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1.
Eur J Med Chem ; 265: 116099, 2024 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-38160618

RESUMO

A series of butylphthalide and scutellarein hybrids 3-(alkyl/alkenyl) hydroxyphthalide derivatives were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease. In vitro bioactivity assays indicated that most of the compounds displayed excellent antioxidant activity and moderate to good inhibition activities of self-induced Aß1-42 aggregation. Among them, compound 7c was demonstrated as a potential and balanced multifunctional candidate displaying the best inhibitory effects on self- and Cu2+-induced Aß1-42 aggregation (90.2 % and 35.4 %, respectively) and moderate activity for disaggregation of Aß1-42 aggregation (42.5 %). In addition, 7c also displayed excellent antioxidant (2.42 Trolox equivalents), metal ions chelating, oxidative stress alleviation, neuroprotective and anti-neuroinflammatory activities. Furthermore, in vivo study demonstrated that 7c could ameliorate the learning and memory impairment induced by sodium nitrite and Aß1-42 in the step-down passive avoidance test. These balanced multifunctional profiles supporting compound 7c as a novel potential candidate for the treatment of AD.


Assuntos
Doença de Alzheimer , Apigenina , Benzofuranos , Fármacos Neuroprotetores , Humanos , Doença de Alzheimer/tratamento farmacológico , Peptídeos beta-Amiloides , Relação Estrutura-Atividade , Inibidores da Colinesterase/farmacologia , Desenho de Fármacos , Antioxidantes , Acetilcolinesterase/metabolismo
2.
J Nanosci Nanotechnol ; 10(10): 6439-45, 2010 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21137744

RESUMO

Stable water-dispersible silver nanoparticles with a narrow size distribution are obtained by light-assisted spontaneous reduction of silver nitrate with gelatin, which acts as both the reducing and the stabilizing agents, in water. The formation mechanism of the silver nanoparticles involves an in-situ conversion of Ag(+)-gelatin aggregates to gelatin-stabilized silver nanoparticles via a Ag(+)-mediated oxidation of primary amine groups of the gelatin to carboxylic acid groups. The resultant silver nanoparticles are well within the quantum size domain (10 nm). In addition, the nanoparticles are stable in aqueous solutions and can be separated easily by simple pH adjustment.


Assuntos
Química Verde/métodos , Nanopartículas Metálicas/química , Nanotecnologia/métodos , Prata/química , Água/química , Gelatina/química , Concentração de Íons de Hidrogênio , Nanopartículas Metálicas/efeitos da radiação , Microscopia Eletrônica de Transmissão , Tamanho da Partícula , Nitrato de Prata/química , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
3.
J Colloid Interface Sci ; 334(2): 153-60, 2009 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-19394956

RESUMO

PAA/gelatin nanoparticles, with interpolymer complexes of gelatin and polyacrylic acid (PAA) as the cores and gelatin as the shells, were prepared via facile polymerization of AA on gelatin template. The morphology change of the nanoparticles during the reaction was traced by a combined use of dynamic light scattering (DLS) and atomic force microscopy (AFM) techniques, which revealed a discrepancy among the structure of the nanoparticles formed at different stages of the reaction: as the reaction proceeds, nanoparticles with larger compact cores and thinner shells are produced. The resultant nanoparticles are multi-responsive. Especially, they exhibit a significant temperature-dependent size change: upon raising the temperature from 25 degrees C, the nanoparticle size decreases monotonically until reaching equilibrium at about 40 degrees C. This temperature-dependence of the nanoparticle size was found to be reversible provided the nanoparticle solution was cooled at a low temperature (4 degrees C). The thermo-sensitivity of the nanoparticles is attributed to the thermo-induced sol-gel transition of the gelatin shells. In addition, the nanoparticles were further converted to hollow spheres via successive locking the shell structure by the reaction of gelatin with cross-linker glutaraldehyde, and cavitation of the cross-linked nanoparticles by switching the medium from acidic to neutral. The cavitation process was monitored by DLS, which indicated a mass decrease and size shrinkage. AFM and transmission electron microscopy (TEM) were used to trace the morphology change of the nanoparticles during the cavitation. The hollow structure was confirmed by TEM observation.


Assuntos
Resinas Acrílicas/química , Gelatina/química , Nanopartículas/química , Reagentes de Ligações Cruzadas/química , Glutaral/química , Concentração de Íons de Hidrogênio , Microscopia de Força Atômica , Microscopia Eletrônica de Transmissão , Nanopartículas/ultraestrutura , Tamanho da Partícula , Sais/química , Temperatura
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