Organic cation transporter function in different in vitro models of human lung epithelium.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
AuthorsSalomon, Johanna J
Gausterer, Julia C
MetadataShow full item record
AbstractOrganic cation transporters (OCT) encoded by members of the solute carrier (SLC) 22 family of genes are involved in the disposition of physiological substrates and xenobiotics, including drugs used in the treatment of chronic obstructive lung diseases and asthma. The aim of this work was to identify continuously growing epithelial cell lines that closely mimic the organic cation transport of freshly isolated human alveolar type I-like epithelial cells (ATI) in primary culture, and which consequently, can be utilised as in vitro models for the study of organic cation transport at the air-blood barrier. OCT activity was investigated by measuring [(14)C]-tetraethylammonium (TEA) uptake into monolayers of Calu-3, NCI-H441 and A549 lung epithelial cell lines in comparison to ATI-like cell monolayers in primary culture. Levels of time-dependent TEA uptake were highest in A549 and ATI-like cells. In A549 cells, TEA uptake had a saturable and a non-saturable component with Km=528.5±373.1μM, Vmax=0.3±0.1nmol/min/mg protein and Kd=0.02μl/min/mg protein. TEA uptake into Calu-3 and NCI-H441 cells did not reach saturation within the concentration range studied. RNAi experiments in A549 cells confirmed that TEA uptake was mainly facilitated by OCT1 and OCT2. Co-incubation studies using pharmacological OCT modulators suggested that organic cation uptake pathways share several similarities between ATI-like primary cells and the NCI-H441 cell line, whereas more pronounced differences exist between primary cells and the A549 and Calu-3 cell lines.
CitationOrganic cation transporter function in different in vitro models of human lung epithelium. 2015, 80:82-8 Eur J Pharm Sci
AffiliationHelmholtz Institute for Pharmaceutical Research Saarland (HIPS);Saarland University, Building A4.1, 66123 Saarbruecken, Germany.
JournalEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
The following license files are associated with this item:
- The cell line NCl-H441 is a useful in vitro model for transport studies of human distal lung epithelial barrier.
- Authors: Salomon JJ, Muchitsch VE, Gausterer JC, Schwagerus E, Huwer H, Daum N, Lehr CM, Ehrhardt C
- Issue date: 2014 Mar 3
- Functional characterization of the organic cation transporters (OCTs) in human airway pulmonary epithelial cells.
- Authors: Ingoglia F, Visigalli R, Rotoli BM, Barilli A, Riccardi B, Puccini P, Dall'Asta V
- Issue date: 2015 Jul
- Drug Transporter Protein Quantification of Immortalized Human Lung Cell Lines Derived from Tracheobronchial Epithelial Cells (Calu-3 and BEAS2-B), Bronchiolar-Alveolar Cells (NCI-H292 and NCI-H441), and Alveolar Type II-like Cells (A549) by Liquid Chromatography-Tandem Mass Spectrometry.
- Authors: Sakamoto A, Matsumaru T, Yamamura N, Suzuki S, Uchida Y, Tachikawa M, Terasaki T
- Issue date: 2015 Sep
- Transport of the fluorescent organic cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (ASP+) in human respiratory epithelial cells.
- Authors: Salomon JJ, Endter S, Tachon G, Falson F, Buckley ST, Ehrhardt C
- Issue date: 2012 Jun
- Beta-2 Adrenergic Agonists Are Substrates and Inhibitors of Human Organic Cation Transporter 1.
- Authors: Salomon JJ, Hagos Y, Petzke S, Kühne A, Gausterer JC, Hosoya K, Ehrhardt C
- Issue date: 2015 Aug 3