Dipartimento di Farmacia & Scienze della Salute & della Nutrizione, 87036 Arcavacata di Rende, Cs, Italy.
Dipartimento di Biotecnologie, Chimica & Farmacia, Università di Siena, Via Aldo Moro 2, 53100 Siena, Italy.
Future Med Chem. 2017 Oct;9(16):1873-1885. doi: 10.4155/fmc-2017-0113. Epub 2017 Oct 24.
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.
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.
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].
在疾病早期通过饮食来控制 2 型糖尿病是可行的；患者通常低估了这种方法，需要适当的药物治疗。
从对胰岛素分泌有影响的槲皮素和油酸出发，合成了一小组混合分子。在体外和体内模型中评估了胰岛素分泌。AV1 能够剂量依赖性地增强胰岛素分泌，可作为 G 蛋白偶联受体 40 的假定激动剂。
AV1 代表了一种与 G 蛋白偶联受体 40 相互作用的有趣工具。将进一步开展研究以评估其确切的结合模式，并扩大这些抗糖尿病药物的库。[化学式：见正文]。
