文献类型： 外文期刊

作者： Yan, Yaoyao ¹ ; Qi, Lv ¹ ; Zhou, Feilong ¹ ; Jian, Yujie ¹ ; Liu, Xinhua ¹ ; Xing, Chen ² ; Yong, Hu ³ ;

作者机构： 1.Anhui Med Univ, Anhui Prov Key Lab Major Autoimmune Dis, Sch Pharm, Hefei, Peoples R China

2.Anhui Med Univ, Sch Publ Hlth, Key Lab Populat Hlth Life Cycle, Hefei, Peoples R China

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

关键词： LPS-induced inflammation; NO; NF-& kappa;B pathway; anti-inflammation small molecule

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： 2023 年 38 卷 1 期

页码：

收录情况： SCI

摘要： In this study, based on the effect of compounds on the activation of NF-kappa B and NO release, compound 51 was discovered as the best one with NO release inhibition IC50 value was 3.1 +/- 1.1 lM and NF-kappa B activity inhibition IC50 value was 172.2 +/- 11.4 nM. Compound 51 could inhibit the activation of NF-kappa B through suppressing phosphorylation and nuclear translocation of NF-kappa B, and suppress LPS-induced inflammatory response in RAW264.7 cells, such as the over-expression of TNF-alpha and IL-6, which were target genes of NF-kappa B. This compound also showed preferable anti-inflammatory activity in vivo, including alleviating significantly gastric distention and splenomegaly caused by LPS stimulation, reducing the level of oxidative stress induced by LPS, and inhibiting the expression of IL-6 and TNF-alpha in serum. Thus, it's reasonable to consider that this compound is a promising small molecule with anti-inflammatory effect for inhibiting the NF-kappa B signalling pathway.