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

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 show...

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Autores principales: Frank, F. M., Ulloa, J., Cazorla, S. I., Maravilla, G., Malchiodi, E. L., Grau, A., Martino, V., Catalán, C., Muschietti, L. V.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3690263/
https://www.ncbi.nlm.nih.gov/pubmed/23840260
http://dx.doi.org/10.1155/2013/627898
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author Frank, F. M.
Ulloa, J.
Cazorla, S. I.
Maravilla, G.
Malchiodi, E. L.
Grau, A.
Martino, V.
Catalán, C.
Muschietti, L. V.
author_facet Frank, F. M.
Ulloa, J.
Cazorla, S. I.
Maravilla, G.
Malchiodi, E. L.
Grau, A.
Martino, V.
Catalán, C.
Muschietti, L. V.
author_sort Frank, F. M.
collection PubMed
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 IC(50) 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 IC(50) 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 IC(50) 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 CC(50) 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.
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spelling pubmed-36902632013-07-09 Trypanocidal Activity of Smallanthus sonchifolius: Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation Frank, F. M. Ulloa, J. Cazorla, S. I. Maravilla, G. Malchiodi, E. L. Grau, A. Martino, V. Catalán, C. Muschietti, L. V. Evid Based Complement Alternat Med Research Article 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 IC(50) 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 IC(50) 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 IC(50) 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 CC(50) 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. Hindawi Publishing Corporation 2013 2013-06-06 /pmc/articles/PMC3690263/ /pubmed/23840260 http://dx.doi.org/10.1155/2013/627898 Text en Copyright © 2013 F. M. Frank et al. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Frank, F. M.
Ulloa, J.
Cazorla, S. I.
Maravilla, G.
Malchiodi, E. L.
Grau, A.
Martino, V.
Catalán, C.
Muschietti, L. V.
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
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_short 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
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3690263/
https://www.ncbi.nlm.nih.gov/pubmed/23840260
http://dx.doi.org/10.1155/2013/627898
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