|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0001884,
umls-concept:C0021469,
umls-concept:C0024432,
umls-concept:C0024728,
umls-concept:C0027950,
umls-concept:C0030306,
umls-concept:C0030685,
umls-concept:C0033268,
umls-concept:C0086418,
umls-concept:C0391871,
umls-concept:C0680255,
umls-concept:C1158882,
umls-concept:C1280500,
umls-concept:C1283071,
umls-concept:C1456331,
umls-concept:C1709843,
umls-concept:C1879547,
umls-concept:C1963578
|
|
pubmed:issue |
8
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|
pubmed:dateCreated |
2011-4-12
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|
pubmed:abstractText |
Some chalcones exert potent anti-inflammatory activities. Mannich bases of heterocyclic chalcones inhibited nitric oxide (NO) production in lipopolysaccharide and interferon-? stimulated RAW 264.7 macrophages. Also Formyl-Met-Leu-Phe and cytochalasin B induced superoxide anion generation (O2·-) and elastase release in human neutrophils. Mannich bases of heterocyclic chalcone analogs exhibited potent inhibitory effects on NO production with IC(50) values ranges between 10.5 and 0.018 ?M, O2·- generation (IC(50) 39.87-0.68 ?M) and elastase release (IC(50) 39.74-0.95 ?M). Compound 29 (IC(50) 0.055 ?M) and 34 (IC(50) 0.018 ?M) were showed excellent inhibition on NO production. On the other hand, compounds 2 and 8 showed potent inhibition on O2·- generation and elastase release. Therefore, these four compounds may be new leads for development of anti-inflammatory activities. The structure-activity relationships are also discussed.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
|
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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 |
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pubmed:copyrightInfo |
Crown Copyright © 2011. Published by 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 |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2751-6
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pubmed:meshHeading |
pubmed-meshheading:21441032-Animals,
pubmed-meshheading:21441032-Anti-Inflammatory Agents,
pubmed-meshheading:21441032-Chalcones,
pubmed-meshheading:21441032-Heterocyclic Compounds,
pubmed-meshheading:21441032-Humans,
pubmed-meshheading:21441032-Macrophage Activation,
pubmed-meshheading:21441032-Macrophages,
pubmed-meshheading:21441032-Mice,
pubmed-meshheading:21441032-Neutrophils,
pubmed-meshheading:21441032-Nitric Oxide,
pubmed-meshheading:21441032-Pancreatic Elastase,
pubmed-meshheading:21441032-Structure-Activity Relationship,
pubmed-meshheading:21441032-Superoxides
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|
pubmed:year |
2011
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pubmed:articleTitle |
Inhibitory effects of Mannich bases of heterocyclic chalcones on NO production by activated RAW 264.7 macrophages and superoxide anion generation and elastase release by activated human neutrophils.
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pubmed:affiliation |
Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, ROC.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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