Inhibition of Nuclear Factor Kappa B (NF-B):

Table 1.

NF-kB Inhibitors that Demonstrate Anti-Inflammatory Activity in Experimental Models

Classa In vitro In vivo
aAn extensive collection of drugs that range widely in structure and activity are now known to inhibit NF-κB activity, and more importantly, they alleviate inflammation in pharmacologically relevant in vivo models. Unfortunately, many of these drugs display significant and harmful side effects, and so the identification of safer, selective inhibitors of NF-κB activation remains a major goal for many pharmaceutical and biotechnology companies.
bODNs, oligodeoxynucleotides
CTFD, transcription factor decoy
Salicylates aspirin, sulfasalazine, triflusal Synovial fibroblast, lung epithelial cells, dendritic cells, monocytes, macrophages, T-cells, endothelial cells, vascular smooth muscle cells. Contact hypersensitivity, zymosan-induced paw inflammation
NSAIDs ibuprofen, sulindac, tepoxalin Macrophages, endothelial cells, T-cells Zymosan-induced inflammation in the paw and spinal cord
Glucocorticoids dexamethasone, hydrocortisone Macrophages, endothelial cells, pulmunory epithelial cells, T-cells Carrageenin-induced air pouch, peritoneal sepsis, myocardial contractile depression
Antisense ODNsb anti-p50, anti-p65 Fibroblast, B-cells, T-cells Graft rejection, septic shock
TFDC-ODNs Endothelial cells, vascular smooth muscle cells, macrophages Rheumatoid arthritis, ischemia-reperfusion injury, nephritis, carrageenin-induced paw inflammation, Arthus reaction
Natural compounds flavanoids, polyphenols, sesquiterpene lactones, curcumin, sesterterpene T-cells, macrophages, fibrosarcoma and epithelial cells Septic shock, TPA-induced skin inflammation
Antioxidants PDTC, N-acetylcysteine, Vitamin E, Vitamin C Macrophages, monocytes, T-cells Septic shock, neutrophilic alveolitis, multiple organ injury, experimental allergic encephalomyelitis
Proteasome inhibitors lactacystin, MG132, TLCK, TPCK, PSI, PS-519, PS-341 Macrophages, monocytes, T-cells, B-cells Asthma, septic shock, neutrophilic alveolitis, cerebral and myocardial ischemia-reperfusion injury
Peptides SN50, NLS, NBD, TIRAP Macrophages, T-cells, endothelial cells, vascular smooth cells Septic shock, zymosan-induced peritonitis, PMA-induced ear edema, carrageenin-induced paw inflammation, Arthus reaction, inflammatory bowel disease

This Article

  1. MI February 2002 vol. 2 no. 1 22-35