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.
Molecules
; 25(21)2020 Oct 29.
Article
em En
| MEDLINE
| ID: mdl-33137907
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 ß-secretase and an acetylcholinesterase inhibitor, preventing the amyloid beta peptide (Aß) aggregation and the formation of fibrils (fAß) from Aß1-42. This work first aimed to assess in in vitro studies to see whether the death of astrocyte cells promoted by Aß1-42 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 Aß1-42 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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fragmentos de Peptídeos
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Escopolamina
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Carbamatos
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Astrócitos
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Peptídeos beta-Amiloides
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Fármacos Neuroprotetores
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Doença de Alzheimer
Limite:
Animals
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Humans
Idioma:
En
Revista:
Molecules
Assunto da revista:
BIOLOGIA
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
México
País de publicação:
Suíça