Nuclear Factor Kappa B Activation and Peroxisome Proliferator-activated Receptor Transactivational Effects of Chemical Components of the Roots of Polygonum multiflorum

BACKGROUND: Polygonum multiflorum is well-known as “Heshouwu” in traditional Chinese herbal medicine. In Northeast Asia, it is often used as a tonic to prevent premature aging of the kidney and liver, tendons, and bones and strengthening of the lower back and knees. OBJECTIVE: To research the anti-inflammatory activities of components from P. multiflorum. MATERIALS AND METHODS: The compounds were isolated by a combination of silica gel and YMC R-18 column chromatography, and their structures were identified by analysis of spectroscopic data (1D, 2D-nuclear magnetic resonance, and mass spectrometry). The anti-inflammatory activities of the isolated compounds 1−15 were evaluated by luciferase reporter gene assays. RESULTS: Fifteen compounds (1–15) were isolated from the roots of P. multiflorum. Compounds 1−5 and 14−15 significantly inhibited tumor necrosis factor-α-induced nuclear factor kappa B-luciferase activity, with IC(50) values of 24.16-37.56 μM. Compounds 1−5 also greatly enhanced peroxisome proliferator-activated receptors transcriptional activity with EC(50) values of 18.26−31.45 μM. CONCLUSION: The anthraquinone derivatives were the active components from the roots of P. multiflorum as an inhibitor on inflammation-related factors in human hepatoma cells. Therefore, we suggest that the roots of P. multiflorum can be used to treat natural inflammatory diseases. SUMMARY: This study presented that fifteen compounds (1-15) isolated from the roots of Polygonum multiflrum exert signifiant anti inflmmatory effects by inhibiting TNF α induced NF κB activation and PPARs transcription. Abbreviation used: NF κB: Nuclear factor kappa B, PPARs: Peroxisome proliferator activated receptors, PPREs: Peroxisome proliferator response elements, TNF α: Tumor necrosis factor α, ESI-MS: Electrospray ionization mass spectrometry, HepG2: Human hepatoma cells