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1.
Drug Dev Res ; 77(5): 251-7, 2016 08.
Artigo em Inglês | MEDLINE | ID: mdl-27455162

RESUMO

Preclinical Research A novel series of ten 5-hydroxy, 5-substituted benzene sulfonamide pyrimidine-2,4,6-triones were synthesized and their structures ascertained using (1) H-NMR, (13) C-NMR, mass and elemental analysis. These compounds were subsequently tested for inhibition of MMP-2 and MMP-9 where most exhibited activity with compound 5i being the most potent against MMP-2 and MMP-9 with IC50 values of 2.35 nM and 8.24 nM, respectively. Compound 5i was further analyzed in a mouse LPS-induced acute lung injury model where it had protective activity. Histochemical studies indicated that 5i improved the vascular integrity of the lung. Drug Dev Res 77 : 251-257, 2016. © 2016 Wiley Periodicals, Inc.


Assuntos
Lesão Pulmonar Aguda/tratamento farmacológico , Pirimidinas/farmacologia , Sulfonamidas/farmacologia , Lesão Pulmonar Aguda/patologia , Animais , Modelos Animais de Doenças , Gelatinases/antagonistas & inibidores , Concentração Inibidora 50 , Lipopolissacarídeos/toxicidade , Espectroscopia de Ressonância Magnética , Masculino , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 9 da Matriz/metabolismo , Inibidores de Metaloproteinases de Matriz/síntese química , Inibidores de Metaloproteinases de Matriz/química , Inibidores de Metaloproteinases de Matriz/farmacologia , Camundongos , Camundongos Endogâmicos BALB C , Pirimidinas/síntese química , Pirimidinas/química , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/química
2.
Chin Med J (Engl) ; 124(11): 1695-9, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21740780

RESUMO

BACKGROUND: Pancreatic cancer is one of the most lethal human cancers with a very low survival rate of 5 years. Conventional cancer treatments including surgery, radiation, chemotherapy or combinations of these show little effect on this disease. Several proteins have been proved critical to the development and the progression of pancreatic cancer. The aim of this study was to investigate the effect of resveratrol on apoptosis in pancreatic cancer cells. METHODS: Several pancreatic cancer cell lines were screened by resveratrol, and its toxicity was tested by normal pancreatic cells. Western blotting was then performed to analyze the molecular mechanism of resveratrol induced apoptosis of pancreatic cancer cell lines. RESULTS: In the screened pancreatic cancer cell lines, capan-2 and colo357 showed high sensitivity to resveratrol induced apoptosis. Resveratrol exhibited insignificant toxicity to normal pancreatic cells. In resveratrol sensitive cells, capan-2 and colo357, the activation of caspase-3 was detected and showed significant caspase-3 activation upon resveratrol treatment; p53 and p21 were also detected up-regulated upon resveratrol treatment. CONCLUSION: Resveratrol provides a promising anti-tumor strategy to fight against pancreatic cancer.


Assuntos
Apoptose/efeitos dos fármacos , Estilbenos/farmacologia , Western Blotting , Caspase 3/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Humanos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Neoplasias Pancreáticas/metabolismo , Resveratrol , Células Tumorais Cultivadas
3.
Zhonghua Wai Ke Za Zhi ; 47(14): 1092-5, 2009 Jul 15.
Artigo em Chinês | MEDLINE | ID: mdl-19781277

RESUMO

OBJECTIVE: To establish a stable high red fluorescent protein (RFP)-expressing orthotopic transplantation nude mice spontaneous metastasis model of pancreatic cancer. METHODS: Stable high RFP-expressing cells SW1990-RFP were injected subcutaneously into mice to establish subcutaneous implantation model. Fluorescent tumor piece from subcutaneous was transplanted into the body of the pancreas to establish surgical orthotopic implantation model. The growth of primary tumor, metastasis and micrometastasis were assessed by whole-body fluorescence imaging system. RESULTS: Twelve RFP orthotopic transplantation nude mice metastasis models of pancreatic cancer were established successfully, the percentage of success rate was 100%. RFP-labeled pancreatic cancer growth could be monitored in real time way. The micrometastasis of primary lesions were detected in early stage with whole-body fluorescence imaging system. CONCLUSIONS: The RFP orthotopic transplantation nude mice metastasis model of pancreatic cancer is stable and reliable, and can be observed dynamically in vitro in a noninvasive way, with much higher sensitivity and specificity.


Assuntos
Proteínas Luminescentes , Neoplasias Pancreáticas/patologia , Ensaios Antitumorais Modelo de Xenoenxerto , Animais , Modelos Animais de Doenças , Feminino , Masculino , Camundongos , Camundongos Nus , Metástase Neoplásica , Pâncreas/patologia
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