Genipin is a specific small molecule inhibitor of uncoupling protein 2 (UCP2), inhibits UCP2-mediated mitochondrial proton leak. Genipin does not scavenge superoxide. Genipin inhibits HNE-activated, UCP2-mediated mitochondrial proton leak. Genipin does not affect other mitochondrial transport functions in liver mitochondria. Genipin increases mitochondrial membrane potential, increases ATP levels, closes KATP channels, and stimulates insulin secretion in a UCP2-dependent manner. Genipin reverses high glucose- and obesity-induced β cell dysfunction.
