Cargando…

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

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 ac...

Descripción completa

Detalles Bibliográficos
Autores principales: Bezerra da Silva, Cristiane, Pott, Arnildo, Elifio-Esposito, Selene, Dalarmi, Luciane, Fialho do Nascimento, Kátia, Moura Burci, Ligia, de Oliveira, Maislian, de Fátima Gaspari Dias, Josiane, Maria Warumby Zanin, Sandra, Gomes Miguel, Obdulio, Dallarmi Miguel, Marilis
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273381/
https://www.ncbi.nlm.nih.gov/pubmed/26760993
http://dx.doi.org/10.3390/molecules21010053
_version_ 1783377371428028416
author Bezerra da Silva, Cristiane
Pott, Arnildo
Elifio-Esposito, Selene
Dalarmi, Luciane
Fialho do Nascimento, Kátia
Moura Burci, Ligia
de Oliveira, Maislian
de Fátima Gaspari Dias, Josiane
Maria Warumby Zanin, Sandra
Gomes Miguel, Obdulio
Dallarmi Miguel, Marilis
author_facet Bezerra da Silva, Cristiane
Pott, Arnildo
Elifio-Esposito, Selene
Dalarmi, Luciane
Fialho do Nascimento, Kátia
Moura Burci, Ligia
de Oliveira, Maislian
de Fátima Gaspari Dias, Josiane
Maria Warumby Zanin, Sandra
Gomes Miguel, Obdulio
Dallarmi Miguel, Marilis
author_sort Bezerra da Silva, Cristiane
collection PubMed
description 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.
format Online
Article
Text
id pubmed-6273381
institution National Center for Biotechnology Information
language English
publishDate 2016
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-62733812018-12-28 Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina Bezerra da Silva, Cristiane Pott, Arnildo Elifio-Esposito, Selene Dalarmi, Luciane Fialho do Nascimento, Kátia Moura Burci, Ligia de Oliveira, Maislian de Fátima Gaspari Dias, Josiane Maria Warumby Zanin, Sandra Gomes Miguel, Obdulio Dallarmi Miguel, Marilis Molecules Article 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. MDPI 2016-01-11 /pmc/articles/PMC6273381/ /pubmed/26760993 http://dx.doi.org/10.3390/molecules21010053 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons by Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Bezerra da Silva, Cristiane
Pott, Arnildo
Elifio-Esposito, Selene
Dalarmi, Luciane
Fialho do Nascimento, Kátia
Moura Burci, Ligia
de Oliveira, Maislian
de Fátima Gaspari Dias, Josiane
Maria Warumby Zanin, Sandra
Gomes Miguel, Obdulio
Dallarmi Miguel, Marilis
Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina
title Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina
title_full Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina
title_fullStr Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina
title_full_unstemmed Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina
title_short Effect of Donepezil, Tacrine, Galantamine and Rivastigmine on Acetylcholinesterase Inhibition in Dugesia tigrina
title_sort effect of donepezil, tacrine, galantamine and rivastigmine on acetylcholinesterase inhibition in dugesia tigrina
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273381/
https://www.ncbi.nlm.nih.gov/pubmed/26760993
http://dx.doi.org/10.3390/molecules21010053
work_keys_str_mv AT bezerradasilvacristiane effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT pottarnildo effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT elifioespositoselene effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT dalarmiluciane effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT fialhodonascimentokatia effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT mouraburciligia effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT deoliveiramaislian effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT defatimagasparidiasjosiane effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT mariawarumbyzaninsandra effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT gomesmiguelobdulio effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina
AT dallarmimiguelmarilis effectofdonepeziltacrinegalantamineandrivastigmineonacetylcholinesteraseinhibitionindugesiatigrina