Source:http://linkedlifedata.com/resource/pubmed/id/10832604
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2000-8-16
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pubmed:abstractText |
The aim of this study was to characterize the transport of organic cations at the intestinal level, by studying the characteristics of the transport of 1-methyl-4-phenylpyridinium (MPP+) in Caco-2 cells. Transepithelial flux as well as cellular accumulation of [3H]MPP+ were quantitatively similar when substrate was applied from the basolateral or apical cell membrane. Verapamil (100 microM) and rhodamine123 (10 microM) significantly reduced [3H]MPP+ transepithelial flux in the apical-to-basolateral direction. When cells were grown on plastic supports, [3H]MPP+ was rapidly accumulated in the cells, both by saturable and nonsaturable mechanisms. The kinetic parameters of the saturable component were: Km: 449 microM and Vmax: 2,249 pmol per mg protein and 5 min. Uptake of [3H]MPP+ was metabolic energy-dependent and Na+-, pH- and potential-independent. It was inhibited by several organic cations (verapamil, rhodamine123, daunomycin, vinblastine, tetrabutylammonium and vecuronium) but not by others (tetraethylammonium and N-methylnicotinamide). Decynium22 and corticosterone inhibited [3H]MPP+ uptake into the cells. The P-glycoprotein antibody UIC2 (20 microg/ml) had no effect. In conclusion, [3H]MPP+ is efficiently transported by Caco-2 cells in both basolateral-to-apical (secretion) and apical-to-basolateral (absorption) directions. Absorption of [3H]MPP+ at the apical membrane seems to occur through a carrier-mediated mechanism belonging to the Amphiphilic Solute Facilitator (ASF) family of transporters, but distinct from the known members of this family.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1-Methyl-4-phenylpyridinium,
http://linkedlifedata.com/resource/pubmed/chemical/Antibiotics, Antineoplastic,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Cations,
http://linkedlifedata.com/resource/pubmed/chemical/Daunorubicin,
http://linkedlifedata.com/resource/pubmed/chemical/Herbicides,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/Verapamil
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0028-1298
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
361
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
505-13
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:10832604-1-Methyl-4-phenylpyridinium,
pubmed-meshheading:10832604-Antibiotics, Antineoplastic,
pubmed-meshheading:10832604-Biological Transport,
pubmed-meshheading:10832604-Caco-2 Cells,
pubmed-meshheading:10832604-Calcium Channel Blockers,
pubmed-meshheading:10832604-Cations,
pubmed-meshheading:10832604-Daunorubicin,
pubmed-meshheading:10832604-Drug Interactions,
pubmed-meshheading:10832604-Herbicides,
pubmed-meshheading:10832604-Humans,
pubmed-meshheading:10832604-Hydrogen-Ion Concentration,
pubmed-meshheading:10832604-Intestinal Mucosa,
pubmed-meshheading:10832604-Kinetics,
pubmed-meshheading:10832604-Sodium,
pubmed-meshheading:10832604-Time Factors,
pubmed-meshheading:10832604-Tritium,
pubmed-meshheading:10832604-Verapamil
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pubmed:year |
2000
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pubmed:articleTitle |
Characterization of the transport of the organic cation [3H]MPP+ in human intestinal epithelial (Caco-2) cells.
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pubmed:affiliation |
Department of Biochemistry, Faculty of Medicine, Porto, Portugal. fatima_martel@hotmail.com
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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