Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6185-7. doi: 10.1016/j.bmcl.2010.08.123. Epub 2010 Aug 31.

Abstract

Through bioassay-guided fractionation and chromatography technique, eight indole alkaloids were furnished from the stems of Ervatamia hainanensis. All isolates were evaluated for acetylcholinesterase (AChE) inhibition activities, in which compounds 1 and 3 exhibited the same level of activities as galantamine, a marketed cholinesterase inhibitor for the treatment of Alzheimer's disease. Discussion about the relationships between structure and activity of these alkaloids was also presented.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / metabolism
  • Alkaloids / isolation & purification
  • Alkaloids / pharmacology*
  • Animals
  • Apocynaceae / chemistry*
  • Cholinesterase Inhibitors / isolation & purification
  • Cholinesterase Inhibitors / pharmacology*
  • Galantamine / pharmacology
  • Hydrogen Bonding
  • Indoles / isolation & purification
  • Indoles / pharmacology*
  • Models, Molecular
  • Molecular Conformation
  • Torpedo
  • X-Ray Diffraction

Substances

  • Alkaloids
  • Cholinesterase Inhibitors
  • Indoles
  • Galantamine
  • Acetylcholinesterase