Discovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB.

ABSTRACT: In this study, based on the effect of compounds on the activation of NF-κB and NO release, compound 51 was discovered as the best one with NO release inhibition IC₅₀ value was 3.1 ± 1.1 μM and NF-κB activity inhibition IC₅₀ value was 172.2 ± 11.4 nM. Compound 51 could inhibit the activation of NF-κB through suppressing phosphorylation and nuclear translocation of NF-κB, and suppress LPS-induced inflammatory response in RAW264.7 cells, such as the over-expression of TNF-α and IL-6, which were target genes of NF-κB. 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 inhibi

SUBMITTER: Yan Y 

PROVIDER: S-EPMC10281321 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature