Neolignan Licarin A presents effect against Leishmania (Leishmania) major associated with immunomodulation in vitro.

Autor: Néris PL; Universidade Federal da Paraíba, Centro de Ciências Exatas e da Natureza, Departamento de Biologia Molecular, Laboratório de Leishmanioses, João Pessoa, Paraíba, Brazil., Caldas JP, Rodrigues YK, Amorim FM, Leite JA, Rodrigues-Mascarenhas S, Barbosa-Filho JM, Rodrigues LC, Oliveira MR
Jazyk: angličtina
Zdroj: Experimental parasitology [Exp Parasitol] 2013 Oct; Vol. 135 (2), pp. 307-13. Date of Electronic Publication: 2013 Jul 24.
DOI: 10.1016/j.exppara.2013.07.007
Abstrakt: Leishmaniasis' treatment is based mostly on pentavalent antimonials or amphotericin B long-term administration, expensive drugs associated with severe side effects. Considering these aforementioned, the search for alternative effective and safe leishmaniasis treatments is a necessity. This work evaluated a neolignan, licarin A anti-leishmanial activity chemically synthesized by our study group. It was observed that licarin A effectively inhibited Leishmania (Leishmania) major promastigotes (IC₅₀ of 9.59 ± 0.94 μg/mL) growth, by inducing in these parasites genomic DNA fragmentation in a typical death pattern by apoptosis. Additionally, the neolignan proved to be even more active against intracellular amastigotes of the parasite (EC₅₀ of 4.71 ± 0.29 μg/mL), and significantly more effective than meglumine antimoniate (EC₅₀ of 216.2 ± 76.7 μg/mL) used as reference drug. The antiamastigote activity is associated with an immunomodulatory activity, since treatment with licarin A of the infected macrophages induced a decrease in the interleukin (IL)-6 and IL-10 production. This study demonstrates for the first time the antileishmanial activity of licarin A and suggests that the compound may be a promising in the development of a new leishmanicidal agent.
(Copyright © 2013 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE