Source:http://linkedlifedata.com/resource/pubmed/id/16366593
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
26
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pubmed:dateCreated |
2005-12-21
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pubmed:abstractText |
A series of cinnamic and phosphonocinnamic derivatives have been synthesized and their ability to inhibit cell-mediated LDL oxidation and oxidized LDL-induced cytotoxicity was investigated. Electron-donating substituents surrounding the necessary 4-OH group of the aromatic ring showed the best results. Among the different series tested, amide 1, thioester 5c, phosphonoester 7c, and the fluorophosphonocinnamic analogue 12c exhibited a potent inhibitory effect against LDL oxidation (and subsequent toxicity) mediated by cultured human microvascular endothelial cells (HMEC-1), with an efficacy comparable to that observed with probucol. Beside this indirect protective effect, these compounds exhibited a direct protective effect against the toxicity of previously oxidized LDL in HMEC-1. These data suggest that the newly synthesized cinnamic compounds should protect against early events (cell-mediated LDL oxidation) occurring within the vascular wall in atherosclerosis.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antioxidants,
http://linkedlifedata.com/resource/pubmed/chemical/Cinnamates,
http://linkedlifedata.com/resource/pubmed/chemical/Lipoproteins, LDL,
http://linkedlifedata.com/resource/pubmed/chemical/Probucol,
http://linkedlifedata.com/resource/pubmed/chemical/oxidized low density lipoprotein
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
29
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
8115-24
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16366593-Antioxidants,
pubmed-meshheading:16366593-Atherosclerosis,
pubmed-meshheading:16366593-Cell Line,
pubmed-meshheading:16366593-Cell Survival,
pubmed-meshheading:16366593-Cinnamates,
pubmed-meshheading:16366593-Cytoprotection,
pubmed-meshheading:16366593-Drug Design,
pubmed-meshheading:16366593-Endothelium, Vascular,
pubmed-meshheading:16366593-Humans,
pubmed-meshheading:16366593-Lipoproteins, LDL,
pubmed-meshheading:16366593-Microcirculation,
pubmed-meshheading:16366593-Probucol
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pubmed:year |
2005
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pubmed:articleTitle |
Design, synthesis, and evaluation of pharmacological properties of cinnamic derivatives as antiatherogenic agents.
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pubmed:affiliation |
Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, Université Paul Sabatier, 118, Route de Narbonne, F-31062 Toulouse Cedex 4, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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