Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions
Autor(a) principal: | |
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Data de Publicação: | 2023 |
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/10400.14/40722 |
Resumo: | Chalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, the effect of chalcones 1–18 against the metabolic viability of cervical (HeLa) and prostate (PC-3 and LNCaP) tumor cell lines was tested, to compare the activity against solid and liquid tumor cells. Their effect was also evaluated on the Jurkat cell line. Chalcone 16 showed the highest inhibitory effect on the metabolic viability of the tested tumor cells and was selected for further studies. Recent antitumor therapies include compounds with the ability to influence immune cells on the tumor microenvironment, with immunotherapy being one actual goal in cancer treatment. Therefore, the effect of chalcone 16 on the expression of mTOR, HIF-1α, IL-1β, TNF-α, IL-10, and TGF-β, after THP-1 macrophage stimulation (none, LPS or IL-4), was evaluated. Chalcone 16 significantly increased the expression of mTORC1, IL-1β, TNF-α, and IL-10 of IL-4 stimulated macrophages (that induces an M2 phenotype). HIF-1α and TGF-β were not significantly affected. Chalcone 16 also decreased nitric oxide production by the RAW 264.7 murine macrophage cell line, this effect probably being due to an inhibition of iNOS expression. These results suggest that chalcone 16 may influence macrophage polarization, inducing the pro-tumoral M2 macrophages (IL-4 stimulated) to adopt a profile closer to the antitumor M1 profile. |
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Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functionsCancerChalconesImmunotherapyTumor associated macrophagesChalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, the effect of chalcones 1–18 against the metabolic viability of cervical (HeLa) and prostate (PC-3 and LNCaP) tumor cell lines was tested, to compare the activity against solid and liquid tumor cells. Their effect was also evaluated on the Jurkat cell line. Chalcone 16 showed the highest inhibitory effect on the metabolic viability of the tested tumor cells and was selected for further studies. Recent antitumor therapies include compounds with the ability to influence immune cells on the tumor microenvironment, with immunotherapy being one actual goal in cancer treatment. Therefore, the effect of chalcone 16 on the expression of mTOR, HIF-1α, IL-1β, TNF-α, IL-10, and TGF-β, after THP-1 macrophage stimulation (none, LPS or IL-4), was evaluated. Chalcone 16 significantly increased the expression of mTORC1, IL-1β, TNF-α, and IL-10 of IL-4 stimulated macrophages (that induces an M2 phenotype). HIF-1α and TGF-β were not significantly affected. Chalcone 16 also decreased nitric oxide production by the RAW 264.7 murine macrophage cell line, this effect probably being due to an inhibition of iNOS expression. These results suggest that chalcone 16 may influence macrophage polarization, inducing the pro-tumoral M2 macrophages (IL-4 stimulated) to adopt a profile closer to the antitumor M1 profile.Veritati - Repositório Institucional da Universidade Católica PortuguesaHorta, BrunoFreitas-Silva, JoanaSilva, JaniDias, FranciscaTeixeira, Ana LuísaMedeiros, RuiCidade, HonorinaPinto, MadalenaCerqueira, Fátima2023-03-27T16:47:29Z2023-02-252023-02-25T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10400.14/40722eng1420-304910.3390/molecules2805215985149901074PMC1000449736903405info: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:RCAAP2023-07-12T17:46:16Zoai:repositorio.ucp.pt:10400.14/40722Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T18:33:25.294031Repositório 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 |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions |
title |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions |
spellingShingle |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions Horta, Bruno Cancer Chalcones Immunotherapy Tumor associated macrophages |
title_short |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions |
title_full |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions |
title_fullStr |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions |
title_full_unstemmed |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions |
title_sort |
Antitumor effect of chalcone derivatives against human prostate (LNCaP and PC-3), cervix HPV-Positive (HeLa) and lymphocyte (Jurkat) cell lines and their effect on macrophage functions |
author |
Horta, Bruno |
author_facet |
Horta, Bruno Freitas-Silva, Joana Silva, Jani Dias, Francisca Teixeira, Ana Luísa Medeiros, Rui Cidade, Honorina Pinto, Madalena Cerqueira, Fátima |
author_role |
author |
author2 |
Freitas-Silva, Joana Silva, Jani Dias, Francisca Teixeira, Ana Luísa Medeiros, Rui Cidade, Honorina Pinto, Madalena Cerqueira, Fátima |
author2_role |
author author author author author author author author |
dc.contributor.none.fl_str_mv |
Veritati - Repositório Institucional da Universidade Católica Portuguesa |
dc.contributor.author.fl_str_mv |
Horta, Bruno Freitas-Silva, Joana Silva, Jani Dias, Francisca Teixeira, Ana Luísa Medeiros, Rui Cidade, Honorina Pinto, Madalena Cerqueira, Fátima |
dc.subject.por.fl_str_mv |
Cancer Chalcones Immunotherapy Tumor associated macrophages |
topic |
Cancer Chalcones Immunotherapy Tumor associated macrophages |
description |
Chalcones are synthetic and naturally occurring compounds that have been widely investigated as anticancer agents. In this work, the effect of chalcones 1–18 against the metabolic viability of cervical (HeLa) and prostate (PC-3 and LNCaP) tumor cell lines was tested, to compare the activity against solid and liquid tumor cells. Their effect was also evaluated on the Jurkat cell line. Chalcone 16 showed the highest inhibitory effect on the metabolic viability of the tested tumor cells and was selected for further studies. Recent antitumor therapies include compounds with the ability to influence immune cells on the tumor microenvironment, with immunotherapy being one actual goal in cancer treatment. Therefore, the effect of chalcone 16 on the expression of mTOR, HIF-1α, IL-1β, TNF-α, IL-10, and TGF-β, after THP-1 macrophage stimulation (none, LPS or IL-4), was evaluated. Chalcone 16 significantly increased the expression of mTORC1, IL-1β, TNF-α, and IL-10 of IL-4 stimulated macrophages (that induces an M2 phenotype). HIF-1α and TGF-β were not significantly affected. Chalcone 16 also decreased nitric oxide production by the RAW 264.7 murine macrophage cell line, this effect probably being due to an inhibition of iNOS expression. These results suggest that chalcone 16 may influence macrophage polarization, inducing the pro-tumoral M2 macrophages (IL-4 stimulated) to adopt a profile closer to the antitumor M1 profile. |
publishDate |
2023 |
dc.date.none.fl_str_mv |
2023-03-27T16:47:29Z 2023-02-25 2023-02-25T00:00:00Z |
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/10400.14/40722 |
url |
http://hdl.handle.net/10400.14/40722 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
1420-3049 10.3390/molecules28052159 85149901074 PMC10004497 36903405 |
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.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 |
instname_str |
Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
repository.name.fl_str_mv |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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1799132060538896384 |