Curcumin Conjugates and Methods of Use Thereof

Description:

The current state of the art

Breast cancer is the second most common cancer in women with an estimated 268,600 cases in 2019 and 41,760 deaths in the US. Curcumin, a phenolic compound and the major ingredient in the spice, turmeric, has anti-inflammatory and pro-apoptotic activities against many solid tumors.  

The problems with the current art

Curcumin is one of the well-studied molecules for anticancer properties; however, it has poor bioavailability when given orally and poor tissue penetrance when infused. Dichloroacetate (DCA) is an anticancer drug and inhibits PDK1 at micromolar concentration. But much higher doses (~100 times more) are needed for anticancer efficacy. Such high doses are frequently associated with neuropathy and other adverse side effects, which limits its therapeutic usefulness in cancer patients.

The advantages of our invention

The scientists at AU utilized use various amino acids to link curcumin and DCA to synthesize hybrid conjugates. Among six curcumin-modified compounds (CMCs). CMC 1 and CMC 2 showed the most promising anticancer property against breast cancer cell lines (MB231 and T47D) and animal models. The conjugates inhibit human breast cancer cell growth at nanomolar concentration. In a genetically engineered mouse model of breast cancer, CMC2 is safe and inhibits tumor cell proliferation and tumor growth. The computational studies showed that CM2 has the highest docking score, binding energy as well as ligand efficiency toward dual-specificity tyrosine-regulated kinase 2 (DYRK2). Therefore, curcumin conjugates have great potential as a new treatment for breast cancer.

AURI-2020-042

Lead Inventor: Siva Panda, PhD https://www.augusta.edu/scimath/chemistryandphysics/siva-panda.php

IP status: US Provisional 63/113,586 (Filing date 11/03/2020)

Reference: to be published

Patent Information:
Category(s):
Therapeutics
For Information, Contact:
Carl Clark
Director Technology Transfer
Augusta University
caclark@augusta.edu
Inventors:
Siva Panda
Muthusamy Thangaraju
Balakrishna Lokeshwar
Keywords:
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