Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae)
Autor(a) principal: | |
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Data de Publicação: | 2013 |
Outros Autores: | , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.3390/molecules18011053 http://hdl.handle.net/11449/74290 |
Resumo: | The present study describes the leishmanicidal and trypanocidal activities of two quinonemethide triterpenes, maytenin (1) and pristimerin (2), isolated from Maytenus ilicifolia root barks (Celastraceae). The compounds were effective against the Trypanosomatidae Leishmania amazonensis and Leishmania chagasi and Trypanosoma cruzi, etiologic agents of leishmaniasis and Chagas' disease, respectively. The quinonemethide triterpenes 1 and 2 exhibited a marked in vitro leishmanicidal activity against promastigotes and amastigotes with 50% inhibitory concentration (IC50) values of less than 0.88 nM. Both compounds showed IC50 lower than 0.3 nM against Trypanosoma cruzi epimastigotes. The selectivity indexes (SI) based on BALB/c macrophages for L. amazonensis and L. chagasi were 243.65 and 46.61 for (1) and 193.63 and 23.85 for (2) indicating that both compounds presented high selectivity for Leishmania sp. The data here presented suggests that these compounds should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas' disease. © 2013 by the authors. |
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Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae)CelastraceaeLeishmanicidalMayteninMaytenus ilicifoliaPristimerinQuinone-methide triterpenesTrypanocidalantitrypanosomal agentplant extractquinone derivativetriterpeneanimalBagg albino mousecell culturechemistrydrug effectIC 50LD 50LeishmaniamacrophageMaytenusmouseparasitologyphysiologyplant rootTrypanosoma cruziAnimalsCells, CulturedInhibitory Concentration 50Lethal Dose 50MacrophagesMiceMice, Inbred BALB CPlant ExtractsPlant RootsQuinonesTriterpenesTrypanocidal AgentsThe present study describes the leishmanicidal and trypanocidal activities of two quinonemethide triterpenes, maytenin (1) and pristimerin (2), isolated from Maytenus ilicifolia root barks (Celastraceae). The compounds were effective against the Trypanosomatidae Leishmania amazonensis and Leishmania chagasi and Trypanosoma cruzi, etiologic agents of leishmaniasis and Chagas' disease, respectively. The quinonemethide triterpenes 1 and 2 exhibited a marked in vitro leishmanicidal activity against promastigotes and amastigotes with 50% inhibitory concentration (IC50) values of less than 0.88 nM. Both compounds showed IC50 lower than 0.3 nM against Trypanosoma cruzi epimastigotes. The selectivity indexes (SI) based on BALB/c macrophages for L. amazonensis and L. chagasi were 243.65 and 46.61 for (1) and 193.63 and 23.85 for (2) indicating that both compounds presented high selectivity for Leishmania sp. The data here presented suggests that these compounds should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas' disease. © 2013 by the authors.Instituto de Quimica Universidade Estadual Paulista UNESP, PO BOX 355, Araraquara-SP 14801-970Faculdade de Ciencias Farmaceuticas Universidade Estadual Paulista UNESP, Araraquara-SP 14801-902Instituto de Ciencias Biomedicas Universidade de São Paulo, São Paulo 05508-000Departamento de Biotecnologia Vegetal Universidade de Ribeirão Preto, Ribeirão Preto-SP 14096-900Instituto de Quimica Universidade Estadual Paulista UNESP, PO BOX 355, Araraquara-SP 14801-970Faculdade de Ciencias Farmaceuticas Universidade Estadual Paulista UNESP, Araraquara-SP 14801-902Universidade Estadual Paulista (Unesp)Universidade de São Paulo (USP)Universidade de Ribeirão PretoDos Santos, Vania A. F. F. M. [UNESP]Leite, Karoline M. [UNESP]Da Costa Siqueira, Mariana [UNESP]Regasini, Luis O. [UNESP]Martinez, Isabel [UNESP]Nogueira, Camila T. [UNESP]Galuppo, Mariana KolosStolf, Beatriz S.Pereira, Ana Maria SoaresCicarelli, Regina Maria Barreto [UNESP]Furlan, Maysa [UNESP]Graminha, Márcia Aparecida Silva [UNESP]2014-05-27T11:27:32Z2014-05-27T11:27:32Z2013-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article1053-1062application/pdfhttp://dx.doi.org/10.3390/molecules18011053Molecules, v. 18, n. 1, p. 1053-1062, 2013.1420-3049http://hdl.handle.net/11449/7429010.3390/molecules18011053WOS:0003140329000652-s2.0-848728704932-s2.0-84872870493.pdf1308042794786872Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengMolecules3.0980,855info:eu-repo/semantics/openAccess2023-10-08T06:07:04Zoai:repositorio.unesp.br:11449/74290Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462023-10-08T06:07:04Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) |
title |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) |
spellingShingle |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) Dos Santos, Vania A. F. F. M. [UNESP] Celastraceae Leishmanicidal Maytenin Maytenus ilicifolia Pristimerin Quinone-methide triterpenes Trypanocidal antitrypanosomal agent plant extract quinone derivative triterpene animal Bagg albino mouse cell culture chemistry drug effect IC 50 LD 50 Leishmania macrophage Maytenus mouse parasitology physiology plant root Trypanosoma cruzi Animals Cells, Cultured Inhibitory Concentration 50 Lethal Dose 50 Macrophages Mice Mice, Inbred BALB C Plant Extracts Plant Roots Quinones Triterpenes Trypanocidal Agents |
title_short |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) |
title_full |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) |
title_fullStr |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) |
title_full_unstemmed |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) |
title_sort |
Antiprotozoal activity of quinonemethide triterpenes from Maytenus ilicifolia (Celastraceae) |
author |
Dos Santos, Vania A. F. F. M. [UNESP] |
author_facet |
Dos Santos, Vania A. F. F. M. [UNESP] Leite, Karoline M. [UNESP] Da Costa Siqueira, Mariana [UNESP] Regasini, Luis O. [UNESP] Martinez, Isabel [UNESP] Nogueira, Camila T. [UNESP] Galuppo, Mariana Kolos Stolf, Beatriz S. Pereira, Ana Maria Soares Cicarelli, Regina Maria Barreto [UNESP] Furlan, Maysa [UNESP] Graminha, Márcia Aparecida Silva [UNESP] |
author_role |
author |
author2 |
Leite, Karoline M. [UNESP] Da Costa Siqueira, Mariana [UNESP] Regasini, Luis O. [UNESP] Martinez, Isabel [UNESP] Nogueira, Camila T. [UNESP] Galuppo, Mariana Kolos Stolf, Beatriz S. Pereira, Ana Maria Soares Cicarelli, Regina Maria Barreto [UNESP] Furlan, Maysa [UNESP] Graminha, Márcia Aparecida Silva [UNESP] |
author2_role |
author author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) Universidade de São Paulo (USP) Universidade de Ribeirão Preto |
dc.contributor.author.fl_str_mv |
Dos Santos, Vania A. F. F. M. [UNESP] Leite, Karoline M. [UNESP] Da Costa Siqueira, Mariana [UNESP] Regasini, Luis O. [UNESP] Martinez, Isabel [UNESP] Nogueira, Camila T. [UNESP] Galuppo, Mariana Kolos Stolf, Beatriz S. Pereira, Ana Maria Soares Cicarelli, Regina Maria Barreto [UNESP] Furlan, Maysa [UNESP] Graminha, Márcia Aparecida Silva [UNESP] |
dc.subject.por.fl_str_mv |
Celastraceae Leishmanicidal Maytenin Maytenus ilicifolia Pristimerin Quinone-methide triterpenes Trypanocidal antitrypanosomal agent plant extract quinone derivative triterpene animal Bagg albino mouse cell culture chemistry drug effect IC 50 LD 50 Leishmania macrophage Maytenus mouse parasitology physiology plant root Trypanosoma cruzi Animals Cells, Cultured Inhibitory Concentration 50 Lethal Dose 50 Macrophages Mice Mice, Inbred BALB C Plant Extracts Plant Roots Quinones Triterpenes Trypanocidal Agents |
topic |
Celastraceae Leishmanicidal Maytenin Maytenus ilicifolia Pristimerin Quinone-methide triterpenes Trypanocidal antitrypanosomal agent plant extract quinone derivative triterpene animal Bagg albino mouse cell culture chemistry drug effect IC 50 LD 50 Leishmania macrophage Maytenus mouse parasitology physiology plant root Trypanosoma cruzi Animals Cells, Cultured Inhibitory Concentration 50 Lethal Dose 50 Macrophages Mice Mice, Inbred BALB C Plant Extracts Plant Roots Quinones Triterpenes Trypanocidal Agents |
description |
The present study describes the leishmanicidal and trypanocidal activities of two quinonemethide triterpenes, maytenin (1) and pristimerin (2), isolated from Maytenus ilicifolia root barks (Celastraceae). The compounds were effective against the Trypanosomatidae Leishmania amazonensis and Leishmania chagasi and Trypanosoma cruzi, etiologic agents of leishmaniasis and Chagas' disease, respectively. The quinonemethide triterpenes 1 and 2 exhibited a marked in vitro leishmanicidal activity against promastigotes and amastigotes with 50% inhibitory concentration (IC50) values of less than 0.88 nM. Both compounds showed IC50 lower than 0.3 nM against Trypanosoma cruzi epimastigotes. The selectivity indexes (SI) based on BALB/c macrophages for L. amazonensis and L. chagasi were 243.65 and 46.61 for (1) and 193.63 and 23.85 for (2) indicating that both compounds presented high selectivity for Leishmania sp. The data here presented suggests that these compounds should be considered in the development of new and more potent drugs for the treatment of leishmaniasis and Chagas' disease. © 2013 by the authors. |
publishDate |
2013 |
dc.date.none.fl_str_mv |
2013-01-01 2014-05-27T11:27:32Z 2014-05-27T11:27:32Z |
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/10.3390/molecules18011053 Molecules, v. 18, n. 1, p. 1053-1062, 2013. 1420-3049 http://hdl.handle.net/11449/74290 10.3390/molecules18011053 WOS:000314032900065 2-s2.0-84872870493 2-s2.0-84872870493.pdf 1308042794786872 |
url |
http://dx.doi.org/10.3390/molecules18011053 http://hdl.handle.net/11449/74290 |
identifier_str_mv |
Molecules, v. 18, n. 1, p. 1053-1062, 2013. 1420-3049 10.3390/molecules18011053 WOS:000314032900065 2-s2.0-84872870493 2-s2.0-84872870493.pdf 1308042794786872 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Molecules 3.098 0,855 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
1053-1062 application/pdf |
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 |
|
_version_ |
1799964484117200896 |