title: Uptake and intracellular activity of trovafloxacin in human phagocytes and tissue-cultured epithelial cells.
abstract: The penetration of trovafloxacin into human polymorphonuclear leukocytes (PMNs), human peritoneal macrophages, and tissue-cultured epithelial cells (McCoy cells) was evaluated. The cellular concentration to extracellular concentration (C/E) ratios of trovafloxacin were greater than 9 for extracellular concentrations ranging from 0.5 to 25 micrograms/ml. The uptake of trovafloxacin by PMNs was rapid, reversible, nonsaturable, not energy dependent, and significantly increased at 4 degrees C. Ingestion of opsonized zymosan, but not opsonized Staphylococcus aureus, significantly increased the amount of PMN-associated trovafloxacin. This agent at concentrations of 0.5 and 1 microgram/ml induced a greater reduction in the survival of intracellular S. aureus in PMNs than ciprofloxacin and ofloxacin. It was concluded that trovafloxacin reaches concentrations within phagocytic and nonphagocytic cells several times higher than the extracellular ones, while it remains active in PMNs.
authors.affiliation: Department of Microbiology, School of Medicine, University of Seville, Spain.
authors.forename: A
authors.initials: A
authors.lastname: Pascual
authors.forename: I
authors.initials: I
authors.lastname: García
authors.forename: S
authors.initials: S
authors.lastname: Ballesta
authors.forename: E J
authors.initials: EJ
authors.lastname: Perea
mesh_terms: D000890:Anti-Infective Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D002470:Cell Survival; D002478:Cells, Cultured; D002939:Ciprofloxacin / Q000494:pharmacology; D004848:Epithelium / Q000187:drug effects / Q000378:metabolism / Q000382:microbiology; D024841:Fluoroquinolones; D006801:Humans; D006863:Hydrogen-Ion Concentration; D017737:Macrophages, Peritoneal / Q000187:drug effects* / Q000378:metabolism / Q000382:microbiology; D009287:Naphthyridines / Q000493:pharmacokinetics / Q000494:pharmacology*; D009504:Neutrophils / Q000187:drug effects* / Q000378:metabolism / Q000382:microbiology; D015242:Ofloxacin / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013696:Temperature
chemical_list: D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D002939:Ciprofloxacin; C080163:trovafloxacin; D015242:Ofloxacin