Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 4 de 4
Filtrar
Adicionar filtros








Intervalo de ano
1.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 231-240, 2018.
Artigo em Inglês | WPRIM | ID: wpr-812408

RESUMO

Novel series of limonin derivatives (V-A-1-V-A-8, V-B-1-V-B-8) were synthesized by adding various tertiary amines onto the C (7)-position of limonin. The synthesized compounds possessed favorable physicochemical property, and the intrinsic solubility of the novel compounds were significantly improved, compared with limonin. Different pharmacological models were used to evaluate the analgesic and anti-inflammatory activities of the target compounds. Compound V-A-8 exhibited the strongest in vivo activity among the novel limonin analogs; its analgesic activity was more potent than aspirin and its anti-inflammatory activity was stronger than naproxen under our testing conditions.


Assuntos
Animais , Humanos , Camundongos , Analgésicos , Química , Anti-Inflamatórios , Química , Descoberta de Drogas , Edema , Tratamento Farmacológico , Limoninas , Química , Estrutura Molecular , Dor , Tratamento Farmacológico
2.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 231-240, 2018.
Artigo em Inglês | WPRIM | ID: wpr-773618

RESUMO

Novel series of limonin derivatives (V-A-1-V-A-8, V-B-1-V-B-8) were synthesized by adding various tertiary amines onto the C (7)-position of limonin. The synthesized compounds possessed favorable physicochemical property, and the intrinsic solubility of the novel compounds were significantly improved, compared with limonin. Different pharmacological models were used to evaluate the analgesic and anti-inflammatory activities of the target compounds. Compound V-A-8 exhibited the strongest in vivo activity among the novel limonin analogs; its analgesic activity was more potent than aspirin and its anti-inflammatory activity was stronger than naproxen under our testing conditions.


Assuntos
Animais , Humanos , Camundongos , Analgésicos , Química , Anti-Inflamatórios , Química , Descoberta de Drogas , Edema , Tratamento Farmacológico , Limoninas , Química , Estrutura Molecular , Dor , Tratamento Farmacológico
3.
Journal of Huazhong University of Science and Technology (Medical Sciences) ; (6): 591-595, 2014.
Artigo em Inglês | WPRIM | ID: wpr-351034

RESUMO

Recent studies indicated that interleukin (IL)-17, growth-related oncogene (GRO)-α and IL-8 play an important role in the pathogenesis of nasal polyps. However, the effects of the increased amount of IL-17 and the production of GRO-α and IL-8 in human nasal polyp fibroblasts are not completely understood. This study aimed to determine the effects of the increased IL-17 on the changes of GRO-α and IL-8 expression in human nasal polyp fibroblasts and further investigate the mechanism of neutrophil infiltration in nasal polyps. Nasal polyp fibroblasts were isolated from six cases of human nasal polyps, and the cells were stimulated with five different concentrations of IL-17. Real-time fluorescence quantitative polymerase chain reaction (RT-PCR) was used to detect the mRNA expression of GRO-α and IL-8. The mRNA of GRO-α and IL-8 was expressed in unstimulated controls and remarkably increased by stimulation with IL-17. Moreover, the levels of GRO-α and IL-8 produced by fibroblasts were increased gradually with the increases in IL-17 concentrations. The present study showed that nasal fibroblasts can produce GRO-α and IL-8, and their production is remarkably enhanced by IL-17 stimulation, thereby clarifying the mechanism of the IL-17 mediated neutrophil infiltration in nasal polyps. These findings might provide a rationale for using IL-17 inhibitors as a treatment for nasal inflammatory diseases such as nasal polyps.


Assuntos
Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Células Cultivadas , Quimiocina CXCL1 , Fibroblastos , Metabolismo , Patologia , Interleucina-17 , Farmacologia , Interleucina-8 , Pólipos Nasais , Metabolismo , Patologia , Infiltração de Neutrófilos , RNA Mensageiro
4.
Journal of Huazhong University of Science and Technology (Medical Sciences) ; (6): 591-5, 2014.
Artigo em Inglês | WPRIM | ID: wpr-636769

RESUMO

Recent studies indicated that interleukin (IL)-17, growth-related oncogene (GRO)-α and IL-8 play an important role in the pathogenesis of nasal polyps. However, the effects of the increased amount of IL-17 and the production of GRO-α and IL-8 in human nasal polyp fibroblasts are not completely understood. This study aimed to determine the effects of the increased IL-17 on the changes of GRO-α and IL-8 expression in human nasal polyp fibroblasts and further investigate the mechanism of neutrophil infiltration in nasal polyps. Nasal polyp fibroblasts were isolated from six cases of human nasal polyps, and the cells were stimulated with five different concentrations of IL-17. Real-time fluorescence quantitative polymerase chain reaction (RT-PCR) was used to detect the mRNA expression of GRO-α and IL-8. The mRNA of GRO-α and IL-8 was expressed in unstimulated controls and remarkably increased by stimulation with IL-17. Moreover, the levels of GRO-α and IL-8 produced by fibroblasts were increased gradually with the increases in IL-17 concentrations. The present study showed that nasal fibroblasts can produce GRO-α and IL-8, and their production is remarkably enhanced by IL-17 stimulation, thereby clarifying the mechanism of the IL-17 mediated neutrophil infiltration in nasal polyps. These findings might provide a rationale for using IL-17 inhibitors as a treatment for nasal inflammatory diseases such as nasal polyps.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA