Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 3 de 3
Filtrar
Mais filtros

Base de dados
País/Região como assunto
Ano de publicação
Tipo de documento
País de afiliação
Intervalo de ano de publicação
1.
J Enzyme Inhib Med Chem ; 38(1): 2237701, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37489043

RESUMO

In this work, a series of novel arylamide derivatives containing piperazine moiety were designed and synthesised as tubulin polymerisation inhibitors. Among 25 target compounds, compound 16f (MY-1121) exhibited low nanomolar IC50 values ranging from 0.089 to 0.238 µM against nine human cancer cells. Its inhibitory effects on liver cancer cells were particularly evident with IC50 values of 89.42 and 91.62 nM for SMMC-7721 and HuH-7 cells, respectively. Further mechanism studies demonstrated that compound 16f (MY-1121) could bind to the colchicine binding site of ß-tubulin and directly act on ß-tubulin, thus inhibiting tubulin polymerisation. Additionally, compound 16f (MY-1121) could inhibit colony forming ability, cause morphological changes, block cell cycle arrest at the G2 phase, induce cell apoptosis, and regulate the expression of cell cycle and cell apoptosis related proteins in liver cancer cells. Overall, the promising bioactivities of compound 16f (MY-1121) make the novel arylamide derivatives have the value for further development as tubulin polymerisation inhibitors with potent anticancer activities.


Assuntos
Neoplasias Hepáticas , Tubulina (Proteína) , Humanos , Apoptose , Sítios de Ligação , Piperazina , Moduladores de Tubulina
2.
J Pak Med Assoc ; 65(8): 898-900, 2015 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-26228342

RESUMO

Porphyria is a group of disorders caused by the accumulation of porphyrin and porphyrin precursors due to the abnormalities in certain enzymes that normally participate in the production of haem. We report a case of a woman with severe menstruation-related abdominal pain, hyponatraemia, and psychiatric symptoms. Excessive porphobilinogen was found in her urine. A new mutation in intron 2 (IVS2-2Ag→G), which had never previously been reported in patients with porphyria or in healthy Chinese population, was identified in the heterozygous state in the patient and her mother.


Assuntos
Hidroximetilbilano Sintase/genética , Porfiria Aguda Intermitente/genética , Povo Asiático/genética , China , Feminino , Humanos , Íntrons , Mutação , Período Pós-Parto , Adulto Jovem
3.
Exp Neurol ; 370: 114550, 2023 12.
Artigo em Inglês | MEDLINE | ID: mdl-37774766

RESUMO

Preterm birth is a public health priority worldwide, with approximately 15 million premature babies born each year. Oxygen supplementation is one of the most common interventions for preterm infants. However, prolonged oxygen inhalation at supraphysiological concentrations can lead to the development of bronchopulmonary dysplasia (BPD). In addition to lifelong pulmonary sequelae, clinical evidence suggests that BPD is associated with adverse neurodevelopmental outcomes, such as motor impairment, cognitive impairment, and behavioral deficits, severely affecting the quality of life of preterm infants. However, the mechanisms underlying the combination of neurodevelopmental impairment with BPD remain unclear. Therefore, in recent years, attention has also been focused on the effects of hyperoxia on brain development in preterm infants. In this review, we outline the pathophysiological mechanisms of brain injury caused by developmental hyperoxia exposure in current animal models and briefly describe the pharmacological therapies that may be applicable to the associated brain injury. Overall, more studies are needed to assess the effects of hyperoxia on the immature brain, particularly combined analyses of the lungs and brain in the same experimental setting, to elucidate the potential causes of combined neurodevelopmental impairment in BPD.


Assuntos
Lesões Encefálicas , Displasia Broncopulmonar , Hiperóxia , Nascimento Prematuro , Lactente , Animais , Feminino , Recém-Nascido , Humanos , Recém-Nascido Prematuro , Hiperóxia/complicações , Qualidade de Vida , Displasia Broncopulmonar/etiologia , Lesões Encefálicas/etiologia , Encéfalo
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA