Related Experiment Video
Updated: Jun 21, 2026

Isolation and Differentiation of Stromal Vascular Cells to Beige/Brite Cells
Published on: March 28, 2013
The effect of substituted thiophene and benzothiophene derivates on PPARgamma expression and glucose metabolism
1Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Abstract:
Eighteen substituted thiophene and benzothiophene derivatives were studied for their effects on peroxisome proliferator-activated receptor gamma (PPARgamma) in HepG2 cells. Three derivatives (compounds 5, 120.97%; 15, 102.14%; and 17, 113.82%) were found to transactivate PPARgamma in vitro. By comparison, the positive control rosiglitazone (Ros) transactivated PPARgamma by 311.53%. The three compounds were studied for their effects on glucose metabolism in vivo in KK/Ay diabetic mice. In vivo, the 2-(beta-carbonyl/sulfonyl) butyryl-thiophene compounds 5 and 15 significantly decreased blood glucose levels (compounds 5, to<15.6mmol/L; 15, to<10mmol/L), improved glucose tolerance, improved impaired pancreatic islet beta-cells, and lowered serum insulin levels.
Related Concept Videos
Cell Specific Gene Expression
Oral Hypoglycemic Agents: Biguanides and Glitazones
Glucagon-like Receptor Agonists
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Dipeptidyl Peptidase 4 Inhibitors
Global Regulatory Systems
