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Discovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB.
- Source :
- Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2023, Vol. 38 Issue 1, p1-9, 9p
- Publication Year :
- 2023
-
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 IC<subscript>50</subscript> value was 3.1 ± 1.1 μM and NF-κB activity inhibition IC<subscript>50</subscript> 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 inhibiting the expression of IL-6 and TNF-α in serum. Thus, it's reasonable to consider that this compound is a promising small molecule with anti-inflammatory effect for inhibiting the NF-κB signalling pathway. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14756366
- Volume :
- 38
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Journal of Enzyme Inhibition & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 174161191
- Full Text :
- https://doi.org/10.1080/14756366.2023.2225135