Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione

Detalhes bibliográficos
Autor(a) principal: Espuri, Patrícia Ferreira
Data de Publicação: 2019
Outros Autores: dos Reis, Larissa Luiza, de Figueiredo Peloso, Eduardo, Gontijo, Vanessa Silva, Colombo, Fábio Antônio, Nunes, Juliana Barbosa, de Oliveira, Carine Ervolino, De Almeida, Eduardo T., Silva, Débora E. S. [UNESP], Bortoletto, Jessica [UNESP], Segura, Daniel Fonseca [UNESP], Netto, Adelino V. G. [UNESP], Marques, Marcos José
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.1007/s00775-019-01657-2
http://hdl.handle.net/11449/187555
Resumo: Abstract: A new series of silver compounds could be of interest on designing new drugs for the treatment of leishmaniasis. The compounds [Ag(phen)(imzt)]NO3(1), [Ag(phen)(imzt)]CF3SO3(2), [Ag(phen)2](BF4)·H2O (3), [Ag2(imzt)6](NO3)2(4), and imzt have been synthesized and evaluated in vitro for antileishmanial activity against Leishmania. (L.) amazonensis (La) and L. (L.) chagasi (Lc), and two of them were selected for in vivo studies. In addition to investigating the action on Leishmania, their effects on the hydrogen peroxide production and cysteine protease inhibition have also been investigated. As for antileishmanial activity, compound (4) was the most potent against promastigote and amastigote forms of La (IC50 = 4.67 and 1.88 μM, respectively) and Lc (IC50 = 9.35 and 8.05 μM, respectively); and comparable to that of amphotericin B, reference drug. Beside showing excellent activity, it also showed a low toxicity. In the in vivo context, compound (4) reduced the number of amastigotes in the liver and spleen when compared to the untreated group. In evaluating the effect of the compounds on Leishmania, the level of hydrogen peroxide production was maintained between the lag and log phases; however, in the treatment with compound (4) it was possible to observe a reduction of 25.44 and 49.13%, respectively, in the hydrogen peroxide rates when compared to the lag and log phases. It was noticed that the presence of a nitrate ion and imzt in compound (4) was important for the modulation of the antileishmanial activity. Thus, this compound can represent a potentially new drug for the treatment of leishmaniasis. Graphical abstract: [Figure not available: see fulltext.].
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spelling Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thioneBiological effectsLeishmaniaSilver compoundsAbstract: A new series of silver compounds could be of interest on designing new drugs for the treatment of leishmaniasis. The compounds [Ag(phen)(imzt)]NO3(1), [Ag(phen)(imzt)]CF3SO3(2), [Ag(phen)2](BF4)·H2O (3), [Ag2(imzt)6](NO3)2(4), and imzt have been synthesized and evaluated in vitro for antileishmanial activity against Leishmania. (L.) amazonensis (La) and L. (L.) chagasi (Lc), and two of them were selected for in vivo studies. In addition to investigating the action on Leishmania, their effects on the hydrogen peroxide production and cysteine protease inhibition have also been investigated. As for antileishmanial activity, compound (4) was the most potent against promastigote and amastigote forms of La (IC50 = 4.67 and 1.88 μM, respectively) and Lc (IC50 = 9.35 and 8.05 μM, respectively); and comparable to that of amphotericin B, reference drug. Beside showing excellent activity, it also showed a low toxicity. In the in vivo context, compound (4) reduced the number of amastigotes in the liver and spleen when compared to the untreated group. In evaluating the effect of the compounds on Leishmania, the level of hydrogen peroxide production was maintained between the lag and log phases; however, in the treatment with compound (4) it was possible to observe a reduction of 25.44 and 49.13%, respectively, in the hydrogen peroxide rates when compared to the lag and log phases. It was noticed that the presence of a nitrate ion and imzt in compound (4) was important for the modulation of the antileishmanial activity. Thus, this compound can represent a potentially new drug for the treatment of leishmaniasis. Graphical abstract: [Figure not available: see fulltext.].Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de Minas Gerais (FAPEMIG)Financiadora de Estudos e ProjetosLaboratory of Parasitology Department of Pathology and Parasitology Institute of Biomedical Sciences Universidade Federal de AlfenasDepartment of Biochemistry Institute of Biomedical Sciences Universidade Federal de AlfenasLaboratory of Researche on Medicinal Chemistry Institute of Chemistry Universidade Federal de AlfenasInstitute of Chemistry UNESP-Univ. Estadual Paulista, P.O. Box 355Institute of Biomedical Sciences Federal University of Alfenas, 700 Gabriel Monteiro da Silva StInstitute of Chemistry UNESP-Univ. Estadual Paulista, P.O. Box 355Universidade Federal de AlfenasUniversidade Estadual Paulista (Unesp)Federal University of AlfenasEspuri, Patrícia Ferreirados Reis, Larissa Luizade Figueiredo Peloso, EduardoGontijo, Vanessa SilvaColombo, Fábio AntônioNunes, Juliana Barbosade Oliveira, Carine ErvolinoDe Almeida, Eduardo T.Silva, Débora E. S. [UNESP]Bortoletto, Jessica [UNESP]Segura, Daniel Fonseca [UNESP]Netto, Adelino V. G. [UNESP]Marques, Marcos José2019-10-06T15:40:01Z2019-10-06T15:40:01Z2019-05-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article419-432http://dx.doi.org/10.1007/s00775-019-01657-2Journal of Biological Inorganic Chemistry, v. 24, n. 3, p. 419-432, 2019.1432-13270949-8257http://hdl.handle.net/11449/18755510.1007/s00775-019-01657-22-s2.0-85064256508Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengJournal of Biological Inorganic Chemistryinfo:eu-repo/semantics/openAccess2021-10-23T20:19:26Zoai:repositorio.unesp.br:11449/187555Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T22:56:22.404647Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
title Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
spellingShingle Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
Espuri, Patrícia Ferreira
Biological effects
Leishmania
Silver compounds
title_short Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
title_full Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
title_fullStr Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
title_full_unstemmed Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
title_sort Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
author Espuri, Patrícia Ferreira
author_facet Espuri, Patrícia Ferreira
dos Reis, Larissa Luiza
de Figueiredo Peloso, Eduardo
Gontijo, Vanessa Silva
Colombo, Fábio Antônio
Nunes, Juliana Barbosa
de Oliveira, Carine Ervolino
De Almeida, Eduardo T.
Silva, Débora E. S. [UNESP]
Bortoletto, Jessica [UNESP]
Segura, Daniel Fonseca [UNESP]
Netto, Adelino V. G. [UNESP]
Marques, Marcos José
author_role author
author2 dos Reis, Larissa Luiza
de Figueiredo Peloso, Eduardo
Gontijo, Vanessa Silva
Colombo, Fábio Antônio
Nunes, Juliana Barbosa
de Oliveira, Carine Ervolino
De Almeida, Eduardo T.
Silva, Débora E. S. [UNESP]
Bortoletto, Jessica [UNESP]
Segura, Daniel Fonseca [UNESP]
Netto, Adelino V. G. [UNESP]
Marques, Marcos José
author2_role author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade Federal de Alfenas
Universidade Estadual Paulista (Unesp)
Federal University of Alfenas
dc.contributor.author.fl_str_mv Espuri, Patrícia Ferreira
dos Reis, Larissa Luiza
de Figueiredo Peloso, Eduardo
Gontijo, Vanessa Silva
Colombo, Fábio Antônio
Nunes, Juliana Barbosa
de Oliveira, Carine Ervolino
De Almeida, Eduardo T.
Silva, Débora E. S. [UNESP]
Bortoletto, Jessica [UNESP]
Segura, Daniel Fonseca [UNESP]
Netto, Adelino V. G. [UNESP]
Marques, Marcos José
dc.subject.por.fl_str_mv Biological effects
Leishmania
Silver compounds
topic Biological effects
Leishmania
Silver compounds
description Abstract: A new series of silver compounds could be of interest on designing new drugs for the treatment of leishmaniasis. The compounds [Ag(phen)(imzt)]NO3(1), [Ag(phen)(imzt)]CF3SO3(2), [Ag(phen)2](BF4)·H2O (3), [Ag2(imzt)6](NO3)2(4), and imzt have been synthesized and evaluated in vitro for antileishmanial activity against Leishmania. (L.) amazonensis (La) and L. (L.) chagasi (Lc), and two of them were selected for in vivo studies. In addition to investigating the action on Leishmania, their effects on the hydrogen peroxide production and cysteine protease inhibition have also been investigated. As for antileishmanial activity, compound (4) was the most potent against promastigote and amastigote forms of La (IC50 = 4.67 and 1.88 μM, respectively) and Lc (IC50 = 9.35 and 8.05 μM, respectively); and comparable to that of amphotericin B, reference drug. Beside showing excellent activity, it also showed a low toxicity. In the in vivo context, compound (4) reduced the number of amastigotes in the liver and spleen when compared to the untreated group. In evaluating the effect of the compounds on Leishmania, the level of hydrogen peroxide production was maintained between the lag and log phases; however, in the treatment with compound (4) it was possible to observe a reduction of 25.44 and 49.13%, respectively, in the hydrogen peroxide rates when compared to the lag and log phases. It was noticed that the presence of a nitrate ion and imzt in compound (4) was important for the modulation of the antileishmanial activity. Thus, this compound can represent a potentially new drug for the treatment of leishmaniasis. Graphical abstract: [Figure not available: see fulltext.].
publishDate 2019
dc.date.none.fl_str_mv 2019-10-06T15:40:01Z
2019-10-06T15:40:01Z
2019-05-01
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/10.1007/s00775-019-01657-2
Journal of Biological Inorganic Chemistry, v. 24, n. 3, p. 419-432, 2019.
1432-1327
0949-8257
http://hdl.handle.net/11449/187555
10.1007/s00775-019-01657-2
2-s2.0-85064256508
url http://dx.doi.org/10.1007/s00775-019-01657-2
http://hdl.handle.net/11449/187555
identifier_str_mv Journal of Biological Inorganic Chemistry, v. 24, n. 3, p. 419-432, 2019.
1432-1327
0949-8257
10.1007/s00775-019-01657-2
2-s2.0-85064256508
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Journal of Biological Inorganic Chemistry
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 419-432
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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