Design, synthesis chalcone derivatives as AdipoR agonist for type 2 diabetes

作者:Zhu, Panhu; Huang, Weijun; Li, Jiaming*; Ma, Xiaodong; Hu, Mengqi; Wang, Yujun; Xu, Qinlong; Wang, Xianna
来源:Chemical Biology & Drug Design, 2018, 92(2): 1525-1536.
DOI:10.1111/cbdd.13319

摘要

Two structurally novel series of chalcone derivatives were designed and synthesized as potential agents against type 2 diabetes. As a result of the antidiabetic biological evaluation in streptozotocin (STZ)-induced type 2 diabetes animal model, 13e, 13g, and 19f showed more significant reduction in serum Glu, TG, TC levels by contrast to the positive control AdipoRon. In addition to upregulating the expression of AdipoR1 and AdipoR2, 13e and 19f treatment also increased expression of AMPK and PPAR-alpha. Taken together, these results suggested that 13e and 19f might be a promising compound for type 2 diabetes treatment.