Estudo da atividade antineoplásica do complexo rutênio (II) com ligante 2-mercaptotiazolina
Autor(a) principal: | |
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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 |
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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 |
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por |
language |
por |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
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openAccess |
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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 |
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Centro Universitário Braz Cubas (CUB) |
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CUB |
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CUB |
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Repositório do Centro Universitário Braz Cubas |
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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 |
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