Small-Molecule Activators of AMP-Activated Protein Kinase (AMPK), RSVA314 and RSVA405, Inhibit Adipogenesis

摘要

Obesity is an increasing problem in today's world, particularly in the United States. AMP-activated protein kinase (AMPK) is a sensor and regulator of cellular energy metabolism and a potential drug target in metabolic diseases, such as diabetes and obesity. Studies show pharmacological activation of AMPK can be achieved using resveratrol, a natural polyphenol associated with protective effects against the deregulation of energy homeostasis. Vingtdeux et al. evaluated the antiadipogenic potential of resveratrol analogues. Their work identified novel-small molecules with potent inhibitory effects against adipocyte differentiation in vitro and weight gain. The analogues triggered early activation of AMPK in proliferating preadipocytes without inducing toxicity. These results identify novel small-molecule activators of AMPK as potent inhibitors of adipogenesis and thus show therapeutic potential against obesity.