タイトル（掲載誌）Biopharmaceutics & Drug Disposition
一般注記It was reported previously that specific levofloxacin uptake in Caco- 2 cells was inhibited by nicotine, enalapril, L-carnitine and fexofenadine. The aim of the present study was to characterize the cellular uptake of levofloxacin using another human intestinal cell, line, LS180. Levofloxacin uptake in LS180 cells was temperature-dependent and optimal at neutral pH, but was Na+-independent. The rank order of inhibitory effects of the four compoundson[14C]levofloxacin uptake in LS180 cells was nicotine>enalapril> L- carnitine> fexofenadine, which is consistent with that in Caco- 2 cells. The mRNA levels of OATP1A2, 1B1, 1B3 and 2B1 in LS180 cells were markedly different from those in Caco-2 cells, and OATP substrates/inhibitors had no systematic effect on thelevofloxacin uptake.The mRNA levels of OCTN1 and 2 in LS180 cells were similar to those inCaco-2 cells.However, the inhibitory effect of nicotine on L-[3H]carnitine uptake was much less potent than that of unlabeled L-carnitine. These results in dicate that the specific uptake system for levofloxacin in LS180 cells isidentical/similar to that in Caco-2 cells, but that OATPs and OCTNs contribute little to levofloxacin uptake in the human intestinal epithelial cells.
一次資料へのリンクURLhttps://u-fukui.repo.nii.ac.jp/?action=repository_action_common_download&item_id=19953&item_no=1&attribute_id=22&file_no=1
連携機関・データベース国立情報学研究所 : 学術機関リポジトリデータベース（IRDB）（機関リポジトリ）