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Molecules 2016, 21(1), 53; doi:10.3390/molecules21010053

Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina

1
Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil
2
Department of Biology, Federal University of Mato Grosso do Sul (UFMS), Av. Senador Filinto Müller, Campo Grande 79046-460, Brazil
3
Post-Graduation in Health Sciences, Pontíficia Universidade Católica do Paraná, Imaculada Conceição, 1155, Prado Velho, Curitiba 80215-901, Brazil
4
Department of Celular Biology, Federal University of Paraná (UFPR), Centro Politécnico, Jardim das Américas, Curitiba 81530-900, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: D. Hadjipavlou-Litina
Received: 25 May 2015 / Revised: 26 July 2015 / Accepted: 15 September 2015 / Published: 11 January 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1353 KB, uploaded 11 January 2016]   |  

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. View Full-Text
Keywords: Alzheimer’s disease; anticholinesterasic; convulsant activity; spontaneous locomotion; planarian Alzheimer’s disease; anticholinesterasic; convulsant activity; spontaneous locomotion; planarian
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Bezerra da Silva, C.; Pott, A.; Elifio-Esposito, S.; Dalarmi, L.; Fialho do Nascimento, K.; Moura Burci, L.; de Oliveira, M.; de Fátima Gaspari Dias, J.; Maria Warumby Zanin, S.; Gomes Miguel, O.; Dallarmi Miguel, M. Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina. Molecules 2016, 21, 53.

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