In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis
Autor(a) principal: | |
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Data de Publicação: | 2012 |
Outros Autores: | , , , , , , , , |
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=S0074-02762012000300012 |
Resumo: | The activity of five (1-5) abietane phenol derivatives against Leishmania infantum and Leishmania braziliensis was studied using promastigotes and axenic and intracellular amastigotes. Infectivity and cytotoxicity tests were performed with J774.2 macrophage cells using Glucantime as a reference drug. The mechanisms of action were analysed by performing metabolite excretion and transmission electron microscopy ultrastructural studies. Compounds 1-5 were more active and less toxic than Glucantime. The infection rates and mean number of parasites per cell observed in amastigote experiments showed that derivatives 2, 4 and 5 were the most effective against both L. infantum and L. braziliensis. The ultrastructural changes observed in the treated promastigote forms confirmed that the greatest cell damage was caused by the most active compound (4). Only compound 5 caused changes in the nature and amounts of catabolites excreted by the parasites, as measured by ¹H nuclear magnetic resonance spectroscopy. All of the assayed compounds were active against the two Leishmania species in vitro and were less toxic in mammalian cells than the reference drug. |
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Memórias do Instituto Oswaldo Cruz |
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In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensisabietane phenol compoundsLeishmania infantumLeishmania braziliensisbiological evaluation of activitypromastigoteamastigote formsThe activity of five (1-5) abietane phenol derivatives against Leishmania infantum and Leishmania braziliensis was studied using promastigotes and axenic and intracellular amastigotes. Infectivity and cytotoxicity tests were performed with J774.2 macrophage cells using Glucantime as a reference drug. The mechanisms of action were analysed by performing metabolite excretion and transmission electron microscopy ultrastructural studies. Compounds 1-5 were more active and less toxic than Glucantime. The infection rates and mean number of parasites per cell observed in amastigote experiments showed that derivatives 2, 4 and 5 were the most effective against both L. infantum and L. braziliensis. The ultrastructural changes observed in the treated promastigote forms confirmed that the greatest cell damage was caused by the most active compound (4). Only compound 5 caused changes in the nature and amounts of catabolites excreted by the parasites, as measured by ¹H nuclear magnetic resonance spectroscopy. All of the assayed compounds were active against the two Leishmania species in vitro and were less toxic in mammalian cells than the reference drug.Instituto Oswaldo Cruz, Ministério da Saúde2012-05-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762012000300012Memórias do Instituto Oswaldo Cruz v.107 n.3 2012reponame:Memórias do Instituto Oswaldo Cruzinstname:Fundação Oswaldo Cruzinstacron:FIOCRUZ10.1590/S0074-02762012000300012info:eu-repo/semantics/openAccessRamírez-Macías,InmaculadaMarín,ClotildeChahboun,RachidOlmo,FranciscoMessouri,IbtisamHuertas,OscarRosales,María JoseGutierrez-Sánchez,RamónAlvarez-Manzaneda,EnriqueSánchez-Moreno,Manueleng2020-04-25T17:51:11Zhttp://www.scielo.br/oai/scielo-oai.php0074-02761678-8060opendoar:null2020-04-26 02:18:17.151Memórias do Instituto Oswaldo Cruz - Fundação Oswaldo Cruztrue |
dc.title.none.fl_str_mv |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis |
title |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis |
spellingShingle |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis Ramírez-Macías,Inmaculada abietane phenol compounds Leishmania infantum Leishmania braziliensis biological evaluation of activity promastigote amastigote forms |
title_short |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis |
title_full |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis |
title_fullStr |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis |
title_full_unstemmed |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis |
title_sort |
In vitro evaluation of new terpenoid derivatives against Leishmania infantum and Leishmania braziliensis |
author |
Ramírez-Macías,Inmaculada |
author_facet |
Ramírez-Macías,Inmaculada Marín,Clotilde Chahboun,Rachid Olmo,Francisco Messouri,Ibtisam Huertas,Oscar Rosales,María Jose Gutierrez-Sánchez,Ramón Alvarez-Manzaneda,Enrique Sánchez-Moreno,Manuel |
author_role |
author |
author2 |
Marín,Clotilde Chahboun,Rachid Olmo,Francisco Messouri,Ibtisam Huertas,Oscar Rosales,María Jose Gutierrez-Sánchez,Ramón Alvarez-Manzaneda,Enrique Sánchez-Moreno,Manuel |
author2_role |
author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Ramírez-Macías,Inmaculada Marín,Clotilde Chahboun,Rachid Olmo,Francisco Messouri,Ibtisam Huertas,Oscar Rosales,María Jose Gutierrez-Sánchez,Ramón Alvarez-Manzaneda,Enrique Sánchez-Moreno,Manuel |
dc.subject.por.fl_str_mv |
abietane phenol compounds Leishmania infantum Leishmania braziliensis biological evaluation of activity promastigote amastigote forms |
topic |
abietane phenol compounds Leishmania infantum Leishmania braziliensis biological evaluation of activity promastigote amastigote forms |
dc.description.none.fl_txt_mv |
The activity of five (1-5) abietane phenol derivatives against Leishmania infantum and Leishmania braziliensis was studied using promastigotes and axenic and intracellular amastigotes. Infectivity and cytotoxicity tests were performed with J774.2 macrophage cells using Glucantime as a reference drug. The mechanisms of action were analysed by performing metabolite excretion and transmission electron microscopy ultrastructural studies. Compounds 1-5 were more active and less toxic than Glucantime. The infection rates and mean number of parasites per cell observed in amastigote experiments showed that derivatives 2, 4 and 5 were the most effective against both L. infantum and L. braziliensis. The ultrastructural changes observed in the treated promastigote forms confirmed that the greatest cell damage was caused by the most active compound (4). Only compound 5 caused changes in the nature and amounts of catabolites excreted by the parasites, as measured by ¹H nuclear magnetic resonance spectroscopy. All of the assayed compounds were active against the two Leishmania species in vitro and were less toxic in mammalian cells than the reference drug. |
description |
The activity of five (1-5) abietane phenol derivatives against Leishmania infantum and Leishmania braziliensis was studied using promastigotes and axenic and intracellular amastigotes. Infectivity and cytotoxicity tests were performed with J774.2 macrophage cells using Glucantime as a reference drug. The mechanisms of action were analysed by performing metabolite excretion and transmission electron microscopy ultrastructural studies. Compounds 1-5 were more active and less toxic than Glucantime. The infection rates and mean number of parasites per cell observed in amastigote experiments showed that derivatives 2, 4 and 5 were the most effective against both L. infantum and L. braziliensis. The ultrastructural changes observed in the treated promastigote forms confirmed that the greatest cell damage was caused by the most active compound (4). Only compound 5 caused changes in the nature and amounts of catabolites excreted by the parasites, as measured by ¹H nuclear magnetic resonance spectroscopy. All of the assayed compounds were active against the two Leishmania species in vitro and were less toxic in mammalian cells than the reference drug. |
publishDate |
2012 |
dc.date.none.fl_str_mv |
2012-05-01 |
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=S0074-02762012000300012 |
url |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762012000300012 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1590/S0074-02762012000300012 |
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.107 n.3 2012 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_ |
1669937711976284160 |