LIGSTROSIDE AGLYCONE INHIBITS THE GROWTH OF BREAST CANCER
tabAnti-HER2 (erbB-2) oncogene effects of phenolic compounds directly isolated from commercial Extra-Virgin Olive Oil (EVOO)
Menendez et al in their study explored the ability of ligstroside 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 ligstrocide aglycon and its inhibitory activities on the tyrosine kinase activity of the HER2 oncoprotein. When compared with untreated cells, MCF10A/HER2 cells, treated with ligstroside aglycone, grew less dense, were significantly bigger in volume and showed a profound reorganization of cell-cell contacts with the appearance of multiple extrusions.
Ligstroside aglycone was one of the most active inhibitors of HER2 expression in MCF10A/HER2 cells, with a reduction 68%, and IC50 10μΜ. HER2 overexpression further promoted an exacerbated sensitivity to the apoptotic effects of ligstroside aglycone. These findings molecularly support epidemiological evidence revealing that lingstrocide aglycon anti-breast cancer effects primarily affect the occurrence of breast tumors overexpressing the type I receptor tyrosine kinase HER2 but further suggest that its stereochemistry might provide an excellent and safe platform for the design of new HER2 targeted anti-breast cancer drugs.
Ligstroside aglycone inhibits the growth of breast cancer as well causes a decrease in the number of HER2 tyrosine kinase receptors, which is present in large percentages in breast cancer cells and leads to their uncontrolled proliferation.
Fig. Effects of the EVOO polyphenols on the transforming ability of HER2.