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Screening of Non‐Alkaloidal Natural Compounds as Acetylcholinesterase Inhibitors
Author(s) -
Brühlmann Corinne,
Marston Andrew,
Hostettmann Kurt,
Carrupt PierreAlain,
Testa Bernard
Publication year - 2004
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200490064
Subject(s) - chemistry , acetylcholinesterase , natural (archaeology) , organic chemistry , stereochemistry , enzyme , biology , paleontology
Acetylcholinesterase (AChE) inhibitors are currently the only approved therapy for the treatment of Alzheimer 's disease, only a limited number of drugs are commercially available. A library of non‐alkaloidal natural compounds was investigated. To this end, a convenient microtitre plate method for assaying AChE inhibition, which allows a complete kinetic analysis of AChE inhibitors, was developed. Seven active compounds with K i values in the micromolar range were identified, six of which were xanthones. This is the first report that a promising potential for AChE inhibition exists in such non‐nitrogenous natural compounds. Furthermore, four xanthones among these xanthones had already been described as monoamine oxidase (MAO) inhibitors, making then dual AChE/MAO inhibitors of great interest.