Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells

The need to find new EGFR inhibitors for use in combination with radiotherapy in the treatment of solid tumors has drawn our attention to compounds derived from genistein, a natural isoflavonoid. The antiproliferative potential of synthetic genistein derivatives used alone or in combination with ion...

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Autores principales: Gruca, Aleksandra, Krawczyk, Zdzisław, Szeja, Wiesław, Grynkiewicz, Grzegorz, Rusin, Aleksandra
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270897/
https://www.ncbi.nlm.nih.gov/pubmed/25401399
http://dx.doi.org/10.3390/molecules191118558
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author Gruca, Aleksandra
Krawczyk, Zdzisław
Szeja, Wiesław
Grynkiewicz, Grzegorz
Rusin, Aleksandra
author_facet Gruca, Aleksandra
Krawczyk, Zdzisław
Szeja, Wiesław
Grynkiewicz, Grzegorz
Rusin, Aleksandra
author_sort Gruca, Aleksandra
collection PubMed
description The need to find new EGFR inhibitors for use in combination with radiotherapy in the treatment of solid tumors has drawn our attention to compounds derived from genistein, a natural isoflavonoid. The antiproliferative potential of synthetic genistein derivatives used alone or in combination with ionizing radiation was evaluated in cancer cell lines using clonogenic assay. EGFR phosphorylation was assessed with western blotting. Genistein derivatives inhibited clonogenic growth of HCT 116 cancer cells additively or synergistically when used in combination with ionizing radiation, and decreased EGFR activation. Our preclinical evaluation of genistein-derived EGFR inhibitors suggests that these compounds are much more potent sensitizers of cells to radiation than the parent isoflavonoid, genistein and indicate that these compounds may be useful in the treatment of colon cancer with radiation therapy.
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spelling pubmed-62708972019-01-07 Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells Gruca, Aleksandra Krawczyk, Zdzisław Szeja, Wiesław Grynkiewicz, Grzegorz Rusin, Aleksandra Molecules Article The need to find new EGFR inhibitors for use in combination with radiotherapy in the treatment of solid tumors has drawn our attention to compounds derived from genistein, a natural isoflavonoid. The antiproliferative potential of synthetic genistein derivatives used alone or in combination with ionizing radiation was evaluated in cancer cell lines using clonogenic assay. EGFR phosphorylation was assessed with western blotting. Genistein derivatives inhibited clonogenic growth of HCT 116 cancer cells additively or synergistically when used in combination with ionizing radiation, and decreased EGFR activation. Our preclinical evaluation of genistein-derived EGFR inhibitors suggests that these compounds are much more potent sensitizers of cells to radiation than the parent isoflavonoid, genistein and indicate that these compounds may be useful in the treatment of colon cancer with radiation therapy. MDPI 2014-11-13 /pmc/articles/PMC6270897/ /pubmed/25401399 http://dx.doi.org/10.3390/molecules191118558 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Gruca, Aleksandra
Krawczyk, Zdzisław
Szeja, Wiesław
Grynkiewicz, Grzegorz
Rusin, Aleksandra
Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells
title Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells
title_full Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells
title_fullStr Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells
title_full_unstemmed Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells
title_short Synthetic Genistein Glycosides Inhibiting EGFR Phosphorylation Enhance the Effect of Radiation in HCT 116 Colon Cancer Cells
title_sort synthetic genistein glycosides inhibiting egfr phosphorylation enhance the effect of radiation in hct 116 colon cancer cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270897/
https://www.ncbi.nlm.nih.gov/pubmed/25401399
http://dx.doi.org/10.3390/molecules191118558
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