rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
1-2
|
pubmed:dateCreated |
2003-6-17
|
pubmed:abstractText |
Drugs currently available for visceral leishmaniasis treatment are potentially toxic, have to be administered by parenteral route and frequently give rise to drug resistance, due to the involvement of P-glycoproteins (P-gp) in Leishmania. The purpose of this study was to investigate a possible inhibitory effect of 2n-propylquinoline (2nPQ) on P-gp activity. 2nPQ is a new oral anti-leishmanial drug that has demonstrated its efficacy in BALB/c infected mice with Leishmania donovani [Antimicrob. Agents Chemother. 37 (1993) 859]. Rat everted gut sacs and human intestinal Caco-2 cell lines were used to study the effect of 2nPQ on P-gp activity. Our results demonstrate an inhibitory effect of 2nPQ on the P-gp activity with two P-gp substrates (rhodamine 123 and digoxin), two P-gp inhibitors (cyclosporin A and verapamil), and in two different species. Alone or associated with other active drugs, 2nPQ would be very useful to control Leishmania Multi-Drug-Resistance and intestinal P-gp in humans with kala-azar.
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pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:issn |
0014-4894
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
103
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
51-6
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:12810046-Animals,
pubmed-meshheading:12810046-Antiprotozoal Agents,
pubmed-meshheading:12810046-Caco-2 Cells,
pubmed-meshheading:12810046-Cyclosporine,
pubmed-meshheading:12810046-Digoxin,
pubmed-meshheading:12810046-Drug Resistance,
pubmed-meshheading:12810046-Fluorescent Dyes,
pubmed-meshheading:12810046-Humans,
pubmed-meshheading:12810046-Ileum,
pubmed-meshheading:12810046-Leishmaniasis, Visceral,
pubmed-meshheading:12810046-Male,
pubmed-meshheading:12810046-P-Glycoprotein,
pubmed-meshheading:12810046-Quinolines,
pubmed-meshheading:12810046-Rats,
pubmed-meshheading:12810046-Rats, Sprague-Dawley,
pubmed-meshheading:12810046-Rhodamine 123,
pubmed-meshheading:12810046-Verapamil
|
pubmed:articleTitle |
Decrease of intestinal P-glycoprotein activity by 2n-propylquinoline, a new oral treatment for visceral leishmaniasis.
|
pubmed:affiliation |
Laboratoire de Pharmacie Clinique-Physiologie, UPRES 2706, Faculté de Pharmacie, 92296, Châtenay-Malabry Cedex, France.
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pubmed:publicationType |
Journal Article,
In Vitro
|