MCW and French Researchers are Inventors of US Patent Mito-MGN Compounds to Treat Cancer

Collaborators in the Department of Biophysics – Balaraman Kalyanaraman, PhD, Harry R. & Angeline E. Quadracci Professor in Parkinson’s Research; Jacek Zielonka, PhD, DSc, assistant professor; and Gang Cheng, PhD, assistant professor – as well as Micael Hardy, PhD, and Olivier Ouari, PhD, of Aix-Marseille Université, France, are inventors on MCW’s recently awarded US Patent 11,612,610 B2 for Mito-Magnolol Compounds and Methods of Synthesis and Use Thereof.

This patent, which pertains to methods of using mitochondria-targeted magnolol (Mito-MGN) compounds to treat cancer, particularly anti-cancer therapy or kinase-resistant cancers (Cheng GC et al. Cancer Treat Res Commun. 2020;25:100210), is a continuation of a previously issued US patent for Mito-MGN. It covers additional analogs of Mito-MGN not covered by the previous patent.

The new compounds include Mito-MGN analogs containing methoxy, trifluoromethyl, chloride ion, methyl, acetoxy, and trimethylammonium cation substituents. These substituents are also included in the pegylated Mito-MGN (Mito-PEG-MGN). These substituents could influence the selectivity and potency of Mito-MGN analogs in cancer therapy.

Mito-MGN is a synthetic compound developed by adding a mitochondria-targeting molecule, triphenylphosphonium, to the naturally occurring polyphenol. Magnolol is the most abundant bioactive component of magnolia extract, a traditional herbal formula used effectively for centuries in East Asia to treat multiple inflammatory diseases. One advantage of magnolol is its ability to be modified into a single monosubstituted isomer that is easily separated and purified, enabling synthesis of large quantities of Mito-MGN. The novel Mito-MGN compounds are selective inhibitors of oxidative phosphorylation in tumor cells, and they induce apoptosis and inhibit melanoma cell proliferation.

Thanks to the Office of Technology Development at MCW for facilitating the effort that led to this patent.