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In vitro and in vivo activity of lignan lactones derivatives against Trypanosoma cruzi

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Abstract

The trypanocidal effect of six lignan lactones, (−)-cubebin (1), (−)-O-methyl cubebin (2), (−)-O-benzyl cubebin (3), (−)-6,6′-dinitrohinokinin (4), (−)-hinokinin (5) and dimethoxymorelensin (6), previously synthesized by our research group, was evaluated in vitro and in vivo. The compounds with higher anti-epimastigote activity were screened against intracellular amastigote of Trypanosoma cruzi. Among these, compound 5 was selected to be assayed in vivo. It was observed that compounds 5, 6 and 2 showed higher trypanocidal activity against epimastigote forms of T. cruzi, displaying inhibitory concentration (IC50) values of 0.67, 3.89 and 31.35 μM, respectively. These compounds were also evaluated against intracellular amastigote forms of T. cruzi, with five displaying similar activity to benznidazole. In vivo assays showed significant reduction of parasitaemia after administration of five in mice infected.

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Acknowledgment

We would like to thank FAPESP for the financial support. The undertaken experiments comply with the current laws of the country in which they were performed.

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Authors and Affiliations

  1. Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, Avenida do Café s/n, 14040-903, Ribeirão Preto, SP, Brazil

    Juliana Saraiva, Jairo Kenupp Bastos & Sérgio de Albuquerque

  2. Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense de Madrid, Ciudad Universitaria s/n, 28040, Madrid, Spain

    Celeste Vega, Mirian Rolon & Alícia Gomez-Barrio

  3. Núcleo de Pesquisa em Ciências Exatas e Tecnológicas da Universidade de Franca, 14404-600, Franca, SP, Brazil

    Rosangela da Silva & Márcio Luis Andrade e Silva

  4. Departamento de Química da Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, 14040-901, Ribeirão Preto, SP, Brazil

    Paulo Marcos Donate

Authors
  1. Juliana Saraiva
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  2. Celeste Vega
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  3. Mirian Rolon
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  4. Rosangela da Silva
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  5. Márcio Luis Andrade e Silva
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  6. Paulo Marcos Donate
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  7. Jairo Kenupp Bastos
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  8. Alícia Gomez-Barrio
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  9. Sérgio de Albuquerque
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Corresponding author

Correspondence to Juliana Saraiva.

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Saraiva, J., Vega, C., Rolon, M. et al. In vitro and in vivo activity of lignan lactones derivatives against Trypanosoma cruzi . Parasitol Res 100, 791–795 (2007). https://doi.org/10.1007/s00436-006-0327-4

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  • DOI: https://doi.org/10.1007/s00436-006-0327-4

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