Design, synthesis, in vitro and in vivo biological evaluation of pterostilbene derivatives for anti-inflammation therapy
文献类型： 外文期刊
作者： Chen, Liuzeng 1 ; Wang, Ke 1 ; Liu, Xiaohan 1 ; Wang, Lifan 1 ; Zou, Hui 1 ; Hu, Shuying 1 ; Zhou, Lingling 1 ; Li, Rong 1 ; Cao, Shiying 1 ; Ruan, Banfeng 1 ; Cui, Quanren 2 ;
作者机构： 1.Hefei Univ, Sch Biol Food & Environm, Hefei, Peoples R China
2.Anhui Acad Agr Sci, Inst Tobacoo Res, Hefei, Peoples R China
关键词： Anti-inflammation therapy; NF-kappa B/MAPK signalling pathway; pterostilbene; drug discovery; inflammatory bowel diseases
期刊名称：JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY （ 影响因子：5.6； 五年影响因子：5.2 ）
ISSN： 1475-6366
年卷期： 2024 年 39 卷 1 期
页码：
收录情况： SCI
摘要： 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 E2 was the most active (against NO: IC50 = 0.7 mu M) than celecoxib. Further studies showed that compound E2 exerted anti-inflammatory activity by blocking LPS-induced NF-kappa B/MAPK signalling pathway activation. In vivo experiments revealed that compound E2 had a good alleviating effect on acute colitis in mice. In conclusion, compound E2 may be a promising anti-inflammatory lead compound.
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