Source:http://linkedlifedata.com/resource/pubmed/id/18816430
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
2008-10-17
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pubmed:abstractText |
A systematic structure-activity relationship of 3beta-hydroxy-27- P- E-coumaroyloxyurs-12-en-28-oic acid ( 7), a triterpene ester isolated from UNCARIA RHYNCHOPHYLLA as a phospholipase Cgamma1 inhibitor, was undertaken with a view toward elucidating its chemical mode of action on PLCgamma1. Related derivatives and analogues of 7 were synthesized and their inhibitory activities against PLCgamma1 were evaluated IN VITRO. The results indicate that 3-OH and 27-esterification may be essential, and that 28-COOH and the 2' double bond appear to be important for activity. Furthermore, the compound possessing a P-coumaroyloxy at position 27 rather than at the 3 and 28 positions shows the greatest inhibitory activity against PLCgamma1. Therefore, this inhibitor will be providing a chemical lead for the further development of cancer chemopreventive or cancer chemotherapeutic agents that have lower toxicity against normal tissues.
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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 |
Oct
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pubmed:issn |
0032-0943
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
74
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1481-7
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pubmed:meshHeading |
pubmed-meshheading:18816430-Animals,
pubmed-meshheading:18816430-Cattle,
pubmed-meshheading:18816430-Enzyme Inhibitors,
pubmed-meshheading:18816430-Esters,
pubmed-meshheading:18816430-Pentacyclic Triterpenes,
pubmed-meshheading:18816430-Phospholipase C gamma,
pubmed-meshheading:18816430-Structure-Activity Relationship,
pubmed-meshheading:18816430-Uncaria
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pubmed:year |
2008
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pubmed:articleTitle |
Structure-activity relationship of pentacylic triterpene esters from Uncaria rhynchophylla as inhibitors of phospholipase Cgamma1.
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pubmed:affiliation |
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Korea. jslee103@snu.ac.kr
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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