Isoflavone derivatives inhibit NF-κB-dependent transcriptional activity

The transcription factor NF-κB regulates diverse biological activities, such as inflammatory responses, cell proliferation, and cell survival. Isoflavones are known to have anti-inflammatory and anti-tumor activities, due, in part, to inhibition of NF-κB activity. However, the structural moiety of isoflavones responsible for the inhibition of NF-κB is not clearly understood. In this work, structure–activity relationships of isoflavone derivatives were examined with regard to NF-κB inhibition, using CoMFA and CoMSIA. The results show that substituents at the C-7 and C-4′ positions are crucial for the inhibition of TNFα-induced transcriptional activity of NF-κB.

Graphical abstractIsoflavones are known to have anti-inflammatory and anti-tumor activities, due, in part, to inhibition of NF-κB activity. However, the structural moiety of isoflavones responsible for the inhibition of NF-κB is not clearly understood. In this work, structure–activity relationships of isoflavone derivatives were examined with regard to NF-κB inhibition, using CoMFA and CoMSIA.Figure optionsDownload full-size imageDownload as PowerPoint slide