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Benzofurans from Styrax agrestis As Acetylcholinesterase Inhibitors: Structure-Activity Relationships and Molecular Modeling Studies.
MedLine Citation:
PMID:  21939219     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
An extract of Styrax agrestis fruits, collected in Vietnam, significantly inhibited acetylcholinesterase (AChE) in vitro. Bioassay-guided fractionation revealed three new egonol-type benzofurans: egonol-9(Z),12(Z) linoleate (1), 7-demethoxyegonol-9(Z),12(Z) linoleate (2), and 7-demethoxyegonol oleate (4). Ten known egonol-type benzofurans were also isolated (3, 5, 6-13). In order to better understand structure-activity relationships in this series, egonol derivatives 14-19 were prepared by chemical modifications and evaluated for their inhibition of AChE, butyrylcholinesterase (BChE), and AChE-induced Aβ aggregation. Compounds 1-4 were the most potent inhibitors of the series, which exhibited inhibitory activity against AChE (IC(50) 1.4-3.1 μM) and, for 1, Aβ aggregation (77.6%). Molecular docking studies were also performed to investigate interaction of these compounds with the active site of AChE.
Authors:
Jiawei Liu; Vincent Dumontet; Anne-Laure Simonin; Bogdan I Iorga; Vincent Guerineau; Marc Litaudon; Van Hung Nguyen; Françoise Gueritte
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-9-22
Journal Detail:
Title:  Journal of natural products     Volume:  -     ISSN:  1520-6025     ISO Abbreviation:  -     Publication Date:  2011 Sep 
Date Detail:
Created Date:  2011-9-23     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7906882     Medline TA:  J Nat Prod     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Research Center of Medicinal Plants Resource Science and Engineering, Guangzhou University of Chinese Medicine , 232 Waihuandong Road, Higher Education Mega Center, Guangzhou 510006, People's Republic of China.
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