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Preparation and activity of diterpenoids against trypomastigotes of Trypanosoma cruzi

Abstract

A systematic investigation on the trypanocidal effect of several natural products isolated from Brazilian plant species has been carried out. In this paper we report on the results obtained from the screening of 26 diterpenes from natural sources or of synthetic/microbial transformations origin (mainly derivatives of kaurenoic acid) against trypomastigote forms of Trypanosoma cruzi, the causative agent of Chagas'disease. In the in vitro assays, kaurenoic acid, kaurenol, acutifloric acid and stemodin showed a complete elimination of parasites from the blood. Therefore, such diterpenoids can be considered as starting materials for molecular modification in the search for lead compounds for clearance of infected blood to be used in transfusions. Blood previously treated with active compounds was submitted to an infectivity test. Samples proceeded from treatment with kaurenol and kaurenoic acid showed to be completly clean from T. cruzi as no infection was observed in mice inoculated with contaminated blood treated by these compounds.


Preparation and activity of diterpenoids against trypomastigotes of Trypanosoma cruzi

Jacqueline A. TakahashiI,* * jacque@Ag.arizona.edu ; Henriete S. VieiraI; Eliane A. SilvaI; Maria A. D. BoaventuraI; Alaíde B. de OliveiraII; Egler ChiariIII

IDepartamento de Química, ICEx, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, 31270-901, Belo Horizonte, MG, Brazil

IIDepartamento de Produtos Farmacêuticos, Faculdade de Farmácia, UFMG, Av. Olegário Maciel, 2360, 30180-112, Belo Horizonte, MG

IIIDepartamento de Parasitologia, ICB, UFMG, Av. Antônio Carlos, 6627, CP 2486, 31270-901, Belo Horizonte, MG

ABSTRACT

A systematic investigation on the trypanocidal effect of several natural products isolated from Brazilian plant species has been carried out. In this paper we report on the results obtained from the screening of 26 diterpenes from natural sources or of synthetic/microbial transformations origin (mainly derivatives of kaurenoic acid) against trypomastigote forms of Trypanosoma cruzi, the causative agent of Chagas'disease. In the in vitro assays, kaurenoic acid, kaurenol, acutifloric acid and stemodin showed a complete elimination of parasites from the blood. Therefore, such diterpenoids can be considered as starting materials for molecular modification in the search for lead compounds for clearance of infected blood to be used in transfusions. Blood previously treated with active compounds was submitted to an infectivity test. Samples proceeded from treatment with kaurenol and kaurenoic acid showed to be completly clean from T. cruzi as no infection was observed in mice inoculated with contaminated blood treated by these compounds.

Full text available only in PDF format.

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Acknowledgments

The authors thank CNPq and FAPEMIG (Brazil) for fellowships and financial support.

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  • Publication Dates

    • Publication in this collection
      05 Oct 2009
    • Date of issue
      2002
    Sociedade Brasileira de Farmacognosia Universidade Federal do Paraná, Laboratório de Farmacognosia, Rua Pref. Lothario Meissner, 632 - Jd. Botânico, 80210-170, Curitiba, PR, Brasil, Tel/FAX (41) 3360-4062 - Curitiba - PR - Brazil
    E-mail: revista@sbfgnosia.org.br