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1.
Toxicol Appl Pharmacol ; 356: 127-138, 2018 10 01.
Artículo en Inglés | MEDLINE | ID: mdl-30092250

RESUMEN

Copper (II) complexes are promising in the development of new synthetic models for cancer treatment. In this context, we synthesized a new copper complex containing the pharmacophore group 1,4-dioxo-2-butenyl, the Bis(((Z)-4-((4-chlorophenyl) amino)-4-oxobut-2-enoyl)oxy) copper compound and we evaluated its antitumor activity in 4 T1 murine mammary adenocarcinoma cells and their toxicogenic effect in Swiss mice. The compound demonstrated cytotoxicity and genotoxicity to 4 T1 cells, and after cell cycle arrest in G1, which occurred by the increase in ATM and p21 expression, it induced the cells to apoptosis by increasing BAX and caspase-7. In vivo the compound was genotoxic in mice but did not show permanent damage, observed by the absence of increased micronucleus frequency, and did not induce changes in the biometric parameters of the animals. These results indicate that the new copper complex, described firstly in this work, presents therapeutic potential for breast cancer.


Asunto(s)
Antineoplásicos/farmacología , Complejos de Coordinación/uso terapéutico , Cobre/uso terapéutico , Adenocarcinoma/tratamiento farmacológico , Animales , Antineoplásicos/toxicidad , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Membrana Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Ensayo Cometa , Cobre/química , Femenino , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Neoplasias Mamarias Experimentales/tratamiento farmacológico , Ratones , Bazo/citología , Bazo/efectos de los fármacos
2.
Environ Sci Pollut Res Int ; 26(9): 9193-9202, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30719661

RESUMEN

The amphyphylic triazoanilines recently synthesized 1-(4-(3-aminophenyl)-1H-1,2,3- triazole-1-yl)-3-(3-pentadecylphenoxy)propan-2-ol (1) and 1-(4-(4-aminophenyl)-1H- 1,2,3-triazole-1-yl)-3-(3-pentadecylphenoxy)propan-2-ol (2), synthesized from cardanol and glycerol, have photophysical properties which allow their use in the development of fluorescent biomarkers with applicability in the biodiesel quality control. Based on this, the present research evaluated the toxic effects of both compounds in different biological models through the investigation of survival and mortality percentages as a measure of acute toxicity on Daphnia similis and Oreochromis niloticus, larvicidal assay against Aedes aegypti, and cytotoxic activity on mammary cells. Results demonstrate that these triazoanilines 1 and 2 have shown low acute toxicity to the biological models investigated in this study up to the following concentrations: 4.0 mg L-1 (D. similis), 4.0 mg L-1 (A. aegypti larvae), 1.0 mg L-1 (O. niloticus), and 1.0 mg mL-1 (mammary cells). This fact suggests the potential for safe use of compounds 1 and 2 as fluorescent markers for the monitoring of biodiesel quality, even in the case of environmental exposure. Besides all of that, the reuse of cardanol and glycerol, both industrial wastes, favors the maintenance of environmental health and is in agreement with the assumptions of green chemistry. Graphical abstract ᅟ.


Asunto(s)
Glicerol/toxicidad , Sustancias Peligrosas/toxicidad , Residuos Industriales , Fenoles/toxicidad , Pruebas de Toxicidad Aguda/métodos , Aedes/efectos de los fármacos , Animales , Biomarcadores/metabolismo , Daphnia/efectos de los fármacos , Insecticidas/toxicidad , Larva/efectos de los fármacos , Modelos Biológicos , Extractos Vegetales/toxicidad
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