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Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model

Alzheimer’s disease (AD) is a neurodegenerative disease with no cure nowadays; there is no treatment either to prevent or to stop its progression. In vitro studies suggested that tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl) carbamate named the M4 compound can act as bot...

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Autores principales: Camarillo-López, Raúl Horacio, Hernández Rodríguez, Maricarmen, Torres-Ramos, Mónica Adriana, Arciniega-Martínez, Ivonne Maciel, García-Marín, Iohanan Daniel, Correa Basurto, José, Méndez Méndez, Juan Vicente, Rosales-Hernández, Martha Cecilia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7672627/
https://www.ncbi.nlm.nih.gov/pubmed/33137907
http://dx.doi.org/10.3390/molecules25215009
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author Camarillo-López, Raúl Horacio
Hernández Rodríguez, Maricarmen
Torres-Ramos, Mónica Adriana
Arciniega-Martínez, Ivonne Maciel
García-Marín, Iohanan Daniel
Correa Basurto, José
Méndez Méndez, Juan Vicente
Rosales-Hernández, Martha Cecilia
author_facet Camarillo-López, Raúl Horacio
Hernández Rodríguez, Maricarmen
Torres-Ramos, Mónica Adriana
Arciniega-Martínez, Ivonne Maciel
García-Marín, Iohanan Daniel
Correa Basurto, José
Méndez Méndez, Juan Vicente
Rosales-Hernández, Martha Cecilia
author_sort Camarillo-López, Raúl Horacio
collection PubMed
description Alzheimer’s disease (AD) is a neurodegenerative disease with no cure nowadays; there is no treatment either to prevent or to stop its progression. In vitro studies suggested that tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl) carbamate named the M4 compound can act as both β-secretase and an acetylcholinesterase inhibitor, preventing the amyloid beta peptide (Aβ) aggregation and the formation of fibrils (fAβ) from Aβ(1-42). This work first aimed to assess in in vitro studies to see whether the death of astrocyte cells promoted by Aβ(1-42) could be prevented. Second, our work investigated the ability of the M4 compound to inhibit amyloidogenesis using an in vivo model after scopolamine administration. The results showed that M4 possesses a moderate protective effect in astrocytes against Aβ(1-42) due to a reduction in the TNF-α and free radicals observed in cell cultures. In the in vivo studies, however, no significant effect of M4 was observed in comparison with a galantamine model employed in rats, in which case this outcome was attributed to the bioavailability of M4 in the brain of the rats.
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spelling pubmed-76726272020-11-19 Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model Camarillo-López, Raúl Horacio Hernández Rodríguez, Maricarmen Torres-Ramos, Mónica Adriana Arciniega-Martínez, Ivonne Maciel García-Marín, Iohanan Daniel Correa Basurto, José Méndez Méndez, Juan Vicente Rosales-Hernández, Martha Cecilia Molecules Article Alzheimer’s disease (AD) is a neurodegenerative disease with no cure nowadays; there is no treatment either to prevent or to stop its progression. In vitro studies suggested that tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl) carbamate named the M4 compound can act as both β-secretase and an acetylcholinesterase inhibitor, preventing the amyloid beta peptide (Aβ) aggregation and the formation of fibrils (fAβ) from Aβ(1-42). This work first aimed to assess in in vitro studies to see whether the death of astrocyte cells promoted by Aβ(1-42) could be prevented. Second, our work investigated the ability of the M4 compound to inhibit amyloidogenesis using an in vivo model after scopolamine administration. The results showed that M4 possesses a moderate protective effect in astrocytes against Aβ(1-42) due to a reduction in the TNF-α and free radicals observed in cell cultures. In the in vivo studies, however, no significant effect of M4 was observed in comparison with a galantamine model employed in rats, in which case this outcome was attributed to the bioavailability of M4 in the brain of the rats. MDPI 2020-10-29 /pmc/articles/PMC7672627/ /pubmed/33137907 http://dx.doi.org/10.3390/molecules25215009 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Camarillo-López, Raúl Horacio
Hernández Rodríguez, Maricarmen
Torres-Ramos, Mónica Adriana
Arciniega-Martínez, Ivonne Maciel
García-Marín, Iohanan Daniel
Correa Basurto, José
Méndez Méndez, Juan Vicente
Rosales-Hernández, Martha Cecilia
Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model
title Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model
title_full Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model
title_fullStr Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model
title_full_unstemmed Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model
title_short Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model
title_sort tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate has moderated protective activity in astrocytes stimulated with amyloid beta 1-42 and in a scopolamine model
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7672627/
https://www.ncbi.nlm.nih.gov/pubmed/33137907
http://dx.doi.org/10.3390/molecules25215009
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