N-Heterocyclic functionalized chalcone derivatives as anti-inflammatory agents for atopic dermatitis treatment by inhibiting JAK1/STAT3 signaling pathway

Atopic dermatitis (AD) is difficult to cure as a chronic inflammatory skin disease. In the present study, a series of N-heterocyclic functionalized chalcone derivatives have been prepared to investigate their in vitro and in vivo anti-inflammatory activities. The results indicated that many derivatives could effectively inhibit NO generation with low toxicity. In vivo studies revealed that 4f could improve the skin condition of AD-like mice, reduce inflammatory infiltration, inhibit the expressions of p-JAK1/JAK1 and p-STAT3/STAT3, and mitigate the excessive immune response on MC903-induced AD-like mice. The molecular docking study indicated that 4f had an obvious binding site with the target 4ehz and 6QHD. Therefore, these derivatives may be considered as potent agents for AD treatment by inhibiting JAK1/STAT3 signaling pathway.

Anti-inflammatory; Atopic dermatitis; Chalcone derivatives; JAK1/STAT3; Molecular docking.