In vitro anti-parasitic activity of Cyclosporin A analogs on Trypanosoma cruzi

dc.creatorBúa, Jacqueline
dc.creatorRuiz, Andrés M
dc.creatorPotenza, Mariana
dc.creatorFichera, Laura E
dc.date2020-11-25T21:46:27Z
dc.date2020-11-25T21:46:27Z
dc.date2004-09-20
dc.date.accessioned2023-08-29T20:07:16Z
dc.date.available2023-08-29T20:07:16Z
dc.identifier0960-894X
dc.identifierhttp://sgc.anlis.gob.ar/handle/123456789/1741
dc.identifier10.1016/j.bmcl.2004.07.003
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8519574
dc.descriptionFil: Búa, Jacqueline. ANLIS Dr.C.G.Malbrán. Instituto Nacional de Parasitología. Consejo Nacional de Investigaciones, Científicas y Técnicas; Argentina.
dc.descriptionCyclosporin 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.
dc.formatpdf
dc.languageen
dc.relationBioorganic & medicinal chemistry letters
dc.rightsopen
dc.sourceBioorganic & Medicinal Chemistry Letters 2004;14:4633-4637.
dc.subjectAnimales
dc.subjectChlorocebus aethiops
dc.subjectCiclofilinas
dc.subjectCiclosporinas
dc.subjectInmunosupresores
dc.subjectRelación Estructura-Actividad
dc.subjectTripanocidas
dc.subjectTrypanosoma cruzi
dc.subjectCélulas Vero
dc.titleIn vitro anti-parasitic activity of Cyclosporin A analogs on Trypanosoma cruzi
dc.typeArtículo


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