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Molecules 2015, 20(12), 22157-22169;

Leishmanicidal Activity of (+)-Phyllanthidine and the Phytochemical Profile of Margaritaria nobilis (Phyllanthaceae)

Laboratório de Parasitologia e Biologia Estrutural, Instituto de Ciências Biológicas, Universidade Federal do Pará, Belém, Pará 66075-110, Brazil
Instituto Nacional de Biologia Estrutural e Bioimagem, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21941-901, Brazil
Programa de Pós-Graduação em Química, Instituto de Ciências Exatas e Naturais, Universidade Federal do Pará, Belém, Pará 66075-110, Brazil
Laboratório de Microscopia Eletrônica, Instituto Evandro Chagas, Secretaria de Vigilância em Saúde, Ministério da Saúde, Belém, Pará 66090-000, Brazil
Coordenação de Botânica, Museu Paraense Emílio Goeldi, Belém, Pará 66077-901, Brazil
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 7 October 2015 / Revised: 26 November 2015 / Accepted: 27 November 2015 / Published: 11 December 2015
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The effects of the Securinega alkaloid (+)-phyllanthidine on Leishmania (L.) amazonensis and the first chemical investigation of Margaritaria nobilis L.f. (Phyllanthaceae) are described. Treating the parasites with this alkaloid caused a dose-dependent reduction in promastigote growth of 67.68% (IC50 82.37 μg/mL or 353 µM) and in amastigote growth of 83.96% (IC50 49.11 μg/mL or 210 µM), together with ultrastructural alterations in the promastigotes. No cytotoxic effect was detected in mammalian cells (CC50 1727.48 µg/mL or CC50 5268 µM). Classical chromatographic techniques and spectral methods led to the isolation and identification of betulinic acid, kaempferol, corilagin, gallic acid and its methyl ester, besides (+)-phyllanthidine from M. nobilis leaves and stems. Margaritaria nobilis is another source of the small group of Securinega alkaloids, together with other Phyllanthaceae (Euphorbiaceae s.l.) species. The low toxicity to macrophages and the effects against promastigotes and amastigotes are suggestive that (+)-phyllanthidine could be a promising antileishmanial agent for treating cutaneous leishmaniasis. View Full-Text
Keywords: Leishmania (L.) amazonensis; leishmanicidal activity; alkaloid (+)-phyllanthidine Leishmania (L.) amazonensis; leishmanicidal activity; alkaloid (+)-phyllanthidine

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Moraes, L.S.; Donza, M.R.H.; Rodrigues, A.P.D.; Silva, B.J.M.; Brasil, D.S.B.; Zoghbi, M.D.G.B.; Andrade, E.H.A.; Guilhon, G.M.S.P.; Silva, E.O. Leishmanicidal Activity of (+)-Phyllanthidine and the Phytochemical Profile of Margaritaria nobilis (Phyllanthaceae). Molecules 2015, 20, 22157-22169.

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