In vitro anticholinesterase activity of various alkaloids

Z Naturforsch C J Biosci. 2007 Sep-Oct;62(9-10):684-8. doi: 10.1515/znc-2007-9-1010.

Abstract

In the current study, a number of alkaloids including retamine, cytisine, and sparteine (quinolizidine-type), yohimbine and vincamine (indole-type), scopolamine and atropine (tropane-type), colchicine (tropolone-type), allantoin (imidazolidine-type), trigonelline (pyridine-type) as well as octopamine, synephrine, and capsaicin (exocyclic amine-type) were tested in vitro for their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) at 1 mg/ml concentration by the Ellman method using an ELISA microplate reader. Among the alkaloids tested, only capsaicin exerted a remarkable inhibitory effect towards both AChE and BChE [(62.7 +/- 0.79)% and (75.3 +/- 0.98)%, respectively]. While the rest of the alkaloids did not show any significant inhibition against AChE, three of the alkaloids, namely retamine, sparteine, and yohimbine, exerted a noteworthy anti-BChE effect as compared to galanthamine, the reference drug.

MeSH terms

  • Acetylcholinesterase / drug effects
  • Acetylcholinesterase / metabolism
  • Alkaloids / classification
  • Alkaloids / pharmacology*
  • Butyrylcholinesterase / drug effects
  • Butyrylcholinesterase / metabolism
  • Capsaicin / pharmacology
  • Cholinesterase Inhibitors / pharmacology*
  • Kinetics
  • Octopamine / pharmacology
  • Structure-Activity Relationship
  • Synephrine / pharmacology

Substances

  • Alkaloids
  • Cholinesterase Inhibitors
  • Octopamine
  • Acetylcholinesterase
  • Butyrylcholinesterase
  • Synephrine
  • Capsaicin