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Nostocarboline: isolation and synthesis of a new cholinesterase inhibitor from Nostoc 78-12A.
Journal article

Nostocarboline: isolation and synthesis of a new cholinesterase inhibitor from Nostoc 78-12A.

  • 2005-12-28
Published in:
  • Journal of natural products. - 2005
Brain
Butyrylcholinesterase
Carbolines
Cholinesterase Inhibitors
Galantamine
Humans
Inhibitory Concentration 50
Molecular Structure
Nostoc
Parkinson Disease
English A new quaternary beta-carboline alkaloid, nostocarboline, was isolated from the freshwater cyanobacterium Nostoc 78-12A, and its constitution was assigned by 2D-NMR methods. The structure was proven by its total synthesis starting from norharmane via chlorination at C-6 and methylation at N-2. Nostocarboline was found to be a potent butyrylcholinesterase (BChE) inhibitor, with an IC(50) of 13.2 microM. The related 2-methylnorharmane, which is present in the human brain and might be relevant to Parkinson's disease (PD), was also determined to be a BChE inhibitor (11.2 microM). These inhibitory concentrations are comparable to galanthamine, an approved drug for the treatment of Alzheimer's disease (AD). Nostocarboline can thus be considered as a lead for the development of novel neurochemicals.
Language
  • English
Open access status
closed
Identifiers
Persistent URL
https://sonar.ch/global/documents/163536
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