In vitro antileishmanial and antitrypanosomal activities of flavanones from Baccharis retusa DC. (Asteraceae)

In vitro antileishmanial and antitrypanosomal activities of flavanones from Baccharis retusa DC. (Asteraceae)

Author Grecco, Simone dos Santos Autor UNIFESP Google Scholar
Reimao, Juliana Q. Google Scholar
Tempone, Andre G. Google Scholar
Sartorelli, Patricia Autor UNIFESP Google Scholar
Cunha, Rodrigo Luiz Oliveira Rodrigues Autor UNIFESP Google Scholar
Romoff, Paulete Google Scholar
Ferreira, Marcelo J. P. Google Scholar
Favero, Oriana A. Google Scholar
Lago, Joao Henrique Ghilardi Autor UNIFESP Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
Inst Adolfo Lutz Registro
Universidade Federal do ABC (UFABC)
Univ Presbiteriana Mackenzie
Abstract Leishmaniasis and Chagas' are parasitic protozoan diseases that affect the poorest population in the world, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, novel, safe and more efficacious drugs are essential. in this work, the CH2Cl2 phase from MeOH extract from the leaves of Baccharis retusa DC. (Asteraceae) was fractioned to afford two flavonoids: naringenin (1) and sakuranetin (2). These compounds were in vitro tested against Leishmania spp. promastigotes and amastigotes and Ttypanosoma cruzi trypomastigotes and amastigotes. Compound 2 presented activity against Leishmania (L) amazonensis, Leishmania (V.) braziliensis, Leishmania (L) major, and Leishmania (L) chagasi with IC50 values in the range between 43 and 52 mu g/mL and against T. cruzi trypomastigotes (IC50= 20.17 mu g/mL). Despite of the chemical similarity, compound 1 did not show antiparasitic activity. Additionally, compound 2 was subjected to a methylation procedure to give sakuranetin-4'-methyl ether (3), which resulted in an inactive compound against both Leishmania spp. and T. cnizi. the obtained results indicated that the presence of one hydroxyl group at C-4' associated to one methoxyl group at C-7 is important to the antiparasitic activity. Further drug design studies aiming derivatives could be a promising tool for the development of new therapeutic agents for Leishmaniasis and Chagas' disease. (C) 2011 Elsevier Inc. All rights reserved.
Keywords Baccharis retusa DC
Asteraceae
Leishmania
Trypanosoma cruzi
Flavanones
Language English
Sponsor Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Conselho Nacional de Pesquisa e Desenvolvimento
Grant number FAPESP: 06/57626-5
FAPESP: 08/11496-9
Conselho Nacional de Pesquisa e Desenvolvimento: 473405/2008-3
Conselho Nacional de Pesquisa e Desenvolvimento: 477422/2009-8
Date 2012-02-01
Published in Experimental Parasitology. San Diego: Academic Press Inc Elsevier Science, v. 130, n. 2, p. 141-145, 2012.
ISSN 0014-4894 (Sherpa/Romeo, impact factor)
Publisher Elsevier B.V.
Extent 141-145
Origin http://dx.doi.org/10.1016/j.exppara.2011.11.002
Access rights Open access Open Access
Type Article
Web of Science ID WOS:000300129500009
URI http://repositorio.unifesp.br/handle/11600/34542

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