Leishmanicidal activity of nine novel flavonoids from Delphinium staphisagria.
OBJECTIVE
To evaluate the in vitro leishmanicidal activity of nine flavonoid derivatives from Delphinium staphisagria against L. infantum and L. braziliensis.


METHODS
The in vitro activity of compounds 1-9 was assayed on extracellular promastigote and axenic amastigote forms and on intracellular amastigote forms of the parasites. Infectivity and cytotoxicity tests were carried on J774.2 macrophage cells using Glucantime as the reference drug. The mechanisms of action were analysed performing metabolite excretion and transmission electronic microscope ultrastructural alteration studies.


RESULTS
Nine flavonoids showed leishmanicidal activity against promastigote as well as amastigote forms of Leishmania infantum and L. braziliensis. These compounds were nontoxic to mammalian cells and were effective at similar concentrations up to or lower than that of the reference drug (Glucantime). The results showed that 2(″)-acetylpetiolaroside (compound 8) was clearly the most active.


CONCLUSIONS
This study has demonstrated that flavonoid derivatives are active against L. infantum and L. braziliensis.
Department of Parasitology, University of Granada, Severo Ochoa s/n, 18071 Granada, Spain.
Inmaculada
I
Ramírez-Macías
Clotilde
C
Marín
Jesús G
JG
Díaz
María José
MJ
Rosales
Ramón
R
Gutiérrez-Sánchez
Manuel
M
Sánchez-Moreno
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D002460:Cell Line; D031882:Delphinium / Q000737:chemistry*; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D007892:Leishmania braziliensis / Q000187:drug effects* / Q000648:ultrastructure; D018314:Leishmania infantum / Q000187:drug effects* / Q000648:ultrastructure; D051379:Mice; D046529:Microscopy, Electron, Transmission
D000981:Antiprotozoal Agents; D005419:Flavonoids