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Biological activity of 1,2,3,4-tetrahydro-β-carboline-3-carboxamides against Trypanosoma cruzi

Authors
  • Valdez, Rodrigo Hinojosa
  • Tonin, Lilian Tatiani Düsman
  • Ueda-Nakamura, Tânia
  • Filho, Benedito Prado Dias
  • Morgado-Diaz, José Andrés
  • Sarragiotto, Maria Helena
  • Nakamura, Celso Vataru
Type
Published Article
Journal
Acta Tropica
Publisher
Elsevier
Publication Date
Jan 01, 2008
Accepted Date
Nov 12, 2008
Volume
110
Issue
1
Pages
7–14
Identifiers
DOI: 10.1016/j.actatropica.2008.11.008
Source
Elsevier
Keywords
License
Unknown

Abstract

Several β-carboline compounds were evaluated for in vitro trypanocidal activity against Trypanosoma cruzi and their potential toxic effects was also assessed. β-Carboline derivative 4 showed good activity against epimastigote, trypomastigote, and amastigote forms of T. cruzi, with a dose-dependent inhibitory effect. It showed an IC 50 of 14.9 μM against the epimastigote form and an EC 50 of 45 μM and 33 μM against trypomastigote and amastigote forms, respectively. Additionally, 4 was able to be active on mammalian cell–protozoan interaction, reducing the number of infected cells and the number of internalized parasites. The compound showed low cytotoxicity, with a selective index 31 times higher to the parasite than for mammalian cells. In human red-blood cells β-Carboline 4 at 14.9 μM not caused haemolysis. Observed at electron microscopy 4-treated epimastigotes showed abnormal swelling of the mitochondrion, a diffuse kinetoplast, and distortions of the parasite cell body. The present data support the potential effect of this class of compounds against T. cruzi and encourage further experiments in vitro to evaluate the action mechanism of this drug and also with in vivo models.

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