Screening of Non‐Alkaloidal Natural Compounds as Acetylcholinesterase Inhibitors

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.