Trypanocidal Activity of Smallanthus sonchifolius: Identification of Active Sesquiterpene Lactones by Bioassay-Guided FractionationReportar como inadecuado




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Evidence-Based Complementary and Alternative MedicineVolume 2013 2013, Article ID 627898, 8 pages

Research Article

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

Cátedra de Farmacognosia, IQUIMEFA UBA-CONICET, Facultad de Farmacia y Bioquímica, Junín 956, 1113 Buenos Aires, Argentina

Instituto de Ecología Regional IER, Facultad de Ciencias Naturales, Universidad Nacional de Tucumán, 4107 Yerba Buena, Tucumán, Argentina

INQUINOA CONICET, Facultad de Bioquímica, Química y Farmacia, UNT, Ayacucho 471, 4000 San Miguel de Tucumán, Argentina

Received 8 April 2013; Accepted 15 May 2013

Academic Editor: Valdir Cechinel Filho

Copyright © 2013 F. M. Frank et al. 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.

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 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.





Autor: F. M. Frank, J. Ulloa, S. I. Cazorla, G. Maravilla, E. L. Malchiodi, A. Grau, V. Martino, C. Catalán, and L. V. Muschiett

Fuente: https://www.hindawi.com/



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