Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat
| Autor: | Mónica Barrón-González, Martha C. Rosales-Hernández, Antonio Abad-García, Ana L. Ocampo-Néstor, José M. Santiago-Quintana, Teresa Pérez-Capistran, José G. Trujillo-Ferrara, Itzia I. Padilla-Martínez, Eunice D. Farfán-García, Marvin A. Soriano-Ursúa |
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| Rok vydání: | 2022 |
| Předmět: |
Male
Receptor Melatonin MT2 Receptor Melatonin MT1 Organic Chemistry Tryptophan boron Alzheimer boroxazolidone melatonin male rat androgen depletion cognitive deficit boron-containing compounds amyloid melatonin receptors General Medicine Catalysis Rats Computer Science Applications Inorganic Chemistry Cognition Animals Physical and Theoretical Chemistry Molecular Biology Spectroscopy Melatonin |
| Zdroj: | International Journal of Molecular Sciences; Volume 23; Issue 6; Pages: 3229 |
| ISSN: | 1422-0067 |
| DOI: | 10.3390/ijms23063229 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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