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.
ABSTRACT
Objective: To analyze the change rule of main chemical components in Asarum heterotropoidesvar.mandshuricum seedling during the growing process.Method:Whole seedling samples (one week and two weeks) and the mature plant (three months) of A.heterotropoidesvar.mandshuricum were collected and every sample was divided to aerial part (stems and leaves) and underground part (roots).The secondary metabolites were qualitatively identified by HPLC-TOF-MS and the quantitative identification was carried out at the same time with asarinin as index component.Result: A total of 6 known compounds were identified from the underground part of A.heterotropoidesvar.mandshuricum as α-asarone (1),N-isobutyl-2,4,8,10-dodecatetraenamide (2),9-methoxyaristolactam Ⅳ(3),asarinin (4),caulesnarinside (6) and chalcononaringenin 2',4'-di-O-β-D-glucopyranoside (7),respectively,the peak area values showed that the contents of these compounds increased gradually with the growth time.A total of 4 known compounds were identified from the aerial part of this herb as N-isobutyl-2,4,8,10-dodecatetraenamide (2),caulesauroneside (5),caulesnarinside (6) or chalcononaringenin 2',4'-di-O-β-D-glucopyranoside (7) and peonidin 3-caffeoylgentiobioside (8).Asarinin was identified only in the underground part of mature plant,its content was 155.4 μg·g-1.Conclusion: The species and contents of secondary metabolites are quite different in the aerial and underground parts of A.heterotropoidesvar.mandshuricum.At different growth stages of A.heterotropoides var.mandshuricum seedling,the types and contents of secondary metabolites in the same site are also different,while the contents of main components show an increasing trend with the growth time.