X-ray Crystallography Detects Cancer Fighting Compound in Pepper

Highlights

• Long pepper has medicinal properties including the ability to fight cancer.
• Piperlongumine, the chemical in pepper acts against prostate, breast, lung, colon, lymphoma, leukemia, primary brain tumors and gastric cancer.
• PL converts to hPL, an active drug that silences a gene which produces an enzyme found in tumors.

The chemical process behind anti-cancer properties of a spicy Indian pepper plant called the long pepper, has been uncovered by the UT Southwestern Medical Center scientists. The secret lies in a chemical called Piperlongumine (PL), which has shown activity against many cancers including prostate, breast, lung, colon, lymphoma, leukemia, primary brain tumors and gastric cancer.

Using x-ray crystallography, researchers were able to create molecular structures that show how the chemical is transformed after being ingested. PL converts to hPL, an active drug that silences a gene called GSTP1. The GSTP1 gene produces a detoxification enzyme that is often overly abundant in tumors.

Dr. Westover, a member of the Harold C. Simmons Comprehensive Cancer Center, used cutting edge technologies in UT Southwestern's Structural Biology Core (SBC) - the University's world-renowned facility for X-ray crystallography, to better understand the anticancer properties of PL.

X-ray crystallography allows scientists to determine molecular structures that reveal how molecules interact with targets - in this case how PL interacts with GSTP1. Viewing the structures helps in developing drugs for those targets.

"We are hopeful that our structure will enable additional drug development efforts to improve the potency of PL for use in a wide range of cancer therapies," said Dr. Kenneth Westover, Assistant Professor of Biochemistry and Radiation Oncology. "This research is a spectacular demonstration of the power of x-ray crystallography."

The long pepper, a plant native to India, is found in southern India and southeast Asia. It dates back thousands of years in the Indian subcontinent tied to Ayurveda.

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"This study illustrates the importance of examining and re-examining our theories. In this case we learned something fundamentally new about a 3,000-year-old medical claim using modern science," said Dr. Westover.

Reference

1. Dr. Kenneth Westover et al., Researchers uncover mechanism for cancer-killing properties of pepper plant, Journal of Biological Chemistry (2016).

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Source-Medindia