Quercetin/oleic acid-based G-protein-coupled receptor 40 ligands as new insulin secretion modulators.

AIM

Management of Type 2 diabetes mellitus by diet is achievable at the early stage of the disease; patients usually underestimate this approach and an appropriate drug therapy is required.

RESULTS

Starting from quercetin and oleic acid, that have effect on insulin secretion, a small set of hybrid molecules was synthesized. Insulin secretion was evaluated in both in vitro and ex vivo models.  AV1  was able to enhance insulin secretion dose dependently, behaving as a conceivable agonist of G-protein-coupled receptor 40.

CONCLUSION

AV1 represents an interesting tool that interacts with G-protein-coupled receptor 40. Further studies will be carried out to evaluate the exact binding mode, and also to enlarge the library of these antidiabetic agents. [Formula: see text].