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1.
ACS Omega ; 9(20): 21948-21963, 2024 May 21.
Artigo em Inglês | MEDLINE | ID: mdl-38799368

RESUMO

Due to the growth in the number of patients and the complexity involved in anticancer therapies, new therapeutic approaches are urgent and necessary. In this context, compounds containing the selenium atom can be employed in developing new medicines due to their potential therapeutic efficacy and unique modes of action. Furthermore, tellurium, a previously unknown element, has emerged as a promising possibility in chalcogen-containing compounds. In this study, 13 target compounds (9a-i, 10a-c, and 11) were effectively synthesized as potential anticancer agents, employing a CuI-catalyzed Csp-chalcogen bond formation procedure. The developed methodology yielded excellent results, ranging from 30 to 85%, and the compounds were carefully characterized. Eight of these compounds showed promise as potential therapeutic drugs due to their high yields and remarkable selectivity against SCC-9 cells (squamous cell carcinoma). Compound 10a, in particular, demonstrated exceptional selectivity, making it an excellent choice for cancer cell targeting while sparing healthy cells. Furthermore, complementing in silico and molecular docking studies shed light on their physical features and putative modes of action. This research highlights the potential of these compounds in anticancer treatments and lays the way for future drug development efforts.

2.
J Med Food ; 24(9): 916-924, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33739872

RESUMO

Epilepsy is one of the most common neurological disorders. About one-third of people with epilepsy are refractory to available treatments. Studies suggest that mechanisms linked to the immune response and inflammatory process are related to seizure disorders. Citral is a monoterpene found in the essential oil of several plants, as in Cymbopogon citratus, used to make teas and has been the subject of numerous researches, from which it has been possible to demonstrate antiseizure and anti-inflammatory activities. In this study, the effects of citral on status epilepticus (SE) induced by the lithium-pilocarpine model in rats were investigated. Quantitative reverse transcription PCR (RT-qPCR) evaluated latency for seizure development, neuronal death in the hippocampus, and expression of the brain-derived neurotrophic factor (BDNF), tumor necrosis factor-alpha (TNF-α), interleukin 6 (IL-6), interleukin-1ß ( IL-1ß) and factor nuclear kappa B (NF-κB) genes. The results revealed that citral was able to increase latency until the first seizure, decrease neuronal death 2 h after SE and inhibit overexpression of proinflammatory genes.


Assuntos
Pilocarpina , Estado Epiléptico , Monoterpenos Acíclicos , Animais , Fator Neurotrófico Derivado do Encéfalo , Citocinas/genética , Citocinas/metabolismo , Modelos Animais de Doenças , Hipocampo/metabolismo , Lítio , Ratos , Ratos Sprague-Dawley , Estado Epiléptico/induzido quimicamente , Estado Epiléptico/tratamento farmacológico , Estado Epiléptico/genética
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