A new chalcone derivative with promising antiproliferative and anti-invasion activities in glioblastoma cells
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/1822/74028 |
Resumo: | 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. |
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A new chalcone derivative with promising antiproliferative and anti-invasion activities in glioblastoma cellsGlioblastomaChalconeCell deathDrug deliveryLiposomesScience & TechnologyGlioblastoma (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.This research was funded by FCT to the PhD grant of DM fellowship (PD/BD/143038/2018) and the projects PATH (PD/00169/2013), FROnTHERA (NORTE-01-0145-FEDER-000023), Cells4_IDs (PTDC/BTM-SAL/28882/2017) and the NORTE 2020 Structured Project, co-funded by Norte2020 (NORTE-01-0145-FEDER-000021). This research was also supported by the Strategic Funding UIDB/04423/2020 and UIDP/04423/2020 (Group of Natural Products and Medicinal ChemistryCIIMAR) through national funds provided by the FCT and ERDF, within the framework of the program PT2020. Joana Moreira acknowledges her grant (SFRH/BD/135852/2018).Multidisciplinary Digital Publishing Institute (MDPI)Universidade do MinhoMendanha, DanielCastro, Joana Isabel Martins Cosme VieiraMoreira, JoanaCosta, Bruno MarquesCidade, HonorinaPinto, MadalenaFerreira, Helena Susana Costa MachadoNeves, N. M.2021-06-032021-06-03T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/1822/74028engMendanha, D.; Vieira de Castro, J.; Moreira, J.; Costa, B.M.; Cidade, H.; Pinto, M.; Ferreira, H.; Neves, N.M. A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells. Molecules 2021, 26, 3383. https://doi.org/10.3390/molecules261133831420-304910.3390/molecules2611338334205043https://www.mdpi.com/1420-3049/26/11/3383info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-07-21T12:36:34Zoai:repositorium.sdum.uminho.pt:1822/74028Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T19:32:41.134803Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
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 |
spellingShingle |
A new chalcone derivative with promising antiproliferative and anti-invasion activities in glioblastoma cells Mendanha, Daniel Glioblastoma Chalcone Cell death Drug delivery Liposomes Science & Technology |
title_short |
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_sort |
A new chalcone derivative with promising antiproliferative and anti-invasion activities in glioblastoma cells |
author |
Mendanha, Daniel |
author_facet |
Mendanha, Daniel Castro, Joana Isabel Martins Cosme Vieira Moreira, Joana Costa, Bruno Marques Cidade, Honorina Pinto, Madalena Ferreira, Helena Susana Costa Machado Neves, N. M. |
author_role |
author |
author2 |
Castro, Joana Isabel Martins Cosme Vieira Moreira, Joana Costa, Bruno Marques Cidade, Honorina Pinto, Madalena Ferreira, Helena Susana Costa Machado Neves, N. M. |
author2_role |
author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade do Minho |
dc.contributor.author.fl_str_mv |
Mendanha, Daniel Castro, Joana Isabel Martins Cosme Vieira Moreira, Joana Costa, Bruno Marques Cidade, Honorina Pinto, Madalena Ferreira, Helena Susana Costa Machado Neves, N. M. |
dc.subject.por.fl_str_mv |
Glioblastoma Chalcone Cell death Drug delivery Liposomes Science & Technology |
topic |
Glioblastoma Chalcone Cell death Drug delivery Liposomes Science & Technology |
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. |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-06-03 2021-06-03T00:00:00Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/1822/74028 |
url |
http://hdl.handle.net/1822/74028 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Mendanha, D.; Vieira de Castro, J.; Moreira, J.; Costa, B.M.; Cidade, H.; Pinto, M.; Ferreira, H.; Neves, N.M. A New Chalcone Derivative with Promising Antiproliferative and Anti-Invasion Activities in Glioblastoma Cells. Molecules 2021, 26, 3383. https://doi.org/10.3390/molecules26113383 1420-3049 10.3390/molecules26113383 34205043 https://www.mdpi.com/1420-3049/26/11/3383 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Multidisciplinary Digital Publishing Institute (MDPI) |
publisher.none.fl_str_mv |
Multidisciplinary Digital Publishing Institute (MDPI) |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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1799132839620378624 |