title: Alkaloids from stems of Esenbeckia leiocarpa Engl. (Rutaceae) as potential treatment for Alzheimer disease.
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.
authors.affiliation: Section of Plant Physiology and Biochemistry, Institute of Botany, Box 3005, 01061-970 São Paulo, SP, Brazil.
authors.forename: Elaine Monteiro
authors.initials: EM
authors.lastname: Cardoso-Lopes
authors.forename: James Andreas
authors.initials: JA
authors.lastname: Maier
authors.forename: Marcelo Rogério
authors.initials: MR
authors.lastname: da Silva
authors.forename: Luis Octávio
authors.initials: LO
authors.lastname: Regasini
authors.forename: Simone Yasue
authors.initials: SY
authors.lastname: Simote
authors.forename: Norberto Peporine
authors.initials: NP
authors.lastname: Lopes
authors.forename: José Rubens
authors.initials: JR
authors.lastname: Pirani
authors.forename: Vanderlan da Silva
authors.initials: Vda S
authors.lastname: Bolzani
authors.forename: Maria Cláudia Marx
authors.initials: MC
authors.lastname: Young
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism; D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000544:Alzheimer Disease / Q000188:drug therapy* / Q000201:enzymology; D000818:Animals; D001156:Artemia / Q000201:enzymology; D001938:Brazil; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D018547:Plant Stems / Q000737:chemistry*; D027821:Rutaceae / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D000110:Acetylcholinesterase