In vitro and in vivo antitumoral activity of a ternary copper (II) complex
Autor(a) principal: | |
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Data de Publicação: | 2020 |
Outros Autores: | , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1016/j.bbrc.2020.09.104 http://hdl.handle.net/11449/205253 |
Resumo: | Recently, a high number of copper derivatives has been evaluated as DNA-targeting metallodrugs, due to the lower toxicity and its potential to cleave DNA. Several strategies have been testing to develop metal compounds effective against tumour cells. In this work, the ternary copper (doxycycline)-(1,10-phenanthroline) complex [Cu(dox)(phen)]2+ was especially designed as an antitumoral drug, previously showing high cytotoxicity and DNA cleavage activity. We aimed to further investigate the in vitro cytotoxic activity in both tumoral and non-tumoral cells, in vitro genotoxic potential, and in vivo antitumor activity using BALB/C mouse injected with sarcoma S180 and Ehrlich cell lines. Our results indicated that this compound exhibits a moderate genotoxic potential, with selective growth inhibition of tumor cells, especially the murine melanoma B16F10. Its main mechanism of action seems to be through ROS generation. We have further shown a significant reduction of the implanted tumor size in the animal model, suggesting that this compound has great antitumoral potential against many tumor types. [Cu(dox)(phen)]2+ is selectively cytotoxic for melanoma B16F10 and showed high chemotherapeutic potential in vivo against implanted sarcoma S180 and Ehrlich ascites tumours. |
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In vitro and in vivo antitumoral activity of a ternary copper (II) complexAntitumoral activityCytotoxicityGenotoxicityMelanomaSarcomaTernary copper (II) complexRecently, a high number of copper derivatives has been evaluated as DNA-targeting metallodrugs, due to the lower toxicity and its potential to cleave DNA. Several strategies have been testing to develop metal compounds effective against tumour cells. In this work, the ternary copper (doxycycline)-(1,10-phenanthroline) complex [Cu(dox)(phen)]2+ was especially designed as an antitumoral drug, previously showing high cytotoxicity and DNA cleavage activity. We aimed to further investigate the in vitro cytotoxic activity in both tumoral and non-tumoral cells, in vitro genotoxic potential, and in vivo antitumor activity using BALB/C mouse injected with sarcoma S180 and Ehrlich cell lines. Our results indicated that this compound exhibits a moderate genotoxic potential, with selective growth inhibition of tumor cells, especially the murine melanoma B16F10. Its main mechanism of action seems to be through ROS generation. We have further shown a significant reduction of the implanted tumor size in the animal model, suggesting that this compound has great antitumoral potential against many tumor types. [Cu(dox)(phen)]2+ is selectively cytotoxic for melanoma B16F10 and showed high chemotherapeutic potential in vivo against implanted sarcoma S180 and Ehrlich ascites tumours.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de Minas Gerais (FAPEMIG)Institute of Genetics and Biochemistry Federal University of UberlândiaInstitute of Biomedical Sciences Federal University of UberlândiaDepartment of Chemistry Federal Center of Technological Education of Minas GeraisDepartment of Chemistry Federal University of Minas GeraisLaboratory of Cytogenetics and Mutagenesis University Center of Patos de MinasChemistry Institute São Paulo State University - UNESPChemistry Institute São Paulo State University - UNESPUniversidade Federal de Uberlândia (UFU)Federal Center of Technological Education of Minas GeraisUniversidade Federal de Minas Gerais (UFMG)University Center of Patos de MinasUniversidade Estadual Paulista (Unesp)Lopes, Jeyson CésaryBotelho, Françoise VasconcelosBarbosa Silva, Marcelo JoséSilva, Suélen Fernandes [UNESP]Polloni, LorenaAlves Machado, Pedro HenriqueRodrigues de Souza, TiagoGoulart, Luiz RicardoSilva Caldeira, Priscila PereiraPereira Maia, Elene CristinaMorelli, Sandrade Oliveira-Júnior, Robson J.2021-06-25T10:12:19Z2021-06-25T10:12:19Z2020-12-17info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article1021-1026http://dx.doi.org/10.1016/j.bbrc.2020.09.104Biochemical and Biophysical Research Communications, v. 533, n. 4, p. 1021-1026, 2020.1090-21040006-291Xhttp://hdl.handle.net/11449/20525310.1016/j.bbrc.2020.09.1042-s2.0-85092028332Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengBiochemical and Biophysical Research Communicationsinfo:eu-repo/semantics/openAccess2021-10-23T12:23:59Zoai:repositorio.unesp.br:11449/205253Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T19:39:49.588145Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex |
title |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex |
spellingShingle |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex Lopes, Jeyson Césary Antitumoral activity Cytotoxicity Genotoxicity Melanoma Sarcoma Ternary copper (II) complex |
title_short |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex |
title_full |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex |
title_fullStr |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex |
title_full_unstemmed |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex |
title_sort |
In vitro and in vivo antitumoral activity of a ternary copper (II) complex |
author |
Lopes, Jeyson Césary |
author_facet |
Lopes, Jeyson Césary Botelho, Françoise Vasconcelos Barbosa Silva, Marcelo José Silva, Suélen Fernandes [UNESP] Polloni, Lorena Alves Machado, Pedro Henrique Rodrigues de Souza, Tiago Goulart, Luiz Ricardo Silva Caldeira, Priscila Pereira Pereira Maia, Elene Cristina Morelli, Sandra de Oliveira-Júnior, Robson J. |
author_role |
author |
author2 |
Botelho, Françoise Vasconcelos Barbosa Silva, Marcelo José Silva, Suélen Fernandes [UNESP] Polloni, Lorena Alves Machado, Pedro Henrique Rodrigues de Souza, Tiago Goulart, Luiz Ricardo Silva Caldeira, Priscila Pereira Pereira Maia, Elene Cristina Morelli, Sandra de Oliveira-Júnior, Robson J. |
author2_role |
author author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Federal de Uberlândia (UFU) Federal Center of Technological Education of Minas Gerais Universidade Federal de Minas Gerais (UFMG) University Center of Patos de Minas Universidade Estadual Paulista (Unesp) |
dc.contributor.author.fl_str_mv |
Lopes, Jeyson Césary Botelho, Françoise Vasconcelos Barbosa Silva, Marcelo José Silva, Suélen Fernandes [UNESP] Polloni, Lorena Alves Machado, Pedro Henrique Rodrigues de Souza, Tiago Goulart, Luiz Ricardo Silva Caldeira, Priscila Pereira Pereira Maia, Elene Cristina Morelli, Sandra de Oliveira-Júnior, Robson J. |
dc.subject.por.fl_str_mv |
Antitumoral activity Cytotoxicity Genotoxicity Melanoma Sarcoma Ternary copper (II) complex |
topic |
Antitumoral activity Cytotoxicity Genotoxicity Melanoma Sarcoma Ternary copper (II) complex |
description |
Recently, a high number of copper derivatives has been evaluated as DNA-targeting metallodrugs, due to the lower toxicity and its potential to cleave DNA. Several strategies have been testing to develop metal compounds effective against tumour cells. In this work, the ternary copper (doxycycline)-(1,10-phenanthroline) complex [Cu(dox)(phen)]2+ was especially designed as an antitumoral drug, previously showing high cytotoxicity and DNA cleavage activity. We aimed to further investigate the in vitro cytotoxic activity in both tumoral and non-tumoral cells, in vitro genotoxic potential, and in vivo antitumor activity using BALB/C mouse injected with sarcoma S180 and Ehrlich cell lines. Our results indicated that this compound exhibits a moderate genotoxic potential, with selective growth inhibition of tumor cells, especially the murine melanoma B16F10. Its main mechanism of action seems to be through ROS generation. We have further shown a significant reduction of the implanted tumor size in the animal model, suggesting that this compound has great antitumoral potential against many tumor types. [Cu(dox)(phen)]2+ is selectively cytotoxic for melanoma B16F10 and showed high chemotherapeutic potential in vivo against implanted sarcoma S180 and Ehrlich ascites tumours. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-12-17 2021-06-25T10:12:19Z 2021-06-25T10:12:19Z |
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://dx.doi.org/10.1016/j.bbrc.2020.09.104 Biochemical and Biophysical Research Communications, v. 533, n. 4, p. 1021-1026, 2020. 1090-2104 0006-291X http://hdl.handle.net/11449/205253 10.1016/j.bbrc.2020.09.104 2-s2.0-85092028332 |
url |
http://dx.doi.org/10.1016/j.bbrc.2020.09.104 http://hdl.handle.net/11449/205253 |
identifier_str_mv |
Biochemical and Biophysical Research Communications, v. 533, n. 4, p. 1021-1026, 2020. 1090-2104 0006-291X 10.1016/j.bbrc.2020.09.104 2-s2.0-85092028332 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Biochemical and Biophysical Research Communications |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
1021-1026 |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808129103874752512 |