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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

In vitro and experimental therapeutic studies of the calcium channel blocker bepridil.: Detection of viable Leishmania (L.) chagasi by real-time PCR

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Reimao, Juliana Q. [1] ; Colombo, Fabio A. [2] ; Pereira-Chioccola, Vera L. [2] ; Tempone, Andre G. [1]
Total Authors: 4
[1] Dept Parasitol, Lab Appl Toxinol Antiparasit Drugs, BR-01246902 Sao Paulo - Brazil
[2] Dept Parasitol, Mol Biol Lab, BR-01246902 Sao Paulo - Brazil
Total Affiliations: 2
Document type: Journal article
Source: Experimental Parasitology; v. 128, n. 2, p. 111-115, JUN 2011.
Web of Science Citations: 24

The need for novel and efficacious drugs against neglected parasitic diseases, such as Leishmaniasis and American Trypanosomiasis, is certainly apparent. In this work, we evaluated the in vitro potential of the calcium channel blocker bepridil against Leishmania spp. and Trypanosoma cruzi parasites and exploited an experimental assay using a hamster model with Leishmania (L.) chagasi, with a real-time PCR method for therapeutic evaluation. Bepridil was in vitro effective against promastigotes and intracellular amastigotes of L. (L.) chagasi, with 50% inhibitory concentration (IC(50)) values of 3.81 and 21.55 mu M, respectively. Leishmania (L.) amazonensis, L. (L.) major and L. (V.) braziliensis promastigotes and T. cruzi trypomastigotes were also susceptible to bepridil, with in vitro selectivity toward parasites and IC(50) values in the range of 3 to 7 mu M. The mammalian cytotoxicity using LLC-MK2 cells resulted in an IC(50) value of 62.67 mu M. However, bepridil showed lack of activity at 12 mg/kg in the experimental hamster model infected with L. (L.) chagasi parasites. However, the real-time PCR was a promising tool for the accurate and fast quantification of RNA of living parasites in the liver and spleen of infected hamsters after treatment, eliminating time-consuming light microscopy evaluations. (C) 2011 Elsevier Inc. All rights reserved. (AU)

FAPESP's process: 08/09260-7 - Therapeutic combinations for visceral leishmaniasis: the antileishmanial potential of calcium channel blockers and the use of liposomal nanoformulations
Grantee:André Gustavo Tempone Cardoso
Support type: Regular Research Grants
FAPESP's process: 08/11434-3 - Therapeutic combinations in Visceral Leishmaniasis: the antileishmanial potential of calcium channel blockers
Grantee:Juliana Quero Reimão Dalla Zanna
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 08/00520-6 - American visceral leishmaniasis in Sao Paulo State: study of alternative way of transmission and genetic diversity between autochthonous isolates
Grantee:Vera Lúcia Pereira Chioccola
Support type: Regular Research Grants