Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/196192
Type: Artigo de periódico
Title: Trypanocidal Activity Of 2-propen-1-amine Derivatives On Trypomastigotes Culture And In Animal Model.
Author: Oliveira, D A
Pereira, D G
Fernandes, A M A P
De Castro, S L
Souza Brito, A R M
De Souza, A O
Durán, N
Abstract: The cis and trans isomers (either E or Z isomers) of the unsubstituted and bromo-2-propen-1-amine derivatives were evaluated in vitro on Trypanosoma cruzi. The results showed that cis is the most active isomeric form against trypomastigote forms of T. cruzi, indicating that it may contribute most to the trypanocidal effect. All mice which received 5 mg kg(-1) daily for 9 consecutive days, or 200 mg kg(-1) in a single dose of the bromo derivative of 2-propen-1-amine, survived after an infection with 10(4) trypomastigotes/ml of the Y-strain of T. cruzi. They also had a significantly lower parasitemia than the controls. However, with 100 mg kg(-1) of benznidazol for 9 consecutive days, 25% of the animals died by the end of the evaluation 40 days after infection. The involvement of the biosynthesis of ergosterol in the trypanocidal effect of the unsubstituted 2-propen-1-amine derivative was investigated on proliferative epimastigote forms of the parasite. The chromatographic analyses of the lipid extracts obtained from parasites treated with 2-propen-1-amine derivatives and controls (not treated) revealed that growth inhibition is correlated with the accumulation of squalene and the decrease of ergosterol levels. These results suggest that inhibition of the biosynthesis of ergosterol is an important target for the action of the 2-propen-1-amine derivative on T. cruzi through the inhibition of the enzyme squalene epoxidase.
Subject: Amines
Animals
Chagas Disease
Culture Media
Humans
Male
Mice
Trypanocidal Agents
Trypanosoma Cruzi
Rights: fechado
Identifier DOI: 10.1007/s00436-004-1247-9
Address: http://www.ncbi.nlm.nih.gov/pubmed/15616861
Date Issue: 2005
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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