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Trypanosoma cruzi: Activities of lapachol and α- and β-lapachone derivatives against epimastigote and trypomastigote forms

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2008-01-15
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Salas, Cristian
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Trypanosoma cruzi: Activities of lapachol and α- and β-lapachone derivatives against epimastigote and trypomastigote forms
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Author
  • Salas, Cristian;
  • Tapia, Ricardo A.;
  • Ciudad, Karina;
  • Armstrong, Verónica;
  • Orellana Bown, Myriam;
  • Kemmerling Weis, Ulrike;
  • Ferrada Parker, Jorge;
  • Maya Arango, Juan;
  • Morello Casté, Antonio;
Abstract
Derivatives of natural quinones with biological activities, such as lapachol, α- and β-lapachones, have been synthesized and their trypanocidal activity evaluated in vitro in Trypanosoma cruzi cells. All tested compounds inhibited epimastigote growth and trypomastigote viability. Several compounds showed similar or higher activity as compared with current trypanocidal drugs, nifurtimox and benznidazole. The results presented here show that the anti-T. cruzi activity of the α-lapachone derivatives can be increased by the replacement of the benzene ring by a pyridine moiety. Free radical production and consequently oxidative stress through redox cycling or production of electrophilic metabolites are the potential biological mechanism of action for these synthetic quinones.
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This research was supported by FONDECYT (Research Grants 1020874 and 1061072), Proyecto Anillo ACT 29 CONICYT/PBCT, and DIPUC (Proyecto de Inicio 22 PI/2005).
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URI: https://repositorio.uchile.cl/handle/2250/128400
ISSN: 0968-0896
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Bioorganic & Medicinal Chemistry, Volume 16, Issue 2, Pages 668-674, 2008
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