Abstract
This study evaluated the anti-Leishmania amazonensis activity of a lipophilic extract from the brown alga Stypopodium zonale and atomaric acid, its major compound. Our initial results revealed high inhibitory activity for intracellular amastigotes in a dose-dependent manner and an IC50 of 0.27 μg/mL. Due to its high anti-Leishmania activity and low toxicity toward host cells, we fractionated the lipophilic extract. A major meroditerpene in this extract, atomaric acid, and its methyl ester derivative, which was obtained by a methylation procedure, were identified by nuclear magnetic resonance (NMR) spectroscopy. Both compounds inhibited intracellular amastigotes, with IC50 values of 20.2 μM (9 μg/mL) and 22.9 μM (10 μg/mL), and selectivity indexes of 8.4 μM and 11.5 μM. The leishmanicidal activity of both meroditerpenes was independent of nitric oxide (NO) production, but the generation of reactive oxygen species (ROS) may be at least partially responsible for the amastigote killing. Our results suggest that the lipophilic extract of S. zonale may represent an important source of compounds for the development of anti-Leishmania drugs.
Highlights
Leishmaniasis comprises a wide spectrum of diseases that are characterized by cutaneous, mucosal, and visceral organ lesions
Lamouroux) Papenfuss were collected in Búzios, Specimens of Stypopodium zonale
We showed a leishmanicidal activity of Stypopodium zonale extract (SZE) against Leishmania amazonensis, promastigotes, and intracellular amastigotes
Summary
Leishmaniasis comprises a wide spectrum of diseases that are characterized by cutaneous, mucosal, and visceral organ lesions. Pentavalent antimonials, pentamidine, amphotericin B, and paromomycin are the drugs available for the treatment of leishmaniasis. As a rich source of structurally‐unique and diterpenes of mixed (meroditerpenoids) These compounds exhibit interesting biologically‐active diterpenes of mixed biogenesis [16,17,18,19,20,21,22,23]. We describe the anti‐leishmanial activity of lipophilic extract of Stypopodium zonale and meroditerpenoid atomaric acid, the major compound isolated from the lipophilic extract of S. zonale. Meroditerpenoid atomaric acid, the major compound isolated from the lipophilic extract of S. zonale. Stypopodium as zonale a potential source of substances for the development of drugs for leishmaniasis treatment. As a potential source of substances for the development of drugs for leishmaniasis treatment
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