In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi
An intensive effort has been directed toward finding alternative drugs for treatment of Chagas' disease, caused by Trypanosoma cruzi (T. cruzi), and prophylaxis of blood in endemic areas. The preparation and in vitro evaluation as potential anti-protozoal agent of (2E)-N-(1,3-benzothiazol-2-yl)...
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todo:paper_00044172_v59_n4_p207_Andreu2023-10-03T13:57:13Z In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi Andreu, G.L.P. Inada, N.M. Pellón, R.F. Docampo, M.L. Fascio, M.L. D'Accorso, N.B. Vercesi, A.E. Anti-protozoal agents Chagas' disease Cinnamic acid Epimastigotes Mitochondria Oxidative stress Trypanosoma cruzi cad 1 cinnamic acid derivative n (1,3 benzothiazol 2 yl) 3 (2,5 dimethoxyphenyl) 2 propenamide reactive oxygen metabolite unclassified drug antiprotozoal activity article drug mechanism drug structure epimastigote in vitro study mitochondrial membrane potential nonhuman Trypanosoma cruzi Amides Animals Annexin A5 Benzothiazoles Cinnamates Coloring Agents Enzyme Inhibitors Flow Cytometry Indicators and Reagents Membrane Potentials Propidium Reactive Oxygen Species Trypanocidal Agents Trypanosoma cruzi An intensive effort has been directed toward finding alternative drugs for treatment of Chagas' disease, caused by Trypanosoma cruzi (T. cruzi), and prophylaxis of blood in endemic areas. The preparation and in vitro evaluation as potential anti-protozoal agent of (2E)-N-(1,3-benzothiazol-2-yl)-3-(2,5- dimethoxyphenyl)-2-propenamide (CAD-1) is presented. The results show that 0.05 mMCAD-1 induced 58.1% of T. cruzi epimastigotes death; mainly by apoptosis. The diminution in the transmembrane mitochondrial electrical potential together with the increase in the intracellular generation/accumulation of reactive oxygen species, suggest the parasites mitochondria as the main target for CAD-1-induced death. The concentration of 0.05 mM CAD-1 is not low enough to consider it as a potent tripanocydal agent. However the novel mechanismthat induce s T. cruzi death, together with the novelty of its chemical structure, point out CAD-1 as a head group compound that could serve as a template to obtain new, more potent anti-Chagas disease agents. © ECV Editio Cantor Verlag. Fil:Fascio, M.L. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:D'Accorso, N.B. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_00044172_v59_n4_p207_Andreu |
institution |
Universidad de Buenos Aires |
institution_str |
I-28 |
repository_str |
R-134 |
collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
topic |
Anti-protozoal agents Chagas' disease Cinnamic acid Epimastigotes Mitochondria Oxidative stress Trypanosoma cruzi cad 1 cinnamic acid derivative n (1,3 benzothiazol 2 yl) 3 (2,5 dimethoxyphenyl) 2 propenamide reactive oxygen metabolite unclassified drug antiprotozoal activity article drug mechanism drug structure epimastigote in vitro study mitochondrial membrane potential nonhuman Trypanosoma cruzi Amides Animals Annexin A5 Benzothiazoles Cinnamates Coloring Agents Enzyme Inhibitors Flow Cytometry Indicators and Reagents Membrane Potentials Propidium Reactive Oxygen Species Trypanocidal Agents Trypanosoma cruzi |
spellingShingle |
Anti-protozoal agents Chagas' disease Cinnamic acid Epimastigotes Mitochondria Oxidative stress Trypanosoma cruzi cad 1 cinnamic acid derivative n (1,3 benzothiazol 2 yl) 3 (2,5 dimethoxyphenyl) 2 propenamide reactive oxygen metabolite unclassified drug antiprotozoal activity article drug mechanism drug structure epimastigote in vitro study mitochondrial membrane potential nonhuman Trypanosoma cruzi Amides Animals Annexin A5 Benzothiazoles Cinnamates Coloring Agents Enzyme Inhibitors Flow Cytometry Indicators and Reagents Membrane Potentials Propidium Reactive Oxygen Species Trypanocidal Agents Trypanosoma cruzi Andreu, G.L.P. Inada, N.M. Pellón, R.F. Docampo, M.L. Fascio, M.L. D'Accorso, N.B. Vercesi, A.E. In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi |
topic_facet |
Anti-protozoal agents Chagas' disease Cinnamic acid Epimastigotes Mitochondria Oxidative stress Trypanosoma cruzi cad 1 cinnamic acid derivative n (1,3 benzothiazol 2 yl) 3 (2,5 dimethoxyphenyl) 2 propenamide reactive oxygen metabolite unclassified drug antiprotozoal activity article drug mechanism drug structure epimastigote in vitro study mitochondrial membrane potential nonhuman Trypanosoma cruzi Amides Animals Annexin A5 Benzothiazoles Cinnamates Coloring Agents Enzyme Inhibitors Flow Cytometry Indicators and Reagents Membrane Potentials Propidium Reactive Oxygen Species Trypanocidal Agents Trypanosoma cruzi |
description |
An intensive effort has been directed toward finding alternative drugs for treatment of Chagas' disease, caused by Trypanosoma cruzi (T. cruzi), and prophylaxis of blood in endemic areas. The preparation and in vitro evaluation as potential anti-protozoal agent of (2E)-N-(1,3-benzothiazol-2-yl)-3-(2,5- dimethoxyphenyl)-2-propenamide (CAD-1) is presented. The results show that 0.05 mMCAD-1 induced 58.1% of T. cruzi epimastigotes death; mainly by apoptosis. The diminution in the transmembrane mitochondrial electrical potential together with the increase in the intracellular generation/accumulation of reactive oxygen species, suggest the parasites mitochondria as the main target for CAD-1-induced death. The concentration of 0.05 mM CAD-1 is not low enough to consider it as a potent tripanocydal agent. However the novel mechanismthat induce s T. cruzi death, together with the novelty of its chemical structure, point out CAD-1 as a head group compound that could serve as a template to obtain new, more potent anti-Chagas disease agents. © ECV Editio Cantor Verlag. |
format |
JOUR |
author |
Andreu, G.L.P. Inada, N.M. Pellón, R.F. Docampo, M.L. Fascio, M.L. D'Accorso, N.B. Vercesi, A.E. |
author_facet |
Andreu, G.L.P. Inada, N.M. Pellón, R.F. Docampo, M.L. Fascio, M.L. D'Accorso, N.B. Vercesi, A.E. |
author_sort |
Andreu, G.L.P. |
title |
In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi |
title_short |
In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi |
title_full |
In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi |
title_fullStr |
In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi |
title_full_unstemmed |
In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi |
title_sort |
in vitro effect of a new cinnamic acid derivative against the epimastigote form of trypanosoma cruzi |
url |
http://hdl.handle.net/20.500.12110/paper_00044172_v59_n4_p207_Andreu |
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