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...
Autores principales: | , , , , |
---|---|
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 |
_version_ | 1783376804535336960 |
---|---|
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. |
format | Online Article Text |
id | pubmed-6270897 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT grucaaleksandra syntheticgenisteinglycosidesinhibitingegfrphosphorylationenhancetheeffectofradiationinhct116coloncancercells AT krawczykzdzisław syntheticgenisteinglycosidesinhibitingegfrphosphorylationenhancetheeffectofradiationinhct116coloncancercells AT szejawiesław syntheticgenisteinglycosidesinhibitingegfrphosphorylationenhancetheeffectofradiationinhct116coloncancercells AT grynkiewiczgrzegorz syntheticgenisteinglycosidesinhibitingegfrphosphorylationenhancetheeffectofradiationinhct116coloncancercells AT rusinaleksandra syntheticgenisteinglycosidesinhibitingegfrphosphorylationenhancetheeffectofradiationinhct116coloncancercells |