TY - JOUR
T1 - Synthesis, In Silico, and Biological Evaluation of a Borinic Tryptophan-Derivative That Induces Melatonin-like Amelioration of Cognitive Deficit in Male Rat
AU - Barrón-González, Mónica
AU - Rosales-Hernández, Martha C.
AU - Abad-García, Antonio
AU - Ocampo-Néstor, Ana L.
AU - Santiago-Quintana, José M.
AU - Pérez-Capistran, Teresa
AU - Trujillo-Ferrara, José G.
AU - Padilla-Martínez, Itzia I.
AU - Farfán-García, Eunice D.
AU - Soriano-Ursúa, Marvin A.
N1 - Publisher Copyright:
© 2022 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2022/3/1
Y1 - 2022/3/1
N2 - 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.
AB - 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.
KW - Alzheimer
KW - Amyloid
KW - Androgen depletion
KW - Boron
KW - Boron-containing compounds
KW - Boroxazolidone
KW - Cognitive deficit
KW - Male rat
KW - Melatonin
KW - Melatonin receptors
UR - http://www.scopus.com/inward/record.url?scp=85126654997&partnerID=8YFLogxK
U2 - 10.3390/ijms23063229
DO - 10.3390/ijms23063229
M3 - Artículo
C2 - 35328650
AN - SCOPUS:85126654997
SN - 1661-6596
VL - 23
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
IS - 6
M1 - 3229
ER -