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Previous issue date: 2013Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Laboratório de Biologia Parasitária. Salvador, BA, BrasilUniversidade de São Paulo. Faculdade de Zootecnia e Engenharia de Alimentos. Departamento de Medicina Veterinária. São Paulo, SP, BRasilUniversidade de São Paulo. Faculdade de Medicina de Ribeirão Preto. Departamento de Fisiologia. Ribeirão Preto, SP, BrasilFundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Laboratório de Biologia Parasitária. Salvador, BA, BrasilUniversidade de São Paulo. Faculdade de Zootecnia e Engenharia de Alimentos. Pirassununga, SP, BrazilUniversidade de São Paulo. Faculdade de Zootecnia e Engenharia de Alimentos. Departamento de Medicina Veterinária. São Paulo, SP, BRasilCurso de Farmácia. Unidade de Ensino Superior Ingá. Maringa, SP, BrazilUniversidade Federal da Bahia. Instituto de Química. Departamento de Química Orgânica. Salvador, BA, BrazilFundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Laboratório de Biologia Parasitária. Salvador, BA, BrasilThe plant Cecropia pachystachya Trécul is widely used in Brazilian ethnomedicine to treat hypertension, asthma, and diabetes. Arginase is an enzyme with levels that are elevated in these disorders, and it is central to Leishmania polyamine biosynthesis. The aims of this study were to evaluate antileishmanial activity and inhibition of the arginase enzyme by C. pachystachya extracts, and to study changes in cellular organization using electron microscopy. The ethanol extract of C. pachystachya was tested on Leishmania (Leishmania) amazonensis promastigote survival/proliferation and arginase activity in vitro. Qualitative ultrastructural analysis was also used to observe changes in cell organization. The major bioactive molecules of the ethanol extract were characterized using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS). The ethyl acetate fraction of the ethanol extract diminished promastigote axenic growth/survival, inhibited arginase activity, and altered a mitochondrial kinetoplast DNA (K-DNA) array. The bioactive compounds of C. pachystachya were characterized as glucoside flavonoids. Orientin (9) (luteolin-8-C-glucoside) was the main component of the methanol-soluble ethyl acetate fraction obtained from the ethanol extract and is an arginase inhibitor (IC50 15.9 µM). The ethyl acetate fraction was not cytotoxic to splenocytes at a concentration of 200 µg/mL. In conclusion, C. pachystachya contains bioactive compounds that reduce the growth of L. (L.) amazonensis promastigotes, altering mitochondrial K-DNA arrangement and inhibiting arginase
