Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina

Detalhes bibliográficos
Autor(a) principal: Melo, Matheus Reis Santos de
Data de Publicação: 2022
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Repositório do Centro Universitário Braz Cubas
Texto Completo: https://repositorio.cruzeirodosul.edu.br/handle/123456789/4068
Resumo: Melanoma is the least affected type of skin cancer in the world, however, it is the most aggressive and lethal due to its characteristics such as high metastatic potential and low response rate to existing treatment modalities. Thus, new drug prototypes are being developed to solve the problem of treating patients with melanomas. Among the prototypes, metallopharmaceuticals such as ruthenium have emerged as promising alternatives due to their selective antitumor characteristics and low systemic toxicity. In this context, the present study evaluated the complex effect of ruthenium [Ru(mtz)(dppe)2]PF6 (RuMTZ) on human (A-375) and murine (B16-F10) melanoma tumor cell lines, considering different approaches. The results demonstrate that RuMTZ has cytotoxic activity, with IC50 values ranging from 2.1 to 19.6 µM in the XTT colorimetric assay and from 0.3 to 1.28 µM in the clonogenic efficiency assay. RuMTZ also induced changes in cell morphology and inhibited cell migration by 35.17% and 43.87%, respectively, for A-375 and B16-F10. Furthermore, an increase in cell populations with fragmented DNA in the sub-G0 phase was observed in both melanoma cell lines and an increase in the level of apoptosis in A-375. Molecular assays showed the absence of cleaved capase-3 for both cell lines. The data obtained indicate that RuMTZ has promising antitumor and anti-metastatic activity against melanoma. Keywords: Thiazoline, melanoma, antitumor activity, metallodrug
id CUB_59b7ec1f93ef6c96b07b88db480935dd
oai_identifier_str oai:repositorio.cruzeirodosul.edu.br:123456789/4068
network_acronym_str CUB
network_name_str Repositório do Centro Universitário Braz Cubas
repository_id_str
spelling Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolinaStudy of the antineoplastic activity of the ruthenium (II) complex with 2-mercaptothiazoline ligandTiazolinaMelanomaAtividade antitumoralMetalofármacoCNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICAMelanoma is the least affected type of skin cancer in the world, however, it is the most aggressive and lethal due to its characteristics such as high metastatic potential and low response rate to existing treatment modalities. Thus, new drug prototypes are being developed to solve the problem of treating patients with melanomas. Among the prototypes, metallopharmaceuticals such as ruthenium have emerged as promising alternatives due to their selective antitumor characteristics and low systemic toxicity. In this context, the present study evaluated the complex effect of ruthenium [Ru(mtz)(dppe)2]PF6 (RuMTZ) on human (A-375) and murine (B16-F10) melanoma tumor cell lines, considering different approaches. The results demonstrate that RuMTZ has cytotoxic activity, with IC50 values ranging from 2.1 to 19.6 µM in the XTT colorimetric assay and from 0.3 to 1.28 µM in the clonogenic efficiency assay. RuMTZ also induced changes in cell morphology and inhibited cell migration by 35.17% and 43.87%, respectively, for A-375 and B16-F10. Furthermore, an increase in cell populations with fragmented DNA in the sub-G0 phase was observed in both melanoma cell lines and an increase in the level of apoptosis in A-375. Molecular assays showed the absence of cleaved capase-3 for both cell lines. The data obtained indicate that RuMTZ has promising antitumor and anti-metastatic activity against melanoma. Keywords: Thiazoline, melanoma, antitumor activity, metallodrugO melanoma é o tipo de câncer de pele menos acometido no mundo, entretanto, é o mais agressivo e letal devido suas características como alto potencial metastático e baixa taxa de resposta para as modalidades de tratamentos existentes. Desta forma, novos protótipos de fármacos estão sendo desenvolvidos para solucionar a problemática do tratamento de pacientes com melanomas. Dentre os protótipos, metalofármacos como rutênio surgiram como alternativas promissoras devido as características seletivas antitumorais e baixa toxicidade sistêmica. Neste contexto, o presente estudo avaliou o efeito complexo de rutênio [Ru(mtz)(dppe)2]PF6 (RuMTZ) sobre linhagens celulares tumorais de melanoma humano (A-375) e murino (B16-F10), considerando diferentes abordagens. Os resultados demonstram que RuMTZ possui atividade citotóxica, com valores de IC50 que variaram de 2,1 a 19,6 µM no ensaio colorimétrico de XTT e de 0,3 a 1,28 µM no ensaio de eficiência clonogênica. RuMTZ também induziu alteração na morfologia celular e inibiu a migração celular em 35,17 % e 43,87 %, respectivamente, para A-375 e B16-F10. Ademais, observou-se aumento de populações celulares com DNA fragmentado na fase sub-G0 em ambas as linhagens de melanoma e aumento no nível de apoptose em A-375. Os ensaios moleculares demonstraram ausência de capase-3 clivada para ambas as linhagens celulares. Os dados obtidos indicam que RuMTZ possui atividade promissora antitumoral e anti-metastática contra melanoma. Palavras-chave: Tiazolina, melanoma, atividade antitumoral, metalofármacoUniversidade de francaBrasilPós-GraduaçãoPrograma de Mestrado em CiênciasUNIFRANTavares, Denise Crispim5342181863190744http://lattes.cnpq.br/5342181863190744Nicolella, Heloiza Diniz1843100482076952http://lattes.cnpq.br/1843100482076952Oliveira, Pollyanna Francielli de2070113210417605http://lattes.cnpq.br/2070113210417605Melo, Matheus Reis Santos de2022-10-05T21:03:02Z2022-10-05T21:03:02Z2022-03-03info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfMELO, Matheus Reis Santos de. Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina. Franca, SP, 2022. 66 f. Dissertação (Mestrado em Ciências) - Universidade de Franca, 2022https://repositorio.cruzeirodosul.edu.br/handle/123456789/4068porinfo:eu-repo/semantics/openAccessreponame:Repositório do Centro Universitário Braz Cubasinstname:Centro Universitário Braz Cubas (CUB)instacron:CUB2022-10-05T21:04:17Zoai:repositorio.cruzeirodosul.edu.br:123456789/4068Repositório InstitucionalPUBhttps://repositorio.brazcubas.edu.br/oai/requestbibli@brazcubas.edu.bropendoar:2022-10-05T21:04:17Repositório do Centro Universitário Braz Cubas - Centro Universitário Braz Cubas (CUB)false
dc.title.none.fl_str_mv Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
Study of the antineoplastic activity of the ruthenium (II) complex with 2-mercaptothiazoline ligand
title Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
spellingShingle Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
Melo, Matheus Reis Santos de
Tiazolina
Melanoma
Atividade antitumoral
Metalofármaco
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
title_short Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
title_full Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
title_fullStr Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
title_full_unstemmed Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
title_sort Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
author Melo, Matheus Reis Santos de
author_facet Melo, Matheus Reis Santos de
author_role author
dc.contributor.none.fl_str_mv Tavares, Denise Crispim
5342181863190744
http://lattes.cnpq.br/5342181863190744
Nicolella, Heloiza Diniz
1843100482076952
http://lattes.cnpq.br/1843100482076952
Oliveira, Pollyanna Francielli de
2070113210417605
http://lattes.cnpq.br/2070113210417605
dc.contributor.author.fl_str_mv Melo, Matheus Reis Santos de
dc.subject.por.fl_str_mv Tiazolina
Melanoma
Atividade antitumoral
Metalofármaco
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
topic Tiazolina
Melanoma
Atividade antitumoral
Metalofármaco
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
description Melanoma is the least affected type of skin cancer in the world, however, it is the most aggressive and lethal due to its characteristics such as high metastatic potential and low response rate to existing treatment modalities. Thus, new drug prototypes are being developed to solve the problem of treating patients with melanomas. Among the prototypes, metallopharmaceuticals such as ruthenium have emerged as promising alternatives due to their selective antitumor characteristics and low systemic toxicity. In this context, the present study evaluated the complex effect of ruthenium [Ru(mtz)(dppe)2]PF6 (RuMTZ) on human (A-375) and murine (B16-F10) melanoma tumor cell lines, considering different approaches. The results demonstrate that RuMTZ has cytotoxic activity, with IC50 values ranging from 2.1 to 19.6 µM in the XTT colorimetric assay and from 0.3 to 1.28 µM in the clonogenic efficiency assay. RuMTZ also induced changes in cell morphology and inhibited cell migration by 35.17% and 43.87%, respectively, for A-375 and B16-F10. Furthermore, an increase in cell populations with fragmented DNA in the sub-G0 phase was observed in both melanoma cell lines and an increase in the level of apoptosis in A-375. Molecular assays showed the absence of cleaved capase-3 for both cell lines. The data obtained indicate that RuMTZ has promising antitumor and anti-metastatic activity against melanoma. Keywords: Thiazoline, melanoma, antitumor activity, metallodrug
publishDate 2022
dc.date.none.fl_str_mv 2022-10-05T21:03:02Z
2022-10-05T21:03:02Z
2022-03-03
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
format masterThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv MELO, Matheus Reis Santos de. Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina. Franca, SP, 2022. 66 f. Dissertação (Mestrado em Ciências) - Universidade de Franca, 2022
https://repositorio.cruzeirodosul.edu.br/handle/123456789/4068
identifier_str_mv MELO, Matheus Reis Santos de. Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina. Franca, SP, 2022. 66 f. Dissertação (Mestrado em Ciências) - Universidade de Franca, 2022
url https://repositorio.cruzeirodosul.edu.br/handle/123456789/4068
dc.language.iso.fl_str_mv por
language por
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 Universidade de franca
Brasil
Pós-Graduação
Programa de Mestrado em Ciências
UNIFRAN
publisher.none.fl_str_mv Universidade de franca
Brasil
Pós-Graduação
Programa de Mestrado em Ciências
UNIFRAN
dc.source.none.fl_str_mv reponame:Repositório do Centro Universitário Braz Cubas
instname:Centro Universitário Braz Cubas (CUB)
instacron:CUB
instname_str Centro Universitário Braz Cubas (CUB)
instacron_str CUB
institution CUB
reponame_str Repositório do Centro Universitário Braz Cubas
collection Repositório do Centro Universitário Braz Cubas
repository.name.fl_str_mv Repositório do Centro Universitário Braz Cubas - Centro Universitário Braz Cubas (CUB)
repository.mail.fl_str_mv bibli@brazcubas.edu.br
_version_ 1798311335537147904