Linked Life Data

8862725

Source:http://linkedlifedata.com/resource/pubmed/id/8862725

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
1997-3-5
pubmed:abstractText
In order to compare the capacities of a variety of compounds to interfere with P-glycoprotein (Pgp) function, a novel assay was set up to work on a large screening scale. The model assay measures the capacity of parental sensitive (Par) and multidrug-resistant (MDR) cells to efflux a small fixed amount of acetoxymethyl calcein (calcein-AM) after their pretreatment with concentration ranges of known Pgp modulators. This microplate cytometry-based assay was performed with two different pairs of cell lines, the human lymphocytic leukemia CEM cells and the murine monocytic leukemia P388 cells. For a given Pgp-expressing MDR cell line, a Pgp modulator EC50 was defined as the concentration required to restore half of the calcein retention shown by similarly treated Par cells. With both MDR-P388 and MDR-CEM cells, EC50 comparisons ranked five reference Pgp modulators as follows: SDZ 280-446 > SDZ PSC 833 > cyclosporin A > verapamil > vinblastine. Further use of the MDR-CEM cells could rank 15 Pgp modulators for their capacity to interfere with calcein-AM efflux as follows: SDZ 280-446 1.9 x > SDZ PSC 833 8.3 x > cyclosporin A 3.8 x > amiodarone 1.1 x > quinacrine 1.6 x > verapamil 1.4 x > quinidine 1.1 x > vinblastine 11 x > vincristine 2 x > chloroquine > beta-lumicolchicine > or = gamma-lumicolchicine > or = colchicine > etoposide > or = doxorubicin. This calcein-AM assay should open the way for ranking large numbers of novel structures for their potential Pgp modulator properties, particularly for an efficient screening of Pgp function antagonists, but it does not allow defining whether their inhibition may be competitive or not.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0959-4973
pubmed:author
pubmed:issnType
Print
pubmed:volume
7
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
568-78
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1996
pubmed:articleTitle
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.
pubmed:affiliation
Laboratoire d'Immunologie, Pharmacological Research Center, Strasbourg 1 University, France.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't