Matsumoto S, Saito H, Inui K
Department of Hospital Pharmacy, School of Medicine, Tokyo Medical and Dental University, Japan.
Pharm Res. 1995 Oct;12(10):1483-7. doi: 10.1023/a:1016235404598.
The intestinal epithelial cell line Caco-2 possesses the H+/dipeptide cotransport system responsible for uptake of oral cephalosporins. In this study, the transport characteristics of ceftibuten were examined from the viewpoint of cell growth in the Caco-2 cells.
The uptake of cephalosporins by Caco-2 cell monolayers grown on plastic dishes was measured and analyzed kinetically.
The uptake of ceftibuten was increased by lowering pH of the incubation medium and was inhibited by excess dipeptide. The transport activity of ceftibuten was dependent on the duration of analysis revealed that the development of ceftibuten uptake was due to not only a decrease in Km but also to an increase in Vmax value.
The uptake of ceftibuten is mediated by the apical H+/dipeptide cotransport system which is regulated by cell growth and/or differentiation in the Caco-2 cells.
肠道上皮细胞系Caco-2拥有负责口服头孢菌素摄取的H⁺/二肽共转运系统。在本研究中，从Caco-2细胞的细胞生长角度研究了头孢布烯的转运特性。
测量并动力学分析在塑料培养皿上生长的Caco-2细胞单层对头孢菌素的摄取。
降低孵育培养基的pH值可增加头孢布烯的摄取，而过量的二肽可抑制其摄取。头孢布烯的转运活性取决于分析持续时间，结果显示头孢布烯摄取的增加不仅归因于Km值的降低，还归因于Vmax值的增加。
头孢布烯的摄取由顶端H⁺/二肽共转运系统介导，该系统受Caco-2细胞中的细胞生长和/或分化调节。
