Georgopapadakou N H, Bertasso A
Roche Research Center, Nutley, New Jersey 07110.
Antimicrob Agents Chemother. 1991 Dec;35(12):2645-8. doi: 10.1128/AAC.35.12.2645.
The effects of quinolone antibiotics on nucleoid segregation in growing Escherichia coli were examined by using fleroxacin (Ro 23-6240, AM 833) as a prototype compound. At levels that were close to its MIC and induced growth arrest and filamentation, fleroxacin caused large nucleoids to appear in midcell, suggesting inhibition of nucleoid segregation. With increasing fleroxacin concentrations, nucleoids became progressively smaller, suggesting inhibition of DNA replication. Removal of fleroxacin restored normal cell and nucleoid morphology in filaments with large nucleoids but not in filaments with small nucleoids. The results are consistent with inhibition of chromosome decatenation at low quinolone concentrations (bacteriostatic effect) and DNA supercoiling at high concentrations (bactericidal effect).
以氟罗沙星(Ro 23-6240,AM 833)作为原型化合物,研究了喹诺酮类抗生素对生长中的大肠杆菌类核分离的影响。在接近其最低抑菌浓度并导致生长停滞和丝状化的水平下,氟罗沙星使大的类核出现在细胞中部,提示类核分离受到抑制。随着氟罗沙星浓度增加,类核逐渐变小,提示DNA复制受到抑制。去除氟罗沙星可使具有大类核的丝状菌恢复正常的细胞和类核形态,但不能使具有小类核的丝状菌恢复正常。这些结果与低喹诺酮浓度下抑制染色体解连环(抑菌作用)和高浓度下抑制DNA超螺旋(杀菌作用)相一致。