García I, Pascual A, Conejo M C, Perea E J
Departmento de Microbiología, Facultad de Medicina, Universidad de Sevilla.
Enferm Infecc Microbiol Clin. 1996 Mar;14(3):167-70.
The intracellular penetration and activity of antimicrobial agents can be an important factor in the treatment of infections caused by intracellular pathogens. The new quinolones are able to penetrate into phagocytes, but only a few studies have evaluated other types of cells. The purpose of this study is to evaluate the intracellular penetration of ofloxacin, levofloxacin, lomefloxacin, sparfloxacin and BAY Y 3118 into human polymorphonuclear leukocytes and tissue cultured epithelial cells.
Intracellular penetration was evaluated by a fluorometric assay for all the quinolones evaluated except for sparfloxacin, which was evaluated by a radiometric assay.
All the quinolones evaluated reached intracellular concentrations higher than extracellular ones. The penetration of sparfloxacin and BAY Y 3118 into the epithelial cells was similar to those observed for PMNs (cellular to extracellular concentration ratio; C/E > or = 4). The C/E values of ofloxacin, levofloxacin and lomefloxacin for epithelial cells were lower than those observed in PMN, but still yielding C/E values > or = 2.
抗菌药物的细胞内渗透及活性可能是治疗细胞内病原体所致感染的一个重要因素。新型喹诺酮类药物能够渗透进入吞噬细胞，但仅有少数研究评估了对其他类型细胞的作用。本研究的目的是评估氧氟沙星、左氧氟沙星、洛美沙星、司帕沙星及BAY Y 3118在人多形核白细胞及组织培养上皮细胞中的细胞内渗透情况。
除司帕沙星采用放射性测定法评估外，所有评估的喹诺酮类药物均采用荧光测定法评估细胞内渗透情况。
所有评估的喹诺酮类药物在细胞内的浓度均高于细胞外浓度。司帕沙星和BAY Y 3118在上皮细胞中的渗透情况与在多形核白细胞中观察到的情况相似（细胞内与细胞外浓度比；C/E≥4）。氧氟沙星、左氧氟沙星和洛美沙星在上皮细胞中的C/E值低于在多形核白细胞中观察到的值，但仍产生C/E值≥2。
