Novel Radiation Protection and Treatment Compounds

University of Arkansas for Medical Sciences
posted on 03/25/2011

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New tocopherol and tocotrienol compositions with enhanced transport properties and uses in nutrition and radiation protection.

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

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 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 frequently recommended supplement, and is taken by consumers for its antioxidant properties and its impact on the regulation of blood sugar. Additionally, its dermatological benefits as an anti-aging additive have been documented and it has therefore also seen use in the cosmetics industry. Further, recent studies show that tocotrienol and tocopherol compounds offer considerably effective functionality as radioprotectors against lethal doses of radiation in animal studies.

University researchers have disclosed a novel synthesis of unique tocopherol and tocotrienol derivatives and the mechanisms responsible for increasing the bio delivery and availablility of these compounds. These new compounds appear to be much more potent agents than known tocopherol derivatives — including gamma and delta-tocotrienols that have documented anti-oxidant applications in cardiovascular disease and are used as radioprotectors in conjunction with both radiological disaster 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 compositions of the naturally occurring tocopherols and tocotrienols which contain uniquely positioned desaturations on the phytyl tail.

The unique tocol compositions 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.

Thorough searching of patents, applications and scientific papers related to the tocols has not revealed any evidence that the compounds included in this discovery have previously been prepared or discovered in nature. As such, these compounds are correctly considered to be novel.

The availability of compounds that potentially have the ability to increase the bioactivity of the tocotrienols, show improved bioavailability over the tocopherols, and also offer considerable radiation protection should be of great interest to the pharmaceutical industry and public safety officials.

Although successful animal testing has already taken lace, additional research is currently ongoing to obtain additional in vivo data in animal models to better illustrate each of the different potential uses for these unique derivatives.

Patent Pending

Available for Exclusive Licensing

10-01 COMPADRE, et al