The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi

Detalhes bibliográficos
Autor(a) principal: Lopes,Marcela Silva
Data de Publicação: 2011
Outros Autores: Sales Júnior,Policarpo Ademar, Lopes,Amanda Gervásio Ferreira, Yoshida,Maria Irene, Silva,Thais Horta Alvares da, Romanha,Alvaro José, Alves,Ricardo José, Oliveira,Renata Barbosa de
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Memórias do Instituto Oswaldo Cruz
Texto Completo: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000800027
Resumo: In this study we prepared an inclusion complex between an iodide analogue of metronidazole (MTZ-I) and cyclodextrin (CD) to develop a safer and more effective method of treating Trypanosoma cruzi infections. According to our results, MTZ-I and MTZ-I:β-CD were 10 times more active than MTZ, demonstrating that the presence of an iodine atom on the side chain increased the trypanocidal activity while maintaining its cytotoxicity. The selective index shows that MTZ-I was 10 times more active against T. cruzi than it was against mammalian cells. The modification of MTZ side chains provides a promising avenue for the development of new drugs.
id FIOCRUZ-4_e1f13d534161096cb912870ee32d6ce3
oai_identifier_str oai:scielo:S0074-02762011000800027
network_acronym_str FIOCRUZ-4
network_name_str Memórias do Instituto Oswaldo Cruz
spelling The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzinitroaromaticcyclodextrinChagas diseaseTrypanosoma cruziIn this study we prepared an inclusion complex between an iodide analogue of metronidazole (MTZ-I) and cyclodextrin (CD) to develop a safer and more effective method of treating Trypanosoma cruzi infections. According to our results, MTZ-I and MTZ-I:β-CD were 10 times more active than MTZ, demonstrating that the presence of an iodine atom on the side chain increased the trypanocidal activity while maintaining its cytotoxicity. The selective index shows that MTZ-I was 10 times more active against T. cruzi than it was against mammalian cells. The modification of MTZ side chains provides a promising avenue for the development of new drugs.Instituto Oswaldo Cruz, Ministério da Saúde2011-12-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000800027Memórias do Instituto Oswaldo Cruz v.106 n.8 2011reponame:Memórias do Instituto Oswaldo Cruzinstname:Fundação Oswaldo Cruzinstacron:FIOCRUZ10.1590/S0074-02762011000800027info:eu-repo/semantics/openAccessLopes,Marcela SilvaSales Júnior,Policarpo AdemarLopes,Amanda Gervásio FerreiraYoshida,Maria IreneSilva,Thais Horta Alvares daRomanha,Alvaro JoséAlves,Ricardo JoséOliveira,Renata Barbosa deeng2020-04-25T17:51:05Zhttp://www.scielo.br/oai/scielo-oai.php0074-02761678-8060opendoar:null2020-04-26 02:18:01.06Memórias do Instituto Oswaldo Cruz - Fundação Oswaldo Cruztrue
dc.title.none.fl_str_mv The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
title The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
spellingShingle The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
Lopes,Marcela Silva
nitroaromatic
cyclodextrin
Chagas disease
Trypanosoma cruzi
title_short The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
title_full The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
title_fullStr The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
title_full_unstemmed The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
title_sort The activity of a metronidazole analogue and its β-cyclodextrin complex against Trypanosoma cruzi
author Lopes,Marcela Silva
author_facet Lopes,Marcela Silva
Sales Júnior,Policarpo Ademar
Lopes,Amanda Gervásio Ferreira
Yoshida,Maria Irene
Silva,Thais Horta Alvares da
Romanha,Alvaro José
Alves,Ricardo José
Oliveira,Renata Barbosa de
author_role author
author2 Sales Júnior,Policarpo Ademar
Lopes,Amanda Gervásio Ferreira
Yoshida,Maria Irene
Silva,Thais Horta Alvares da
Romanha,Alvaro José
Alves,Ricardo José
Oliveira,Renata Barbosa de
author2_role author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Lopes,Marcela Silva
Sales Júnior,Policarpo Ademar
Lopes,Amanda Gervásio Ferreira
Yoshida,Maria Irene
Silva,Thais Horta Alvares da
Romanha,Alvaro José
Alves,Ricardo José
Oliveira,Renata Barbosa de
dc.subject.por.fl_str_mv nitroaromatic
cyclodextrin
Chagas disease
Trypanosoma cruzi
topic nitroaromatic
cyclodextrin
Chagas disease
Trypanosoma cruzi
dc.description.none.fl_txt_mv In this study we prepared an inclusion complex between an iodide analogue of metronidazole (MTZ-I) and cyclodextrin (CD) to develop a safer and more effective method of treating Trypanosoma cruzi infections. According to our results, MTZ-I and MTZ-I:β-CD were 10 times more active than MTZ, demonstrating that the presence of an iodine atom on the side chain increased the trypanocidal activity while maintaining its cytotoxicity. The selective index shows that MTZ-I was 10 times more active against T. cruzi than it was against mammalian cells. The modification of MTZ side chains provides a promising avenue for the development of new drugs.
description In this study we prepared an inclusion complex between an iodide analogue of metronidazole (MTZ-I) and cyclodextrin (CD) to develop a safer and more effective method of treating Trypanosoma cruzi infections. According to our results, MTZ-I and MTZ-I:β-CD were 10 times more active than MTZ, demonstrating that the presence of an iodine atom on the side chain increased the trypanocidal activity while maintaining its cytotoxicity. The selective index shows that MTZ-I was 10 times more active against T. cruzi than it was against mammalian cells. The modification of MTZ side chains provides a promising avenue for the development of new drugs.
publishDate 2011
dc.date.none.fl_str_mv 2011-12-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000800027
url http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762011000800027
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/S0074-02762011000800027
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv text/html
dc.publisher.none.fl_str_mv Instituto Oswaldo Cruz, Ministério da Saúde
publisher.none.fl_str_mv Instituto Oswaldo Cruz, Ministério da Saúde
dc.source.none.fl_str_mv Memórias do Instituto Oswaldo Cruz v.106 n.8 2011
reponame:Memórias do Instituto Oswaldo Cruz
instname:Fundação Oswaldo Cruz
instacron:FIOCRUZ
reponame_str Memórias do Instituto Oswaldo Cruz
collection Memórias do Instituto Oswaldo Cruz
instname_str Fundação Oswaldo Cruz
instacron_str FIOCRUZ
institution FIOCRUZ
repository.name.fl_str_mv Memórias do Instituto Oswaldo Cruz - Fundação Oswaldo Cruz
repository.mail.fl_str_mv
_version_ 1669937710973845504

Registros relacionados