Design, synthesis, and biological evaluation of pterostilbene derivatives for anti-inflammation therapy.

Pterostilbene (PST) is a naturally derived stilbene compound in grapes, blueberries, and other fruits. It is also a natural dietary compound with a wide range of biological activities such as antioxidant, anti-inflammatory, antitumor, and so on. Structural modifications based on the chemical scaffold of the pterostilbene skeleton are of great importance for drug discovery. In this study, pterostilbene skeletons were used to design novel anti-inflammatory compounds with high activity and low toxicity. A total of 30 new were found and synthesised, and their anti-inflammatory activity and safety were screened. Among them, compound was the most active (against NO: IC = 0.7 μM) than celecoxib. Further studies showed that compound exerted anti-inflammatory activity by blocking LPS-induced NF-κB/MAPK signalling pathway activation. experiments revealed that compound had a good alleviating effect on acute colitis in mice. In conclusion, compound may be a promising anti-inflammatory lead compound.