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1.
Int J Dev Neurosci ; 80(8): 709-716, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33030219

RESUMO

OBJECTIVES: Caffeine is extensively consumed as a psychostimulant drug, acting on A1 and A2A adenosine receptors blockade. Chronic exposure to caffeine during gestation and breast-feeding may be involved in infant rat's behavioral and biochemical alterations. Our goal was to evaluate the effect of chronic caffeine exposure during gestation and breast-feeding in the functionality of adenosine A1 receptors in infant rats at P14. NTPDase and 5'-nucleotidase activities were also evaluated. METHODS: Mating of adult female Wistar rats was confirmed by presence of sperm in vaginal smears. Rats were divided into three groups on the first day of pregnancy: (1) control: tap water, (2) caffeine: 0.3 g/L until P14, and (3) washout caffeine: caffeine was changed to tap water at P7. Evaluation of nociceptive response was performed at P14 using hot plate (HP) and tail-flick latency (TFL) tests. A1 receptor involvement was assessed using caffeine agonist (CPA) and antagonist (DPCPX). Enzymatic activities assays were conducted in the spinal cord. RESULTS: Gestational and breastfeeding exposure to caffeine (caffeine and washout groups) did not induce significant alterations in thermal nociceptive thresholds (HP and TF tests). Both caffeine groups did not show analgesic response induced by CPA when compared to the control group at P14, indicating chronic exposure to caffeine in the aforementioned periods inhibits the antinociceptive effects of the systemic A1 receptor agonist administration. No effect was observed upon ectonucleotidase activities. CONCLUSIONS: Our results demonstrate that chronic caffeine exposure in gestational and breastfeeding alters A1-mediated analgesic response in rats.


Assuntos
Cafeína , Lactação , Receptor A1 de Adenosina , Adenosina , Animais , Cafeína/farmacologia , Feminino , Gravidez , Ratos , Ratos Wistar , Receptor A1 de Adenosina/metabolismo
2.
Anticancer Res ; 40(9): 5151-5158, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32878803

RESUMO

BACKGROUND/AIM: Magnetic stimulation is used in the treatment of a diversity of diseases, but a complete understanding of the underlying mechanisms of action requires further investigation. We examined the effect of static magnetic stimulation (SMS) in different cell lines. MATERIALS AND METHODS: A culture plate holder with attached NeFeB magnets was developed. Different magnetic field intensities and periods were tested in tumoral and non-tumoral cell lines. To verify the cellular responses to SMS, cell viability, cell death, cell cycle and BDNF expression were evaluated. RESULTS: Exposure of SH-SY5Y cells to SMS for 24 hours led to a decrease in cell viability. Analysis 24 h after stimulation revealed a decrease in apoptotic and double-positive cells, associated with an increase in the number of necrotic cells. CONCLUSION: The effects of SMS on cell viability are cell type-specific, inducing a decrease in cell viability in SH-SY5Y cells. This suggests that SMS may be a potential tool in the treatment of neuronal tumors.


Assuntos
Sobrevivência Celular/efeitos da radiação , Fenômenos Magnéticos , Apoptose/efeitos da radiação , Fator Neurotrófico Derivado do Encéfalo/genética , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Ciclo Celular/efeitos da radiação , Linhagem Celular Tumoral , Regulação Neoplásica da Expressão Gênica/efeitos da radiação , Humanos , Neuroblastoma/genética , Neuroblastoma/metabolismo , Especificidade de Órgãos/efeitos da radiação
3.
J Org Chem ; 83(7): 4044-4053, 2018 04 06.
Artigo em Inglês | MEDLINE | ID: mdl-29547280

RESUMO

The current manuscript describes the use of a heteropolyacid-containing task-specific ionic liquid, supported in imidazolium-based ionic liquids, as the catalyst for an efficient multicomponent synthesis of hexahydroimidazo[1,2-α]pyridine derivatives. The reactions conditions were fully optimized, and the bridgehead nitrogen heterocycle derivatives could be obtained in just 1 h exclusively as a single isomer ( trans). Single crystal X-ray analysis confirmed the trans derivative as the only isomer. The mechanism of the reaction was investigated by ESI(+)-MS(/MS), and the use of the elegant charge-tag strategy allowed a catalytic cycle to be proposed for the current transformation and revealed the possibility of at least two reaction pathways. One derivative bearing a coumarin scaffold was synthesized, and its fluorescent properties allowed it to be tested as a probe for live-cell imaging experiments with a preference for mitochondria.


Assuntos
Compostos Heterocíclicos/síntese química , Líquidos Iônicos/química , Mitocôndrias/química , Nitrogênio/química , Piridinas/síntese química , Coloração e Rotulagem , Ácidos/química , Catálise , Compostos Heterocíclicos/química , Humanos , Células MCF-7 , Estrutura Molecular , Piridinas/química
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