Desnottes J F, Diallo N, Loubeyre C, Moreau N
Rhône-Poulenc Santé, Centre de Recherches de Vitry-Alfortville, Vitry-sur-Seine, France.
J Antimicrob Chemother. 1990 Oct;26 Suppl B:17-26. doi: 10.1093/jac/26.suppl_b.17.
Recent evidence indicates that certain antibiotics affect bacterial adherence and phagocyte-micro-organism interactions. These interactions are important in the early stages of bacterial pathogenesis, that is, attachment to mucosal surfaces and invasion. Among the antibiotics of interest in this field are the fluoroquinolones. Sub-MICs of pefloxacin can alter the ability of Gram-positive cocci (Staphylococcus aureus, Enterococcus faecalis) and Gram-negative bacilli (Escherichia coli) to adhere to different eukaryotic cells (uroepithelial and buccal cells) and to fibrin-platelet matrices. The mechanism by which pefloxacin reduces adhesion is not completely understood. However in the case of Esch. coli, the inhibition of haemagglutination and adherence corresponds to: (1) a decrease in production of fimbriae; (2) changes in the composition of outer membrane proteins; and (3) an effect on partition coefficient (carried out with the PEG/dextran system) which can be attributed to changes in electric and/or hydrophobic properties of the Esch. coli surface. The first step of phagocytosis is represented by adherence of opsonized bacteria to the membrane receptors of phagocytes. Consequently, the action of pefloxacin on phagocytosis is also of importance. Pretreatment of bacteria (Staph. aureus, Ent. faecalis, Esch. coli and Legionella pneumophila) with 1/4 the MIC of pefloxacin leads to an increase in uptake of the different strains by phagocytes (polymorphonuclear leucocytes and macrophages). Exposure of the phagocytes to 10 mg/l of pefloxacin enhances phagocytosis of strains that have not been pretreated. Finally, entry of antibiotics into phagocytic cells is a prerequisite for activity against intracellular organisms. The concentration of pefloxacin by polymorphs and macrophages is high (intracellular concentration/extracellular concentration = 5-10). Such findings correlate well with the intracellular activity of pefloxacin, demonstrated with guinea pig macrophages and different bacteria (Staph. aureus, L. pneumophila).
近期证据表明，某些抗生素会影响细菌黏附以及吞噬细胞与微生物的相互作用。这些相互作用在细菌致病的早期阶段很重要，即细菌附着于黏膜表面和侵入机体的过程。该领域中备受关注的抗生素包括氟喹诺酮类。培氟沙星的亚抑菌浓度可改变革兰氏阳性球菌（金黄色葡萄球菌、粪肠球菌）和革兰氏阴性杆菌（大肠杆菌）黏附不同真核细胞（尿道上皮细胞和颊细胞）以及纤维蛋白 - 血小板基质的能力。培氟沙星降低黏附的机制尚未完全明确。然而，就大肠杆菌而言，其对血细胞凝集和黏附的抑制作用对应于：（1）菌毛产生减少；（2）外膜蛋白组成改变；（3）对分配系数的影响（通过聚乙二醇/葡聚糖系统测定），这可归因于大肠杆菌表面电学和/或疏水性的变化。吞噬作用的第一步表现为经调理的细菌黏附于吞噬细胞膜受体。因此，培氟沙星对吞噬作用的影响也很重要。用培氟沙星1/4抑菌浓度预处理细菌（金黄色葡萄球菌、粪肠球菌、大肠杆菌和嗜肺军团菌）会导致吞噬细胞（多形核白细胞和巨噬细胞）对不同菌株的摄取增加。将吞噬细胞暴露于10mg/l的培氟沙星可增强未预处理菌株的吞噬作用。最后，抗生素进入吞噬细胞是其对细胞内微生物发挥活性的前提条件。多形核白细胞和巨噬细胞内培氟沙星的浓度很高（细胞内浓度/细胞外浓度 = 5 - 10）。这些发现与培氟沙星在豚鼠巨噬细胞和不同细菌（金黄色葡萄球菌、嗜肺军团菌）上所显示的细胞内活性密切相关。
