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Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat
Preclinical and clinical evidence supports melatonin and its analogues as potential treatment for diseases involving cognitive deficit such as Alzheimer’s disease. In this work, we evaluated by in silico studies a set of boron-containing melatonin analogues on MT1 and MT2 receptors. Then, we synthes...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8952423/ https://www.ncbi.nlm.nih.gov/pubmed/35328650 http://dx.doi.org/10.3390/ijms23063229 |
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author | Barrón-González, Mónica Rosales-Hernández, Martha C. Abad-García, Antonio Ocampo-Néstor, Ana L. Santiago-Quintana, José M. Pérez-Capistran, Teresa Trujillo-Ferrara, José G. Padilla-Martínez, Itzia I. Farfán-García, Eunice D. Soriano-Ursúa, Marvin A. |
author_facet | Barrón-González, Mónica Rosales-Hernández, Martha C. Abad-García, Antonio Ocampo-Néstor, Ana L. Santiago-Quintana, José M. Pérez-Capistran, Teresa Trujillo-Ferrara, José G. Padilla-Martínez, Itzia I. Farfán-García, Eunice D. Soriano-Ursúa, Marvin A. |
author_sort | Barrón-González, Mónica |
collection | PubMed |
description | Preclinical and clinical evidence supports melatonin and its analogues as potential treatment for diseases involving cognitive deficit such as Alzheimer’s disease. In this work, we evaluated by in silico studies a set of boron-containing melatonin analogues on MT1 and MT2 receptors. Then, we synthesized a compound (borolatonin) identified as potent agonist. After chemical characterization, its evaluation in a rat model with cognitive deficit showed that it induced ameliorative effects such as those induced by equimolar administration of melatonin in behavioral tests and in neuronal immunohistochemistry assays. Our results suggest the observed effects are by means of action on the melatonin system. Further studies are required to clarify the mechanism(s) of action, as the beneficial effects on disturbed memory by gonadectomy in male rats are attractive. |
format | Online Article Text |
id | pubmed-8952423 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-89524232022-03-26 Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat Barrón-González, Mónica Rosales-Hernández, Martha C. Abad-García, Antonio Ocampo-Néstor, Ana L. Santiago-Quintana, José M. Pérez-Capistran, Teresa Trujillo-Ferrara, José G. Padilla-Martínez, Itzia I. Farfán-García, Eunice D. Soriano-Ursúa, Marvin A. Int J Mol Sci Article Preclinical and clinical evidence supports melatonin and its analogues as potential treatment for diseases involving cognitive deficit such as Alzheimer’s disease. In this work, we evaluated by in silico studies a set of boron-containing melatonin analogues on MT1 and MT2 receptors. Then, we synthesized a compound (borolatonin) identified as potent agonist. After chemical characterization, its evaluation in a rat model with cognitive deficit showed that it induced ameliorative effects such as those induced by equimolar administration of melatonin in behavioral tests and in neuronal immunohistochemistry assays. Our results suggest the observed effects are by means of action on the melatonin system. Further studies are required to clarify the mechanism(s) of action, as the beneficial effects on disturbed memory by gonadectomy in male rats are attractive. MDPI 2022-03-17 /pmc/articles/PMC8952423/ /pubmed/35328650 http://dx.doi.org/10.3390/ijms23063229 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Barrón-González, Mónica Rosales-Hernández, Martha C. Abad-García, Antonio Ocampo-Néstor, Ana L. Santiago-Quintana, José M. Pérez-Capistran, Teresa Trujillo-Ferrara, José G. Padilla-Martínez, Itzia I. Farfán-García, Eunice D. Soriano-Ursúa, Marvin A. Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat |
title | Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat |
title_full | Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat |
title_fullStr | Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat |
title_full_unstemmed | Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat |
title_short | Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat |
title_sort | synthesis, in silico, and biological evaluation of a borinic tryptophan-derivative that induces melatonin-like amelioration of cognitive deficit in male rat |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8952423/ https://www.ncbi.nlm.nih.gov/pubmed/35328650 http://dx.doi.org/10.3390/ijms23063229 |
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