New tocopherol and tocotrienol analogues with enhanced transport properties and uses in therapy and nutrition.

Applications: Greatly enhanced anti oxidation properties for pharmaceutical uses including radiation cancer treatments, cardio- and neuro-protection.

Tocotrienols and tocopherols are fat-soluble antioxidants (each with four forms – alpha-, beta-, gamma-, and delta-) that together make up the vitamin E family. They share an identical structure except that tocotrienols have multiple double bonds added to their side chains. The compounds in this invention represent new composition of matter relatives of tocopherols that have not previously been chemically synthesized or extracted from natural sources. In the multivitamin industry, Vitamin E as alpha tocopherol is the most recommended supplement consumed by consumers daily for its antioxidant and its impact on the regulation of blood sugar. Additionally, its dermatological benefits as an anti-aging additive have been documented and used in the cosmetics industry.

University researchers have disclosed the novel synthesis of unique tocopherol and tocotrienol derivatives and the mechanisms responsible for the increasing the bio delivery and availability of these compounds. These new compounds appear to be much more potent agents than current tocopherol derivatives including gamma and delta-tocotrienols that have documented anti-oxidant applications in cardiovascular disease and as unique agents as radioprotectors for use in conjunction with both radiological events and medical procedures involving radiation.

Of the eight naturally occurring tocols, four are tocopherols (which possess a saturated phytyl tail) while four others are tocotrienols (which possess three trans double bonds in the phytyl tail). The present invention relates to the previously unknown derivatives of the naturally occurring tocopherols and tocotrienols which contain uniquely positioned unsaturations on the phytyl tail.

The unique tocol derivatives described in this invention have preferred binding to the membrane and tocopherol transport protein than the current tocopherols and tocotrienols and are likely to be more bioactive than the totally unsaturated tocopherols.

In the literally thousands of patents, applications and scientific papers related to the tocols, a detailed search of the Chemical Abstracts has not revealed that the compounds included in this discovery have not been prepared or discovered in nature.

The availability of compounds that potentially have the ability to both increase the bioactivity of the tocotrienols and with improved bioavailability over the tocopherols should be very appealing to the pharmaceutical industry.

Currently, research is ongoing to obtain additional in vivo data in animal models that illustrates each of the different potential uses for these unique derivatives.

Patent Pending and Available for Exclusive Licensing

10-01 COMPADRE, et al

none noted by the inventors

File Number: 10-01 

Web site: http://www.uams.edu/bioventures

Disease: Metabolic/Endocrinology