Efficacy of a diarylheptanoid derivative against Leishmania amazonensis.
The activity of several diarylheptanoid derivatives (curcuminoids) was previously evaluated against Leishmania amazonensis promastigotes and among them the most active compound was the [1-(4-methoxy-phenyl)-7-(3,4-methoxy-4-hydroxy-phenyl)-1,6-heptadien-3, 5-dione]. This derivative was chosen to be assayed in vivo in a treatment trial. For these experiments, the curcuminoid compound was used in a concentration equivalent to the IC50/24 h, obtained from the previous study. Balb/c mice were inoculated subcutaneously in the footpad with L. amazonensis infective promastigotes and 4 weeks after the inoculation, the animals were treated with different schemes, varying from 1 to 3 doses. In all the experiments, Pentamidine Isethionate was used as reference drug under the same experimental conditions. The results showed that one dose was not enough to heal the lesion, however, with 2 and 3 doses the efficiency of the assayed compound was clear. On the other hand, treatment with Pentamidine Isethionate using the three different schemes was not satisfactory when compared to the curcuminoid derivative.
Alves
Luciana Vignólio
LV
Departamento de Imunologia, Instituto Oswaldo Cruz-Fiocruz, Rio de Janeiro, RJ, 21045-900, Brasil.
Temporal
Rosane Maria
RM
Cysne-Finkelstein
Léa
L
Leon
Leonor Laura
LL
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D003474:Curcumin / Q000031:analogs & derivatives*; D007891:Leishmania / Q000187:drug effects*; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D021261:Parasitic Sensitivity Tests; D010419:Pentamidine / Q000737:chemistry / Q000494:pharmacology*
D000981:Antiprotozoal Agents; D010419:Pentamidine; D003474:Curcumin