Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands
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.yrtph.2020.104653 http://hdl.handle.net/11449/200243 |
Resumo: | Considering the promising previous results of Cu (II) complexes with isoniazid active ligand against Mycobacterium tuberculosis, the main causative agent of tuberculosis, novel biological assays evaluating its toxicogenic potential were performed to ensure the safe use. The genotoxicity/mutagenicity of the complexes CuCl2(INH)2.H2O (I1), Cu(NCS)2(INH)2.5H2O (I2) and Cu(NCO)2(INH)2.4H2O (I3) was evaluated by the Comet, Micronucleus-cytome and Salmonella microsome (Ames test) assays. The cell viability using resazurin assay indicated that I1, I2 e I3 had moderate to low capacity to reduce the viability of colorectal cells (Caco-2), liver cells (HepG2), lung cells (GM 07492-A and A549) and endothelial cells (HU-VE-C). On genotoxicity/mutagenicity, I1 complex did not induce sizable levels of DNA damage in HepG2 cells (Comet assay), and gene (Ames test) and chromosomal (Micronucleus-cytome assay) mutations. Already, I2 and I3 complexes were considered mutagenic in the highest concentrations used. In light of the above, these results contribute to valuable data on the safe use of Cu(II) complexes. Considering the absence of mutagenicity and cytotoxicity of I1, this complex is a potential candidate for the development of a new drug to the treatment tuberculosis, while I2 and I3 require caution in its use. |
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Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligandsAmes testCitotoxicityComet assayCopper(II) complexesMicronucleus-cytome assayConsidering the promising previous results of Cu (II) complexes with isoniazid active ligand against Mycobacterium tuberculosis, the main causative agent of tuberculosis, novel biological assays evaluating its toxicogenic potential were performed to ensure the safe use. The genotoxicity/mutagenicity of the complexes CuCl2(INH)2.H2O (I1), Cu(NCS)2(INH)2.5H2O (I2) and Cu(NCO)2(INH)2.4H2O (I3) was evaluated by the Comet, Micronucleus-cytome and Salmonella microsome (Ames test) assays. The cell viability using resazurin assay indicated that I1, I2 e I3 had moderate to low capacity to reduce the viability of colorectal cells (Caco-2), liver cells (HepG2), lung cells (GM 07492-A and A549) and endothelial cells (HU-VE-C). On genotoxicity/mutagenicity, I1 complex did not induce sizable levels of DNA damage in HepG2 cells (Comet assay), and gene (Ames test) and chromosomal (Micronucleus-cytome assay) mutations. Already, I2 and I3 complexes were considered mutagenic in the highest concentrations used. In light of the above, these results contribute to valuable data on the safe use of Cu(II) complexes. Considering the absence of mutagenicity and cytotoxicity of I1, this complex is a potential candidate for the development of a new drug to the treatment tuberculosis, while I2 and I3 require caution in its use.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)ASCRS Research FoundationUNIARA- University of Araraquara Department of Biological Sciences and HealthUNESP-São Paulo State University Faculty of Pharmaceutical Sciences of Araraquara- Department of Biological SciencesUNESP-São Paulo State University Faculty of Pharmaceutical Sciences of Araraquara- Department of Biological SciencesFAPESP: 2013/09265-7ASCRS Research Foundation: 2017/16278-9FAPESP: 2017/16278-9ASCRS Research Foundation: D:\MYFILES\ELSEVIER\YRTPH\00104653\S-CESTRUCTURING\gs3UNIARA- University of AraraquaraUniversidade Estadual Paulista (Unesp)Fregonezi, Nathália FerreiraAparecida de Souza, FabianaAleixo, Nadia AndradeStefany da Silva Gomes, PietraSilvestre, Rafaela BaldassariDe Grandis, Rone Aparecido [UNESP]Bento da Silva, Patricia [UNESP]Pavan, Fernando Rogério [UNESP]Chorilli, Marlus [UNESP]Resende, Flavia Aparecida2020-12-12T02:01:21Z2020-12-12T02:01:21Z2020-06-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1016/j.yrtph.2020.104653Regulatory Toxicology and Pharmacology, v. 113.1096-02950273-2300http://hdl.handle.net/11449/20024310.1016/j.yrtph.2020.1046532-s2.0-85082876111Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengRegulatory Toxicology and Pharmacologyinfo:eu-repo/semantics/openAccess2024-06-24T13:08:13Zoai:repositorio.unesp.br:11449/200243Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T21:30:42.087378Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands |
title |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands |
spellingShingle |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands Fregonezi, Nathália Ferreira Ames test Citotoxicity Comet assay Copper(II) complexes Micronucleus-cytome assay |
title_short |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands |
title_full |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands |
title_fullStr |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands |
title_full_unstemmed |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands |
title_sort |
Cyto-genotoxic evaluation of novel anti-tubercular copper (II) complexes containing isoniazid-based ligands |
author |
Fregonezi, Nathália Ferreira |
author_facet |
Fregonezi, Nathália Ferreira Aparecida de Souza, Fabiana Aleixo, Nadia Andrade Stefany da Silva Gomes, Pietra Silvestre, Rafaela Baldassari De Grandis, Rone Aparecido [UNESP] Bento da Silva, Patricia [UNESP] Pavan, Fernando Rogério [UNESP] Chorilli, Marlus [UNESP] Resende, Flavia Aparecida |
author_role |
author |
author2 |
Aparecida de Souza, Fabiana Aleixo, Nadia Andrade Stefany da Silva Gomes, Pietra Silvestre, Rafaela Baldassari De Grandis, Rone Aparecido [UNESP] Bento da Silva, Patricia [UNESP] Pavan, Fernando Rogério [UNESP] Chorilli, Marlus [UNESP] Resende, Flavia Aparecida |
author2_role |
author author author author author author author author author |
dc.contributor.none.fl_str_mv |
UNIARA- University of Araraquara Universidade Estadual Paulista (Unesp) |
dc.contributor.author.fl_str_mv |
Fregonezi, Nathália Ferreira Aparecida de Souza, Fabiana Aleixo, Nadia Andrade Stefany da Silva Gomes, Pietra Silvestre, Rafaela Baldassari De Grandis, Rone Aparecido [UNESP] Bento da Silva, Patricia [UNESP] Pavan, Fernando Rogério [UNESP] Chorilli, Marlus [UNESP] Resende, Flavia Aparecida |
dc.subject.por.fl_str_mv |
Ames test Citotoxicity Comet assay Copper(II) complexes Micronucleus-cytome assay |
topic |
Ames test Citotoxicity Comet assay Copper(II) complexes Micronucleus-cytome assay |
description |
Considering the promising previous results of Cu (II) complexes with isoniazid active ligand against Mycobacterium tuberculosis, the main causative agent of tuberculosis, novel biological assays evaluating its toxicogenic potential were performed to ensure the safe use. The genotoxicity/mutagenicity of the complexes CuCl2(INH)2.H2O (I1), Cu(NCS)2(INH)2.5H2O (I2) and Cu(NCO)2(INH)2.4H2O (I3) was evaluated by the Comet, Micronucleus-cytome and Salmonella microsome (Ames test) assays. The cell viability using resazurin assay indicated that I1, I2 e I3 had moderate to low capacity to reduce the viability of colorectal cells (Caco-2), liver cells (HepG2), lung cells (GM 07492-A and A549) and endothelial cells (HU-VE-C). On genotoxicity/mutagenicity, I1 complex did not induce sizable levels of DNA damage in HepG2 cells (Comet assay), and gene (Ames test) and chromosomal (Micronucleus-cytome assay) mutations. Already, I2 and I3 complexes were considered mutagenic in the highest concentrations used. In light of the above, these results contribute to valuable data on the safe use of Cu(II) complexes. Considering the absence of mutagenicity and cytotoxicity of I1, this complex is a potential candidate for the development of a new drug to the treatment tuberculosis, while I2 and I3 require caution in its use. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-12-12T02:01:21Z 2020-12-12T02:01:21Z 2020-06-01 |
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.yrtph.2020.104653 Regulatory Toxicology and Pharmacology, v. 113. 1096-0295 0273-2300 http://hdl.handle.net/11449/200243 10.1016/j.yrtph.2020.104653 2-s2.0-85082876111 |
url |
http://dx.doi.org/10.1016/j.yrtph.2020.104653 http://hdl.handle.net/11449/200243 |
identifier_str_mv |
Regulatory Toxicology and Pharmacology, v. 113. 1096-0295 0273-2300 10.1016/j.yrtph.2020.104653 2-s2.0-85082876111 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Regulatory Toxicology and Pharmacology |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
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 |
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_version_ |
1808129328855121920 |