title: Investigation of the in vitro and ex vivo acetylcholinesterase and antioxidant activities of traditionally used Lycopodium species from South America on alkaloid extracts.
abstract: BACKGROUND
  The study was aimed at evaluating medicinal and therapeutic potentials of two Lycopodiaceae species, Lycopodium clavatum (L.) and Lycopodium thyoides (Humb. & Bonpl. ex Willd), both used in South American folk medicine for central nervous system conditions. Alkaloid extracts were evaluated for chemical characterization, acetylcholinesterase and antioxidant activities.
  
  
  METHODS
  The alkaloid extracts obtained by alkaline extraction were determined for each species by GC/MS examination. The evaluation of the anticholinesterase and the antioxidant activities of the extracts were tested by determining in vitro and ex vivo models. Effects on acetylcholinesterase (AChE) were tested in vitro using rat brain homogenates and ex vivo after a single administration (25, 10 and 1mg/kg i.p.) of the alkaloid extracts in mice. The in vitro antioxidant effects were tested for the 2-deoxyribose degradation, nitric oxide (NO) interaction, 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical scavenging activity and total reactive antioxidant potential (TRAP). After an acute administration (25 and 10mg/kg i.p.) of the extracts in middle-aged (12 months) mice, the antioxidant effects were estimated through the thiobarbituric acid reactive substances test (TBARS), and the antioxidant enzymes activities for catalase (CAT) and superoxide dismutase (SOD) were measured.
  
  
  RESULTS
  AChE activity was inhibited in vitro by the alkaloid-enriched extracts of both Lycopodium species in a dose and time-dependent manner in rat cortex, striatum and hippocampus. A significant inhibition was also observed in areas of the brain after acute administration of extracts, as well as decreased lipid peroxidation and increased CAT activity in the cortex, hippocampus and cerebellum. A moderate antioxidant activity was observed in vitro for the extracts. Chemically, the main alkaloids found for the two species were lycopodine and acetyldihidrolycopodine.
  
  
  CONCLUSIONS
  This study showed that the biological properties of the folk medicinal plants Lycopodium clavatum and Lycopodium thyoides include AChE inhibitory activity and antioxidant effects, two possible mechanisms of action in Alzheimer's related processes.
authors: Programa de Pós Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Av Ipiranga, 2752 90610-000, Porto Alegre - RS, Brazil. edukonrath@yahoo.com.br
authors: Eduardo Luis
authors: EL
authors: Konrath
authors: Bruna Medeiros
authors: BM
authors: Neves
authors: Paula Santana
authors: PS
authors: Lunardi
authors: Carolina Dos Santos
authors: Cdos S
authors: Passos
authors: André
authors: A
authors: Simões-Pires
authors: María Gabriela
authors: MG
authors: Ortega
authors: Carlos Alberto
authors: CA
authors: Gonçalves
authors: José L
authors: JL
authors: Cabrera
authors: José Cláudio Fonseca
authors: JC
authors: Moreira
authors: Amélia T
authors: AT
authors: Henriques
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism; D000818:Animals; D000975:Antioxidants / Q000302:isolation & purification / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D002800:Cholinesterase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D003855:Deoxyribose / Q000378:metabolism; D015227:Lipid Peroxidation / Q000187:drug effects; D032502:Lycopodium / Q000737:chemistry; D008297:Male; D008519:Medicine, Traditional; D051379:Mice; D009569:Nitric Oxide / Q000378:metabolism; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013020:South America
chemical_list: D000975:Antioxidants; D002800:Cholinesterase Inhibitors; D010936:Plant Extracts; D009569:Nitric Oxide; D003855:Deoxyribose; D000110:Acetylcholinesterase