In vitro antileishmanial and antitrypanosomal activities of flavanones from Baccharis retusa DC. (Asteraceae)
| Autor: | Paulete Romoff, Rodrigo L. O. R. Cunha, Oriana A. Fávero, Simone S. Grecco, Juliana Quero Reimão, Marcelo J. P. Ferreira, Patricia Sartorelli, Andre G. Tempone, João Henrique G. Lago |
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| Přispěvatelé: | Universidade Federal de São Paulo (UNIFESP), Inst Adolfo Lutz Registro, Universidade Federal do ABC (UFABC), Univ Presbiteriana Mackenzie |
| Jazyk: | angličtina |
| Rok vydání: | 2012 |
| Předmět: |
Trypanosoma
Antiparasitic medicine.drug_class Trypanosoma cruzi Population Immunology Antiprotozoal Agents Asteraceae Sakuranetin chemistry.chemical_compound Inhibitory Concentration 50 Mice Structure-Activity Relationship Cricetinae Baccharis retusa DC Botany parasitic diseases medicine Animals Amastigote education Flavonoids Leishmania education.field_of_study Mice Inbred BALB C biology Traditional medicine Mesocricetus Baccharis Plant Extracts Leishmaniasis General Medicine biology.organism_classification medicine.disease Plant Leaves Infectious Diseases chemistry Flavanones Macrophages Peritoneal Biological Assay Parasitology |
| Zdroj: | Repositório Institucional da UNIFESP Universidade Federal de São Paulo (UNIFESP) instacron:UNIFESP |
| Popis: | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Pesquisa e Desenvolvimento 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. Universidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP, Brazil Inst Adolfo Lutz Registro, Dept Parasitol, São Paulo, Brazil Univ Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre, SP, Brazil Univ Presbiteriana Mackenzie, Ctr Ciencias & Humanidades, São Paulo, Brazil Universidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP, Brazil 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 Web of Science |
| Databáze: | OpenAIRE |
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