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Article Index

 

 

OLEUROPEINAGLYCONE

1. The Polyphenol Oleuropein Aglycone Protects TgCRND8 Mice against Aß Plaque Pathology

In their research, Grossi et al. used the double transgenic TgCRND8 mice, which overexpressing the Swedish and Indiana mutations in the human amyloid precursor protein, to examine in vivo the effects of 8 weeks dietary supplementation of oleuropein aglycone at the dose of 50 mg/kg. The dietary supplementation of oleuropein aglycone strongly improves the cognitive performance of young/ middleaged TgCRND8 mice. Immunofluorescence analysis of cerebral tissue in these mice showed remarkably reduced ß-amyloid levels and plaque deposits. Moreover, microglia migration to the plaques for phagocytosis and a remarkable reduction of the astrocyte reaction were evident. Finally, oleuropein aglycone-fed mice brain displayed an astonishingly intense autophagic reaction, as shown by the increase of autophagic markers expression and of lysosomal activity. Data obtained with cultured cells confirmed the latter evidence, suggesting mTOR regulation by oleuropein aglycone. These results support, and provide mechanistic insights into, the beneficial effects against Alzheimer-associated neurodegeneration of oleuropein aglycone.


SUMMURY

Experiments in mice show the beneficial effect of oleuropein aglyconon the progression of Alzheimer's disease

In their research, Grossi et al. used special mice, which produce a special mutant human protein, which is associated with Alzheimer's disease. The dietary supplementation of oleuropein aglycone for 8 weeks at the dose of 50 mg/kg showed a remarkable improvement of the cognitive performance of mice. The effect of oleuropein aglycone on the stabilization of disease progression was also examined by biochemical analysis of mouse brains, showing significant results. These results support the beneficial role of oleuropein aglycone against Alzheimer's disease.

The dietary supplementation of oleuropein aglycone strongly improves the cognitive performance of young/ middle-aged mice, fact that indicates the beneficial effect of oleuropein aglyconeon the progressionof Alzheimer's Disease.

 

2. Oleuropein aglyconeprevents cytotoxic amyloid aggregation of human amylin

Here, Rigacci S. et al. investigated the effects on amylin aggregation and cytotoxicity of the oleuropein aglycon. It was showed that oleuropein, when present during the aggregation of amylin, consistently prevented its cytotoxicity to RIN-5F pancreatic β- cells, as determined by the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide test and caspase-3 activity assay. A lack of interaction with the cell membrane of amylin aggregates grown in the presence of oleuropein was shown by fluorescence microscopy and synthetic lipid vesicle permeabilization. Moreover, the ThT assay, circular dichroism analysis and electron microscopy images suggested that oleuropein interferes with amylin aggregation, resulting in a different path skipping the formation of toxic prefibrillar aggregates. These results provide a molecular basis for some of the benefits potentially coming from extra virgin olive oil consumption and pave the way to further studies on the possible pharmacological use of oleuropein to prevent or to slow down the progression of type II diabetes.


SUMMURY

The beneficial effect of Oleuropein aglyconeagainst type II diabetes

Here, Rigacci S. et al. investigated the effects on amylin aggregation and cytotoxicity of the oleuropein aglycon. Amylin is a substance that is quite similar to insulin. When amylin aggregates in pagreatic cells, it generates amyloid, which is directly related to the pathogenesis of type II diabetes. Specifically, oleuropein aglycone inhibits the aggregation of amylin and its toxicity action on pagreatic cells. These results provide a molecular basis for some of the benefits potentially coming from extra virgin olive oil consumption and pave the way to further studies on the possible pharmacological use of oleuropein to prevent or to slow down the progression of type II diabetes

Oleuropein aglycone inhibits or slowsdown the progressionof type II diabetes, by inhibiting the aggregation and toxicity of amylin in pancreatic cells, a substance that isdirectly related to the pathogenicity of the disease

 

3. 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 HER2

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. These findings molecularly support epidemiological evidence revealing that oleuropein 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.


SUMMURY

The effect of oleuropein aglyconeon breast cancer
Menendez et al. in their study explored the ability of oleuropein aglycone to modulate HER2 tyrosine kinase receptor-induced, which is present in large amounts in breast cancer cells and causes their uncontrolled proliferation. Oleuropein 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.

Oleuropein aglycone 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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