期刊
FASEB JOURNAL
卷 31, 期 6, 页码 2603-2611出版社
FEDERATION AMER SOC EXP BIOL
DOI: 10.1096/fj.201601339R
关键词
GLP-1 receptor; oral agonist; insulin secretagogue; glucose tolerance test
资金
- Ministry of Science and Technology of China [2014ZX09507005-003]
- National Natural Science [81400932]
- Science and Technology of Tianjin [13RCGFSY19700]
- Natural Science Foundation of Tianjin, China [12JCYBJC31500]
The physiologic properties of glucagon-like peptide 1 (GLP-1) make it a potent candidate drug target in the treatment of type 2 diabetes mellitus (T2DM). GLP-1 is capable of regulating the blood glucose level by insulin secretion after administration of oral glucose. The advantages of GLP-1 for the avoidance of hypoglycemia and the control of body weight are attractive despite its poor stability. The clinical efficacies of long-acting GLP-1 derivatives strongly support discovery pursuits aimed at identifying and developing orally active, small-molecule GLP-1 receptor (GLP-1R) agonists. The purpose of this study was to identify and characterize a novel oral agonist of GLP-1R (i.e., myricetin). The insulinotropic characterization of myricetin was performed in isolated islets and in Wistar rats. Long-termoral administration of myricetin demonstrated glucoregulatory activity. The data in this study suggest that myricetin might be a potential drug candidate for the treatment of T2DM as a GLP-1R agonist. Further structural modifications on myricetin might improve its pharmacology and pharmacokinetics.
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