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Screening of non-alkaloidal natural compounds as acetylcholinesterase inhibitors

Brehlmann, Corinne
Marston, Andrew
Testa, Bernard
Published in Chemistry and Biodiversity. 2004, vol. 1, no. 6, p. 819-829
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 Ki 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.
Keywords Acetylcholinesterase/metabolismAlkaloids/*chemistry/isolation & purification/pharmacokineticsAnimalsBiological Products/*chemistry/isolation & purification/pharmacokineticsCholinesterase Inhibitors/*chemistry/isolation &Purification/pharmacokineticsDrug Evaluation, Preclinical/methodsEels
PMID: 17191882
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BREHLMANN, Corinne et al. Screening of non-alkaloidal natural compounds as acetylcholinesterase inhibitors. In: Chemistry and Biodiversity, 2004, vol. 1, n° 6, p. 819-829. doi: 10.1002/cbdv.200490064 https://archive-ouverte.unige.ch/unige:10544

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Deposited on : 2010-08-06

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