Sasaya M, Oda M, Endo T, Saitoh H, Takada M
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Japan.
Biol Pharm Bull. 1997 Aug;20(8):887-91. doi: 10.1248/bpb.20.887.
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.
在本研究中，对环丙沙星（CPFX）在LLC-PK1肾上皮细胞系中的转运特性进行了研究。结果表明，在塑料培养皿上，CPFX从顶侧培养基进入LLC-PK1细胞的摄取过程具有温度依赖性。胍和西咪替丁抑制CPFX的摄取，而四乙氯化铵（TEA）和N1-甲基烟酰胺（NMN）则无此作用。在可渗透支持物上培养的LLC-PK1细胞单层中，CPFX从基底外侧到顶侧的转运约为从顶侧到基底外侧转运的1.8倍。胍抑制CPFX从基底外侧到顶侧以及从顶侧到基底外侧的转运，而TEA、NMN或西咪替丁均不抑制CPFX在两个方向上的转运。CPFX从基底外侧到顶侧的转运对顶侧培养基的pH敏感，在酸性pH条件下增加。依诺沙星（ENX）以及胍抑制CPFX从基底外侧到顶侧的转运，且ENX的抑制作用对单层顶侧的pH敏感。
