INTEQUI   20941
INSTITUTO DE INVESTIGACIONES EN TECNOLOGIA QUIMICA
Unidad Ejecutora - UE
artículos
Título:
NATURAL SESQUITERPENE LACTONES ARE ACTIVE AGAINST LEISHMANIA MEXICANA
Autor/es:
PATRICIA A. BARRERA; VERO NICA JIMENEZ-ORTIZ; CARLOS TONN; OSCAR GIORDANO; NORBEL GALANTI; MIGUEL A. SOSA
Revista:
JOURNAL OF PARASITOLOGY
Referencias:
Año: 2008 vol. 95 p. 87 - 93
ISSN:
0022-3395
Resumen:
In this paper, the effects of 3 natural sesquiterpene lactones, i.e., helenalin (Hln), mexicanin (Mxc), and dehydroleucodine
(DhL), were evaluated using cultured Leishmania mexicana promastigotes. It was observed that the compounds inhibited
the in vitro growth of the parasites at relatively low concentrations. The effect was rapid and irreversible with an estimated IC50
the in vitro growth of the parasites at relatively low concentrations. The effect was rapid and irreversible with an estimated IC50
the in vitro growth of the parasites at relatively low concentrations. The effect was rapid and irreversible with an estimated IC50
the in vitro growth of the parasites at relatively low concentrations. The effect was rapid and irreversible with an estimated IC50
the in vitro growth of the parasites at relatively low concentrations. The effect was rapid and irreversible with an estimated IC50
the in vitro growth of the parasites at relatively low concentrations. The effect was rapid and irreversible with an estimated IC50
Leishmania mexicana promastigotes. It was observed that the compounds inhibited
the in vitro growth of the parasites at relatively low concentrations. The effect was rapid and irreversible with an estimated IC5050
of 24 M, while all the lactones were more effective than ketoconazole. Moreover, these compounds exhibited low cytotoxicity
for mammalian cells. Hln induced strong vacuolization of the parasite cytoplasm, although pericellular microtubules were preserved.
The 3 lactones induced DNA fragmentation as judged by the high labeling with the fluorescent TUNEL method, which
was confirmed by electrophoresis on agarose gels. The ability of the parasites to invade Vero cells was also decreased by exposure
to low concentrations of the compounds. We conclude that these compounds can affect the parasites life cycle, possibly through
multiple mechanisms. Identification of the molecular targets of these natural products and their effects on amastigotes should be
determined to evaluate the possible therapeutic use of the compounds against leishmaniasis.