Uptake characteristics of levofloxacin for the eradication of Helicobacter pylori by GES-1 and MGC80-3 cells.

OBJECTIVE: The aim of this study was to study the uptake of levofloxacin for the eradication of Helicobacter pylori by human gastric epithelial cell lines, GES-1 and MGC80-3. MATERIALS AND METHODS: High performance liquid chromatography (HPLC) and coomassie brilliant blue staining, among other methods, were used to study the uptake of levofloxacin in GES-1 and MGC80-3 cells. The effect of time, concentration, temperature, pH, cyclosporine A, verapamil, and cimetidine on uptake was analyzed. RESULTS: The uptake of levofloxacin by GES-1 and MGC80-3 cells reached a steady state after 15 minutes of incubation, and was enhanced by increasing the extracellular levofloxacin concentration, although not in a linear manner. A maximum uptake was observed at 37 °C and pH 7.4. Cyclosporin A and verapamil enhanced uptake in GES-1 cells by 2.07%-13.23% (p > 0.05), and 17.5%-35.3% in MGC80-3 cells (p < 0.05). The uptake of levofloxacin was not affected by cimetidine. CONCLUSIONS: P-glycoprotein mediates levofloxacin uptake in MGC80-3 cell. Further, P-glycoprotein may be involved in levofloxacin uptake in GES-1 cells. However, organic cation transporters were not involved in levofloxacin uptake in MGC80-3 and GES-1 cells.