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Screening of Non-Alkaloidal Natural Compounds as Acetylcholinesterase Inhibitors

✍ Scribed by Corinne Brühlmann; Andrew Marston; Kurt Hostettmann; Pierre-Alain Carrupt; Bernard Testa

Publisher
John Wiley and Sons
Year
2004
Tongue
English
Weight
194 KB
Volume
1
Category
Article
ISSN
1612-1872

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✦ Synopsis

Abstract

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.

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