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1.
J Inorg Biochem ; 203: 110944, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31794895

RESUMO

Bridge splitting reactions between [Pd(C2,N-dmba)(µ-X)]2 (dmba = N,N-dimethylbenzylamine; X = Cl, I, N3, NCO) and 2,6-lutidine (lut) in the 1:2 molar ratio at room temperature afforded cyclopalladated compounds of general formulae [Pd(C2,N-dmba)(X)(lut)] {X = Cl- (1), I-(2), NNN-(3), NCO-(4)}, which were characterized by elemental analyses and infrared (IR), 1H NMR spectroscopy. The molecular structures of all synthesized palladacycles have been solved by single-crystal X-ray crystallography. The cytotoxicity of the cyclopalladated compounds has been evaluated against a panel of murine {mammary carcinoma (4T1) and melanoma (B16F10-Nex2)} and human {melanoma (A2058, SK-MEL-110 and SK-MEL-5) tumor cell lines. All complexes were about 10 to 100-fold more active than cisplatin, depending on the tested tumor cell line. For comparison purposes, the cytotoxic effects of 1-4 towards human lung fibroblasts (MRC-5) have also been tested. The late apoptosis-inducing properties of 1-4 compounds in SK-MEL-5 cells were verified 24 h incubation using annexin V-Fluorescein isothiocyanate (FITC)/propidium iodide (PI). The binding properties of the model compound 1 on human serum albumin (HSA) and calf thymus DNA (ct-DNA) have been studied using circular dichroism and fluorescence spectroscopy. Docking simulations have been carried out to gain more information about the interaction of the palladacycle and HSA. The ability of compounds 1-4 to inhibit the activity of cathepsin B and L has also been investigated in this work.


Assuntos
Antineoplásicos/síntese química , Compostos Organometálicos/síntese química , Paládio/química , Inibidores de Proteases/síntese química , Piridinas/química , Animais , Antineoplásicos/farmacologia , Benzilaminas/química , Catepsinas/antagonistas & inibidores , Catepsinas/química , Linhagem Celular , Linhagem Celular Tumoral , DNA/metabolismo , Humanos , Camundongos , Simulação de Acoplamento Molecular , Compostos Organometálicos/farmacologia , Inibidores de Proteases/farmacologia , Ligação Proteica , Albumina Sérica/química , Albumina Sérica/metabolismo
2.
Biomed Pharmacother ; 92: 1045-1054, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28618649

RESUMO

To evaluate the antitumor properties of Cafestol four leukemia cell lines were used (NB4, K562, HL60 and KG1). Cafestol exhibited the highest cytotoxicity against HL60 and KG1 cells, as evidenced by the accumulation of cells in the sub-G1 fraction, mitochondrial membrane potential reduction, accumulation of cleaved caspase-3 and phosphatidylserine externalization. An increase in CD11b and CD15 differentiation markers with attenuated ROS generation was also observed in Cafestol-treated HL60 cells. These results were similar to those obtained following exposure of the same cell line to cytarabine (Ara-C), an antileukemic drug. Cafestol and Ara-C reduced the clonogenic potential of HL60 cells by 100%, but Cafestol spared murine colony forming unit- granulocyte/macrophage (CFU-GM), which retained their clonogenicity. The co-treatment of Cafestol and Ara-C reduced HL60 cell viability compared with both drugs administered alone. In conclusion, despite the distinct molecular mechanisms involved in the activity of Cafestol and Ara-C, a similar cytotoxicity towards leukemia cells was observed, which suggests a need for prophylactic-therapeutic pre-clinical studies regarding the anticancer properties of Cafestol.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Coffea/química , Diterpenos/farmacologia , Leucemia/tratamento farmacológico , Animais , Antimetabólitos Antineoplásicos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose/efeitos dos fármacos , Antígeno CD11b/metabolismo , Caspase 3/metabolismo , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citarabina/farmacologia , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Fucosiltransferases/metabolismo , Células HL-60 , Células-Tronco Hematopoéticas/efeitos dos fármacos , Células-Tronco Hematopoéticas/metabolismo , Células-Tronco Hematopoéticas/patologia , Humanos , Células K562 , Leucemia/metabolismo , Leucemia/patologia , Antígenos CD15/metabolismo , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , Fosfatidilserinas/metabolismo , Fitoterapia , Plantas Medicinais , Espécies Reativas de Oxigênio/metabolismo
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