OLEUROPEIN AGLYCONE INHIBITS THE GROWTH OF BREAST CANCER
Extra-virgin olive oil polyphenols inhibit HER2 (erbB-2)-induced malignant transformation in human breast epithelial cells: Relationship between the chemical structures of extravirgin olive oil secoiridoids and lignans and their inhibitory activities on the tyrosine kinase activity of HER260
Menendez et al in their study explored the ability of oleuropein aglycone to modulate HER2 tyrosine kinase receptor-induced in vitro transformed phenotype in human breast epithelial cells. Using MCF10A normal breast epithelial cells it was further determined the relationship between chemical structure of oleuropein aglycone and its inhibitory activities on the tyrosine kinase activity of the HER2 oncoprotein. When compared with untreated cells, MCF10A/HER2 cells, treated with oleuropein aglycone, grew less dense, were significantly bigger in volume and showed a profound
reorganization of cell-cell contacts with the appearance of multiple extrusions. Oleuropein aglycone was one of the most active inhibitors of HER2 expression in MCF10A/HER2 cells, with a reduction 63%, and IC50 64μΜ. HER2 overexpression further promoted an exacerbated sensitivity to the apoptotic effects of oleuropein aglycone.
Oleuropein aglycone inhibits the growth of breast cancer as it causes a decrease in the number of HER2 tyrosine kinase receptors, which is present in large percentages in breast cancer cells and leads in their uncontrolled proliferation.
Fig– Effects of a 15-min preincubation with 3,4 DHPEAEA, 3,4 DHPEA-EDA or hydroxytyrosol (1, 30 and 100 M) on the increases in fluo-4 fluorescence (indicative of [Ca2+ ]c increases) induced by the administration of AVP (control; CT) in A7r5 vascular myocytes84