Para-Amino Substituent on the D Ring of Green Tea Polyphenol Epigallocatechin-3-Gallate as Novel Proteasome Inhibitor and Cancer Apoptosis Inducer

This technology is a group of (-)EGCG analogs with stable and improved anti-tumor activities.

Background & Unmet Need:

Catechins are a type of plant-derived antioxidant whose biological activities may play an effect on cancer prevention.  Green tea has long been lauded to have ingredients that protect cells from the DNA damage that causes cancer.  The most abundant and active catechin found in green tea is (‑)‑epigallocatechin-3-gallate (EGCG).  However, EGCG is unstable under neutral and alkaline conditions and in vivo. 

Technology Description:

In an attempt to increase stability and thus efficacy of EGCG, WSU researchers have synthesized compounds and found that they were novel proteasome inhibitors and cancer apoptosis inducers.  High proteasome activity is essential for the growth and spread of tumors.  By suppressing proteasome activity with these newly synthesized compounds, this technology has the potential to be effective anti‑cancer agents.

Commercial Applications:

• Powerful chemotherapeutic and chemo- preventive agents
• Novel proteasome inhibitors and cancer apoptosis inducers

Stage of Development:

Preclinical

Competitive Advantages:

• Compound is more stable
• Compound more active in killing tumor cells
• Compound is less polar
• Compound is more easily absorbed through cell membrane

Intellectual Property Status:

Patent Pending