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Biophysics Researchers Publish Study on Modified Polyphenols for Use in Cancer and Immune Therapies

First author Gang Cheng, PhD, assistant professor of biophysics; corresponding author, Balaraman Kalyanaraman, PhD, professor of biophysics and the Harry R. & Angeline E. Quadracci Professor in Parkinson’s Research; and international collaborating authors, Micael Hardy, PhD, and Hakim Karoui, PhD, of Aix-Marseille Université, France, published an article in Cancers, which discusses the selective modification of several plant-based compounds that inhibit tumor growth in order to increase their potency.

As detailed in the article, titled “Polyphenolic Boronates Inhibit Tumor Cell Proliferation: Potential Mitigators of Oxidants in the Tumor Microenvironment,” the goal was to develop less toxic, more potent natural compounds for use in cancer and immune therapies. To this end, the authors modified the structures of honokiol and magnolol, the two active components of magnolia extract.

The modified compounds—honokiol boronate and mitochondria-targeted honokiol boronate—target the mitochondria of tumor cells and inhibit cell proliferation. These boronate derivatives also react with oxidants that are potentially generated in tumor mitochondria and the tumor microenvironment. During this process, these boronate derivatives are also converted back to the original compounds with antitumor potencies. Thus, the boronation of naturally occurring plant-derived compounds could make them more active in tumor cells as well as in the adjoining tumor microenvironment.

These novel polyphenolic derivatives may enhance the scope of cancer immunotherapies.