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

Molecules

Lienne S. Moraes⁴  Marcio R. H. Donza¹  Ana Paula D. Rodrigues²  Bruno J. M. Silva⁴  Davi S. B. Brasil¹  Maria das Gra๺sB. Zoghbi³  Eloísa H. A. Andrade¹  Giselle M. S. P. Guilhon¹  Edilene O. Silva⁴ 

[1] Programa de Pós-Graduação em Química, Instituto de Ciências Exatas e Naturais, 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;Coordenação de Botânica, Museu Paraense Emílio Goeldi, Belém, Pará 66077-901, Brazil;Laboratório de Parasitologia e Biologia Estrutural, Instituto de Ciências Biológicas, Universidade Federal do Pará, Belém, Pará 66075-110, Brazil;

关键词: Leishmania (L.) amazonensis;    leishmanicidal activity;    alkaloid (+)-phyllanthidine;   

DOI  :  10.3390/molecules201219829

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.