The mechanism of anti-inflammatory activity of 2'-hydroxychalcone derivatives

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It is reported that chalcone derivatives have various biological activities such as anti-inflammatory, anti-tumor and anti-oxidant activity. We examined effects of 2-hydroxychalcone derivatives on the production of prostaglandin (PG) E2, nitric oxide (NO) and tumor necrosis factor (TNF)-α. Among fourteen 2-hydroxychalcone derivatives, 2,4-dihydroxy-4-methoxychalcone (compound 3), 2,4-dihydroxy-6-methoxychalcone (compound 8) and 2-hydroxy-4-methoxychalcone (compound 9) showed potent inhibitory activity forward the 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced PGE2 production in rat peritoneal macrophages through the suppression of the induction of cyclooxygenase (COX)-2. Moreover, these three compounds inhibited both NO and TNF-α production through the inhibition of the expression of iNOS and TNF-α mRNA in the murine macrophage cell line RAW 264.7. These three compounds also suppressed the LPS-induced activation of NF-κB and AP-1 in RAW 264.7 cells, indicating that the inhibition of the production of PGE2, NO and TNF-α is due to the inhibition of NF-κB and AP-1 activation. Our findings suggested that the anti-inflammatory activity of the 2-hydroxychalcone derivatives is induced by the inhibition of the production of pro-inflammatory mediators such as PGE2, NO and TNF-α. It was also suggest that the chalcone derivatives might be lead compounds for anti-inflammatory drugs.
日本炎症・再生医学会の論文
2005-03-25