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.

Badolato, M., Carullo, G., Perri, M., Cione, E., Manetti, F., Di Gioia, M.L., et al. (2017). Quercetin/oleic acid-based G-protein-coupled receptor 40 ligands as new insulin secretion modulators. FUTURE MEDICINAL CHEMISTRY, 9(16), 1873-1885 [10.4155/fmc-2017-0113].

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

Carullo, Gabriele
Investigation
;
MANETTI, FABRIZIO
Investigation
;
BRIZZI, ANTONELLA
Investigation
;
2017-01-01

Abstract

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.
2017
Badolato, M., Carullo, G., Perri, M., Cione, E., Manetti, F., Di Gioia, M.L., et al. (2017). Quercetin/oleic acid-based G-protein-coupled receptor 40 ligands as new insulin secretion modulators. FUTURE MEDICINAL CHEMISTRY, 9(16), 1873-1885 [10.4155/fmc-2017-0113].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/1015810