Design, synthesis and bioactivity evaluation of fisetin derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury. (1st November 2021)

• Record Type: Journal Article
• Authors: Wang, Xiemin; Yang, Jun; Ding, Bingyu; Chen, Pan; Xu, Zhengwei; Zhao, Yunxi; Chen, Pengqin; Chattipakorn, Nipon; Liang, Guang; Wu, Di; Tang, Qidong
• Is Part Of: Bioorganic & medicinal chemistry. Volume 49(2021)
• Publication Date: 2021-11-01
• Subjects: Acute lung injury -- Natural product -- Fisetin derivatives -- Anti-inflammatory; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2021.116456
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: 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.