In vitro activity of N-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms

In vitro activity of N-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms

N-Benzenesulfonylbenzotriazole (BSBZT) could be a prototype for the development of anti-Trypanosoma cruzi drugs. Incubation of epimastigotes and trypomastigotes with BSBZT resulted in a decrease in the parasite number. [Display omitted] ► N-Benzenesulfonylbenzotriazole (BSBZT) showed activity agains...

Full description

Saved in:
Bibliographic Details
Published in:Experimental parasitology Vol. 131; no. 1; pp. 57 - 62
Main Authors: Becerra, M.C., Guiñazú, N., Hergert, L.Y., Pellegrini, A., Mazzieri, M.R., Gea, S., Albesa, I.
Format: Journal Article
Language:English
Published: United States Elsevier Inc 01-05-2012
Subjects:
adverse effects
Animals
Benzenesulfonylbenzotriazole
Benzotriazole
Cell Line
Cell Survival - drug effects
Chagas disease
Chagas Disease - parasitology
cytotoxicity
dose response
drugs
epimastigotes
Erythrocytes - drug effects
flow cytometry
hemolysis
Humans
Inhibitory Concentration 50
lethal concentration 50
Macrophages - drug effects
Mice
Mice, Inbred BALB C
Nitroimidazoles - pharmacology
Nitroimidazoles - toxicity
parasites
parasitology
Prototype
Sulfonamides - pharmacology
Sulfonamides - toxicity
therapeutics
Triazoles - pharmacology
Triazoles - toxicity
Trypanocidal activity
Trypanocidal Agents - pharmacology
Trypanocidal Agents - toxicity
Trypanosoma cruzi
Trypanosoma cruzi - drug effects
Trypanosoma cruzi - growth & development
trypomastigotes
South America
Benzenesulfonylbenzotriazole
Prototype
Trypanocidal activity
Benzotriazole
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:N-Benzenesulfonylbenzotriazole (BSBZT) could be a prototype for the development of anti-Trypanosoma cruzi drugs. Incubation of epimastigotes and trypomastigotes with BSBZT resulted in a decrease in the parasite number. [Display omitted] ► N-Benzenesulfonylbenzotriazole (BSBZT) showed activity against Trypanosoma cruzi. ► Benznidazole (BZL), BSBZT and benzotriazole (BZT) were tested in parallel. ► BSBZT reduced the number of epimastigotes and trypomastigotes. ► Size reduction of epimastigotes was detected by flow cytometry. ► BSBZT presented low cytotoxic and hemolytic activities. Chagas disease is still an important health problem in Central and South America. However, the only drugs currently available for specific treatment of this disease may induce toxic side effects in the host. The aim of this work was to determine the activity of N-benzenesulfonylbenzotriazole (BSBZT) against the protozoan parasite Trypanosoma cruzi. The effects of BSBZT and benzotriazole (BZT) were compared to those of benznidazole (BZL) on epimastigote and trypomastigote forms. BSBZT was found to have an in vitro growth inhibitory dose-dependent activity against epimastigotes, with flow cytometry analysis confirming that the treated parasites presented size reduction. BSBZT showed an IC50 of 21.56μg/mL (81.07μM) against epimastigotes at 72h of incubation, whereas BZT did not affect the growth of this parasite form. Furthermore, the toxic effect of BSBZT, was stronger and appeared earlier (at 24h) in trypomastigotes than in epimastigotes, with the LC50 of this compound being 28.40μg/mL (106.79μM) against trypomastigotes. The concentrations of BSBZT used in this study presented low hemolytic activity and cytotoxicity. Consequently, at concentrations near IC50 and LC50 (25μg/mL), BSBZT caused only 2.4% hemolysis and 15% of RAW 264.7 cell cytotoxicity. These results reveal the potential of BSBZT as a prototype in drug design for developing new anti-T. cruzi compounds.
Bibliography:http://dx.doi.org/10.1016/j.exppara.2012.02.028
ISSN:0014-4894
1090-2449
DOI:10.1016/j.exppara.2012.02.028