用于监测喹诺酮类抗菌效力的体外可裂解复合物测定法。

Walton L, Elwell L P

Department of Microbiology, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27707.

Antimicrob Agents Chemother. 1988 Jul;32(7):1086-9. doi: 10.1128/AAC.32.7.1086.

Seven quinolones were evaluated to determine whether their ability to generate the DNA gyrase-mediated cleavable complex correlated with their ability to inhibit the catalytic activity of purified DNA gyrase and inhibit the growth of Escherichia coli. The rank order of potency of these drugs in the cleavable-complex assay was essentially the same as in the DNA supercoiling-inhibition assay. It required 2- to 10-fold-lower drug concentrations to generate the cleavable complex than to inhibit E. coli DNA gyrase. With the newer fluoroquinolones, a 25- to 100-fold-greater concentration was required for DNA gyrase inhibition than for cell growth inhibition, suggesting a more subtle interaction between these inhibitors and DNA gyrase than mere enzyme inhibition.

评估了七种喹诺酮类药物，以确定它们产生DNA回旋酶介导的可裂解复合物的能力是否与其抑制纯化的DNA回旋酶的催化活性以及抑制大肠杆菌生长的能力相关。这些药物在可裂解复合物测定中的效力排名顺序与在DNA超螺旋抑制测定中基本相同。产生可裂解复合物所需的药物浓度比抑制大肠杆菌DNA回旋酶所需的浓度低2至10倍。对于新型氟喹诺酮类药物，抑制DNA回旋酶所需的浓度比抑制细胞生长所需的浓度高25至100倍，这表明这些抑制剂与DNA回旋酶之间的相互作用比单纯的酶抑制更为微妙。