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1.
Acta Pharmaceutica Sinica ; (12): 694-698, 2010.
Artigo em Chinês | WPRIM | ID: wpr-354547

RESUMO

With the continuous development in microfluidic fabrication technology, microfluidic analysis has evolved from a concept to one of research frontiers in last twenty years. The research of enzymes and enzyme inhibitors based on microfluidic devices has also made great progress. Microfluidic technology improved greatly the analytical performance of the research of enzymes and enzyme inhibitors by reducing the consumption of reagents, decreasing the analysis time, and developing automation. This review focuses on the development and classification of enzymes and enzyme inhibitors research based on microfluidic devices.


Assuntos
Inibidores Enzimáticos , Metabolismo , Enzimas , Metabolismo , Técnicas Analíticas Microfluídicas , Métodos , Microfluídica , Métodos
2.
Acta Pharmaceutica Sinica ; (12): 1371-1375, 2009.
Artigo em Chinês | WPRIM | ID: wpr-344069

RESUMO

5-Aryl-4-cyano-1H-1, 2, 3-triazoles bearing a variety of substituting groups on 5-phenyl were synthesized. Their structures were established by MS, IR and 1H NMR spectra. The crystal structures of compounds 3f and 3m were determined by X-ray diffraction analysis. The active H of the triazole was on 1-N from the crystal structures. The compounds, designed as HER2 tyrosine kinase inhibitors, were screened for bioactivity of growth-inhibition of breast cancer MDA-MB-453 cells. The lowest IC50 value of inhibiting HER2 tyrosine kinase phosphorylation in breast cancer cells is 6.6 micromol x L(-1). The inhibiting-growth of breast cancer cells was enhanced from electron-drawing groups joining 5-phenyl on the triazole.


Assuntos
Feminino , Humanos , Neoplasias da Mama , Metabolismo , Patologia , Linhagem Celular Tumoral , Proliferação de Células , Cristalização , Cristalografia por Raios X , Fosforilação , Proteínas Tirosina Quinases , Metabolismo , Receptor ErbB-2 , Metabolismo , Triazóis , Química , Farmacologia
3.
Acta Pharmaceutica Sinica ; (12): 384-387, 2003.
Artigo em Chinês | WPRIM | ID: wpr-251079

RESUMO

<p><b>AIM</b>To test the enhancing activity and the mechanism of oleyl pyroglutamate used as transdermal enhancer.</p><p><b>METHODS</b>The penetration-enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of oleyl pyroglutamate was studied with the attenuated total reflectance Fourier-transfer infrared spectroscopy(ATR-FTIR) of the human stratum corneum in vivo.</p><p><b>RESULTS</b>The penetration-enhancing ratio of the three drugs was 7.9 fold, 41.8 fold and 2.8 fold, respectively. The absorptions at 2,800-2,950 cm-1 and 1,642-1,646 cm-1 (amide-I) in the ATR-FTIR spectrum of the stratum were found to be shifted differently following removal of the stratum corneum which was treated with oleyl pyroglutamate.</p><p><b>CONCLUSION</b>Oleyl pyroglutamate showed better penetration-enhancing effect on the penetration of drugs. Its transdermal enhancing mechanism may be that oleyl pyroglutamate induced not only disordering of the stratum corneum lipid, but also change of the secondary structure of keratin.</p>


Assuntos
Adulto , Animais , Humanos , Masculino , Camundongos , Administração Cutânea , Cafeína , Farmacocinética , Cortisona , Farmacocinética , Álcoois Graxos , Farmacologia , Ácido Oleico , Farmacologia , Ácido Pirrolidonocarboxílico , Química , Farmacologia , Absorção Cutânea , Tinidazol , Farmacocinética
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