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Article Index

 

LINGSTROSDEAGLYCONE

 

1. Olive secoiridoids and semisynthetic bioisostere analogues for the control of metastatic breast cancer.

In the study of Busnena et al., ligstroside aglycone showed the best antimigratory activity against the highly metastatic human breast cancer cell line MDAMB231. Generally, tyrosol esters showed better activities versus carbamate analogues. Tyrosol esters with a phenolic acid containing hydrogen bond donor and/or acceptor groups at the para-position have better anticancer and c-MET protein inhibitory activities. Olive oil secoiridoids, like ligstroside aglycon, are excellent scaffolds for the design of novel c-MET inhibitors.

Busnena BA, Bioorg Med Chem. 2013


SUMMURY

Ligstroside aglyconeagainst metastatic breast cancer

In the study of Busnena et al., ligstroside aglycone showed the best antimigratory activity in experiments performed in highly metastatic human breast cancer cells. Due to its particular chemical structure, it inhibits the activity of a specific protein, the c-MET protein, associated with the development of malignant tumor.


Ligstroside aglycone showed the best antimigratory activity against the highly metastatic human breast cancercells.

 

2. 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 ligstrocide 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 aglycone 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 aglycone 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.


SUMMURY

The effect of Ligstrocide aglyconeon breast cancer
Menendez et al. in their study explored the ability of ligstrocide aglycone to modulate HER2 tyrosine kinase receptor-induced, which is present in large amounts in breast cancer cells and causes their uncontrolled proliferation. Ligstrocide aglycone was one of the most active inhibitors of HER2 expression in cells, with a reduction 63%, even in very small doses and eventually the cancer cells were led to programmed cell death. These findings provide an excellent and safe platform for the design of new anti-breast cancer drugs

Ligstrocideaglycone inhibits the growth of breast cancer. It causesa reduction in the number of HER2 tyrosine kinase receptors, which are presented in large amountsin breast cancercellsand lead to their uncontrolledproliferation.

 

 

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