New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification

Detalhes bibliográficos
Autor(a) principal: Munkert, Jennifer
Data de Publicação: 2019
Outros Autores: Gomes, Eliza R, Marostica, Lucas L, Cota, Betânia Barros, Lopes, Cristina L M, Andrade, Saulo F, Souza Filho, José D de, Alves, Ricardo J, Oliveira, Monica C, Braga, Fernão C, Simões, Cláudia M O, Pádua, Rodrigo M, Barros, André L B de
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/57494
Resumo: Department of Biology. Friedrich-Alexander-Universität Erlangen-Nürnberg. Staudtstrasse 5, 91058 Erlangen, Germany.
id CRUZ_995a08e5d0c3d8ab6102df0426719f30
oai_identifier_str oai:www.arca.fiocruz.br:icict/57494
network_acronym_str CRUZ
network_name_str Repositório Institucional da FIOCRUZ (ARCA)
repository_id_str 2135
spelling Munkert, JenniferGomes, Eliza RMarostica, Lucas LCota, Betânia BarrosLopes, Cristina L MAndrade, Saulo FSouza Filho, José D deAlves, Ricardo JOliveira, Monica CBraga, Fernão CSimões, Cláudia M OPádua, Rodrigo MBarros, André L B de2023-03-21T18:35:33Z2023-03-21T18:35:33Z2019MUNKERT, Jennifer et al. New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification. ACS Omega, v. 4, n. 26, p. 22048-22056, 2019. doi: 10.1021/acsomega.9b03167.2470-1343https://www.arca.fiocruz.br/handle/icict/57494engAmerican Chemical SocietyNew 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identificationinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleDepartment of Biology. Friedrich-Alexander-Universität Erlangen-Nürnberg. Staudtstrasse 5, 91058 Erlangen, Germany.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.Department of Pharmaceutical Sciences. Universidade Federal de Santa Catarina. Florianópolis, SC, Brazil.Fundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Química de Produtos Naturais Bioativos. Belo Horizonte, MG, Brazil.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.Faculty of Pharmaceutical Sciences. Universidade Federal de Rio Grande do Sul. Porto Alegre, RS, Brazil.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.Department of Pharmaceutical Sciences. Universidade Federal de Santa Catarina. Florianópolis, SC, Brazil.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.Faculty of Pharmacy and Department of Chemistry. Universidade Federal de Minas Gerais. Belo Horizonte, MG, Brazil.In recent years, cardiac glycosides (CGs) have been investigated as potential antiviral and anticancer drugs. Digitoxigenin (DIG) and other CGs have been shown to bind and inhibit Na+/K+-adenosinetriphosphatase (ATPase). Tumor cells show a higher expression rate of the Na+/K+-ATPase protein or a stronger affinity towards the binding of CGs and are therefore more prone to CGs than non-tumor cells. Cancer imaging techniques using radiotracers targeted at specific receptors have yielded successful results. Technetium-99m (99mTc) is one of the radionuclides of choice to radiolabel pharmaceuticals because of its favorable physical and chemical properties along with reasonable costs. Herein, we describe a new Na+/K+-ATPase targeting radiotracer consisting of digitoxigenin and diethylenetriaminepentaacetic acid (DTPA), a bifunctional chelating ligand used to prepare 99mTc-labeled complexes, and its evaluation as an imaging probe. We report the synthesis and characterization of the radiolabeled compound including stability tests, blood clearance, and biodistribution in healthy mice. Additionally, we investigated the binding of the compound to A549 human non-small-cell lung cancer cells and the inhibition of the Na+/K+-ATPase by the labeled compound in vitro. The 99mTc-labeled DTPA-digitoxigenin (99mTc-DTPA-DIG) compound displayed high stability in vitro and in vivo, a fast renal excretion, and a specific binding towards A549 cancer cells in comparison to non-tumor cells. Therefore, 99mTc-DTPA-DIG could potentially be used for non-invasive visualization of tumor lesions by means of scintigraphic imaging.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/57494/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALNew 99mTc-Labeled Digitoxigenin Derivative.pdfNew 99mTc-Labeled Digitoxigenin Derivative.pdfapplication/pdf1420503https://www.arca.fiocruz.br/bitstream/icict/57494/2/New%2099mTc-Labeled%20Digitoxigenin%20Derivative.pdf754b09cf849d119c44ac400a7d77dee3MD52icict/574942023-03-21 15:35:34.488oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352023-03-21T18:35:34Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.en_US.fl_str_mv New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
title New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
spellingShingle New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
Munkert, Jennifer
title_short New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
title_full New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
title_fullStr New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
title_full_unstemmed New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
title_sort New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification
author Munkert, Jennifer
author_facet Munkert, Jennifer
Gomes, Eliza R
Marostica, Lucas L
Cota, Betânia Barros
Lopes, Cristina L M
Andrade, Saulo F
Souza Filho, José D de
Alves, Ricardo J
Oliveira, Monica C
Braga, Fernão C
Simões, Cláudia M O
Pádua, Rodrigo M
Barros, André L B de
author_role author
author2 Gomes, Eliza R
Marostica, Lucas L
Cota, Betânia Barros
Lopes, Cristina L M
Andrade, Saulo F
Souza Filho, José D de
Alves, Ricardo J
Oliveira, Monica C
Braga, Fernão C
Simões, Cláudia M O
Pádua, Rodrigo M
Barros, André L B de
author2_role author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Munkert, Jennifer
Gomes, Eliza R
Marostica, Lucas L
Cota, Betânia Barros
Lopes, Cristina L M
Andrade, Saulo F
Souza Filho, José D de
Alves, Ricardo J
Oliveira, Monica C
Braga, Fernão C
Simões, Cláudia M O
Pádua, Rodrigo M
Barros, André L B de
description Department of Biology. Friedrich-Alexander-Universität Erlangen-Nürnberg. Staudtstrasse 5, 91058 Erlangen, Germany.
publishDate 2019
dc.date.issued.fl_str_mv 2019
dc.date.accessioned.fl_str_mv 2023-03-21T18:35:33Z
dc.date.available.fl_str_mv 2023-03-21T18:35:33Z
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.citation.fl_str_mv MUNKERT, Jennifer et al. New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification. ACS Omega, v. 4, n. 26, p. 22048-22056, 2019. doi: 10.1021/acsomega.9b03167.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/57494
dc.identifier.issn.en_US.fl_str_mv 2470-1343
identifier_str_mv MUNKERT, Jennifer et al. New 99mTc-Labeled Digitoxigenin Derivative for Cancer Cell Identification. ACS Omega, v. 4, n. 26, p. 22048-22056, 2019. doi: 10.1021/acsomega.9b03167.
2470-1343
url https://www.arca.fiocruz.br/handle/icict/57494
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv American Chemical Society
publisher.none.fl_str_mv American Chemical Society
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/57494/1/license.txt
https://www.arca.fiocruz.br/bitstream/icict/57494/2/New%2099mTc-Labeled%20Digitoxigenin%20Derivative.pdf
bitstream.checksum.fl_str_mv 5a560609d32a3863062d77ff32785d58
754b09cf849d119c44ac400a7d77dee3
bitstream.checksumAlgorithm.fl_str_mv MD5
MD5
repository.name.fl_str_mv Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)
repository.mail.fl_str_mv repositorio.arca@fiocruz.br
_version_ 1813009171601162240

Registros relacionados