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Title: | In vitro anti-parasitic activity of Cyclosporin A analogs on Trypanosoma cruzi | Authors: | Búa, Jacqueline Ruiz, Andrés M Potenza, Mariana Fichera, Laura E |
Keywords: | Animales;Chlorocebus aethiops;Ciclofilinas;Ciclosporinas;Inmunosupresores;Relación Estructura-Actividad;Tripanocidas;Trypanosoma cruzi;Células Vero | Issue Date: | 20-Sep-2004 | Journal: | Bioorganic & medicinal chemistry letters | Abstract: | Cyclosporin A (CsA) nonimmunosuppressive analogs were evaluated against Trypanosoma cruzi and on TcCyP19, a cyclophilin of 19 kDa. Two out of eight CsA analogs, H-7-94 and F-7-62 showed the best anti-parasitic effects on all in vitro assays. Their IC(50) values were 0.82 and 3.41 microM, respectively, compared to CsA IC(50) value 5.39 microM on epimastigote proliferation; and on trypomastigote lysis their IC(50) values were 0.97 and 2.66 microM compared to CsA IC(50) value 7.19 microM. H-7-94 and F-7-62 were also more effective than CsA in inhibiting trypomastigote infection. The enzymatic activity of TcCyP19 was inhibited by all CsA derivatives, suggesting this target is involved in the trypanocidal effects observed. |
Description: | Fil: Búa, Jacqueline. ANLIS Dr.C.G.Malbrán. Instituto Nacional de Parasitología. Consejo Nacional de Investigaciones, Científicas y Técnicas; Argentina. |
URI: | http://sgc.anlis.gob.ar/handle/123456789/1741 | ISSN: | 0960-894X | DOI: | 10.1016/j.bmcl.2004.07.003 | Rights: | Open Access Creative Commons Attribution 4.0 International License |
Appears in Collections: | Publicaciones INP |
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Bioorganic&MedicinalChemistryLetters-2004-14-p4633-p4637.pdf | Bioorganic&MedicinalChemistryLetters-2004-14-p4633-p4637.pdf | 307.98 kB | Adobe PDF | View/Open |
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