Antiprotozoan activity of Brazilian marine cnidarian extracts and of a modified steroid from the octocoral Carijoa riisei.
In the present investigation, we have evaluated the antileishmanial and antitrypanosomal activity of methanolic crude extracts obtained from eight species of cnidarians and of a modified steroid isolated from the octocoral Carijoa riisei. The antileishmanial activity of cnidarians crude extracts showed 50% inhibitory concentration (IC50) values in the concentration range between 2.8 and 93.3 microg/mL. Trypomastigotes of Trypanosoma cruzi were less susceptible to the crude extracts, with IC50 values in the concentration range between 40.9 and 117.9 microg/mL. The steroid (18-acetoxipregna-1,4,20-trien-3-one) displayed a strong antileishmanial activity, with an IC50 value of 5.5 microg/mL against promastigotes and 16.88 microg/mL against intracellular amastigotes. The steroid also displayed mammalian cytotoxicity (IC50 of 10.6 microg/mL), but no hemolytic activity was observed at the highest concentration of 12.5 microg/mL. The antileishmanial effect of the steroid in macrophages suggested other mechanism than macrophage activation, as no upregulation of nitric oxide was observed. The antitrypanosomal activity of the steroid resulted in an IC50 value of 50.5 microg/mL. These results indicate the potential of cnidarian natural compounds as antileishmanial drug candidates.
Reimão
Juliana Quero
JQ
Laboratório de Toxinologia Aplicada, Departamento de Parasitologia, Instituto Adolfo Lutz, Av. Dr. Arnaldo 351, 8 andar, Cerqueira Cesar, CEP 01246-000 São Paulo, São Paulo, Brazil.
Migotto
Alvaro Esteves
AE
Kossuga
Miriam H
MH
Berlinck
Roberto G S
RG
Tempone
André Gustavo
AG