title: Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina.
abstract: Dugesia tigrina is a non-parasitic platyhelminth, which has been recently utilized in pharmacological models, regarding the nervous system, as it presents a wide sensitivity to drugs. Our trials aimed to propose a model for an in vivo screening of substances with inhibitory activity of the enzyme acetylcholinesterase. Trials were performed with four drugs commercialized in Brazil: donepezil, tacrine, galantamine and rivastigmine, utilized in the control of Alzheimer's disease, to inhibit the activity of acetylcholinesterase. We tested five concentrations of the drugs, with an exposure of 24 h, and the mortality and the inhibition of acetylcholinesterase planarian seizure-like activity (pSLA) and planarian locomotor velocity (pLMV) were measured. Galantamine showed high anticholinesterasic activity when compared to the other drugs, with a reduction of 0.05 μmol·min(-1) and 63% of convulsant activity, presenting screw-like movement and hypokinesia, with pLMV of 65 crossed lines during 5 min. Our results showed for the first time the anticholinesterasic and convulsant effect, in addition to the decrease in locomotion induced by those drugs in a model of invertebrates. The experimental model proposed is simple and low cost and could be utilized in the screening of substances with anticholinesterasic action.
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. cris.mpj@gmail.com.
authors.forename: Cristiane
authors.initials: C
authors.lastname: Bezerra da Silva
authors.affiliation: Department of Biology, Federal University of Mato Grosso do Sul (UFMS), Av. Senador Filinto Müller, Campo Grande 79046-460, Brazil. arnildopott@gmail.com.
authors.forename: Arnildo
authors.initials: A
authors.lastname: Pott
authors.affiliation: Post-Graduation in Health Sciences, Pontíficia Universidade Católica do Paraná, Imaculada Conceição, 1155, Prado Velho, Curitiba 80215-901, Brazil. seleneesposito@gmail.com.
authors.forename: Selene
authors.initials: S
authors.lastname: Elifio-Esposito
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. ludalarmi@gmail.com.
authors.forename: Luciane
authors.initials: L
authors.lastname: Dalarmi
authors.affiliation: Department of Celular Biology, Federal University of Paraná (UFPR), Centro Politécnico, Jardim das Américas, Curitiba 81530-900, Brazil. kafialho@hotmail.com.
authors.forename: Kátia
authors.initials: K
authors.lastname: Fialho do Nascimento
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. ligia.burci@gmail.com.
authors.forename: Ligia
authors.initials: L
authors.lastname: Moura Burci
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. maislian@gmail.com.
authors.forename: Maislian
authors.initials: M
authors.lastname: de Oliveira
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. jodias@pop.com.br.
authors.forename: Josiane
authors.initials: J
authors.lastname: de Fátima Gaspari Dias
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. sandramariazanin@gmail.com.
authors.forename: Sandra Maria
authors.initials: SM
authors.lastname: Warumby Zanin
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. obdulio@ufpr.br.
authors.forename: Obdulio
authors.initials: O
authors.lastname: Gomes Miguel
authors.affiliation: Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil. dallarmi@ufpr.br.
authors.forename: Marilis
authors.initials: M
authors.lastname: Dallarmi Miguel
mesh_terms: D000818:Animals; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D003292:Convulsants / Q000494:pharmacology*; D000077265:Donepezil; D005702:Galantamine / Q000494:pharmacology*; D007189:Indans / Q000494:pharmacology*; D008124:Locomotion / Q000187:drug effects; D008954:Models, Biological; D010880:Piperidines / Q000494:pharmacology*; D010932:Planarians / Q000187:drug effects / Q000201:enzymology; D000068836:Rivastigmine / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced; D015996:Survival Rate; D013619:Tacrine / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D003292:Convulsants; D007189:Indans; D010880:Piperidines; D005702:Galantamine; D013619:Tacrine; D000077265:Donepezil; D000068836:Rivastigmine
keywords: Alzheimer’s disease; anticholinesterasic; convulsant activity; planarian; spontaneous locomotion