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

Abstract

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 μ M (1), 1.09 μ M (2), and 4.90 μ M (3). After a 24 h treatment with 10 μ g/mL of enhydrin or uvedalin, parasites were not able to recover their replication rate. Compounds 1 and 2 showed IC50 values of 33.4 μ M and 25.0 μ M 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 μ M, 3.34 μ M, and 9.02 μ M for 1, 2, and 3, respectively. The cytotoxicity of the compounds was evaluated in Vero cells obtaining CC50 values of 46.5 μ M (1), 46.8 μ M (2), and 147.3 μ M (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.

Authors+Show Affiliations

Cátedra de Inmunología, IDEHU (UBA-CONICET), Facultad de Farmacia y Bioquímica Junín 956, 1113, Buenos Aires, Argentina, Instituto de Microbiología y Parasitología Médica, IMPaM (UBA-CONICET), Facultad de Medicina, Paraguay 215, 1121 Buenos Aires, Argentina.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

23840260

Citation

Frank, F M., et al. "Trypanocidal Activity of Smallanthus Sonchifolius: Identification of Active Sesquiterpene Lactones By Bioassay-Guided Fractionation." Evidence-based Complementary and Alternative Medicine : ECAM, vol. 2013, 2013, p. 627898.
Frank FM, Ulloa J, Cazorla SI, et al. Trypanocidal Activity of Smallanthus sonchifolius: Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation. Evidence-based complementary and alternative medicine : eCAM. 2013;2013:627898.
Frank, F. M., Ulloa, J., Cazorla, S. I., Maravilla, G., Malchiodi, E. L., Grau, A., Martino, V., Catalán, C., & Muschietti, L. V. (2013). Trypanocidal Activity of Smallanthus sonchifolius: Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation. Evidence-based Complementary and Alternative Medicine : ECAM, 2013, 627898. https://doi.org/10.1155/2013/627898
Frank FM, et al. Trypanocidal Activity of Smallanthus Sonchifolius: Identification of Active Sesquiterpene Lactones By Bioassay-Guided Fractionation. Evidence-based complementary and alternative medicine : eCAM. 2013;2013:627898. PubMed PMID: 23840260.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Trypanocidal Activity of Smallanthus sonchifolius: Identification of Active Sesquiterpene Lactones by Bioassay-Guided Fractionation. AU - Frank,F M, AU - Ulloa,J, AU - Cazorla,S I, AU - Maravilla,G, AU - Malchiodi,E L, AU - Grau,A, AU - Martino,V, AU - Catalán,C, AU - Muschietti,L V, Y1 - 2013/06/06/ PY - 2013/04/08/received PY - 2013/05/15/accepted PY - 2013/7/11/entrez PY - 2013/7/11/pubmed PY - 2013/7/11/medline SP - 627898 EP - 627898 JF - Evidence-based complementary and alternative medicine : eCAM VL - 2013 N2 - 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 μ M (1), 1.09 μ M (2), and 4.90 μ M (3). After a 24 h treatment with 10 μ g/mL of enhydrin or uvedalin, parasites were not able to recover their replication rate. Compounds 1 and 2 showed IC50 values of 33.4 μ M and 25.0 μ M 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 μ M, 3.34 μ M, and 9.02 μ M for 1, 2, and 3, respectively. The cytotoxicity of the compounds was evaluated in Vero cells obtaining CC50 values of 46.5 μ M (1), 46.8 μ M (2), and 147.3 μ M (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. SN - 1741-427X UR - https://www.unboundmedicine.com/medline/citation/23840260/Trypanocidal_Activity_of_Smallanthus_sonchifolius:_Identification_of_Active_Sesquiterpene_Lactones_by_Bioassay_Guided_Fractionation_ L2 - https://doi.org/10.1155/2013/627898 DB - PRIME DP - Unbound Medicine ER -
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