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

2013; Elsevier BV; Volume: 135; Issue: 2 Linguagem: Inglês

10.1016/j.exppara.2013.07.007

1090-2449

Patrícia Néris Andrade, John P.A. Caldas, Yara Katia Rodrigues, Francianne M. Amorim, Jacqueline Alves Leite, Sandra Rodrigues‐Mascarenhas, José Maria Barbosa‐Filho, Luís Cézar Rodrigues, Márcia Rosa de Oliveira,

Insect Pest Control Strategies

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.