Almudena Bermejo, Aida Collado, Isabel Barrachina, Patrice Marqués, Noureddine El Aouad, Xavier Franck, Francisco Garibotto, Catherine Dacquet, Daniel H Caignard, Fernando D Suvire, Ricardo D Enriz, Laura Piqueras, Bruno Figadère, María-Jesús Sanz, Nuria Cabedo, Diego Cortes
Dual peroxisome proliferator-activated receptor-α/γ (PPARα/γ) agonists regulate both lipid and glucose homeostasis under different metabolic conditions and can exert anti-inflammatory activity. We investigated the potential dual PPARα/γ agonism of prenylated benzopyrans polycerasoidol ( 1 ) and polycerasoidin ( 2 ) and their derivatives for novel drug development. Nine semisynthetic derivatives were prepared from the natural polycerasoidol ( 1 ) and polycerasoidin ( 2 ), which were evaluated for PPARα, -γ, -δ and retinoid X receptor-α activity in transactivation assays...
July 26, 2019: Journal of Natural Products