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Cytotoxic and proapoptotic activity of ent-16beta-17alpha-dihydroxykaurane on human mammary carcinoma cell line MCF-7.

Morales A, Pérez P, Mendoza R, Compagnone R, Suarez AI, Arvelo F, Ramírez JL, Galindo-Castro I

Centro de Biotecnología, Fundación IDEA, Carretera Hoyo de La Puerta-Baruta, Valle de Sartenejas, Baruta, Caracas, Venezuela.

Here we describe the cytotoxic and proapoptotic effect of an ent-kaurane (ent-16beta-17alpha-dihydroxykaurane), compound isolated from Croton malambo barks, on malignant cell growth. When MCF-7 mammary carcinoma cells were treated with increasing concentrations of the ent-kauranoid, its cytotoxic activity showed an IC50 of 12.5microg/ml, dose that is 2.66-fold lower than the corresponding value for non-malignant cells. At this growth inhibitory dose, both mRNA and protein levels for Bcl-2 as well as mRNA for hTERT were significantly reduced. The observed preapoptotic activity seemed to be triggered by a mechanism that is not directly affecting NF-(kappa)B binding ability. The potential use of this plant-derived compound as a cancer chemotherapy agent is discussed.

Published 10 January 2005 in Cancer Lett, 218(1): 109-16.
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