Screening of a natural compound library identifies emodin, a natural compound from Rheum palmatum Linn that inhibits DPP4

作者：Zhaokai Wang, Longhe Yang, Fan Hu, Peng Wu, Fang Zhang, Chao Zhang, Wenjie Liu, Min Li · 发表于：PeerJ · 年份：2017 · DOI：10.7717/peerj.3283 · 被引用次数：24 · 研究领域：Diabetes Treatment and Management、Metabolism, Diabetes, and Cancer、Pancreatic function and diabetes

Historically, Chinese herbal medicines have been widely used in the treatment of hyperglycemia, but the mechanisms underlying their effectiveness remain largely unknown. Here, we screened a compound library primarily comprised of natural compounds extracted from herbs and marine organisms. The results showed that emodin, a natural compound from Rheum palmatum Linn, inhibited DPP4 activity with an in vitro IC 50 of 5.76 µM without inhibiting either DPP8 or DPP9. A docking model revealed that emodin binds to DPP4 protein through Glu205 and Glu206, although with low affinity. Moreover, emodin treatment (3, 10 and 30 mg/kg, P.O.) in mice decreased plasma DPP4 activity in a dose-dependent manner. Our study suggests that emodin inhibits DPP4 activity and may represent a novel therapeutic for the treatment of type 2 diabetes.