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Published on: September 16, 2019
Discovery of novel MIF inhibitors that attenuate microglial inflammatory activation by structures-based virtual
Yu Zhang1, Lei Xu2, Yao Zhang1
1Department of Pharmacy, Hubei Clinical Research Center of Parkinson's disease, Xiangyang Key Laboratory of Movement Disorders, Xiangyang No.1 People'Hospital, Hubei University of Medicine, Xiangyang, 441000, China.
Abstract:
Macrophage migration inhibitory factor (MIF) is a pluripotent pro-inflammatory cytokine and is related to acute and chronic inflammatory responses, immune disorders, tumors, and other diseases. In this study, an integrated virtual screening strategy and bioassays were used to search for potent MIF inhibitors. Twelve compounds with better bioactivity than the prototypical MIF-inhibitor ISO-1 (IC50 = 14.41 μM) were identified by an in vitro enzymatic activity assay. Structural analysis revealed that these inhibitors have novel structural scaffolds. Compound 11 was then chosen for further characterization in vitro, and it exhibited marked anti-inflammatory efficacy in LPS-activated BV-2 microglial cells by suppressing the activation of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPKs). Our findings suggest that MIF may be involved in the regulation of microglial inflammatory activation and that small-molecule MIF inhibitors may serve as promising therapeutic agents for neuroinflammatory diseases.
