lignans and Leishmaniasis--Cutaneous

Yangambin and epi-yangambin are the main lignans found in Louro-de-Cheiro [. Bone marrow-derived mouse macrophages were infected with. Yangambin and epi-yangambin were found to reduce the intracellular viability of either. The present results serve to encourage the development of novel studies aimed at screening natural bioactive compounds with the hope of discovering new therapeutic options for the treatment of Cutaneous Leishmaniasis.

Topics: Animals; Leishmania; Leishmaniasis, Cutaneous; Lignans; Mice; Mice, Inbred BALB C; Ocotea; Plant Extracts

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.

Topics: Amphotericin B; Animals; Antiprotozoal Agents; Apoptosis; Cytokines; DNA Fragmentation; Female; Immunologic Factors; Inhibitory Concentration 50; Leishmania major; Leishmaniasis, Cutaneous; Lignans; Macrophages, Peritoneal; Meglumine; Meglumine Antimoniate; Mice; Mice, Inbred BALB C; Nitric Oxide; Organometallic Compounds