The Brown Alga Stypopodium zonale (Dictyotaceae): A Potential Source of Anti-Leishmania Drugs.
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.
Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21.941-902, Brazil. soaresdc@micro.ufrj.br.
Deivid Costa
DC
Soares
Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21.941-902, Brazil. marcellaszlachta@hotmail.com.
Marcella Macedo
MM
Szlachta
Laboratório Produtos Naturais de Algas Marinhas (ALGAMAR), Departamento de Biologia Marinha, Instituto de Biologia, Universidade Federal Fluminense, Niterói 24.210-150, Brazil. valerialaneuville@gmail.com.
Valéria Laneuville
VL
Teixeira
Grupo de Produtos Naturais de Organismos Aquáticos (GPNOA), Núcleo em Ecologia e Desenvolvimento Sócioambiental de Macaé (NUPEM), Universidade Federal do Rio de Janeiro, Campus-Macaé, Rio de Janeiro 27.965-045, Brazil. angelica.r.soares@gmail.com.
Angelica Ribeiro
AR
Soares
Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21.941-902, Brazil. esaraiva@micro.ufrj.br.
Elvira Maria
EM
Saraiva
D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D004224:Diterpenes / Q000494:pharmacology; D007891:Leishmania / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy* / Q000469:parasitology; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D009569:Nitric Oxide / Q000096:biosynthesis; D000459:Phaeophyceae / Q000737:chemistry*; D017382:Reactive Oxygen Species / Q000378:metabolism
D000981:Antiprotozoal Agents; D004224:Diterpenes; D017382:Reactive Oxygen Species; C570614:atomaric acid; D009569:Nitric Oxide
Stypopodium zonale; leshmanicidal activity; marine natural products; meroditerpenes