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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.)

Antiparasitic activity and effect of casearins isolated from Casearia sylvestris on Leishmania and Trypanosoma cruzi plasma membrane

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Author(s):
Bou, Diego Dinis [1] ; Temporre, Andre G. [2] ; Pinto, Erika G. [2, 3] ; Lagoa, Joao Henrique G. [1] ; Sartorellia, Patricia [1]
Total Authors: 5
Affiliation:
[1] Univ Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 Diadema, SP - Brazil
[2] Adolfo Lutz Inst, Dept Parasitol, BR-01246000 Sao Paulo, SP - Brazil
[3] Univ Sao Paulo, Inst Med Trop Sao Paulo, BR-05403000 Silo Paulo, SP - Brazil
Total Affiliations: 3
Document type: Journal article
Source: Phytomedicine; v. 21, n. 5, p. 676-681, APR 15 2014.
Web of Science Citations: 19
Abstract

Leishmaniasis and Chagas disease are infectious diseases caused by parasite Leishmania sp. and Trypanosoma cruzi, respectively, and are included among the most neglected diseases in several underdeveloped and developing countries, with an urgent demand for new drugs. Considering the antiparasitic potential of MeOH extract from leaves of Casearia sylvestris Sw. (Salicaceae), a bioguided fractionation was conducted and afforded four active clerodane diterpenes (casearins A, B, G, and J). The obtained results indicated a superior efficacy of tested casearins against trypomastigotes of T. cruzi, with IC50 values ranging from 0.53 to 2.77 mu g/ml. Leishmania infantum promastigotes were also susceptible to casearins, with IC50 values in a range between 4.45 and 9.48 mu g/ml. These substances were also evaluated for mammalian cytotoxicity against NOV cells resulting in 50% cytotoxic concentrations (CC50) ranging from 1.46 to 13.76 mu g/ml. Additionally, the action of casearins on parasite membranes was investigated using the fluorescent probe SYTOX Green. The obtained results demonstrated a strong interaction of casearins A and B to the plasma membrane of T. cruzi parasites, corroborating their higher efficacy against these parasites. In contrast, the tested casearins induced no alteration in the permeability of plasma membrane of Leishmania parasites, suggesting that biochemical differences between Leishmania and T. cruzi plasma membrane might have contributed to the target effect of casearins on trypomastigotes. Thus, considering the importance of studying novel and selective drug candidates against protozoans, casearins A, B, G, and J could be used as tools to future drug design studies. (c) 2014 Elsevier GmbH. All rights reserved. (AU)

FAPESP's process: 11/51739-0 - Sustainable use of biodiversity in Atlantic Forest remnants in São Paulo: evaluation, isolation and molecular characterization of bioactive secondary metabolites in plant species
Grantee:João Henrique Ghilardi Lago
Support type: BIOTA-FAPESP Program - Regular Research Grants
FAPESP's process: 13/16320-4 - Prospection of anti-parasitic and anti-tumor metabolites from plant species of the Atlantic Forest
Grantee:Patricia Sartorelli
Support type: Regular Research Grants