RESUMEN
A series of derivatives of salidroside with mirror isomer glucose and different phenyl moieties were synthesized by Schmidt glycosylation in satisfactory yields, and their antioxidant and anti-inflammatory activities were evaluated by using LPS-induced RAW264.7 cells. One of the synthesized derivatives Ê-Sal-4, bearing Ê-glycosyl and -OMe modification at the phenyl ring, exhibited high activity in inhibiting the production of pro-inflammatory cytokines and oxidative stress biomarker MDA as well as in enhancing the activity of SOD enzyme, compared with the natural product and its corresponding á´ -enantiomer. Further proteomic analysis suggested that Ê-Sal-4 exerted its anti-inflammatory activity through metabolic reprogramming. The in vitro activity showed that Ê-Sal-4 is a potent antioxidant and anti-inflammatory agent. Our finding indicated that the Ê-glucose-derived salidroside might be a promising lead compound in the development of salidroside derivatives as therapeutic agents.