A Method to Treat Alzheimer’s, Heart and Liver Diseases

Case ID:
OSU-15-64
Web Published:
3/28/2017
Description:

 

Technology Description

 

This technology describes a process for the preparation of the tripeptide glutathione or its precursors to be delivered to the mitochondria for treating age-related conditions, toxicologic exposures, neurodegeneration, heart disease, and liver damage. More specifically, glutathione precursors and derivatives are coupled to a lipophilic cation, triphenylphosphonium, to target these compounds to mitochondria.

 

Features & Benefits

 

  • Glutathione and its analogs are coupled to a triphenylphosphonium molecule via a cleavable linker. Once inside mitochondria the linker is cleaved to release glutathione or its analogs.

 

Applications

 

  • Delivery of fully functional glutathione and its analogs into mitochondria to treat neurodegeneration, heart and liver diseases

 

Background of Invention

 

Mitochondrial glutathione is independently regulated from the cytoplasmic pool and has major effects upon preserving mitochondrial function in many diseases and after toxicant exposures. No one has successfully developed a means to increase glutathione in mitochondria. However, it is known that chemical coupling the positively charged triphenylphosphonium moiety to hydrophobic molecules can drive hydrophobic compound into mitochondria due to the organelle’s negative charge from the chemi-osmotic potential. Other triphenylphosphonium derivatives of hydrophobic antioxidants (“MitoQ”, or triphenylphosphonium -vitamin E) have been synthesized and are known to therapeutically efficacious. However, these compounds only augment mitochondrial antioxidant status in the lipid bilayer. These compounds furthermore cannot replace the loss of glutathione, which has a myriad of functions in mitochondria outside of being an antioxidant. Despite its obvious benefits, triphenylphosphonium - glutathione has not been successfully synthesized before because of several major challenges.

 

Status

 

Patent pending and availability for licensing

 

Patent Information:
For Information, Contact:
Chris Stoner
Director
Oregon State University
541-737-8329
Chris.Stoner@oregonstate.edu
Inventors:
Tory Hagen
Joseph Beckman
Pamela Beilby
Keywords:
ALS
Alzheimer's
Antioxidant
Cancer
Liver disease
Medical Science & Technologies
Mitochondria
Neurodegenerative disease
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