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

PeerJ

Zhaokai Wang¹  Min Li¹  Hu Fan²  Chao Zhang²  Peng Wu²  Fang Zhang²  Longhe Yang²  Wenjie Liu³ 

[1] College of Life Sciences, Fujian Normal University, Fuzhou, P. R. China;Engineering Research Center of Marine Biological Resource Comprehensive Utilization, Third Institute of Oceanography, State Oceanic Administration, Xiamen, P. R. China;Fujian Provincial Key Laboratory of Innovative Drug Target Research, School of Pharmaceutical Sciences, Xiamen, P. R. China;

关键词: Emodin;    Natural compound;    DPP4;    Hyperglycemia;   

DOI  :  10.7717/peerj.3283

来源: DOAJ

【 摘 要 】

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 IC50 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.

【 授权许可】

Unknown