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Arzneimittelforschung 2009; 59(4): 207-211
DOI: 10.1055/s-0031-1296387
Antibiotics · Antimycotics · Antiparasitics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

In vitro Effect of a New Cinnamic Acid Derivative Against the Epimastigote Form of Trypanosoma cruzi

Gilberto L Pardo Andreu
1   Departamento de Investigaciones Biomédicas, Centro de Química Farmacéutica, Ciudad de La Habana, (Cuba)
2   Centro de Estudios para las Investigaciones y Evaluaciones Biólogicas, Instituto de Farmacia y Alimentos, Universidad de La Habana, Ciudad Habana, (Cuba)
,
Natalia M Inada
3   Departamento de Patologia Clínica, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, (Brasil)
,
Rolando F Pellón
1   Departamento de Investigaciones Biomédicas, Centro de Química Farmacéutica, Ciudad de La Habana, (Cuba)
,
Maite L Docampo
1   Departamento de Investigaciones Biomédicas, Centro de Química Farmacéutica, Ciudad de La Habana, (Cuba)
,
Mirta L Fascio
4   Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, (Argentina)
,
Norma B D’Accorso
4   Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, (Argentina)
,
Anibal E Vercesi
3   Departamento de Patologia Clínica, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, (Brasil)
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Publikationsverlauf

Publikationsdatum:
13. Dezember 2011 (online)

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Abstract

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 mM CAD-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 mechanism that induces 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.

Key words

Anti-protozoal agents - Chagas’ disease - Cinnamic acid - Epimastigotes - Mitochondria - Oxidative stress - Trypanosoma cruzi
 

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