Research progress of indole compounds with potential antidiabetic activity

Y Zhu, J Zhao, L Luo, Y Gao, H Bao, P Li… - European Journal of …, 2021 - Elsevier
New types of antidiabetic agents are continually needed with diabetes becoming the
epidemic in the world. Indole alkaloids play an important role in natural products owing to …

Vincamine, from an antioxidant and a cerebral vasodilator to its anticancer potential

Y Ren, K DeRose, L Li, JC Gallucci, J Yu… - Bioorganic & Medicinal …, 2023 - Elsevier
Vincamine is a naturally occurring indole alkaloid showing antioxidant activity and has been
used clinically for the prevention and treatment of cerebrovascular disorders and …

Vincamine as an agonist of G-protein-coupled receptor 40 effectively ameliorates diabetic peripheral neuropathy in mice

J Xu, X Xu, Y Ling, Y Wang, Y Huang, J Yang… - Acta Pharmacologica …, 2023 - nature.com
Diabetic peripheral neuropathy (DPN) is a common complication of diabetes, which has yet
no curable medication. Neuroinflammation and mitochondrial dysfunction are tightly linked …

[HTML][HTML] Update of Indoles: Promising molecules for ameliorating metabolic diseases

W Hu, G Yan, Q Ding, J Cai, Z Zhang, Z Zhao… - Biomedicine & …, 2022 - Elsevier
Obesity and metabolic disorders have gradually become public health-threatening
problems. The metabolic disorder is a cluster of complex metabolic abnormalities which are …

FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and …

P Governa, MC Caroleo, G Carullo, F Aiello… - Bioorganic & Medicinal …, 2021 - Elsevier
The progress made so far in the elucidation of the structure of free fatty acid receptor 1
(FFAR1) and its secondary and ternary complexes with partial and full allosteric ligands led …

Design, synthesis and biological evaluation of vincamine derivatives as potential pancreatic β-cells protective agents for the treatment of type 2 diabetes mellitus

J Wang, X Lv, J Xu, X Liu, T Du, G Sun, J Chen… - European Journal of …, 2020 - Elsevier
A series of vincamine derivatives were designed, synthesized and evaluated as pancreatic β-
cells protective agents for type 2 diabetes mellitus. Most of the compounds displayed potent …

Discovery and optimization of novel 3-benzyl-N-phenyl-1H-pyrazole-5-carboxamides as bifunctional antidiabetic agents stimulating both insulin secretion and glucose …

J Jo, D Lee, YH Park, H Choi, J Han, DH Park… - European Journal of …, 2021 - Elsevier
A novel series of 3-benzyl-N-phenyl-1H-pyrazole-5-carboxamides was designed,
synthesized and evaluated for their biological activities on glucose-stimulated insulin …

Vincamine as an agonist of G protein-coupled receptor 40 effectively ameliorates pulmonary fibrosis in mice

T Zhao, Z Zhou, S Zhao, H Wan, H Li, J Hou, J Wang… - Phytomedicine, 2023 - Elsevier
Background Pulmonary fibrosis (PF) is an irreversible and fatal lung disease with limited
therapeutic options. G protein-coupled receptor 40 (GPR40) has been developed as a …

Recent updates on free fatty acid receptor 1 (GPR-40) agonists for the treatment of type 2 diabetes mellitus

L Rani, AS Grewal, N Sharma… - Mini Reviews in …, 2021 - ingentaconnect.com
Background: The global incidence of type 2 diabetes mellitus (T2DM) has enthused the
development of new antidiabetic targets with low toxicity and long-term stability. In this …

[HTML][HTML] Xelaglifam, a novel GPR40/FFAR1 agonist, exhibits enhanced β-arrestin recruitment and sustained glycemic control for type 2 diabetes

J Yoon, DG Lee, H Song, D Hong, JS Park… - Biomedicine & …, 2024 - Elsevier
Xelaglifam, developed as a GPR40/FFAR1 agonist, induces glucose-dependent insulin
secretion and reduces circulating glucose levels for Type 2 diabetes treatment. This study …