Source:http://linkedlifedata.com/resource/pubmed/id/12502337
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
12
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| pubmed:dateCreated |
2002-12-27
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| pubmed:abstractText |
Fatty acid synthase (FAS) has been identified as a potential antifungal target. FAS prepared from Saccharomyces cerevisiae was employed for bioactivity-guided fractionation of Chlorophora tinctoria,Paspalum conjugatum, Symphonia globulifera, Buchenavia parviflora, and Miconia pilgeriana. Thirteen compounds (1-13), including three new natural products (1, 4, 12), were isolated and their structures identified by spectroscopic interpretation. They represented five chemotypes, namely, isoflavones, flavones, biflavonoids, hydrolyzable tannin-related derivatives, and triterpenoids. 3'-Formylgenistein (1) and ellagic acid 4-O-alpha-l-rhamnopyranoside (9) were the most potent compounds against FAS, with IC(50) values of 2.3 and 7.5 microg/mL, respectively. Furthermore, 43 (14-56) analogues of the five chemotypes from our natural product repository and commercial sources were tested for their FAS inhibitory activity. Structure-activity relationships for some chemotypes were investigated. All these compounds were further evaluated for antifungal activity against Candida albicans and Cryptococcus neoformans. Although there were several antifungal compounds in the set, correlation between the FAS inhibitory activity and antifungal activity could not be defined.
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| pubmed:grant | |
| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antifungal Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acid Synthetase Complex,
http://linkedlifedata.com/resource/pubmed/chemical/Isoflavones,
http://linkedlifedata.com/resource/pubmed/chemical/Tannins,
http://linkedlifedata.com/resource/pubmed/chemical/Triterpenes
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| pubmed:status |
MEDLINE
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| pubmed:month |
Dec
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| pubmed:issn |
0163-3864
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| pubmed:author |
pubmed-author:BroedelSheldon ESEJr,
pubmed-author:CihlarRonald LRL,
pubmed-author:ElSohlyHala NHN,
pubmed-author:FerreiraDaneelD,
pubmed-author:JacobMelissa RMR,
pubmed-author:JoshiAlpana SAS,
pubmed-author:KhanIkhlas AIA,
pubmed-author:KhanShabana ISI,
pubmed-author:LiXing-CongXC,
pubmed-author:RaulliRobert ERE,
pubmed-author:WalkerLarry ALA,
pubmed-author:ZhangZhizhengZ
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| pubmed:issnType |
Print
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| pubmed:volume |
65
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| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1909-14
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| pubmed:dateRevised |
2007-11-14
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| pubmed:meshHeading |
pubmed-meshheading:12502337-Antifungal Agents,
pubmed-meshheading:12502337-Candida albicans,
pubmed-meshheading:12502337-Combretaceae,
pubmed-meshheading:12502337-Cryptococcus neoformans,
pubmed-meshheading:12502337-Enzyme Inhibitors,
pubmed-meshheading:12502337-Fatty Acid Synthetase Complex,
pubmed-meshheading:12502337-Inhibitory Concentration 50,
pubmed-meshheading:12502337-Isoflavones,
pubmed-meshheading:12502337-Melastomataceae,
pubmed-meshheading:12502337-Molecular Structure,
pubmed-meshheading:12502337-Moraceae,
pubmed-meshheading:12502337-Paspalum,
pubmed-meshheading:12502337-Plants, Medicinal,
pubmed-meshheading:12502337-Saccharomyces cerevisiae,
pubmed-meshheading:12502337-Structure-Activity Relationship,
pubmed-meshheading:12502337-Tannins,
pubmed-meshheading:12502337-Triterpenes
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| pubmed:year |
2002
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| pubmed:articleTitle |
Fatty acid synthase inhibitors from plants: isolation, structure elucidation, and SAR studies.
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| pubmed:affiliation |
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, Department of Pharmacognosy, School of Pharmacy, The University of Mississippi, University, MS 38677, USA. xli@olemiss.edu
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| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.
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