Nakane T, Iyobe S, Sato K, Mitsuhashi S
Episome Institute, Gunma, Japan.
Antimicrob Agents Chemother. 1995 Dec;39(12):2822-6. doi: 10.1128/AAC.39.12.2822.
The in vitro antibacterial activity of DU-6859a, a new fluoroquinolone, against a wide variety of clinical isolates was evaluated and compared with those of tosufloxacin, ofloxacin, ciprofloxacin, and sparfloxacin. DU-6859a showed potent broad-spectrum activity against gram-positive, gram-negative, and anaerobic bacteria, and its activity was greater than those of the control quinolones. By comparison of MICs at which 90% of strains are inhibited, DU-6859a had potent activity against bacteria resistant to the control quinolones. The time-killing curves of quinolones showed that the number of viable cells decreased rapidly during 2 to 4 of incubation, and regrowth was not seen even after 8 h incubation. At a concentration of four times the MIC, the frequencies of appearance of spontaneous mutants of Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa resistant to DU-6859a were < or = 4.0 x 10(-9) to 1.9 x 10(-8). The 50% inhibitory concentrations of DU-6859a were 0.86 and 1.05 micrograms/ml for the supercoiling activities of DNA gyrases isolated from E. coli and P. aeruginosa, respectively. The rank order of the 50% inhibitory concentrations observed for both DNA gyrases roughly paralleled the MICs.
对新型氟喹诺酮类药物DU-6859a针对多种临床分离菌株的体外抗菌活性进行了评估,并与托氟沙星、氧氟沙星、环丙沙星和司帕沙星进行了比较。DU-6859a对革兰氏阳性菌、革兰氏阴性菌和厌氧菌显示出强大的广谱活性,且其活性大于对照喹诺酮类药物。通过比较抑制90%菌株生长的最低抑菌浓度(MIC),DU-6859a对耐对照喹诺酮类药物的细菌具有强大活性。喹诺酮类药物的杀菌曲线表明,在培养2至4小时期间活细胞数量迅速减少,甚至在培养8小时后也未见再生长。在四倍MIC浓度下,金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌对DU-6859a耐药的自发突变体出现频率≤4.0×10⁻⁹至1.9×10⁻⁸。DU-6859a对从大肠杆菌和铜绿假单胞菌中分离的DNA回旋酶超螺旋活性的50%抑制浓度分别为0.86和1.05微克/毫升。观察到的两种DNA回旋酶的50%抑制浓度的排序大致与MICs平行。