Wisconsin Alumni Research Foundation

Materials & Chemicals
Materials Chemicals
Synthesizing Natural Products to Treat High Blood Cholesterol
WARF: P150023US03

Inventors: Weiping Tang, Dongxu Shu, Gabrielle Winston-McPherson, Xiaoxun Li

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing indole compounds to treat health problems associated with high blood cholesterol.
Indole is one of the most abundant heterocycles in pharmaceuticals and bioactive natural products, such as indometacin, a non-steroid anti-inflammatory drug, and vincristine, a natural product used to treat a number of types of cancers. Given the importance of indoles, much effort has been devoted to preparing them from a variety of starting materials. However, inefficiency, low selectivity and low yield remain a problem for polysubstituted indoles or when the indole is in a complex polycyclic system.
The Invention
UW–Madison researchers have developed an efficient method to synthesize indole compounds, specifically polysubstituted dimeric indoles. These compounds have potential health benefits because they are able to reduce the amount of PCSK9 in cells. PCSK9 is an enzyme known to play a major role in controlling the concentration of LDL cholesterol in the bloodstream.

Some of the compounds have been tested in vitro for their ability to increase the secretion of a potent blood sugar hormone in the body called glucagon-like peptide 1 (GLP-1). Others have the ability to selectively inhibit the secretion of interleukin-17 (IL-17), which is essential in many autoimmune diseases including arthritis, multiple sclerosis, psoriasis and inflammatory bowel disease.

The synthesis process involves a cascade reaction with transition metal catalysts. The resulting compounds can be further functionalized to yield more substituted indoles.
  • Synthesizing indole compounds to treat ailments in mammals connected to GLP-1, PCSK9 and/or IL-17
Key Benefits
  • More efficient than other methods
  • Potential health implications are significant – from treating hyperglycemia to high cholesterol and autoimmune diseases.
Stage of Development
The development of this technology was supported by WARF Accelerator. WARF Accelerator selects WARF's most commercially promising technologies and provides expert assistance and funding to enable achievement of commercially significant milestones. WARF believes that these technologies are especially attractive opportunities for licensing.
Additional Information
For More Information About the Inventors
Related Intellectual Property
For current licensing status, please contact Rafael Diaz at [javascript protected email address] or 608-960-9847