Artículo
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" (2009) Arzneimittel-Forschung/Drug Research. 59(4):207-211
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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 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.
Registro:
| Documento: | Artículo |
| Título: | In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi |
| Autor: | Andreu, G.L.P.; Inada, N.M.; Pellón, R.F.; Docampo, M.L.; Fascio, M.L.; D'Accorso, N.B.; Vercesi, A.E. |
| Filiación: | Departamento de Investigaciones Biomédicas, Centro de Química Farmacéutica, Ciudad de La Habana, Cuba Centro de Estudios para Las Investigaciones Y Evaluaciones Biólogicas, Instituto de Farmacia Y Alimentos, Universidad de La Habana, Ciudad Habana, Cuba Departamento de Patologia Clínica, Faculdade de Ciências Médicas, Universidade Estadual de Campinas, Campinas, Brazil Departamento de Química Orgánica, Facultad de Ciencias Exactas Y Naturales, Ciudad Universitaria, Buenos Aires, Argentina Centro de Estudios para Las Investigaciones Y Evaluaciones Biólogicas, Instituto de Farmacia Y Alimentos, Universidad de La Habana, Ave. 23 # 21425e/214 y 222, La Coronela, La Lisa, Ciudad Habana, Cuba |
| Palabras clave: | 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 |
| Año: | 2009 |
| Volumen: | 59 |
| Número: | 4 |
| Página de inicio: | 207 |
| Página de fin: | 211 |
| Título revista: | Arzneimittel-Forschung/Drug Research |
| Título revista abreviado: | Arzneim.-Forsch. Drug Res. |
| ISSN: | 00044172 |
| CODEN: | ARZNA |
| CAS: | (2E)-N-(1,3-benzothiazol-2-yl)-3-(2,5-dimethoxyphenyl)-2-propenamide; Amides; Annexin A5; Benzothiazoles; Cinnamates; Coloring Agents; Enzyme Inhibitors; Indicators and Reagents; Propidium, 36015-30-2; Reactive Oxygen Species; Trypanocidal Agents; cinnamic acid, 621-82-9 |
| Registro: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00044172_v59_n4_p207_Andreu |
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Citas:
---------- APA ----------
Andreu, G.L.P., Inada, N.M., Pellón, R.F., Docampo, M.L., Fascio, M.L., D'Accorso, N.B. & Vercesi, A.E. (2009) . In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi. Arzneimittel-Forschung/Drug Research, 59(4), 207-211.Recuperado de https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00044172_v59_n4_p207_Andreu [ ]
---------- CHICAGO ----------
Andreu, G.L.P., Inada, N.M., Pellón, R.F., Docampo, M.L., Fascio, M.L., D'Accorso, N.B., et al. "In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi" . Arzneimittel-Forschung/Drug Research 59, no. 4 (2009) : 207-211.Recuperado de https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00044172_v59_n4_p207_Andreu [ ]
---------- MLA ----------
Andreu, G.L.P., Inada, N.M., Pellón, R.F., Docampo, M.L., Fascio, M.L., D'Accorso, N.B., et al. "In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi" . Arzneimittel-Forschung/Drug Research, vol. 59, no. 4, 2009, pp. 207-211.Recuperado de https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00044172_v59_n4_p207_Andreu [ ]
---------- VANCOUVER ----------
Andreu, G.L.P., Inada, N.M., Pellón, R.F., Docampo, M.L., Fascio, M.L., D'Accorso, N.B., et al. In vitro effect of a new cinnamic acid derivative against the epimastigote form of Trypanosoma cruzi. Arzneim.-Forsch. Drug Res. 2009;59(4):207-211.Available from: https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00044172_v59_n4_p207_Andreu [ ]
