Source:http://linkedlifedata.com/resource/pubmed/id/20363145
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
2010-4-12
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pubmed:abstractText |
A novel series of diphenolic chromone derivatives were synthesized and their inhibitory activity on nitric oxide (NO) production and cytotoxicity were evaluated using LPS-activated murine macrophages RAW264.7 assay and MTT method, respectively. Among these compounds, (5,7-dihydroxy-4-oxo-4H-chromen-3-yl) methyl esters (6b, 6c, 6f, 6g, and 6h) showed quite potent inhibitory activities with IC(50) values of 2.20, 3.48, 0.35, 0.80, and 0.61microM, respectively. The MTT results showed that all of the active compounds exhibited no cytotoxicity at the effective concentrations. The preliminary mechanism of the most potent compounds (6b, 6c, 6f, 6g, and 6h) was further examined based on the RT-PCR results and the compounds 6f, 6g, and 6h inhibited NO production by suppressing the expression of iNOS mRNA in a dose dependent manner. Furthermore, a computational analysis of physicochemical parameters revealed that the most of the compounds possessed drug-like properties.
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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/Anti-Inflammatory Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Chromones,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Lipopolysaccharides,
http://linkedlifedata.com/resource/pubmed/chemical/Nitric Oxide,
http://linkedlifedata.com/resource/pubmed/chemical/Nitric Oxide Synthase Type II
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2864-71
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pubmed:meshHeading |
pubmed-meshheading:20363145-Animals,
pubmed-meshheading:20363145-Anti-Inflammatory Agents,
pubmed-meshheading:20363145-Cell Line,
pubmed-meshheading:20363145-Chromones,
pubmed-meshheading:20363145-Enzyme Inhibitors,
pubmed-meshheading:20363145-Lipopolysaccharides,
pubmed-meshheading:20363145-Macrophages,
pubmed-meshheading:20363145-Mice,
pubmed-meshheading:20363145-Nitric Oxide,
pubmed-meshheading:20363145-Nitric Oxide Synthase Type II
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis of a novel series of diphenolic chromone derivatives as inhibitors of NO production in LPS-activated RAW264.7 macrophages.
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pubmed:affiliation |
Key Lab of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093, China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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