Alkaloids from stems of Esenbeckia leiocarpa Engl. (Rutaceae) as potential treatment for Alzheimer disease

Molecules. 2010 Dec 13;15(12):9205-13. doi: 10.3390/molecules15129205.

Abstract

Esenbeckia leiocarpa Engl. (Rutaceae), popularly known as guarantã, goiabeira, is a native tree from Brazil. Bioactivity-guided fractionation of the ethanol stems extract afforded the isolation of six alkaloids: leiokinine A, leptomerine, kokusaginine, skimmianine, maculine and flindersiamine. All isolated compounds were tested for acetyl cholinesterase inhibition, in vitro and displayed anticholinesterasic activity. The alkaloid leptomerine showed the highest activity (IC₅₀ = 2.5 mM), similar to that of the reference compound galanthamine (IC₅₀ = 1.7 mM). The results showed for the first time the presence of alkaloids leptomerine and skimmianine in E. leiocarpa (Engl.) with potent anticholinesterasic activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / metabolism
  • Alkaloids* / chemistry
  • Alkaloids* / isolation & purification
  • Alkaloids* / pharmacology
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / enzymology
  • Animals
  • Artemia / enzymology
  • Brazil
  • Cholinesterase Inhibitors* / chemistry
  • Cholinesterase Inhibitors* / isolation & purification
  • Cholinesterase Inhibitors* / pharmacology
  • Humans
  • Plant Stems / chemistry*
  • Rutaceae / chemistry*

Substances

  • Alkaloids
  • Cholinesterase Inhibitors
  • Acetylcholinesterase