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

Gilberto L Pardo Andreu; Natalia M Inada; Rolando F Pellón; Maite L Docampo; Mirta L Fascio; Norma B D’Accorso; Anibal E Vercesi

doi:10.1055/s-0031-1296387

Arzneimittelforschung, Table of Contents

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

¹Departamento de Investigaciones Biomédicas, Centro de Química Farmacéutica, Ciudad de La Habana, (Cuba)

²Centro de Estudios para las Investigaciones y Evaluaciones Biólogicas, Instituto de Farmacia y Alimentos, Universidad de La Habana, Ciudad Habana, (Cuba)

,

Natalia M Inada

³Departamento de Patologia Clínica, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, (Brasil)

,

Rolando F Pellón

¹Departamento de Investigaciones Biomédicas, Centro de Química Farmacéutica, Ciudad de La Habana, (Cuba)

,

Maite L Docampo

¹Departamento de Investigaciones Biomédicas, Centro de Química Farmacéutica, Ciudad de La Habana, (Cuba)

,

Mirta L Fascio

⁴Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, (Argentina)

,

Norma B D’Accorso

⁴Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, (Argentina)

,

Anibal E Vercesi

³Departamento de Patologia Clínica, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, (Brasil)

› Author Affiliations

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

Full Text

References

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