title: Effect of isoquinoline alkaloids from two Hippeastrum species on in vitro acetylcholinesterase activity.
abstract: The treatment of neurological disorders and neurodegenerative diseases is related to the levels of acetylcholine (ACh) through the inhibition of acetylcholinesterase (AChE). Galanthamine, an important alkaloid isolated from the Amaryllidaceae family, is approved for the pharmacological treatment of Alzheimer's disease (AD) and acts by inhibiting the acetylcholinesterase (AChE) activity. In the present study, Ellman's method was used to verify the inhibition of AChE activity of some isoquinolines alkaloids such as galanthamine, montanine, hippeastrine and pretazettine. At the concentrations 1mM, 500 microm and 100 microm, galanthamine presented an AChE inhibition higher than 90%. Montanine inhibited, in a dose-dependent manner, more than 50% of the enzyme at 1mM concentration. With the concentrations 500 microm and 100 microm, 30-45% of AChE activity inhibition was detected. The alkaloids hippeastrine and pretazettine presented no significant inhibition of the AChE activity. The results demonstrate that montanine significantly inhibits AChE activity at the tested concentrations, suggesting the necessity of further investigations on this alkaloid use in treating neurological disorders.
authors.affiliation: Programa de Pós-graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, 90610-000 Porto Alegre, RS, Brazil.
authors.forename: L B
authors.initials: LB
authors.lastname: Pagliosa
authors.forename: S C
authors.initials: SC
authors.lastname: Monteiro
authors.forename: K B
authors.initials: KB
authors.lastname: Silva
authors.forename: J P
authors.initials: JP
authors.lastname: de Andrade
authors.forename: J
authors.initials: J
authors.lastname: Dutilh
authors.forename: J
authors.initials: J
authors.lastname: Bastida
authors.forename: M
authors.initials: M
authors.lastname: Cammarota
authors.forename: J A S
authors.initials: JA
authors.lastname: Zuanazzi
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000470:Alkaloids / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007546:Isoquinolines / Q000494:pharmacology*; D019668:Liliaceae / Q000737:chemistry*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018517:Plant Roots
chemical_list: D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D007546:Isoquinolines; D010936:Plant Extracts; C517208:montanine; D000110:Acetylcholinesterase