Cytotoxic and proapoptotic activity of ent-16beta-17alpha-dihydroxykaurane on human mammary carcinoma cell line MCF-7.
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.
Morales
Alvaro
A
Centro de Biotecnología, Fundación IDEA, Carretera Hoyo de La Puerta-Baruta, Valle de Sartenejas, Baruta, Caracas, Venezuela.
Pérez
Pedro
P
Mendoza
Raifish
R
Compagnone
Reinaldo
R
Suarez
Alírica I
AI
Arvelo
Francisco
F
Ramírez
José Luis
JL
Galindo-Castro
Iván
I
D017209:Apoptosis / Q000187:drug effects*; D001943:Breast Neoplasms / Q000473:pathology*; D049109:Cell Proliferation; D045786:Diterpenes, Kaurane / Q000494:pharmacology*; D006801:Humans; D016328:NF-kappa B / Q000378:metabolism; D019098:Telomerase / Q000494:pharmacology
D045786:Diterpenes, Kaurane; D016328:NF-kappa B; C460239:ent-17,19-dihydroxy-16-H-kaurane; D019098:Telomerase