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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.
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.
Afiliação
  • Camarillo-López RH; Laboratorio de Biofísica y biocatálisis, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Diaz Mirón s/n, 11340 Ciudad de México, Mexico.
  • Hernández Rodríguez M; Laboratorio de Biofísica y biocatálisis, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Diaz Mirón s/n, 11340 Ciudad de México, Mexico.
  • Torres-Ramos MA; Unidad Periférica de Neurociencias, Facultad de Medicina UNAM-Instituto Nacional de Neurología y Neurocirugía, MVS-SSA, Insurgentes sur 3877, La Fama, Tlalpan, 14269 Ciudad de México, Mexico.
  • Arciniega-Martínez IM; Laboratorio de Inmunidad de Mucosas, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón s/n, 11340 Ciudad de México, Mexico.
  • García-Marín ID; Laboratorio de Biofísica y biocatálisis, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Diaz Mirón s/n, 11340 Ciudad de México, Mexico.
  • Correa Basurto J; Laboratorio de Diseño y Desarrollo de Nuevos Fármacos e Innovación Biotecnológica, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón, 11340 Ciudad de México, Mexico.
  • Méndez Méndez JV; Centro de Nanociencias y Micro y Nanotecnologías, Instituto Politécnico Nacional. Av. Luis Enrique Erro s/n, Nueva Industrial Vallejo, Gustavo A. Madero, 07738 Ciudad de México, Mexico.
  • Rosales-Hernández MC; Laboratorio de Biofísica y biocatálisis, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Diaz Mirón s/n, 11340 Ciudad de México, Mexico.
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fragmentos de Peptídeos / Escopolamina / Carbamatos / Astrócitos / Peptídeos beta-Amiloides / Fármacos Neuroprotetores / Doença de Alzheimer Limite: Animals / 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

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fragmentos de Peptídeos / Escopolamina / Carbamatos / Astrócitos / Peptídeos beta-Amiloides / Fármacos Neuroprotetores / Doença de Alzheimer Limite: Animals / 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