Synthesis and evaluation of the antileishmanial activity of silver compounds containing imidazolidine-2-thione
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Outros Autores: | , , , , , , , , , , , |
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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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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1808129476428562432 |