Published on Brock University (http://www.brocku.ca)
Project No. 2002
Principal Investigator/Inventor: Dr. Jeffrey Atkinson, Department of Chemistry
Novel tocopherol derivatives and their use to inhibit the rapid oxidative metabolism of vitamin E
The potentially benefits of of vitamin E components are well established and include anti-inflammatory properties, inhibition of cholesterol biosynthesis, anti-cancer effects and protection against neurodegeneration. Vitamin E is comprised of 8 different compounds found in nature: 4 tocopherols and 4 tocotrienols. Our diet mostly consists of γ-tocopherol, however this compound is quickly metabolized in the body. Dr. Atkinson and his group have synthesized novel chemical compounds that can inhibit the rapid oxidative metabolism of these vitamin E compounds and thereby elevate the circulating levels in the body. These agents allow the increased in vivo half lives of tocopherols and tocotrienols and thus may have applications for treatment of hypercholesterolaemia, diabetes, and neurodegenerative diseases. Currently, there are no known agents used to inhibit tocopherol metabolism. Furthermore, the compounds demonstrated to cause this inhibition do not exist in the chemical literature. The lead compound has been tested in various human cell culture models and has been shown to completely inhibit metabolism of the derivatives in question. Studies are ongoing to evaluate toxicity and efficacy in animal models.
Atkinson, J. et al., “Tocopherol derivatives and uses thereof.” US patent 7,732,617, issued June 8, 2010
References and Publications
Ohnmacht, S. et al., (2008). Inhibition of oxidative metabolism of tocopherols with omega-N-heterocyclic derivatives of vitamin E. Bioorg. Med. Chem. 16: 7631-8.