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OBJECTIVE To evaluate the efficacy of the functional dressing of Polygonum capitatum nanofibers （P-PVP-PCL）. METHODS P-PVP-PCL were prepared by electrospinning technology， and the microstructure of P-PVP-PCL was observed. The antibacterial activity and antioxidant activity of P-PVP-PCL and its effects on the survival rate， adhesion and migration rate of mouse fibroblast L929 cells were investigated. The effects of medical gauze dressing， blank nanofiber dressing （PVP-PCL） and P- PVP-PCL on the healing rate of the wound were investigated by establishing the back skin wound model of rats. The pathological changes of the wound tissue and collagen fiber deposition were observed， as well as the number of platelet endothelial cell adhesion molecule-1 （CD31） positive blood vessels and the expression of transforming growth factor-β （TGF-β） protein in wound tissue. RESULTS P-PVP-PCL had a smooth surface and a double-layer structure at the cross-section. The inhibition rates of P-PVP-PCL against Staphylococcus aureus and Escherichia coli were （98.88±0.66）% and （94.75±1.41）% ， respectively. The antioxidant activity of P-PVP-PCL was （83.69±1.56）%， and the cell activity of the P-PVP-PCL group was significantly higher than those of the control group and PVP-PCL group （P＜0.05）. Compared with medical gauze dressings， P-PVP-PCL was more conducive to L929 cell adhesion； at 48 hours， the cell scratches in this group had basically healed. Compared with the medical gauze dressing group， the wound healing rates of the PVP-PCL group and the P-PVP-PCL group were significantly increased （P＜0.05）. On the 14th day of intervention， the wounds in the P-PVP-PCL group had basically healed， there was no dermal necrosis in the wound tissue， and the collagen fibers were arranged relatively neatly and the density was relatively uniform. The number of CD31 positive blood vessels and the expression of TGF-β protein showed a downward trend compared with the 7th day of intervention， and the number of CD31 positive blood vessels was significantly lower than those of the medical gauze dressing group and PVP-PCL group （P＜0.05）， but the protein expression of TGF- β was significantly higher than those of the medical gauze dressing group and the PVP-PCL group （P＜0.05）. CONCLUSIONS P-PVP-PCL has good antibacterial and antioxidant activity in E-mail：444096585@qq.com vitro， and can promote the proliferation， adhesion and migration of L929 cells. It can promote wound healing of rats in vivo.
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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 identify lipid metabolites of endophytic fungus Aspergillus terreus from Polygonum capitatum, and to investigate their anti-multidrug resistant bacteria and anti-inflammatory effects. METHODS:GC-MS was used to analyze and identify lipid metabolites of A. terreus. MIC of lipid metabolites and main composition to 10 strains of multidrug resistant bacteria (Klebsiella pneumoniae,Proteus common,Staphylococcus epidermidis,Escherichia coli,Staphylococcus aureus,Enterobacter cloacae,Pseudomonas aeruginosa,Proteus mirabilis,Enterococcus faecium and Acinetobacter baumanii) were determined by 96-well plate microdilution method. The spread plate method was used to determine MBC of samples to bacteria. LPS-induced RAW264.7 inflammatory model was used to investigate the effects of different mass concentrations(50,100,200 μg/mL)of lipid metabolites on the release of NO and TNF-α after treated for 24 h. RESULTS:A total of 13 compounds were identified in lipid metabolites of A. terreus,among which palmitic acid,stearic acid,linoleic acid and oleic acid were main components,and relative percentages of them were 29.35％,10.87％,21.94％,34.85％. The lipid metabolites displayed anti-bacterial activity against E. coli and K. pneumonia with MICs of 12.5 mg/mL and 50 mg/mL,MBC of 25 mg/mL and 100 mg/mL,respectively. The main 4 compositions could inhibit the growth of E. coli,with MIC of 0.5-1 mg/mL,among which palmitic acid showed significant antibacterial activity,especially to E. faecium(MIC of 0.25 mg/mL). 50,100 μg/mL lipid metabolites could signifiantly inhibit the release of inflammatory factor of NO and TNF-α in RAW264.7 in vitro. CONCLUSIONS:The lipid metabolites of endophytic fungus A. terreus from P. capitatum show anti- multi-drug resistant bacteria and anti-inflammatory effects.
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Objective The activation of NF-kappa B (NF-κB) signaling pathway plays an important role in the development of helicobacter pylori associated gastritis (HAG). The article aimed to investigate the effects of polygonum capitatum on the treatment of HAG in NF-κB signaling pathway and observe whether the regulation of NF-κB acetylation by silent information regulator 1 (SIRT1) affects the therapeutic effects of HAG. Methods The immortalized human gastric epithelial cells (GES-1) were cultured and the H.pylori stand- ard strain ATCC700392 was used for the replication of HAG cell model by 100∶1. The cells were divided into model group,drug group and normal control group. Cells were treated with 80 μg/mL in drug group,H.pylori and GES-1 were cultured together in model group and untreated GES-1 cells were taken as control group. Real time PCR was used to detect the mRNA levels of SIRT1,NF-κB/p65 and TNF-α. Western blotting was used to detect the expression levels of SIRT1,NF-κB/p65 and its acetylated protein in the total protein,as well as the expression levels of SIRT1 and NF-κB/p65 in cytoplasm and nuclear protein. Results At 12 h after the infection of H. pylori,the level of TNF-α in the supernatant was higher than that in the normal control group(P<0.05). The expression of SIRT1 de-creased in the cytoplasm of model group,while the expression levels of NF-κB/p65,acetyl-NF-κB p65(Lys310) and TNF-α in the nu-cleus increased (P<0.05). But after the treatment of polygonum capitatum,the expression of SIRT1 in the nucleus increased(P<0.05) while the expression of NF-κB/p65,acetyl-NF-κB p65(Lys310) and TNF-α decreased (P<0.05). Conclusion Polygonum capita-tum can activate the SIRT1 in the nucleus,which makes activated NF-κB/p65 in the nucleus carry out deacetylation modification in or-der to antagonize the cell damage induced by H.pylori.
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In this study, we used Ultra Performance Liquid Chromatography-Time-of-Flight Mass Spectrometry(UPLC-TOF-MS)to identify the chemical constituents in both ethanol and water extract of Polygonum capitatum. A Waters ACQUITY UPLC BEH C₁₈ column(2.1 mm×100 mm,1.7 μm) was used for separation. The mobile phase was consisted of(A) 0.10% formic acid in water and(B)0.10% formic acid in acetonitrile, and the flow rate was 0.35 mL•min⁻¹. ESI source in negative ion mode was used for MS detection. Structural identification was carried out according to the accurate mass and matching with database. The results showed that flavonoids, polyphenols and lignans were the main components in both extracts. However, the chemical compositions of both extracts were different, e.g. there are less hydrolyzable tannins, loss of ellagic acid and more anthocyanins in ethanol extract. In a conclusion, this study provides an important scientific basis for identifying the active ingredients in P. capitatum, which also help to reveal the pharmacological effect of P. capitatum.
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Polygonum capitatum is a traditional Chinese medicine widely used for urinary system diseases in the minority areas. Its research began in the 1980s. The major chemical constiturents in Polygonum capitatum is flavonids, phenolic acids, organic acids, al-dehydes, ketones, lignans and triterpen. The pharmacological activities were antibacterial, anti-inflammatory, antioxidant and antipy-retic analgesia. By referring to the relative literatures on Polygonum capitatum from home and abroad, the study advances in the chemi-cal constituents and pharmacological actions of Polygonum capitatum were reviewed to lay foundation for the reasonable exploitation and utilization of Polygonum capitatum.
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OBJECTIVE: To investigate the Polygonum capitatum's influences on the related indicators in db/db mice which is the obesity model of type 2 diabetes mellitus. METHODS: Randomly dividing the mice into 5 groups: model group, rosiglitazone hydrochloride group, low-, moderate-and high-dose groups of Polygonum capitatum (5,10,20 g·kg-1), make the db/m mice as blank control. Give the medicine for four weeks. The body weight, blood sugar were determined every week. At the end of fourth week, measuring the glucose tolerance and INS, IL-6 in serum. After all the mice were killed, testing the cholesterol and triglyceride in liver and skeletal muscle and then collecting the liver tissue for HE staining. At the meantime, the expression level of AMPK and GLUT4 in liver were detected by Q-PCR. RESULTS: Polygonum capitatum can improve the body weight, blood sugar and glucose tolerance of db/db mice as well as the content of INS and IL-6 in serum, but increase the content of SOD and decrease the content of MDA in mice, furthermore, the cholesterol and triglyceride levels in the liver and skeletal muscle were also declined. HE staining showed that Polygonum capitatum could reduce the number of vacuoles in the liver of db/db mice, and make its shape more complete and ordered. What's more, raising the expression of AMPK and GLUT4 in the liver. CONCLUSION: Polygonum capitatum can improve the condition of insulin resistance state, alleviate inflammation and advance the ability of db/db mice, which can also reduce the number of vacuoles in liver, and relieve the tissue lipid metabolic disorder. Meanwhile, Polygonum capitatum can promote the uptake of glucose in liver tissues, which is resulted from upregulation of expression in hepatic AMPK and GLUT4 gene.
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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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Aim Modelorganismzebrafishwasusedto study metabolites and metabolite profile of the gallic acid and protocatechuic acid of effective fractions of Polygonum capitatum,and discuss the feasibility and rationality of the model organism zebrafish in the study ofdrugmetabolism.Methods Thetwocomponents were exposed to model organism zebrafish after 24 h of solution treatment by using ultra-high performance liq-uid chromatography-quadrupole-time-of-flight tandem mass spectrometry technology (UHPLC-Q-TOF MS ) method with mass defect filter (MDF ),and the data was treated with data mining software(Metabolite Tool-sTM).Results Afterzebrafishmetabolism,themain reactions of gallic acid and protocatechuic were methyl-ation sulfated. In addition to the two parent com-pounds,six phase II metabolites were identified,in-cluding four methyl sulfate products and two sulfation products.Conclusions Themetabolismofthegallic acid and protocatechuic acid of effective fractions of Polygonum capitatum by zebrafish presents phase Ⅱmetabolites,which is highly consistent with the meta-bolic mechanism of rats.Thus it indicates the rationali-ty of the methods.At the same time,it also provides the experimental basis for clarifying the substance basis of the drug.
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Polygonum capitatum is a traditional Chinese medicine widely used for urinary system diseases in the minority areas. Its research began in the 1980s. The major chemical constiturents in Polygonum capitatum is flavonids, phenolic acids, organic acids, al-dehydes, ketones, lignans and triterpen. The pharmacological activities were antibacterial, anti-inflammatory, antioxidant and antipy-retic analgesia. By referring to the relative literatures on Polygonum capitatum from home and abroad, the study advances in the chemi-cal constituents and pharmacological actions of Polygonum capitatum were reviewed to lay foundation for the reasonable exploitation and utilization of Polygonum capitatum.
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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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Aim To evaluate the inhibitive and induc-tive effects of Polygonum capitatum water extract on main cytochrome P450 isoforms in human and liver mi-crosomes of mouse in vitro for predicting the herb-drug interactions in clinical application. Methods The in vitro inhibitory effect was evaluated by incubating Po-lygonum capitatum water extract with the probe sub-strates of main phase I metabolic enzymes in human liver microsomes, including CYP1A2, CYP2E1, CYP2C9,CYP2C19 and CYP3A4. Mice were adminis-tered with Polygonum capitatum water extract at dosage of 0 . 58 g · kg-1 and 1 . 16 g · kg-1 by gastric lavage for successive 7 days and 14 days, then the cocktail-LC-MS/MS method was applied to assess the inductive effect of main CYP450 isoforms in mouse liver micro-somes. Results The IC50 values of Polygonum capita-tum water extract on main CYP450 isoforms in human liver microsomes were from 849 . 6 mg · L-1 to 2 287 mg·L-1 . Compared with the blank control group, the activites of CYP2C9 and CYP3A4 in 1. 16 g·kg-1 7 d group were about 49 . 9 % and 21. 1 % higher ( P <0. 01, P < 0. 05 ) respectively, the activities of CYP2C9 and CYP3A4 in 0. 58 g·kg-1 7 d group were 27. 6 % and 15. 5 % higher ( P <0. 01 , P <0. 05 ) respectively, the activities of CYP2C9 and CYP3A4 in 1. 16 g·kg-1 14 d group were 67. 5 % and 32. 1 %higher (P<0. 01) respectively, while the activities of CYP1 A2 , CYP2 E1 and CYP2 C19 were not increased significantly in Polygonum capitatum treatment group. Conclusions Polygonum capitatum water extract do not show the inhibitory effect on main CYP450 in hu-man liver microsomes. There is induction on CYP2C9 and CYP3 A4 in mouse liver microsomes by Polygonum capitatum water extract.
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Objective To establish HPLC characteristic spectrum of Polygonum Capitatum from GAP planting base, and provide reference for the overall quality control of Polygonum Capitatum. Methods HPLC analysis was performed on a DiamonsiL C18 chromatographic column (250 mm× 4.6 mm, 5μm) with the eluting system of gradient consisted of methanol and 0.2% H3PO4. The flow rate was 1.0 mL/min. The column temperature was maintained at 25℃ and the detection wavelength was at 254 nm.Results HPLC characteristic spectrum of Polygonum Capitatum samples from 10 different areas was established, which contained 11 common peaks, and the similarities of comparative results were over 90%.Conclusion The established method can be used to determine the characteristic spectrum of Polygonum Capitatum and can provide a basis for the overall quality control and quality standards of Polygonum 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.