2005 年 25 巻 2 号 p. 130-136
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.
