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1.
J Zhejiang Univ Sci B ; 21(8): 611-627, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32748577

RESUMO

Immunoglobulin Y (IgY) is an effective orally administered antibody used to protect against various intestinal pathogens, but which cannot tolerate the acidic gastric environment. In this study, IgY was microencapsulated by alginate (ALG) and coated with chitooligosaccharide (COS). A response surface methodology was used to optimize the formulation, and a simulated gastrointestinal (GI) digestion (SGID) system to evaluate the controlled release of microencapsulated IgY. The microcapsule formulation was optimized as an ALG concentration of 1.56% (15.6 g/L), COS level of 0.61% (6.1 g/L), and IgY/ALG ratio of 62.44% (mass ratio). The microcapsules prepared following this formulation had an encapsulation efficiency of 65.19%, a loading capacity of 33.75%, and an average particle size of 588.75 µm. Under this optimum formulation, the coating of COS provided a less porous and more continuous microstructure by filling the cracks on the surface, and thus the GI release rate of encapsulated IgY was significantly reduced. The release of encapsulated IgY during simulated gastric and intestinal digestion well fitted the zero-order and first-order kinetics functions, respectively. The microcapsule also allowed the IgY to retain 84.37% immune-activity after 4 h simulated GI digestion, significantly higher than that for unprotected IgY (5.33%). This approach could provide an efficient way to preserve IgY and improve its performance in the GI tract.


Assuntos
Imunoglobulinas/química , Ácido Algínico/química , Quitina/análogos & derivados , Quitina/química , Quitosana , Preparações de Ação Retardada , Digestão , Composição de Medicamentos , Liberação Controlada de Fármacos , Trato Gastrointestinal/metabolismo , Imunoglobulinas/administração & dosagem , Imunoglobulinas/imunologia , Imunoglobulinas/metabolismo , Oligossacarídeos
2.
Sci Rep ; 7: 43758, 2017 03 03.
Artigo em Inglês | MEDLINE | ID: mdl-28256577

RESUMO

An efficient copper-catalyzed direct 2-arylation of benzoxazoles and benzoimidazoles with aryl bromides is presented. The CuI/PPh3-based catalyst promotes the installation of various aryl and heteroaryl groups through a C-H activation process in good to excellent yields. The cytotoxicity of obtained 2-aryl benzoxazoles (benzoimidazoles) was also evaluated and 1-methyl-2-(naphthalen-1-yl)benzoimidazole showed potential cytotoxicity.


Assuntos
Benzeno/química , Benzoxazóis/química , Brometos/química , Cobre/química , Imidazóis/química , Benzoxazóis/síntese química , Benzoxazóis/farmacologia , Catálise , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cristalografia por Raios X , Células HCT116 , Células Hep G2 , Humanos , Imidazóis/síntese química , Imidazóis/farmacologia , Modelos Químicos , Estrutura Molecular
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