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Which activities have been demonstrated for HT?

Several epidemiological studies in Mediterranean countries strongly support the relationship between the Mediterranean diet and low incidence of coronary heart disease as well as certain cancers particularly of the digestive and respiratory tract and breast cancer. Usual components of the Mediterranean diet are vegetables, fruits, legumes, grains and olive oil as a main source of fat. Natural antioxidants present in food are able to control and what is more important, to scavenge free radicals, thus preventing their harming effects.

Biological benefits of olive oil consumption are linked to the presence in high amounts of hydroxytyrosol and its precursor oleuropein in unrefined olive oil. The main activity of HT is based on its antioxidative therapeutic properties listed below, to which it has to be added the proposal of it as an adequate additive for stabilizing foodstuff rich in functional ω-3 polyunsaturated fatty acids. Last but not least, no toxicity due to hydroxytyrosol has been observed in the published scientific data available even at great concentrations in vitro and in vivo.

The quality of Seprox´s hydroxytyrosol produced by chemical and enzymatic synthesis with analytical purity (>99%), without the contaminants and the color of other sources, can dramatically push forward the development of new commercial usages of this compound in the following fields:

1. Decrease of Cardiovascular and Heart Disease Risk:
HT prevents oxidation of low-density lipoprotein (LDL). It acts as a potent inhibitor of metal-induced oxidation of low density lipoprotein, as well as metal-independent oxidation Since oxidized LDL plays a key role in developing atherosclerosis and related pathologies like Coronary Heart Disease and stroke. Therefore, HT is a useful agent for lowering risk of disease development.

2. Cancer prevention:
There are two ways by which HT could be beneficial in protecting cells from oncogenic transformation. The first is by protecting DNA from damage by free radicals (Reactive Oxygen Species, ROS). The second is due to the demonstrated antiproliferative effect in vitro through apoptosis induction.

3. C. N. S. (Central Nervous System):
Hydroxytyrosol: from laboratory investigations to future clinical trials.
Sergio Granados-Principal, José L Quiles, Cesar L Ramirez-Tortosa, Pedro Sanchez-Rovira, and M Carmen Ramirez-Tortosa

4. Antiinflammatory activity:
In in vitro cell models, it has been described that HT blocks the generation of free radicals thus opening new possibilities for using HT as a potential anti-inflammatory agent with natural origin.

5. Skin protection and antiaging:
Based on its antioxidant activity, HT has been shown in in vitro cell assays to effectively protect skin cells from long-wave ultraviolet radiation UVB by scavenging the generated free radicals in a dose-dependent way. Further, and based on the free-radical hypothesis of ageing that has been shown to contribute to the physiological changes during ageing, HT could play an important role in slowing the process, thus blocking the external consequences of the natural process. Both lipophylic and hydrophylic properties of HT makes it an excellent natural antioxidant for cosmetic use.

Beyond the activities of HT based on its antioxidant properties, more recently its demonstrated microbicide activity has been suggested in specialized literature to open new possibilities in its use.

6. Hydroxytyrosol in the prevention of HIV infection:
Hydroxytyrosol has been described to inhibit in a dose-dependent manner HIV proliferation by blocking the enzyme integrase, which plays a crucial role during the infection cycle of the HIV virus at the virus integration step into the lymphocyte DNA. Since the dihydroxyphenol ring binds to two different regions from integrase, HT is supposed to maintain the ability to bind to integrase active site even if mutations occur. Thus, importantly, the likelihood of resistance development will be less than inhibitors that bind to a single site.

7. Hydroxytyrosol as an antiviral agent of broad spectrum:
The reported activity against HIV by blocking integrase is also relevant as an antiviral agent not only against viruses that proliferate with a similar mechanism of action but also against enveloped viruses as has been very recently described with different influenza and rotavirus strains.