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

Author(s)

Grecco, Simone dos S. ^[1] ; Reimao, Juliana Q. ^[2] ; Tempone, Andre G. ^[2] ; Sartorelli, Patricia ^[1] ; Cunha, Rodrigo L. O. R. ^[3] ; Romoff, Paulete ^[4] ; Ferreira, Marcelo J. P. ^[4] ; Favero, Oriana A. ^[4] ; Lago, Joao Henrique G. ^[1]

Affiliation

^[1] Univ Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP - Brazil

^[2] Adolfo Lutz Inst, Dept Parasitol, Sao Paulo - Brazil

^[3] Univ Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre, SP - Brazil

^[4] Univ Presbiteriana Mackenzie, Ctr Ciencias & Humanidades, Sao Paulo - Brazil

• Document type: Journal article
• Source: Experimental Parasitology; v. 130, n. 2, p. 141-145, FEB 2012.
• Web of Science Citations: 46

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. (AU)

• FAPESP's process: 08/11496-9 - Leishmanicidal principles of vegetable species from Atlantic Forest: evaluation, isolation and molecular characterization
• Grantee: Patricia Sartorelli
• Support Opportunities: Regular Research Grants
• FAPESP's process: 06/57626-5 - Selection of potential molecules in plant species of São Paulo State highlands: chemical structure, relationship structure / biological activity associated with ecophysiological considerations
• Grantee: João Henrique Ghilardi Lago
• Support Opportunities: Research Grants - Young Investigators Grants