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1.
Biochem Biophys Res Commun ; 719: 150043, 2024 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-38735206

RESUMO

In this study, a simple green synthesis of vanadium pentoxide nanoparticles (VNPs) was prepared by the extract of Kaffir lime fruit (Citrus hystrix) as a green reducing and stabilizing agent, along with the investigation of calcination temperature was carried out at 450 and 550 °C. It was affirmed that, at higher temperature (550 °C), the VNPs possessed a high degree crystalline following the construction of (001) lattice diffraction within an increase in crystalline size from 47.12 to 53.51 nm, although the band gap of the materials at 450 °C was lower than that of the VNPs-550 (2.53 versus 2.66 eV, respectively). Besides, the materials were assessed for the potential bioactivities toward antibacterial, antifungal, DNA cleavage, anti-inflammatory, and hemolytic performances. As a result, the antibacterial activity, with minimal inhalation concentration (MIC) < 6.25 µg/mL for both strains, and fungicidal one of the materials depicted the dose-dependent effects. Once, both VNPs exhibited the noticeable efficacy of the DNA microbial damage, meanwhile, the outstanding anti-inflammatory agent was involved with the IC50 of 123.636 and 227.706 µg/mL, accounting for VNPs-450 and VNPs-550, respectively. Furthermore, this study also demonstrated the hemolytic potential of the VNPs materials. These consequences declare the prospects of the VNPs as the smart and alternative material from the green procedure in biomedicine.


Assuntos
Antibacterianos , Citrus , Frutas , Extratos Vegetais , Compostos de Vanádio , Citrus/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Compostos de Vanádio/química , Compostos de Vanádio/farmacologia , Frutas/química , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/síntese química , Nanopartículas/química , Testes de Sensibilidade Microbiana , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Antifúngicos/farmacologia , Antifúngicos/química , Antifúngicos/síntese química , Temperatura , Hemólise/efeitos dos fármacos , Química Verde , Humanos
2.
ChemMedChem ; 15(15): 1453-1463, 2020 08 05.
Artigo em Inglês | MEDLINE | ID: mdl-32281263

RESUMO

We have synthesized 50 benzimidazole (BMZ) derivatives with 1,2-phenylenediamines and aromatic aldehydes under mild oxidation conditions by using inexpensive, nontoxic inorganic salt sodium metabisulfite in a one-pot condensation reaction and screened their ability to interfere with Zika virus (ZIKV) infection utilizing a cell-based phenotypic assay. Seven BMZs inhibited an African ZIKV strain with a selectivity index (SI=CC50 /EC50 ) of 9-37. Structure-activity relationship analysis demonstrated that substitution at the C-2, N-1, and C-5 positions of the BMZ ring were important for anti-ZIKV activity. The hybrid structure of BMZ and naphthalene rings was a structural feature responsible for the high anti-ZIKV activity. Importantly, BMZs inhibited ZIKV in human neural stem cells, a physiologically relevant system considering the severe congenital anomalies, like microcephaly, caused by ZIKV infection. Compound 39 displayed the highest antiviral efficacy against the African ZIKV strain in Huh-7 (SI>37) and neural stem cells (SI=12). Compound 35 possessed the highest activity in Vero cells (SI=115). Together, our data indicate that BMZs derivatives have to be considered for the development of ZIKV therapeutic interventions.


Assuntos
Antivirais/farmacologia , Benzimidazóis/farmacologia , Zika virus/efeitos dos fármacos , Aldeídos/química , Aldeídos/farmacologia , Antivirais/síntese química , Antivirais/química , Benzimidazóis/síntese química , Benzimidazóis/química , Células Cultivadas , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Células-Tronco Neurais/efeitos dos fármacos , Células-Tronco Neurais/virologia , Fenilenodiaminas/química , Fenilenodiaminas/farmacologia , Relação Estrutura-Atividade
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