Source:http://linkedlifedata.com/resource/pubmed/id/18192088
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
2008-9-12
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pubmed:abstractText |
The synthesis and potent antiprotozoal activity of 14-hydroxylunularin, a natural hydroxybibenzyl bryophyte constituent is reported. 14-hydroxylunularin was highly active in vitro assays against culture and intracellular forms of Leishmania spp. and Trypanosoma. cruzi, in absence of cytotoxicity against mammalian cells. Preliminary structure-activity relationship studies showed that the reported bioactivity depends on hybridization at the carbon-carbon bridge, position and number of free hydroxy group on the aromatic rings. The reported results were also in agreement with the in silico prediction using Non-Stochastic Quadratic Fingerprints-based algorithms. The same compound also showed antiprotozoal activity in Leishmania spp. infected mice by oral and subcutaneous administration routes, with an optimal treatment of a daily subcutaneous administration of 10 mg/kg of body weight for 15 days. This study suggested that 14-hydroxylunularin may be chosen as a new candidate in the development of leishmanicidal therapy.
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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 |
Sep
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pubmed:issn |
0223-5234
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pubmed:author |
pubmed-author:FerreiraMaria ElenaME,
pubmed-author:Gómez-BarrioAliciaA,
pubmed-author:HeguaburuVivianaV,
pubmed-author:Marrero-PonceYovanniY,
pubmed-author:Montero-TorresAlinaA,
pubmed-author:NakayamaHectorH,
pubmed-author:PandolfiEnriqueE,
pubmed-author:Rojas de AriasAntonietaA,
pubmed-author:RolónMiriamM,
pubmed-author:RoldosVirginiaV,
pubmed-author:SanabriaLuisL,
pubmed-author:TorresSusanaS,
pubmed-author:TruccoFernandoF,
pubmed-author:VegaCelesteC,
pubmed-author:YaluffGloriaG
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pubmed:issnType |
Print
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pubmed:volume |
43
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1797-807
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pubmed:meshHeading |
pubmed-meshheading:18192088-Animals,
pubmed-meshheading:18192088-Antiprotozoal Agents,
pubmed-meshheading:18192088-Bibenzyls,
pubmed-meshheading:18192088-Cattle,
pubmed-meshheading:18192088-Cell Line,
pubmed-meshheading:18192088-Computational Biology,
pubmed-meshheading:18192088-Extracellular Space,
pubmed-meshheading:18192088-Female,
pubmed-meshheading:18192088-Inhibitory Concentration 50,
pubmed-meshheading:18192088-Intracellular Space,
pubmed-meshheading:18192088-Leishmania,
pubmed-meshheading:18192088-Leishmaniasis,
pubmed-meshheading:18192088-Male,
pubmed-meshheading:18192088-Mice,
pubmed-meshheading:18192088-Phenols,
pubmed-meshheading:18192088-Trypanosoma cruzi
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pubmed:year |
2008
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pubmed:articleTitle |
Activity of a hydroxybibenzyl bryophyte constituent against Leishmania spp. and Trypanosoma cruzi: in silico, in vitro and in vivo activity studies.
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pubmed:affiliation |
Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Av.Gral. Flores 2124, CC 1157, Montevideo 11800, Uruguay.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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