Liu_2011_J.Nat.Prod_74_2081

Reference

Title : Benzofurans from Styrax agrestis as acetylcholinesterase inhibitors: structure-activity relationships and molecular modeling studies - Liu_2011_J.Nat.Prod_74_2081
Author(s) : Liu J , Dumontet V , Simonin AL , Iorga BI , Guerineau V , Litaudon M , Nguyen VH , Gueritte F
Ref : Journal of Natural Products , 74 :2081 , 2011
Abstract :

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 Abeta aggregation. Compounds 1-4 were the most potent inhibitors of the series, which exhibited inhibitory activity against AChE (IC50 1.4-3.1 muM) and, for 1, Abeta aggregation (77.6%). Molecular docking studies were also performed to investigate interaction of these compounds with the active site of AChE.

PubMedSearch : Liu_2011_J.Nat.Prod_74_2081
PubMedID: 21939219

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Citations formats

Liu J, Dumontet V, Simonin AL, Iorga BI, Guerineau V, Litaudon M, Nguyen VH, Gueritte F (2011)
Benzofurans from Styrax agrestis as acetylcholinesterase inhibitors: structure-activity relationships and molecular modeling studies
Journal of Natural Products 74 :2081

Liu J, Dumontet V, Simonin AL, Iorga BI, Guerineau V, Litaudon M, Nguyen VH, Gueritte F (2011)
Journal of Natural Products 74 :2081