Leishmanicidal activity of an alkenylphenol from Piper malacophyllum is related to plasma membrane disruption
Contribuinte(s) |
UNIVERSIDADE DE SÃO PAULO |
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Data(s) |
07/11/2013
07/11/2013
2012
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Resumo |
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. FAPESP CNPq |
Identificador |
EXPERIMENTAL PARASITOLOGY, SAN DIEGO, v. 132, n. 3, p. 383-387, NOV, 2012 0014-4894 http://www.producao.usp.br/handle/BDPI/43172 10.1016/j.exppara.2012.08.019 |
Idioma(s) |
eng |
Publicador |
ACADEMIC PRESS INC ELSEVIER SCIENCE SAN DIEGO |
Relação |
EXPERIMENTAL PARASITOLOGY |
Direitos |
closedAccess Copyright ACADEMIC PRESS INC ELSEVIER SCIENCE |
Palavras-Chave | #PIPER MALACOPHYLLUM #PIPERACEAE #LEISHMANIA (L.) INFANTUM CHAGASI #TRYPANOSOMA CRUZI #GIBBILIMBOL B #GIBBILIMBOLS A-D #TRYPANOCIDAL TETRAHYDROFURAN LIGNANS #BENZOIC-ACID DERIVATIVES #TRYPANOSOMA-CRUZI #ANTIBACTERIAL ALKENYLPHENOLS #ANTILEISHMANIAL ACTIVITIES #VAR. PALLESCENS #TUBERCULATUM #ASTERACEAE #ALKALOIDS #PARASITOLOGY |
Tipo |
article original article publishedVersion |