Phytochemical Analysis on Quantification and the Inhibitory Effects on Inflammatory Responses from the Fruit of Xanthii fructus

Objective: Xanthii fructus (Compositae) is a traditional herbal medicine used for treating headache, toothache, pruritus, empyema, and rhinitis. In this study of the quality control of X. fructus, we performed simultaneous analysis of nine marker compounds: Protocatechuic acid (1), chlorogenic acid (2), caffeic acid (3), 4,5‑dicaffeoylquinic acid (4), ferulic acid (5), 3,5‑dicaffeoylquinic acid (6), 1,3‑dicaffeoylquinic acid (7), 1,4‑dicaffeoylquinic acid (8), and 4,5‑dicaffeoylquinic acid (9). Materials and Methods: Nine components were separated using reversed‑phase SunFire™ C18 analytical column and analyzed using high‑performance liquid chromatography. We examined the biological effects of the nine marker compounds by determining their anti‑inflammatory activities in the murine macrophage cell line RAW 264.7. Results: Among the nine marker compounds, eight significantly inhibited lipopolysaccharide (LPS)‑stimulated tumor necrosis factor‑alpha (TNF‑α) production. 1, 3, 5 had significant inhibitory effects on LPS‑induced prostaglandin E2 (PGE2) production in RAW 264.7 cells. None of the tested marker compounds had a significant effect on interleukin‑6 production in LPS‑treated RAW 264.7 cells. Our data demonstrated that each marker compound from X. fructus exerts anti‑inflammatory activity by targeting different inflammation‑related pathways such as the TNF‑α or PGE2 pathway. Conclusion: Further experiments using in vitro and in vivo models are needed to identify the mechanisms responsible for the anti‑inflammatory properties of each marker compound.