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Objective To analyze the components of active anti-gonococcal fractions in the extracts of Polygonum capitatum. Methods Drug sensitive paper method and Neisseria gonorrhoeae culture method were used to detect the antibacterial activity of different parts of the flower bud extract against Neisseria gonorrhoeae. UPLC-TOF-MS was used to identify the effective parts of the flower bud extract with anti-gonococcal effect. Results As a result, in the eluate obtained by extracting with a specific macroporous resin, the hydrolysable tannin was contained in the methanol (35%) eluate (fraction F3), such as trigallocyl glucose. This fraction had a good anti-gonococcal effect. The fractions of F2 and F4-6 had a weak antibacterial effect, while other fractions have no antibacterial effect. Conclusion This study provides a basis for the use of trigalactosyl glucose in the preparation of anti-gonococcal drugs, and lays a foundation for the development of a clinical drug of P. capitatum extracts against Neisseria gonorrhoeae.
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Objective To study the spectrum effect relationship between the water and ethanol extracts of Polygonum capitatum and its anti-inflammatory activity. Methods The inflammatory model of mice RAW264.7 cells induced by lipopolysaccharide (LPS) was established, and the release of inflammatory factors was detected by NO and TNF-α kit. The relationship of chemical constituents of P. capitatum was established by using the partial least square method to associate the fingerprint data established by UPLC-MS method and the pharmacodynamics index of different extracts of P. capitatum. Results Different extracts of P. capitatum had no cytotoxicity in the range of concentration less than 250 mg/L, and all of them had anti-inflammatory effect, which had a dose-effect relationship. By using partial least square method, the correlation degree between TNF-α and chromatographic peak was compared. The results showed that the correlation among the peaks 24, 17, 22, 23, 20 and the anti-inflammatory effect was positive, and the anti-inflammatory effect was negatively correlated with the peaks 11, 1, 7, 15, 5, 3. From the analysis of the five peaks, the results showed that all the four peaks were flavonoids except for the tannic acid at peak 17. Conclusion Different extracts of P. capitatum inhibited the inflammatory response of RAW264.7 cells. The flavonoids in P. capitatum had significant anti-inflammatory activity. The results showed that quercetin, tannic acid, and hyperoside had great contribution to the anti-inflammatory effect of P. capitatum.
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Objective: To investigate the hypoglycemic targets of Polygonum capitatum. Methods: Human liver cancer HepG2 cells were adopted to detect the supernatant culture medium glucose content, and the effect on PPAR-α and GLUT4 gene expression was investigated by qRT-PCR after treatment of P. capitatum extracts (PCB). INS-1 cells similar to islet β cells, divided into drug protection group and repair group, were adopted to determine the cell proliferation activity by MTT; The intracellular SOD and MDA levels were measured by biochemical method; The Cyt C and Caspase-3 protein expression levels were detected by Western blotting. Adopting maltose as substrate of α-glycosidase enzyme inhibition model, the inhibitory efficiency of PCB on glycosidic enzyme was determined. Results: PCB group significantly promoted the absorption of HepG2 cells to supernatant glucose and increased the expression of PPAR-α and GLUT4 genes significantly. Aim at protection and repair of INS-1 cells, PCB group significantly increased cell vitality and SOD level, reduced MDA level compared with model group, and at the same time significantly reduced Cyt C and Caspase-3 protein expression levels. PCB had inhibitory activity to α-glycosidase enzymes, with IC50 of 11.53 mg/mL. Conclusion: PCB could significantly increase the PPAR-α and GLUT4 genes expression to promote the absorption of HepG2 cells to supernatant glucose by blocking the Cyt C-Caspase-3 pathways to reduce apoptosis of islet cells which were damaged by STZ and by raising SOD and declining MDA to improve INS-1 cell oxidative stress; What’s more it has inhibitory activity to α-glycosidase enzymes.
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Objective: To investigate the metabolite profile of effective fractions of Polygonum capitatum in rat feces and bile. Methods: In this study, ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC- ESI-Q/TOF-MS) was applied to the identification of metabolites of P. capitatum extracts in rat bile and feces after ig administration. Mass defect filter and Metabolite Tools software were also used. Results: The four parent components and 26 metabolites were identified in rats metabolic experiments in vivo, including 12 metabolites in feces and 19 metabolites in bile. The major metabolites were glucuronide conjugation, methyl-glucuronide conjugation, and sulfate conjugation of quercetin; Conclusion: The studies have established a high-resolution mass spectrometry method to analyze the metabolites of effective fractions of P. capitatum in vivo. The in vivo metabolic characteristics of the components presented in the fraction have been clarified. The work lays a foundation for the clinical application and development of P. capitatum.
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Objective: To study the chemical constituents of Polygonum capitatum. Methods: Isolation and purification of the chemical constituents were carried out repeatedly by silica gel column and Sephadex gel column chromatography. The structures of compounds were identified by physical-chemical methods and spectral data. Results: Fourteen compounds were identified from the petroleum ether fraction of P. capitatum: tricosanol (I), pentacosanol (II), docosanoic acid (III), lignoceric. acid (IV), hexadecanoic-2,3-dihydroxy-propyleste (V), docosanoic-2,3-dihydroxypropyleste (VI), oleanolic acid (VII), ursolic acid (VIII), octacosa-1,27-diene (IX), docosyl ferulate (X), β-sitosterol (XI), tricosane (XII), hexadecanoic acid (XIII), and linoleic acid (XIV). Conclusion: Compounds I-X are obtained from P. capitatum for the first time. Compounds IX and X are obtained from Polygonum for the first time.