| Rat intestinal precision-cut slices as an in vitro model to study xenobiotic interaction with transporters. | |
| | |
MedLine Citation:
|
PMID: 21527342 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
|
ATP-binding cassette (ABC) proteins play key role in tissue defence by transporting metabolic waste and toxic chemicals out of the cells. Consequently, intact cell systems are required to study xenobiotic interactions with ATP-dependent transporters. The aim of the present study was to set up an intestinal precision-cut slice technique to study the interactions of ABC transporters with xenobiotics. Rat intestinal slices were incubated with verapamil, indomethacin and glibenclamide, and the ability of the above-mentioned drugs to inhibit the multidrug resistance glycoprotein (MDR) and/or multidrug-resistance-associated protein (MRP) was assessed by measuring the intracellular conversion of calcein-AM to fluorescent calcein. The ABC transporters' inhibitors caused a time-dependent florescence increase which reached the maximum value at 30min. Verapamil and glibenclamide promoted a concentration-dependent intracellular accumulation of calcein (IC(50) 8.1×10(-6)M, 1.9×10(-4)M, respectively). The effect of glibenclamide was fully reversed by washing the slices, suggesting the reversible nature of calcein accumulation. These data suggest that the precision-cut intestinal slices are a reliable, simple and fast system to evaluate xenobiotic interactions with ABC transporters in rat and, hopefully, in human intestine. |
| | |
Authors:
|
Mariapia Possidente; Stefania Dragoni; Giulia Franco; Maila Gori; Eugenio Bertelli; Elisabetta Teodori; Maria Frosini; Massimo Valoti |
Publication Detail:
|
Type: JOURNAL ARTICLE Date: 2011-4-18 |
Journal Detail:
|
Title: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V Volume: - ISSN: 1873-3441 ISO Abbreviation: - Publication Date: 2011 Apr |
Date Detail:
|
Created Date: 2011-4-29 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 9109778 Medline TA: Eur J Pharm Biopharm Country: - |
Other Details:
|
Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
|
Copyright © 2011. Published by Elsevier B.V. |
Affiliation:
|
Department of Neurosciences, University of Siena, Italy. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Precipitation in the small intestine may play a more important role in the in vivo performance of po...
Next Document: Comprehensive behavioral phenotyping of Ts65Dn mouse model of down syndrome: Activation of ?(1)-adre...