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1.
Acta Chim Slov ; 67(4): 1281-1289, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33533465

RESUMO

Two vanadium(V) complexes derived from the bromo and chloro-substituted hydrazones N'-(4-bromo-2-hydroxybenzylidene)- 2-chlorobenzohydrazide (H2L1) and N'-(3-bromo-5-chloro-2-hydroxybenzylidene)-3-methylbenzohydrazide (H2L2) with the formula [VOL1(OCH3)(CH3OH)] (1) and [VOL2(OCH3)(CH3OH)] (2) were newly synthesized and characterized by IR, UV-Vis and 1H NMR spectroscopy. The structures of H2L1 and the complexes were further confirmed by single crystal X-ray diffraction. Both vanadium complexes are mononuclear, with the metal atoms coordinated by the hydrazone ligands, methanol ligands, and methanolate ligands, and the oxo groups, forming octahedral geometry. The hydrazones and the vanadium complexes were assayed for the antimicrobial activities on Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Pseudomonas fluorescence, and the fungi Candida albicans and Aspergillus niger. The existence of the bromo and chloro groups in the hydrazone ligands may improve the antimicrobial property.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Complexos de Coordenação/farmacologia , Hidrazonas/farmacologia , Antibacterianos/síntese química , Antifúngicos/síntese química , Aspergillus niger/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Complexos de Coordenação/síntese química , Hidrazonas/síntese química , Ligantes , Testes de Sensibilidade Microbiana , Estrutura Molecular , Vanádio/química
3.
Cell Biol Int ; 38(5): 639-46, 2014 May.
Artigo em Inglês | MEDLINE | ID: mdl-24446394

RESUMO

Artesunate (ART), derived from a common traditional Chinese medicine, has beeen used an antimalarial for several years. In this study, the effect and mechanism of ART on anti-human cervical cancer cells was examined. The level of prostaglandin E2 (PGE2 ) and the population of CD4+CD25+Foxp3 regulatory T cells (Treg) in peripheral blood were detected by flow cytometry. In vivo antitumor activity was investigated in mice with cervical cancer by the subcutaneous injection of various concentrations of ART. The concentrations of PGE2 in the supernatants of CaSki cells were measured using an ELISA kit. Cyclooxygenase-2 (COX-2) and Foxp3 expression were determined using quantitative polymerase chain reaction (qPCR) and western blot analysis. The effect of ART on the viability of CaSki and Hela cells was evaluated with a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. It was identified that the level of PGE2 and the population of CD4+CD25+Foxp3 Treg cells in the peripheral blood were significantly higher in cervical cancer patients and mice with cervical cancer. ART was capable of inhibiting orthotopic tumor growth, which correlated with a decrease in the level of PGE2 and the percentage of Treg cells in mice with cervical cancer. Furthermore, ART decreased COX-2 expression and the production of PGE2 in CaSki and Hela cells. Notably, the supernatants of CaSki cells treated with ART lowered the expression of Foxp3 in Jurkat T cells, which was capable of being reversed by exogenous PGE2 . Our data revealed that ART may elicit an anti-tumor effect against cervical cancer by inhibition of PGE2 production in CaSki and Hela cells, which resulted in the decrease of Foxp3 expression in T cells. Therefore, ART may be an effective drug for immunotherapy of cervical cancer.


Assuntos
Artemisininas/farmacologia , Dinoprostona/antagonistas & inibidores , Fatores de Transcrição Forkhead/antagonistas & inibidores , Regulação Neoplásica da Expressão Gênica , Tolerância Imunológica/efeitos dos fármacos , Neoplasias do Colo do Útero , Animais , Artesunato , Dinoprostona/biossíntese , Feminino , Fatores de Transcrição Forkhead/biossíntese , Células HeLa , Humanos , Tolerância Imunológica/fisiologia , Células Jurkat , Camundongos , Camundongos Endogâmicos C57BL , Neoplasias do Colo do Útero/metabolismo
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