Dimethyl cardamonin inhibits lipopolysaccharide-induced inflammatory factors through blocking NF-κB p65 activation

This study has found that dimethyl cardamonin (2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone; DMC), a naturally occurring chalcone, showed potent anti-inflammatory effects in vitro and in vivo. In a cellular model of inflammation, DMC inhibited production of nitric oxide (NO) and prostaglandin E2 (PGE2) and attenuated expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), IL-1β, inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2). DMC prevented nuclear translocation of the nuclear factor-κB (NF-κB) p65 subunit by reducing inhibitor of κBα (I-κBα) phosphorylation and degradation, which resulted in a suppression of NF-κB activities for its target genes. In a mouse model of endotoxin shock, the intraperitoneal injection (i.p.) of DMC (1–50 mg/kg) suppressed TNF-α, IL-6 and IL-1β secretion in LPS-induced mouse blood serum. These results suggest that DMC exerts anti-inflammatory effects through blocking NF-κB activation, therefore, DMC may act as an effective therapeutic strategy against a variety of inflammatory diseases.