Cargando…
A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells
Glioblastoma (GBM) is the most common and most deadly primary malignant brain tumor. Current therapies are not effective, the average survival of GBM patients after diagnosis being limited to few months. Therefore, the discovery of new treatments for this highly aggressive brain cancer is urgently n...
Autores principales: | , , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8199914/ https://www.ncbi.nlm.nih.gov/pubmed/34205043 http://dx.doi.org/10.3390/molecules26113383 |
_version_ | 1783707487369691136 |
---|---|
author | Mendanha, Daniel Vieira de Castro, Joana Moreira, Joana Costa, Bruno M. Cidade, Honorina Pinto, Madalena Ferreira, Helena Neves, Nuno M. |
author_facet | Mendanha, Daniel Vieira de Castro, Joana Moreira, Joana Costa, Bruno M. Cidade, Honorina Pinto, Madalena Ferreira, Helena Neves, Nuno M. |
author_sort | Mendanha, Daniel |
collection | PubMed |
description | Glioblastoma (GBM) is the most common and most deadly primary malignant brain tumor. Current therapies are not effective, the average survival of GBM patients after diagnosis being limited to few months. Therefore, the discovery of new treatments for this highly aggressive brain cancer is urgently needed. Chalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, three chalcone derivatives were tested regarding their inhibitory activity and selectivity towards GBM cell lines (human and mouse) and a non-cancerous mouse brain cell line. The chalcone 1 showed the most potent and selective cytotoxic effects in the GBM cell lines, being further investigated regarding its ability to reduce critical hallmark features of GBM and to induce apoptosis and cell cycle arrest. This derivative showed to successfully reduce the invasion and proliferation capacity of tumor cells, both key targets for cancer treatment. Moreover, to overcome potential systemic side effects and its poor water solubility, this compound was encapsulated into liposomes. Therapeutic concentrations were incorporated retaining the potent in vitro growth inhibitory effect of the selected compound. In conclusion, our results demonstrated that this new formulation can be a promising starting point for the discovery of new and more effective drug treatments for GBM. |
format | Online Article Text |
id | pubmed-8199914 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-81999142021-06-14 A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells Mendanha, Daniel Vieira de Castro, Joana Moreira, Joana Costa, Bruno M. Cidade, Honorina Pinto, Madalena Ferreira, Helena Neves, Nuno M. Molecules Article Glioblastoma (GBM) is the most common and most deadly primary malignant brain tumor. Current therapies are not effective, the average survival of GBM patients after diagnosis being limited to few months. Therefore, the discovery of new treatments for this highly aggressive brain cancer is urgently needed. Chalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, three chalcone derivatives were tested regarding their inhibitory activity and selectivity towards GBM cell lines (human and mouse) and a non-cancerous mouse brain cell line. The chalcone 1 showed the most potent and selective cytotoxic effects in the GBM cell lines, being further investigated regarding its ability to reduce critical hallmark features of GBM and to induce apoptosis and cell cycle arrest. This derivative showed to successfully reduce the invasion and proliferation capacity of tumor cells, both key targets for cancer treatment. Moreover, to overcome potential systemic side effects and its poor water solubility, this compound was encapsulated into liposomes. Therapeutic concentrations were incorporated retaining the potent in vitro growth inhibitory effect of the selected compound. In conclusion, our results demonstrated that this new formulation can be a promising starting point for the discovery of new and more effective drug treatments for GBM. MDPI 2021-06-03 /pmc/articles/PMC8199914/ /pubmed/34205043 http://dx.doi.org/10.3390/molecules26113383 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Mendanha, Daniel Vieira de Castro, Joana Moreira, Joana Costa, Bruno M. Cidade, Honorina Pinto, Madalena Ferreira, Helena Neves, Nuno M. A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells |
title | A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells |
title_full | A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells |
title_fullStr | A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells |
title_full_unstemmed | A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells |
title_short | A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells |
title_sort | new chalcone derivative with promising antiproliferative and anti-invasion activities in glioblastoma cells |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8199914/ https://www.ncbi.nlm.nih.gov/pubmed/34205043 http://dx.doi.org/10.3390/molecules26113383 |
work_keys_str_mv | AT mendanhadaniel anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT vieiradecastrojoana anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT moreirajoana anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT costabrunom anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT cidadehonorina anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT pintomadalena anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT ferreirahelena anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT nevesnunom anewchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT mendanhadaniel newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT vieiradecastrojoana newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT moreirajoana newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT costabrunom newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT cidadehonorina newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT pintomadalena newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT ferreirahelena newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells AT nevesnunom newchalconederivativewithpromisingantiproliferativeandantiinvasionactivitiesinglioblastomacells |