title: Triclisia sacleuxii (Pierre) Diels (Menispermaceae), a potential source of acetylcholinesterase inhibitors.
abstract: OBJECTIVE
  To search for compounds possibly useful for the treatment of Alzheimer's disease.
  
  
  METHODS
  Alkaloid fractions from the roots, stems and leaves of Triclisia sacleuxii (Menispermaceae) and pure bisbenzylisoquinoline alkaloids isolated from the roots (phaeanthine, N-methylapateline, 1,2-dehydroapateline and gasabiimine) were assessed for acetylcholinesterase inhibitory activity.
  
  
  RESULTS
  All extracts and compounds tested inhibited acetylcholinesterase to varying degrees; the leaf tertiary alkaloid fractions and the root quaternary alkaloid fractions exhibited the strongest inhibitory potential (90% at 0.1 mg/ml). The leaf tertiary alkaloid fraction was selected for further analysis (the quaternary alkaloids, which are too polar for absorption and brain distribution, were presumed to be clinically uninteresting). TLC bioautography using Ellman's reagent allowed the detection of acetylcholinesterase inhibitors and the isolation of the major active constituent, which was identified as lindoldhamine, a one-bridged bisbenzylisoquinoline alkaloid. Lindoldhamine displayed high acetylcholinesterase inhibitory activity with a 50% inhibition concentration in the micromolar range.
  
  
  CONCLUSIONS
  All T. sacleuxii alkaloid fractions tested exhibited anti-acetylcholinesterase activity; isolated bisbenzylisoquinoline alkaloids showed weak-to-high inhibition depending on their structural features. Structure modification could provide interesting derivatives with enhanced anti-acetylcholinesterase activity.
authors.affiliation: Laboratory of Pharmacognosy, Bromatology and Human Nutrition, Institute of Pharmacy, Free University of Brussels (ULB), Brussels, Belgium.
authors.forename: Sengabo
authors.initials: S
authors.lastname: Murebwayire
authors.forename: Kornkanok
authors.initials: K
authors.lastname: Ingkaninan
authors.forename: Kanokwan
authors.initials: K
authors.lastname: Changwijit
authors.forename: Michel
authors.initials: M
authors.lastname: Frédérich
authors.forename: Pierre
authors.initials: P
authors.lastname: Duez
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000544:Alzheimer Disease / Q000188:drug therapy / Q000201:enzymology; D044182:Benzylisoquinolines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005591:Chemical Fractionation / Q000379:methods; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D029583:Menispermaceae / Q000737:chemistry*; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry; D018517:Plant Roots / Q000737:chemistry; D018547:Plant Stems / Q000737:chemistry
chemical_list: D000470:Alkaloids; D044182:Benzylisoquinolines; D002800:Cholinesterase Inhibitors; D010936:Plant Extracts; C038606:phaeanthrine