Quercetin/oleic acid-based G-protein-coupled receptor 40 ligands as new insulin secretion modulators. (October 2017)

• Record Type: Journal Article
• Authors: Badolato, Mariateresa; Carullo, Gabriele; Perri, Mariarita; Cione, Erika; Manetti, Fabrizio; Di Gioia, Maria Luisa; Brizzi, Antonella; Caroleo, Maria Cristina; Aiello, Francesca
• Is Part Of: Future medicinal chemistry. Volume 9:Number 16(2017)
• Page Start: 1873
• Page End: 1885
• Publication Date: 2017-10
• Subjects: antidiabetic drugs -- GPR40 molecular docking -- insulin secretion -- quercetin/oleic acid-based hybrid molecules; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.4155/fmc-2017-0113
• Languages: English
• ISSNs: 1756-8919

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.