title: The transport of ciprofloxacin in cultured kidney epithelial cells LLC-PK1.
abstract: In this study, the transport characteristics of ciprofloxacin (CPFX) were investigated in a LLC-PK1 kidney epithelial cell line. CPFX uptake from the apical medium into LLC-PK1 cells on plastic dishes was shown to be temperature-dependent. Guanidine and cimetidine inhibited the uptake of CPFX, whereas tetraethylammonium chloride (TEA) and N1-methylnicotinamide (NMN) did not. CPFX transport across LLC-PK1 cell monolayers cultured on permeable supports was about 1.8 times larger in the basolateral-to-apical direction than in the apical-to-basolateral direction. Both the basolateral-to-apical and apical-to-basolateral transport of CPFX were inhibited by guanidine, whereas CPFX transport in both directions was not inhibited by TEA, NMN, or cimetidine. The basolateral-to-apical transport of CPFX was sensitive to the pH of the apical medium, and increased in an acidic pH. Enoxacin (ENX) as well as guanidine, inhibited the basolateral-to-apical transport of CPFX, and the inhibitory effect of ENX was sensitive to the pH of the apical side of the monolayers.
authors.affiliation: Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Sasaya
authors.forename: M
authors.initials: M
authors.lastname: Oda
authors.forename: T
authors.initials: T
authors.lastname: Endo
authors.forename: H
authors.initials: H
authors.lastname: Saitoh
authors.forename: M
authors.initials: M
authors.lastname: Takada
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000378:metabolism* / Q000494:pharmacology; D002412:Cations / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D002939:Ciprofloxacin / Q000378:metabolism*; D003470:Culture Media; D015365:Enoxacin / Q000378:metabolism / Q000494:pharmacology; D006146:Guanidines / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D007668:Kidney / Q000166:cytology / Q000378:metabolism*; D018374:LLC-PK1 Cells; D013056:Spectrophotometry, Ultraviolet; D013552:Swine
chemical_list: D000890:Anti-Infective Agents; D002412:Cations; D003470:Culture Media; D006146:Guanidines; D015365:Enoxacin; D002939:Ciprofloxacin