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Título : Potential antitumor and pro-oxidative effects of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenil)acrylate (QNACR)
Autor : Rodrigues, Juan
Ferrer, Rosa
Gamboa, Neira
Charris, Jaime
Antunes, Fernando
Palabras clave : Reactive oxygen species, antioxidant enzyms, oxidative stress, antineoplasic
Fecha de publicación : 1-Oct-2012
Editorial : Journal of Enzyme Inhibition and Medicinal Chemistry 28 (6), 1300-1306, 2013
Resumen : Reactive oxygen species (ROS) induce cellular damage and represent unique opportunities to kill malignant cells. In this study, we synthesized and evaluated the new compound, (E)-methyl 2-(7-chloroquinolin-4- ylthio)-3-(4-hydroxyphenyl) acrylate (QNACR) as potential pro-oxidative agent against breast cancer. Methods: Oxidative stress biomarkers such as ROS, thiobarbuturic acid reactive species (TBARs) and different antioxidant enzyme activities were determined in cell lysates. Results: QNACR showed cytotoxic and more selective effects to tumour MCF7 cells (IC50 < 25 μM) compared to antitumour controls, inducing ROS and TBARs parallel to inhibitions of catalase (CAT), glucose-6-phosphate dehydrogenase (G6PDH) and 6-phosphogluconate dehydrogenase (6PGDH). Longer exposures to QNACR triggered adaptive effects increasing the overall activities of CAT, glutathione reductase, G6PDH and 6PGDH, but eventually the adaptation changes faded and cells died. Conclusion: QNACR led to remarkable modifications in the oxidative status of tumour cells, proposing this compound as potential alternative for antitumour therapy.
ISSN : 1475-6366
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