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Diabetes; inflammation

Peroxisome proliferation-activated receptor-g (PPARG; PPARg)

Cell culture studies identified oxygenated polyketide-based PPARg activators from the Plakinastrella mamillaris sponge that could help treat diabetes and inflammatory diseases. In vitro, the three lead polyketides selectively activated PPARg with EC50 values of 2-9 mM. In a human monocytic cell line, the lead PPARg activator gracilioether C inhibited lipopolysaccharide (LPS)-induced production of two proinflammatory cytokines. Next steps include testing the lead PPARg activators in an animal model.
At least 16 companies have PPARg agonists marketed or in clinical development to treat diabetes.

SciBX 5(37); doi:10.1038/scibx.2012.988
Published online Sept. 20, 2012

Unpatented; available for licensing

Festa, C. et al. J. Med. Chem.;
published online Aug. 30, 2012;
Contact: Angela Zampella,
University of Naples Federico II, Naples, Italy