry , tuberculosis , escherichia coli , antibiotics , gene , medicine , biochemistry , dna replication , pathology

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.

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