ABSTRACT
Species of Piperaceae are known by biological properties, including antiparasitic such as leishmanicidal, antimalarial and in the treatment of schistosomiasis. The aim of this work was to evaluate the antileishmania activity, cytotoxic effect, and macrophage activation patterns of the methanol (MeOH), hexane (HEX), dichloromethane (DCM) and ethyl acetate (EtOAc) extract fractions from the leaves of Piper cabralanum C.DC. The MeOH, HEX and DCM fractions inhibited Leishmanina amazonensis promastigote-like forms growth with a half maximal inhibitory concentration (IC50) of 144.54, 59.92, and 64.87 µg/mL, respectively. The EtOAc fraction did not show any relevant activity. The half maximal cytotoxic concentration (CC50) for macrophages were determined as 370.70, 83.99, 113.68 and 607 µg/mL for the MeOH, HEX and DCM fractions, respectively. The macrophage infectivity was concentration-dependent, especially for HEX and DCM. MeOH, HEX and DCM fractions showed activity against L. amazonensis with low cytotoxicity to murine macrophages and lowering infectivity by the parasite. Our results provide support for in vivo studies related to a potential application of P. cabralanum extract and fractions as a promising natural resource in the treatment of leishmaniasis.
Subject(s)
Antiprotozoal Agents/chemistry , Piper/chemistry , Plant Extracts/chemistry , Animals , Antiprotozoal Agents/isolation & purification , Antiprotozoal Agents/pharmacology , Cell Survival/drug effects , Cells, Cultured , Female , Hexanes/chemistry , Leishmania/drug effects , Leishmania/growth & development , Life Cycle Stages/drug effects , Liquid-Liquid Extraction , Macrophages/cytology , Macrophages/drug effects , Macrophages/metabolism , Male , Methylene Chloride/chemistry , Mice , Mice, Inbred BALB C , Nitric Oxide/metabolism , Phagocytosis/drug effects , Piper/metabolism , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Plant Leaves/chemistry , Plant Leaves/metabolismABSTRACT
Abstract INTRODUCTION: Leishmaniasis, a disease caused by a parasite endemic to large areas of tropical and subtropical countries, is a growing public health problem. METHODS: Male BALB/c mice were infected with Leishmania amazonensis and treated with extracts isolated from Annona mucosa. RESULTS: Treated groups had significantly reduced footpad swelling. The group treated intraperitoneally with hexane extract showed footpad swelling similar to groups treated with Pentamidine® and Glucantime®. Groups treated with dichloromethane extract and hexane extract presented the recovering phenotype associated with reduced parasite levels. CONCLUSIONS: Extracts of A. mucosa are promising sources of novel antileishmanial compounds.
