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The apical uptake transporter of levofloxacin is distinct from the peptide transporter in human intestinal epithelial Caco-2 cells. 2008

Shiro Fukumori, and Toshiya Murata, and Mari Takaai, and Katsutoshi Tahara, and Masato Taguchi, and Yukiya Hashimoto
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama, Toyama, Japan.

The aim of this study was to investigate the involvement of the peptide transporter for absorption of levofloxacin in Caco-2 cells. To evaluate the activity of apical and basolateral peptide transport, we first performed pharmacokinetic analysis of transcellular transport of glycylsarcosine (Gly-Sar) in cell monolayers grown on porous membrane filters. Transcellular transport of Gly-Sar at the medium pH 6 was greater in the apical-to-basolateral direction than in the opposite direction. Influx clearance of Gly-Sar at the apical membrane was much greater than basolateral influx and efflux clearance, indicating that the apical peptide transporter plays an important role in directional transcellular transport of the dipeptide across Caco-2 cell monolayers. We then evaluated the effect of various compounds on the uptake of Gly-Sar and levofloxacin at the apical membrane of Caco-2 cells. The apical uptake of [3H]Gly-Sar was significantly inhibited by Ala-Ala, Gly-Sar, and also levofloxacin, whereas that of [14C]levofloxacin was not inhibited by Ala-Ala and Gly-Sar. On the other hand, the apical uptake of [14C]levofloxacin was inhibited by nicotine, enalapril, fexofenadine, and L-carnitine. These findings indicated that the apical uptake transporter of levofloxacin is distinct from the peptide transporter in Caco-2 cells.

UI MeSH Term Description Entries
D007408 Intestinal Absorption Uptake of substances through the lining of the INTESTINES. Absorption, Intestinal
D002451 Cell Compartmentation A partitioning within cells due to the selectively permeable membranes which enclose each of the separate parts, e.g., mitochondria, lysosomes, etc. Cell Compartmentations,Compartmentation, Cell,Compartmentations, Cell
D004151 Dipeptides Peptides composed of two amino acid units. Dipeptide
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000074011 Peptide Transporter 1 A proton-coupled symporter that transports OLIGOPEPTIDES and DIPEPTIDES. It localizes to the brush-border membrane of the INTESTINAL EPITHELIUM and plays a critical role in the assimilation of dietary proteins. Hydrogen-Peptide Cotransporter PepT1,Intestinal H+-Peptide Cotransporter,PepT1 Protein,Pept-1 Transporter,SLC15A1 Protein,Solute Carrier Family 15 Member 1,hPEPT1 (Cotransporter),H+-Peptide Cotransporter, Intestinal,Hydrogen Peptide Cotransporter PepT1,Intestinal H+ Peptide Cotransporter,PepT1, Hydrogen-Peptide Cotransporter,Pept 1 Transporter,Transporter, Pept-1
D001692 Biological Transport The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments. Transport, Biological,Biologic Transport,Transport, Biologic
D015242 Ofloxacin A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION. DL-8280,DR-3355,Hoe-280,ORF-28489,Ofloxacin Hydrochloride,Ofloxacine,Ru-43280,Tarivid,DL 8280,DL8280,DR 3355,DR3355,Hoe 280,Hoe280,ORF 28489,ORF28489,Ru 43280,Ru43280
D018938 Caco-2 Cells Human colonic ADENOCARCINOMA cells that are able to express differentiation features characteristic of mature intestinal cells, such as ENTEROCYTES. These cells are valuable in vitro tools for studies related to intestinal cell function and differentiation. Caco 2 Cells,Caco-2 Cell,Cell, Caco-2,Cells, Caco-2
D024841 Fluoroquinolones A group of QUINOLONES with at least one fluorine atom and a piperazinyl group. Fluoroquinolone
D026901 Membrane Transport Proteins Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS. Biological Pump,Membrane Transport Protein,Membrane Transporter,Membrane Transporters,Metabolic Pump,Permease,Biological Pumps,Metabolic Pumps,Permeases,Pump, Biologic,Pump, Biological,Pump, Metabolic,Pumps, Biological,Pumps, Metabolic,Biologic Pump,Protein, Membrane Transport,Transport Protein, Membrane,Transport Proteins, Membrane,Transporter, Membrane,Transporters, Membrane

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