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Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo

文献类型： 外文期刊

作者： Xiao, Yun 1 ; Yan, Yaoyao 1 ; Du, Juncheng 1 ; Feng, Xiaoxiao 1 ; Zhang, Famin 1 ; Han, Xu 1 ; Hu, Yong 2 ; Liu, Xinhua 1 ;

作者机构： 1.Anhui Med Univ, Lab Anhui Prov, Sch Pharm Inflammat & Immune Mediated Dis, Hefei, Peoples R China

2.Anhui Acad Agr Sci, Agr Prod Proc Inst, Hefei, Peoples R China

关键词： 2-Phenyl-4H-chromen-4-one derivatives; anti-inflammatory; TLR4/MAPK pathway

期刊名称：JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY （ 影响因子：5.756； 五年影响因子：4.983 ）

ISSN： 1475-6366

年卷期： 2022 年 37 卷 1 期

页码：

收录情况： SCI

摘要： It is significant to design, synthesise and optimise flavonoid derivatives with better anti-inflammatory activity. This study aims to design and synthesise a series of novel 2-phenyl-4H-chromen-4-one compounds with anti-inflammatory; among them, compound 8 was discovered as the best one. And then, the effects of compound 8 on the TLR4/MAPK signalling pathway was carried out in vivo, the results indicated that compound 8 could downregulate NO, IL-6, and TNF-alpha expression, and suppress LPS-induced inflammation by inhibiting the TLR4/MAPK pathways. Furthermore, compound 8 reduced inflammation by a mouse model of LPS-induced inflammatory disease in vivo. The results suggest that compound 8 has the potential against inflammation through regulating TLR4/MAPK pathway and can be assessed further for drug development. [GRAPHICS] .

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