Leishmanicidal activity of an alkenylphenol from Piper malacophyllum is related to plasma membrane disruption

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Date
2012-11-01Author
Oliveira, Alberto de
Mesquita, Juliana T.
Tempone, Andre G.
Lago, Joao Henrique Ghilardi [UNIFESP]
Guimaraes, Elsie F.
Kato, Massuo J.
Type
ArtigoISSN
0014-4894Is part of
Experimental ParasitologyDOI
10.1016/j.exppara.2012.08.019Metadata
Show full item recordAbstract
Leishmaniasis and Chagas disease are parasitic protozoan infections that affect the poorest population in the world, causing high mortality and morbidity. As a result of highly toxic and long-duration treatments, novel, safe and more efficacious drugs are essential. in this work, the methanol (MeOH) extract from the leaves of Piper malacophyllum (Piperaceae) was fractioned to afford one alkenylphenol, which was characterized as 4-[(3'E)-decenyl]phenol (gibbilimbol B) by spectroscopic methods. Anti-protozoan in vitro assays demonstrated for the first time that Leishmania (L.) infantum chagasi was susceptible to gibbilimbol B. with an in vitro EC50 of 23 mu g/mL against axenic promastigotes and an EC50 of 22 mu g/mL against intracellular amastigotes. Gibbilimbol B was also tested for anti-trypanosomal activity (Trypanosoma cruzi) and showed an EC50 value of 17 mu g/mL against trypomastigotes. To evaluate the cytotoxic parameters, this alkenylphenol was tested in vitro against NCTC cells, showing a CC50 of 59 mu g/mL and absent hemolytic activity at the highest concentration of 75 mu g/mL. Using the fluorescent probe SYTOX Green suggested that the alkenylphenol disrupted the Leishmania plasma membrane upon initial incubation. Further drug design studies aiming at derivatives could be a promising tool for the development of new therapeutic agents for leishmaniasis and Chagas disease. (C) 2012 Elsevier Inc. All rights reserved.
Citation
Experimental Parasitology. San Diego: Academic Press Inc Elsevier Science, v. 132, n. 3, p. 383-387, 2012.Keywords
Piper malacophyllumPiperaceae
Leishmania (L.) infantum chagasi
Trypanosoma cruzi
Gibbilimbol B
Sponsorship
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
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