Source:http://linkedlifedata.com/resource/pubmed/id/18824363
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
20
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pubmed:dateCreated |
2008-10-20
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pubmed:abstractText |
The macrocyclic lathyrane diterpene latilagascene B, previously isolated from Euphorbia lagascae, was acylated to afford three new diterpene esters, latilagascenes G (1), H (2), and I (3), whose structures were assigned by spectroscopic methods. These acyl derivatives, and the macrocyclic diterpenes of the jatrophane-type, tuckeyanols A (4) and B (5), and euphotuckeyanol (6), isolated from Euphorbia tuckeyana, were tested for P-gp modulating properties on human MDR1 gene-transfected and parental L5178 mouse lymphoma cell lines. All the compounds displayed very strong activity. The molecular orbital energies (HOMO and LUMO) of diterpenes 1-6 and 7-13, previously isolated, have also been calculated in order to estimate their probable charge transfer interactions with P-gp. Structure-activity relationships (SAR) are discussed. Furthermore, compounds (1-6) were assayed, in vitro, for their antiproliferative effects in combination with epirubicine and all of them synergistically enhance the effect of the antitumor drug.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
9323-30
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pubmed:meshHeading |
pubmed-meshheading:18824363-Animals,
pubmed-meshheading:18824363-Cell Line, Tumor,
pubmed-meshheading:18824363-Cell Proliferation,
pubmed-meshheading:18824363-Drug Resistance, Neoplasm,
pubmed-meshheading:18824363-Drug Synergism,
pubmed-meshheading:18824363-Epirubicin,
pubmed-meshheading:18824363-Humans,
pubmed-meshheading:18824363-Magnetic Resonance Spectroscopy,
pubmed-meshheading:18824363-Mice,
pubmed-meshheading:18824363-Molecular Structure,
pubmed-meshheading:18824363-P-Glycoprotein,
pubmed-meshheading:18824363-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Synergistic interaction between p-glycoprotein modulators and epirubicine on resistant cancer cells.
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pubmed:affiliation |
iMed.UL, Faculty of Pharmacy, University of Lisbon, Av. das Forças Armadas, 1600-083 Lisbon, Portugal.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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