Mozhokina G N, Kunichan A D, Levchenko T N, Smirnova N S
Research Institute of Phthisiopulmonology, I.M. Sechenov Moscow Medical Academy.
Antibiot Khimioter. 1998;43(10):13-6.
The peculiarities of the mechanism of the lomefloxacin bactericidal action on Mycobacterium tuberculosis were studied. The electron microscopy of ultrathin sections of the cells of M.tuberculosis H37Rv exposed to 10 micrograms/ml of lomefloxacin for 24 hours revealed severe changes in their ultrastructure: exfoliation of the cell wall from the cytoplasmic membrane, loosening and fragmentation of the cytoplasmic membrane, lowering of the cytoplasm thickness, vacuolization and twisting of the mesosomes. The exposure of the cells to lomefloxacin for 72 hours resulted in their complete destruction: the cells proved to be a mass of unidentifiable fragments. Some destructions such as exfoliation of the intracytoplasmic membrane and the cytoplasm loosening and vacuolization were observed in the tubercle bacilli localized inside the phagosomes of the murine lung macrophages exposed to lomefloxacin. Such destructions were evident of the antibiotic good penetration not only into the macrophages but also through the phagosome walls as well as of the lomefloxacin intracellular bactericidal activity. In the experiments with the culture of the lung tissue from the tuberculosis foci of mice the basic mechanism fo the lomefloxacin action on M.tuberculosis was demonstrated: the lomefloxacin bactericidal effect was realized through the pathway of mechanism A of the antimicrobial action of fluoroquinolones.
研究了洛美沙星对结核分枝杆菌杀菌作用机制的特点。对暴露于10微克/毫升洛美沙星24小时的结核分枝杆菌H37Rv细胞超薄切片进行电子显微镜检查,发现其超微结构发生了严重变化:细胞壁从细胞膜上脱落、细胞膜松弛和断裂、细胞质厚度降低、中介体空泡化和扭曲。细胞暴露于洛美沙星72小时导致其完全破坏:细胞被证明是一团无法识别的碎片。在暴露于洛美沙星的小鼠肺巨噬细胞吞噬体内的结核杆菌中,观察到一些破坏现象,如胞内膜脱落、细胞质松弛和空泡化。这些破坏现象表明抗生素不仅能很好地穿透巨噬细胞,还能穿透吞噬体壁,以及洛美沙星的细胞内杀菌活性。在对来自小鼠结核病灶的肺组织培养物进行的实验中,证明了洛美沙星对结核分枝杆菌作用的基本机制:洛美沙星的杀菌作用是通过氟喹诺酮类抗菌作用的机制A途径实现的。