Anti-inflammatory Active Ingredient of Chinese Herb Polygoni Cuspidati Rhizoma et Radix Based on Spectrum-effect Relationship / 中国实验方剂学杂志

ABSTRACT

Objective: To study the potential anti-inflammatory active ingredient of Chinese herbal Polygoni Cuspidati Rhizoma et Radix. Method: The inflammatory model of peritoneal macrophages (RAW264.7 cells) induced by lipopolysaccharide (LPS) in mice was used to screen out the anti-inflammatory activity of 95% ethanol extract of Polygoni Cuspidati Rhizoma et Radix and its macroporous resin elution site (30%, 60%, 95% ethanol eluting site). The characteristic fingerprints were established by ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) technology, and then partial least squares method (partial least squares, PLS) was used to study the spectrum-effect relationship between the peak area of the characteristic components and the inhibition rate of nitric oxide (NO), and potential anti-inflammatory active ingredients were identified according to variable important in projection (VIP). Result: The ethanol extract macroporous resin 60% ethanol elution site of Polygoni Cuspidati Rhizoma et Radix had the strongest inhibition ability of nitric oxide formation, with a certain dose-dependent relationship. The study of spectrum-effect relationship showed that 3 components had potential anti-inflammatory activity, namely Emodin-8-O-β-D-glucoside (E-8-G), Emodin-1-O-β-D-giucoside, and Emodin-8-O-(6'-O-malonyl)-glucoside. In addition, the anti-inflammatory activity of E-8-G was further validated at the cell level through molecular docking analysis. Conclusion: Three potential anti-inflammatory active ingredients were found base on the spectrum-effect relationship. This study strategy is helpful to find the active ingredients (group) of traditional Chinese medicine, and provides new research ideas and methods for studying the material basis of Chinese herbal medicine.