Document Detail

Novel and potent inhibitors of fatty acid synthase derived from catechins and their inhibition on MCF-7 cells.
MedLine Citation:
PMID:  18671164     Owner:  NLM     Status:  MEDLINE    
Fatty acid synthase (FAS) is a potential target for cancer, but potent inhibitors against FAS are scarce. In this study, we found that activities of catechins on inhibiting FAS increased greatly by heating them in acid. The enhancement was positively correlated to H(+) concentration. The inhibitory activities of the final products from different catechins were similar, all of which were less than 1 microg/mL. The product from (-)-epigallocatechin gallate (EGCG) was stable at room temperature, and its inhibitory kinetics and reacting sites on FAS were obviously different from the known FAS inhibitors. It also affected the viability of MCF-7 cells more obviously than EGCG. A putative route of the reaction progress was proposed and the effective inhibitors were deduced to be oligomers of 2-hydroxy-3-(3', 4', 5'-trihydroxyphenyl) propenoic acid by analysis of their spectra. The work affords new and potent FAS inhibitors that would be promising candidates for the treatment of cancer.
Shu-Yan Zhang; Xiao-Feng Ma; Chao-Gu Zheng; Yan Wang; Xue-Li Cao; Wei-Xi Tian
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of enzyme inhibition and medicinal chemistry     Volume:  24     ISSN:  1475-6374     ISO Abbreviation:  J Enzyme Inhib Med Chem     Publication Date:  2009 Jun 
Date Detail:
Created Date:  2010-04-08     Completed Date:  2010-10-12     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101150203     Medline TA:  J Enzyme Inhib Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  623-31     Citation Subset:  IM    
College of Life Science, Graduate University of Chinese Academy of Sciences, Beijing, P.R. China.
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MeSH Terms
Breast Neoplasms / drug therapy*,  pathology
Catechin / analogs & derivatives*,  chemistry,  pharmacology*,  therapeutic use
Cell Line, Tumor
Enzyme Inhibitors / chemical synthesis,  chemistry,  pharmacology*,  therapeutic use
Fatty Acid Synthetase Complex / antagonists & inhibitors*
Hydrochloric Acid / chemistry
Inhibitory Concentration 50
Propionic Acids / chemistry
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Sulfuric Acids / chemistry
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Propionic Acids; 0/Sulfuric Acids; 154-23-4/Catechin; 7647-01-0/Hydrochloric Acid; 7664-93-9/sulfuric acid; 989-51-5/epigallocatechin gallate; EC 6.-/Fatty Acid Synthetase Complex

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