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7056348 
Journal Article 
2-Bromo-4 '-methoxychalcone and 2-Iodo-4 '-methoxychalcone Prevent Progression of Hyperglycemia and Obesity via 5 '-Adenosine-Monophosphate-Activated Protein Kinase in Diet-Induced Obese Mice 
Hsieh, C; Chang, FR; Tsai, YiH; Wu, YC; Hsieh, TJ; , 
2018 
Yes 
International Journal of Molecular Sciences
ISSN: 1422-0067
EISSN: 14220067 
MDPI 
BASEL 
19 
9 
English 
30223438 
WOS:000449988100299 
Obesity and diabetes are global health-threatening issues. Interestingly, the mechanism of these pathologies is quite different among individuals. The discovery and development of new categories of medicines from diverse sources are urgently needed for preventing and treating diabetes and other metabolic disorders. Previously, we reported that chalcones are important for preventing biological disorders, such as diabetes. In this study, we demonstrate that the synthetic halogen-containing chalcone derivatives 2-bromo-4'-methoxychalcone (compound 5) and 2-iodo-4'-methoxychalcone (compound 6) can promote glucose consumption and inhibit cellular lipid accumulation via 5'-adenosine-monophosphate-activated protein kinase (AMPK) activation and acetyl-CoA carboxylase 1 (ACC) phosphorylation in 3T3-L1 adipocytes and C2C12 skeletal myotubes. In addition, the two compounds significantly prevented body weight gain and impaired glucose tolerance, hyperinsulinemia, and insulin resistance, which collectively help to delay the progression of hyperglycemia in high-fat-diet-induced obese C57BL/6 mice. These findings indicate that 2-bromo-4'-methoxychalcone and 2-iodo-4'-methoxychalcone could act as AMPK activators, and may serve as lead compounds for a new class of medicines that target obesity and diabetes.