2. Academic Validation
  3. Design, synthesis and bioactivity evaluation of fisetin derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury

Design, synthesis and bioactivity evaluation of fisetin derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury

  • Bioorg Med Chem. 2021 Nov 1;49:116456. doi: 10.1016/j.bmc.2021.116456.
Xiemin Wang 1,  Jun Yang 1,  Bingyu Ding 2,  Pan Chen 1,  Zhengwei Xu 2,  Yunxi Zhao 2,  Pengqin Chen 1,  Nipon Chattipakorn 3,  Guang Liang 4,  Di Wu 5,  Qidong Tang 6
Affiliations

Affiliations

  • 1 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China; Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou, Zhejiang 325001, China.
  • 2 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China.
  • 3 Cardiac Electrophysiology Research and Training Center, Faculty of Medicine, Chiang Mai University, Chiang Mai 50200, Thailand.
  • 4 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China; Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou, Zhejiang 325001, China; School of Pharmaceutical Sciences, Hangzhou Medical College, Hangzhou, Zhejiang 311399, China. Electronic address: wzmcliangguang@163.com.
  • 5 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China. Electronic address: wudi2017@wmu.edu.cn.
  • 6 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China. Electronic address: tangqidongcn@126.com.
PMID: 34628233 DOI: 10.1016/j.bmc.2021.116456
Abstract

Acute lung injury (ALI) refers to a common and life-threatening disease attributed to inflammation. However, effective drug treatments have been rare for ALI. Natural Products have been considered as a vital source of drug discovery which indicates that it's a workable method to find new anti-inflammatory drugs in Natural Products. Inspired by the various biological activities of fisetin, we reported the design and synthesis of a series of fisetin derivatives which were also evaluated for their anti-inflammatory activities in J774A.1 macrophages. Most of the obtain derivatives could effectively inhibit the release of IL-6 and TNF-α in vitro experiments without cytotoxicity. The most promising compound 5b exhibited significant in vivo anti-inflammatory activity in the model of LPS-induced ALI in mice. On the whole, this study could provide novel candidates for the treatment of ALI.

Keywords

Acute lung injury; Anti-inflammatory; Fisetin derivatives; Natural product.

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