Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat

Author:

Barrón-González Mónica,Rosales-Hernández Martha C.,Abad-García Antonio,Ocampo-Néstor Ana L.ORCID,Santiago-Quintana José M.ORCID,Pérez-Capistran Teresa,Trujillo-Ferrara José G.ORCID,Padilla-Martínez Itzia I.ORCID,Farfán-García Eunice D.,Soriano-Ursúa Marvin A.ORCID

Abstract

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.

Funder

Instituto Politécnico Nacional

Consejo Nacional de Ciencia y Tecnología

Publisher

MDPI AG

Subject

Inorganic Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Computer Science Applications,Spectroscopy,Molecular Biology,General Medicine,Catalysis

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