Antiproliferative, cytotoxic and hemolytic activities of a triterpene glycoside from Psolus patagonicus and its desulfated analog

CAREAGA, V.P.; BUENO, C.A.; MUNIAIN, C.; ALCHÉ, L.E.; MAIER, M.S.

CHEMOTHERAPY

KARGER

Año: 2008 vol. 55 p. 60 - 68

0009-3157

Abstract Background: The major triterpene glycoside of the sea cucumber Psolus patagonicus and its desulfated analog were tested for their antiproliferative, cytotoxic and hemolytic activities, and their effect on NF-kB activation. Methods: antiproliferative action of glycosides 1 and 2 were determined on three tumor cell lines; their effect on the activation of NF-kB was evaluated by an indirect immunofluorescence assay staining and the concomitant IkB degradation was studied by western blot. Results: Both compounds were able to suppress the growth of the three tumor cell lines and induced the activation of NF-kB, a key player linking between chronic inflammation and cancer, concomitant with IkB degradation. Compound 1 showed hemolytic activity with an EC50 of 82 mM. Conclusions: Glycosides 1 and 2 exert an antiproliferative effect that might be related to their membranolytic activity. The triggering of NF-kB may be an indirect consequence of the hemolytic activity of these compounds.