Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.

Autores
Frank, Fernanda Maria; Ulloa, Jerónimo Luis; Cazorla, Silvia Ines; Maravilla, G.; Malchiodi, Emilio Luis; Grau, A.; Martino, Virginia Susana; Catalan, Cesar Atilio Nazareno; Muschietti, Liliana
Año de publicación
2013
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
In order to find novel plant-derived biologically active compounds against Trypanosoma cruzi, we isolated, from the organic extract of Smallanthus sonchifolius, the sesquiterpene lactones enhydrin (1), uvedalin (2), and polymatin B (3) by bioassay-guided fractionation technique. These compounds showed a significant trypanocidal activity against the epimastigote forms of the parasite with IC50 values of 0.84 μM (1), 1.09 μM (2), and 4.90 μM (3). After a 24 h treatment with 10 μg/mL of enhydrin or uvedalin, parasites were not able to recover their replication rate. Compounds 1 and 2 showed IC50 values of 33.4 μM and 25.0 μM against T. cruzi trypomastigotes, while polymatin B was not active. When the three compounds were tested against the intracellular forms of T. cruzi, they were able to inhibit the amastigote replication with IC50 of 5.17 μM, 3.34 μM, and 9.02 μM for 1, 2, and 3, respectively. The cytotoxicity of the compounds was evaluated in Vero cells obtaining CC50 values of 46.5 μM (1), 46.8 μM (2), and 147.3 μM (3) and the selectivity index calculated. According to these results, enhydrin and uvedalin might have potentials as agents against Chagas disease and could serve as lead molecules to develop new drugs.
Fil: Frank, Fernanda Maria. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; Argentina
Fil: Ulloa, Jerónimo Luis. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
Fil: Cazorla, Silvia Ines. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; Argentina
Fil: Maravilla, G.. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
Fil: Malchiodi, Emilio Luis. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; Argentina
Fil: Grau, A.. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo. Instituto de Ecología Regional; Argentina
Fil: Martino, Virginia Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
Fil: Catalan, Cesar Atilio Nazareno. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Tucumán. Instituto de Quimica del Noroeste; Argentina
Fil: Muschietti, Liliana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
Materia
Chagas disease
Sesquiterpene lactonas
Smallanthus sonchifolius
bioassay-guided fractionation
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/8064
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/8064
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.Frank, Fernanda MariaUlloa, Jerónimo LuisCazorla, Silvia InesMaravilla, G.Malchiodi, Emilio LuisGrau, A.Martino, Virginia SusanaCatalan, Cesar Atilio NazarenoMuschietti, LilianaChagas diseaseSesquiterpene lactonasSmallanthus sonchifoliusbioassay-guided fractionationhttps://purl.org/becyt/ford/3.3https://purl.org/becyt/ford/3In order to find novel plant-derived biologically active compounds against Trypanosoma cruzi, we isolated, from the organic extract of Smallanthus sonchifolius, the sesquiterpene lactones enhydrin (1), uvedalin (2), and polymatin B (3) by bioassay-guided fractionation technique. These compounds showed a significant trypanocidal activity against the epimastigote forms of the parasite with IC50 values of 0.84 μM (1), 1.09 μM (2), and 4.90 μM (3). After a 24 h treatment with 10 μg/mL of enhydrin or uvedalin, parasites were not able to recover their replication rate. Compounds 1 and 2 showed IC50 values of 33.4 μM and 25.0 μM against T. cruzi trypomastigotes, while polymatin B was not active. When the three compounds were tested against the intracellular forms of T. cruzi, they were able to inhibit the amastigote replication with IC50 of 5.17 μM, 3.34 μM, and 9.02 μM for 1, 2, and 3, respectively. The cytotoxicity of the compounds was evaluated in Vero cells obtaining CC50 values of 46.5 μM (1), 46.8 μM (2), and 147.3 μM (3) and the selectivity index calculated. According to these results, enhydrin and uvedalin might have potentials as agents against Chagas disease and could serve as lead molecules to develop new drugs.Fil: Frank, Fernanda Maria. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; ArgentinaFil: Ulloa, Jerónimo Luis. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); ArgentinaFil: Cazorla, Silvia Ines. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; ArgentinaFil: Maravilla, G.. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); ArgentinaFil: Malchiodi, Emilio Luis. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; ArgentinaFil: Grau, A.. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo. Instituto de Ecología Regional; ArgentinaFil: Martino, Virginia Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); ArgentinaFil: Catalan, Cesar Atilio Nazareno. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Tucumán. Instituto de Quimica del Noroeste; ArgentinaFil: Muschietti, Liliana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); ArgentinaOxford University Press2013-06info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/8064Frank, Fernanda Maria; Ulloa, Jerónimo Luis; Cazorla, Silvia Ines; Maravilla, G.; Malchiodi, Emilio Luis; et al.; Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.; Oxford University Press; Evidence-based Complementary And Alternative Medicine; 6278; 6-2013; 1-101741-427X1741-4288enginfo:eu-repo/semantics/altIdentifier/url/https://www.hindawi.com/journals/ecam/2013/627898/info:eu-repo/semantics/altIdentifier/doi/10.1155/2013/627898info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-10T13:00:37Zoai:ri.conicet.gov.ar:11336/8064instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-10 13:00:37.462CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
title Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
spellingShingle Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
Frank, Fernanda Maria
Chagas disease
Sesquiterpene lactonas
Smallanthus sonchifolius
bioassay-guided fractionation
title_short Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
title_full Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
title_fullStr Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
title_full_unstemmed Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
title_sort Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.
dc.creator.none.fl_str_mv Frank, Fernanda Maria
Ulloa, Jerónimo Luis
Cazorla, Silvia Ines
Maravilla, G.
Malchiodi, Emilio Luis
Grau, A.
Martino, Virginia Susana
Catalan, Cesar Atilio Nazareno
Muschietti, Liliana
author Frank, Fernanda Maria
author_facet Frank, Fernanda Maria
Ulloa, Jerónimo Luis
Cazorla, Silvia Ines
Maravilla, G.
Malchiodi, Emilio Luis
Grau, A.
Martino, Virginia Susana
Catalan, Cesar Atilio Nazareno
Muschietti, Liliana
author_role author
author2 Ulloa, Jerónimo Luis
Cazorla, Silvia Ines
Maravilla, G.
Malchiodi, Emilio Luis
Grau, A.
Martino, Virginia Susana
Catalan, Cesar Atilio Nazareno
Muschietti, Liliana
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Chagas disease
Sesquiterpene lactonas
Smallanthus sonchifolius
bioassay-guided fractionation
topic Chagas disease
Sesquiterpene lactonas
Smallanthus sonchifolius
bioassay-guided fractionation
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.3
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv In order to find novel plant-derived biologically active compounds against Trypanosoma cruzi, we isolated, from the organic extract of Smallanthus sonchifolius, the sesquiterpene lactones enhydrin (1), uvedalin (2), and polymatin B (3) by bioassay-guided fractionation technique. These compounds showed a significant trypanocidal activity against the epimastigote forms of the parasite with IC50 values of 0.84 μM (1), 1.09 μM (2), and 4.90 μM (3). After a 24 h treatment with 10 μg/mL of enhydrin or uvedalin, parasites were not able to recover their replication rate. Compounds 1 and 2 showed IC50 values of 33.4 μM and 25.0 μM against T. cruzi trypomastigotes, while polymatin B was not active. When the three compounds were tested against the intracellular forms of T. cruzi, they were able to inhibit the amastigote replication with IC50 of 5.17 μM, 3.34 μM, and 9.02 μM for 1, 2, and 3, respectively. The cytotoxicity of the compounds was evaluated in Vero cells obtaining CC50 values of 46.5 μM (1), 46.8 μM (2), and 147.3 μM (3) and the selectivity index calculated. According to these results, enhydrin and uvedalin might have potentials as agents against Chagas disease and could serve as lead molecules to develop new drugs.
Fil: Frank, Fernanda Maria. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; Argentina
Fil: Ulloa, Jerónimo Luis. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
Fil: Cazorla, Silvia Ines. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; Argentina
Fil: Maravilla, G.. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
Fil: Malchiodi, Emilio Luis. Consejo Nacional de Investigaciones Cientiâ­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "profesor R. A. Margni"; Argentina
Fil: Grau, A.. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo. Instituto de Ecología Regional; Argentina
Fil: Martino, Virginia Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
Fil: Catalan, Cesar Atilio Nazareno. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Tucumán. Instituto de Quimica del Noroeste; Argentina
Fil: Muschietti, Liliana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco (i); Argentina
description In order to find novel plant-derived biologically active compounds against Trypanosoma cruzi, we isolated, from the organic extract of Smallanthus sonchifolius, the sesquiterpene lactones enhydrin (1), uvedalin (2), and polymatin B (3) by bioassay-guided fractionation technique. These compounds showed a significant trypanocidal activity against the epimastigote forms of the parasite with IC50 values of 0.84 μM (1), 1.09 μM (2), and 4.90 μM (3). After a 24 h treatment with 10 μg/mL of enhydrin or uvedalin, parasites were not able to recover their replication rate. Compounds 1 and 2 showed IC50 values of 33.4 μM and 25.0 μM against T. cruzi trypomastigotes, while polymatin B was not active. When the three compounds were tested against the intracellular forms of T. cruzi, they were able to inhibit the amastigote replication with IC50 of 5.17 μM, 3.34 μM, and 9.02 μM for 1, 2, and 3, respectively. The cytotoxicity of the compounds was evaluated in Vero cells obtaining CC50 values of 46.5 μM (1), 46.8 μM (2), and 147.3 μM (3) and the selectivity index calculated. According to these results, enhydrin and uvedalin might have potentials as agents against Chagas disease and could serve as lead molecules to develop new drugs.
publishDate 2013
dc.date.none.fl_str_mv 2013-06
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/8064
Frank, Fernanda Maria; Ulloa, Jerónimo Luis; Cazorla, Silvia Ines; Maravilla, G.; Malchiodi, Emilio Luis; et al.; Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.; Oxford University Press; Evidence-based Complementary And Alternative Medicine; 6278; 6-2013; 1-10
1741-427X
1741-4288
url http://hdl.handle.net/11336/8064
identifier_str_mv Frank, Fernanda Maria; Ulloa, Jerónimo Luis; Cazorla, Silvia Ines; Maravilla, G.; Malchiodi, Emilio Luis; et al.; Trypanocidal Activity of Smallanthus sonchifolius. Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation.; Oxford University Press; Evidence-based Complementary And Alternative Medicine; 6278; 6-2013; 1-10
1741-427X
1741-4288
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.hindawi.com/journals/ecam/2013/627898/
info:eu-repo/semantics/altIdentifier/doi/10.1155/2013/627898
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Oxford University Press
publisher.none.fl_str_mv Oxford University Press
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 12.993085

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