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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...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2016
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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 |
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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 |
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