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1.
Bioorg Chem ; 127: 105972, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35728290

RESUMO

The popularity of nanogel as nano drug carrier lies in its adjustable physical properties, and the ability to encapsulate drug particles with improved properties is being developed to meet the diverse pH-sensitive nanogel for anticancer agent. Monitoring pH has been identified as an important diagnostic element during the treatment process. A pH-sensitive nanogel consisting of (PEG/PMAc) in the ratio of (50:50%) hasbeen cross-linkedby γ-irradiation techniques at an irradiation dose of 5 kGy. Compound 4 and its nanogel 5 were synthesized and assessed for their anticancer effects against HepG2, A549, MCF-7 and HCT-116 as dual VEGFR-2 and EGFR tyrosine kinases inhibitors. The molecular design was performed to investigate the binding mode of compound 4 with VEGFR-2 and EGFR receptors. Our compound 5 in nanogel showed enhanced anticancer activities against the four tested cancer cell lines and also showed higher inhibition activities against VEGFR-2 and EGFRT790M kinases than the derivative 4. Finally, our derivative 4 showed good in silico calculated ADMET profile. It was expected to show good GIT absorption in human, lower CNS side effects, no hepatotoxic actions and higher acute and oral chronic toxic doses in comparing to sorafenib and erlotinib. The obtained results showed that, our compound could be useful as a template for future design, optimization, adaptation and investigation to produce more potent and selective dual VEGFR-2/EGFRT790M inhibitors with higher anticancer activity.


Assuntos
Antineoplásicos , Neoplasias Pulmonares , Acrilatos , Antineoplásicos/química , Proliferação de Células , Sistemas de Liberação de Medicamentos , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Receptores ErbB , Etilenoglicol/farmacologia , Humanos , Concentração de Íons de Hidrogênio , Simulação de Acoplamento Molecular , Mutação , Nanogéis , Inibidores de Proteínas Quinases/química , Relação Estrutura-Atividade , Receptor 2 de Fatores de Crescimento do Endotélio Vascular
2.
Int J Biol Macromol ; 277(Pt 3): 134200, 2024 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-39069051

RESUMO

Ammonia is a colorless gas, yet it can be fatal if inhaled or ingested in high enough concentrations. Herein, a solid-state colorimetric smart wool (WL) sensor for ammonia was developed. Common hop (Humulus lupulus L.) is a natural resource of spectroscopical dyestuff known as xanthohumol (XN). Wool fabrics were dyed with different concentrations of xanthohumol extract using the high-temperature high-pressure method in the presence of a mordant. The coloration parameters and absorption spectra were employed to explore the yellow-to-white colorimetric shift of the wool fabric after it was exposed to aqueous ammonia. The wool fabric showed an excellent detection limit of 5 to 125 ppm. When the ammonia concentration was increased, the absorbance spectra demonstrated a hypsochromic shift from 498 nm to 367 nm. This could be attributed to changes in the molecular structure of xanthohumol that happen owing to intramolecular charge delocalization. Using transmission electron microscopy (TEM), the mordant/xanthohumol nanoparticles were measured to have diameters of 15-40 nm. The xanthohumol-finished wool fabrics showed good colorfastness properties. The incorporation of mordant/xanthohumol nanoparticles into wool fabrics showed no negative effects on their stiffness or air-permeability.


Assuntos
Amônia , Flavonoides , Humulus , Propiofenonas , Propiofenonas/química , Humulus/química , Flavonoides/química , Flavonoides/análise , Amônia/química , Amônia/análise , Animais , Extratos Vegetais/química , Fibra de Lã/análise , Colorimetria/métodos , Nanopartículas/química
3.
Nanoscale Adv ; 4(24): 5330-5342, 2022 Dec 06.
Artigo em Inglês | MEDLINE | ID: mdl-36540120

RESUMO

The photocatalytic degradation of uranium complexes is considered among the most efficient techniques for the efficient removal of uranium ions/complexes from radioactive wastewater. Described here is a nanostructured photocatalyst based on a cobalt-doped TiO2 composite with induced oxygen vacancies (Co@TiO2-C) for the photocatalytic removal of uranium complexes from contaminated water. The synergy between oxygen vacancies and Co-doping produced a material with a 1.7 eV bandgap, while the carbon network facilitates electron movement and hinders the e-h recombination. As a result, the new photocatalyst enables the decomposition of uranium-arsenazo iii complexes (U-ARZ3), followed by photocatalytic reduction of hexavalent uranium to insoluble tetravalent uranium. Combined with the nanosheet structure's high surface area, the photocatalytic decomposition, reduction efficiency, and kinetics were significantly enhanced, achieving almost complete U(vi) removal in less than 20 minutes from solution with a concentration as high as 1000 mL g-1. Moreover, the designed photocatalyst exhibits excellent stability and reusability without decreasing the photocatalytic performance after 5 cycles.

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