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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...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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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. |
format | Online Article Text |
id | pubmed-7672627 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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