Using Network Pharmacology to Explore Therapeutic Effect of Polygonum capitatum on Renal Calculus in Rats

[Objectives]To explore the therapeutic effect of Polygonum capitatum on renal calculus in rats based on network pharmacology.[Methods]Through the preliminary construction of P.capitatum-urolithiasis disease target network,explore the active components,action pathway and action target of P.capitatum-urolithiasis treatment,and use 1%ethylene glycol+2%ammonium chloride to induce SD rat kidney calcium oxalate stone model to verify the efficacy of P.capitatum-urolithiasis treatment.[Results]Through the network pharmacological prediction,it is found that the important active components in P.capitatum were quercetin,gallic acid,rutin,silybin,catechin,kaempferol and so on;potential active targets include INS,CAT,IL-6,MOCOS,etc.The results also suggest that forkhead transcription factor signaling pathway(FoxO signaling pathway),tumor necrosis factor signaling pathway(TNF signaling pathway)and hypoxia-inducible factor signaling pathway(HIF-1 signaling pathway)are the core pathways.The results of biochemical indicators in animal experiment showed that the contents of serum urea nitrogen(BUN),creatinine(Cr)and malondialdehyde(MDA)in renal tissue in the treatment group(200,500 mg/kg)were significantly lower than those in the model group,while the content of superoxide dismutase(SOD)was significantly higher than that in the model group.In addition,the kidney tissue H&E staining sections showed that P.capitatum alcohol extract administration group rats kidney calcium oxalate crystals were significantly reduced compared with the model group,the degree of renal tubular lumen expansion was lighter than the model group,suggesting that P.capitatum alcohol extract has the effect of improving renal calculus in rats.[Conclusions]This study provides a theoretical reference for the deep development of P.capitatum in the treatment of renal calculus.

Screening for Antioxidant Phenolic Compounds from Polygonum capitatum

[Objectives]To discover antioxidant natural products from the famous Hmong medicinal plant Polygonum capitatum.[Methods]The antioxidant activities of the isolated components were evaluated by ABTS and DPPH assays.[Results]A total of 27 free phenolics were isolated form P.capitatum.Then the in vitro antioxidant potential of these components was evaluated according to the DPPH and ABTS radical scavenging assays.Among them,five compounds(13,14,17,23,and 25)showed most significant ABTS radical-scavenging activity(IC 50 values of 3.81-15.09μg/mL).And 12 components(1,2,6,7,9,12,13,14,16,17,23,and 25)showed notable radical scavenging activity against DPPH(inhibition rates>88%).[Conclusions]Most of the above bioactive compounds were reported for the first time.

A New Flavonoid Glycoside from Polygonum capitatum

[Objectives]To discover novel compounds with significant anti-inflammatory activity in the alcohol extract of Polygonum capitatum.[Methods]Firstly,a new flavonoid glycoside,capitaone B(1),was isolated from the ethyl acetate extract from P.capitatum,and then 27 compounds were screened using NO anti-inflammatory activity model.[Results]Four compounds,such as kaempferol(12),1,2,6-trigalloyl-β-d-glucose(15),catechin(16)andβ-sitosterol(26),could significantly inhibit LPS-induced NO production in macrophages,with IC 50 values of 15.31,8.43,6.92 and 5.72μM,respectively.[Conclusions]The chemical composition and anti-inflammatory activity of P.capitatum were preliminarily studied,and the results provide a theoretical basis for further research on the action mechanism of subsequent anti-inflammatory active compounds of P.capitatum.

In vivo recognition of bioactive substances of Polygonum multiflorum for protecting mitochondria against metabolic dysfunction-associated fatty liver disease

BACKGROUND Metabolic dysfunction-associated fatty liver disease(MAFLD)is a severe threat to human health.Polygonum multiflorum(PM)has been proven to remedy mitochondria and relieve MAFLD,but the main pharmacodynamic ingredients for mitigating MAFLD remain unclear.AIM To research the active ingredients of PM adjusting mitochondria to relieve highfat diet(HFD)-induced MAFLD in rats.METHODS Fat emulsion-induced L02 adipocyte model and HFD-induced MAFLD rat model were used to investigate the anti-MAFLD ability of PM and explore their action mechanisms.The adipocyte model was also applied to evaluate the activities of PM-derived constituents in liver mitochondria from HFD-fed rats(mitochondrial pharmacology).PM-derived constituents in liver mitochondria were confirmed by ultra-high-performance liquid chromatography/mass spectrometry(mitochondrial pharmacochemistry).The abilities of PM-derived monomer and monomer groups were evaluated by the adipocyte model and MAFLD mouse model,respectively.RESULTS PM repaired mitochondrial ultrastructure and prevented oxidative stress and energy production disorder of liver mitochondria to mitigate fat emulsion-induced cellular steatosis and HFD-induced MAFLD.PM-derived constituents that entered the liver mitochondria inhibited oxidative stress damage and improved energy production against cellular steatosis.Eight chemicals were found in the liver mitochondria of PM-administrated rats.The anti-steatosis ability of one monomer and the anti-MAFLD activity of the monomer group were validated.CONCLUSION PM restored mitochondrial structure and function and alleviated MAFLD,which may be associated with the remedy of oxidative stress and energy production.The identified eight chemicals may be the main bioactive ingredients in PM that adjusted mitochondria to prevent MAFLD.Thus,PM provides a new approach to prevent MAFLD-related mitochondrial dysfunction.Mitochondrial pharmacology and pharmacochemistry further showed efficient strategies for determining the bioactive ingredients of Chinese medicines that adjust mitochondria to prevent diseases.

Systematic Evaluation of Pharmacognostic Identification of Polygonum capitatum

[Objectives] To investigate the systematic evaluation of pharmacognostic identification of Polygonum capitatum . [Methods] 10 batches of P. capitatum cultivated in Guizhou were chosen for plant samples. Macroscopical identification was conducted on plant roots, stems, leaves, flowers and fruits. The P. capitatum powder was processed for physical and chemical distinction by FeCl 3 chromogenic reaction, hydrochloric acid magnesium powder reaction, AlCl 3 color development reaction and thin-layer chromatography.Microscope identification was carried out on the powder. Plant genome DNeasy Plant Kit was adopted for DNA molecular marker identification. [Results] The results showed that the stem of P. capitatum was tufted, the leaves were oval, 2 to 5 cm long, and 1 to 2 cm wide;the leaf apex was acute and cuneate at the base, the inflorescence was capitate, paired or solitary;the raceme was erect and nearly spherical, and the perianth was light red. Furthermore, for the chromogenic reaction of FeCl 3 ethanol extract of P. capitatum , appeared blue and turned to dark blue after long time storing at room temperature. For the reaction of hydrochloric acid magnesium powder, the alcohol extract of P. capitatum , exhibited deep red. In the color reaction of AlCl 3, the alcohol extract revealed yellow fluorescence under 360 nm UV lamp. Microscope identification of the powder displayed pollen grains, crystal sheath fibers, cellulose, vessels, starch grains, cork cells, and other characteristic fragments. In addition, DNA barcoding electrophoresis results showed that P. capitatum showed a clear and bright single band near 500 bp, and further sequencing results showed that the sequence differences were mainly concentrated in ITS1 and ITS2 region. [Conclusions] Systematic evaluation for the identification of P. capitatum is established, which combines with macroscopic identification, physicochemical identification, powder microscope identification, and DNA molecular identification. Finally, the original medicinal material is identified as P. capitatum Buch.-Ham. ex D. Don.

Antioxidant,Anti-inflammatory,and Antibacterial Activities of Different Extracts from Polygonum capitatum

[Objectives]To investigate the antioxidant,anti-inflammatory and antibacterial activities of different extracts(aqueous,ethanol,ethyl acetate and n-butanol extracts)of Miao medicine Polygonum capitatum.[Methods]Eleven batches of P.capitatum in Guizhou province were collected,and water,ethanol,ethyl acetate and n-butanol extracts were prepared by reflux extraction.Antioxidant activity was determined by radical scavenging capacity of 1,1 diphenyl-2-picyl hydrazine(DPPH),anti-inflammatory activity was screened by lipopolysaccharide(LPS)induced RAW264.7 cells to produce NO,and the minimum inhibitory concentration(MIC)was screened by broth microdilution method.[Results]When the concentration of ethyl acetate extract was 10 mg/L,the scavenging rate of DPPH ranged from 90%to 99%.The(MIC of the ethyl acetate extract against Staphylococcus aureus(SA),Pseudomonas aeruginosa(PA)and Escherichia coli(EC)was 0.18-0.65,0.13-0.82,and 0.15-0.78 g/L,respectively.In the anti-inflammatory activity,ethyl acetate extract inhibited NO production with inhibition rate of 70%.[Conclusions]The ethyl acetate extract and ethanol extract of Miao medicine P.capitatum have strong antioxidant,anti-inflammatory and antibacterial activities.

Qualitative and Quantitative Analysis of Rhizoma of Polygonum cuspidatum

Aim To establish reliable methods for evaluating the quality of rhizoma of Polygonum cuspidatum( Huzhang in Chinese). Methods TLC and HPLC were employed for the chemical identification and content determination,respectively. Results A qualitative TLC method and a quantitative HPLC method with piceid as the reference substance were established, respectively. With piceid as the reference substance and ethyl acetate-methanol-formic acid-water ( 19:3:0.5:1) as the mobile phase, a TLC method for the identification of Huzhang from the commonly used crude drugs of the same family was also set up. Conclusion The established TLC method can reasonably appraise the quality of the drug and easily distinguish Huzhang from the other commonly used crude drugs of the same family. The HPLC method for determining piceid is simple, reproducible, accurate, and feasible.

Comparison of Photosynthetic Adaptability Between Kobresia humilis and Polygonum viviparum on Qinghai Plateau

The chlorophyll fluorescence parameters of Kobresia humilis Serg. and Polygonum viviparum L. grown at two different altitudes (3?200 m, 3?980 m) were measured and the ultrastructure of chloroplasts were observed for studying the photosynthetic adaptability of plants to the influences of stress conditions in alpine environment. Rfd _values, the vitality index, in leaves of K. humilis and P.viviparum grown at 3?980 m were higher than those at 3?200 m. The higher ratio of F v/F o and F v/F m in leaves of K. humilis and P.viviparum indicated that the rate of photosynthetic conversion of light energy increased at higher altitude. Ratios of F v/F o and F v/F m and Rfd _values in K.humilis were higher than that in P.viviparum grown at the same altitude. There were more irregular chloroplasts in leaves of both species grown at higher altitude. Many irregular chloroplasts such as swollen thylakoid, deformed chloroplast envelope, were observed in P.viviparum grown at 3?980 m, but few in K. humilis . These results were discussed in relation to the photosynthetic adaptability of alpine plants and the different adaptive competence between K.humilis and P.viviparum .

Novel Stilbene Glycosides from Polygonum multiflorum

Two new stilbene glycosides (1 and 2), together with nine known compounds (3-11), were isolated from the water extract of Polygonum multiflorum Thunb. The structures of the new compounds were elucidated by their chemical properties and spectroscopic analyses, including extensive 2D NMR experiments. Compound 2 showed strong DNA cleavage activity, and compounds 1, 2 and 10 (2, 3, 4′, 5_tetrahydroxy_ trans _stilbene_2_O_β_ D _glucopyranoside) exhibited significant inhibition of lipid peroxidation.

Variation and Cluster Analysis on Leaf Characters from Different Provenance Sources of Polygonum multiflorum Thunb

[Objective] The aim was to study the variation of leaf characters from different provenance sources of Polygonum multiflorum Thunb,as well as to carry out cluster analysis on P.multiflorum from different provenance sources to provide basis for the classification,identification,breeding and improved variety selection of P.multiflorum.[Method] Leaf shape characters of 31 copies of germplasm resources in the major distribution region of the whole country were determined,and the genetic variation of P.multiflorum leaves from different producing areas was analyzed.[Result] The leaf characters of single plant of the same experimental provenance source of P.multiflorum were relatively stable,the variation was mainly found on the single leaf area,1/2 leaf width,leaf width and other indicators;the variation of each leaf character among different provenance sources was obvious,and the variation was mainly found on the single leaf weight,leaf area,1/2 leaf width,leaf length and other indicators.The correlation analysis of each leaf character in P.multiflorum suggested that the single leaf area and single leaf weight showed extremely significant positive correlation with leaf length,1/2 leaf width,leaf width,leaf thickness and leaf stem length,while the single leaf area and single leaf weight showed significant negative correlation with WWR（leaf width/1/2 leaf width）and LWR（leaf length/1/2 leaf length）,in addition,several macroscopic leaf characters such as leaf length,1/2 leaf width,leaf width,leaf stem length showed extremely positive correlation.The main component analysis result suggested that the contribution rate of accumulation variance of the front three main components was up to 97.4%,which could better reflect the comprehensive performance of leaf characters of different provenance sources of P.multiflorum.The cluster analysis showed that the experimental 31 copies of P.multiflorum provenance sources should be divided into three classes,the first class was distributed in the Middle,Western of Guizhou,northwestern of Guangxi and western areas with higher altitude;the second class was distributed in Hunan,Hubei,Sichuan,Guangdong and the most area of Guangxi;the third class was distributed in Anhui,Jiangsu and Henan and Shandong.[Conclusion] Cluster analysis of leaf characters indicated that the kinds of provenance sources which the geographical position was closer could be got together.The study had provided a certain basis for the classification of P.multiflorum.

Accumulation Characteristics of Cd in Polygonum pubescens Bl

[Objective] The research aimed to study the response and accumulation characteristics of Cd in Polygonum pubescens Bl.[Method] Taking Hoagland nutritional solution as the culture substrate,eight kinds of Cd concentrations （0,25,50,100,200,500,800,1 000 mg/L） were set up.[Result] Under low concentrations of Cd （25 and 50 mg/L）,the biomass of P.pubescens had no significant difference with CK （P0.05）.Under all the test concentrations of Cd,Cd content in the roots and shoots of P.pubescens exceeded 100 mg/kg and the enrichment coefficients of Cd were over 1.With the increasing of Cd concentration,Cd content and Cd accumulation amount in P.pubescens increased significantly.When Cd concentration exceeded 50 mg/L,translocation capacity coefficient was greater than 1.[Conclusion] Polygonum pubescens has high tolerance and accumulation capacity of Cd,and it may has some potential on the phytoremediation of Cd-contaminated soil.

The New Flavonoids from Polygonum sphaerostachyum(Polygonaceae)

Two novel flavone glycosides, 3′_hydroxy_5,4′_dimethoxy_6,7_methylenedioxyflavone_3_O_[β_D_xylopyranosyl(1→6)]_β_D_glucopyranoside (1) and 5,4′_dimethoxy_3′_isopropenylacetyl_6,7_methylenedioxyflavone_3_O_[β_D_xylopyranoxyl(1→6)]_β_D_glucopyranoside (2), were isolated from Polygonum sphaerostachyum Meisn., and their structures were deduced by spectral and chemical methods. This is the first report on the isolation of flavone glycosides from P. sphaerostachyum.

人工湿地园沼泽植物水蓼(Polygonum hydropiper L.)的蒸腾特性日变化

对人工湿地园中沼泽植物水蓼(PolygonumhydropiperL.)蒸腾特性日变化进行了研究。结果表明:水蓼叶片的蒸腾速率日进程在晴朗的天气呈单峰曲线变化,最高峰值出现在下午的14:00。受光量子通量密度的影响最大,相关系数为0.668。与相对湿度的变化呈正相关(r=0.607),说明水蓼的蒸腾速率日变化是受其自身所具有的特殊生理特性所决定。叶片气孔阻力直接影响蒸腾速率。

Mn对超富集植物短毛蓼(Polygonum pubescens Blume)抗氧化机理的影响

采用水培的方法,研究了不同浓度Mn(0、0.5、1、2、4、8mmol·L-1)对新发现的Mn超富集植物短毛蓼(Polygonum pubescens Blume)生长、Mn吸收及Mn对其抗氧化酶和非酶系统的影响。结果表明,锰处理显著增加了(P<0.05)短毛蓼根、茎、叶中Mn的含量,锰处理还引起了短毛蓼叶片中过氧化氢(H2O2)和丙二醛(MDA)的累积。当Mn处理浓度大于1mmol·L-1时,显著降低了短毛蓼的株高、株重(P<0.05);当Mn处理浓度为8mmol·L-1时,短毛蓼叶片中叶绿素a、叶绿素b、叶绿素a+b含量最低,与对照差异显著(P<0.05)。Mn处理显著提高了短毛蓼叶片中超氧物歧化酶(SOD)活性(P<0.05),而过氧化物酶(POD)、过氧化氢酶(CAT)和抗坏血酸过氧化物酶(APX)的活性呈先升后降趋势,表明Mn处理打破了短毛蓼活性氧物质的正常代谢,并启动了抗氧化酶系统。8mmol·L-1的Mn处理,显著提高了短毛蓼叶片中巯基(-SH)、还原型谷胱甘肽(GSH)的含量(P<0.05),比对照分别提高了10.6%和20%,表明-SH、GSH在短毛蓼缓解Mn毒害的过程中起着重要作用。

Three New Anthraquinones from Polygonum cillinerve

Three new anthraquinones, emodin-8-β-D-（2＂-O-coumarate）glucoside 1, emodin-8-β-D-（6＇-O-acetyl）glucoside 2 and physicon-8-β-D-（6＇-O-acetyl）glucoside 3, were isolated from the roots of Polygonum cillinerve and their structures were established by spectroscopic methods. The biological activity indicated that compound 1 had the scavenging activity on 1,1-diphenyl-2-picrylhydrazyl （DPPH） radicals （the IC50 = 8.5 μmol/L）, and compound 1-3 showed no activities against HL-60 and BCJC-823 cells by MTT method in vitro.

扫描电镜下几种蓼属(Polygonum)植物叶表皮的微形态学特征

应用扫描电镜对蓼属８种植物叶表皮形态进行了观察。结果表明气孔外拱、保卫细胞极区、表皮细胞外壁角质层表面和外角质层的蜡质分泌物等性状状态在８种植物的分布呈现出明显差异。

Single-nucleotide polymorphisms of HLA and Polygonum multiflorum-induced liver injury in the Han Chinese population

BACKGROUND Polygonum multiflorum is one of the leading causes of herb-induced liver injury in China.HLA-B*35:01 is reported to be a potential biomarker of Polygonum multiflorum-induced liver injury(PM-DILI).However,little is known about the relationship between single-nucleotide polymorphisms(SNPs) and PM-DILI.AIM To identify SNPs that indicate susceptibility to PM-DILI METHODS We conducted a systematic study enrolling 382 participants from four independent hospitals,including 73 PM-DILI patients,118 patients with other drug-induced liver injury(other-DILI) and 191 healthy controls.Whole-exome sequencing was performed for 8 PM-DILI patients and 8 healthy controls who were randomly selected from the above subjects.Nineteen SNPs that showed high frequencies in the 8 PM-DILI patients were selected as candidate SNPs and then screened in 65 PM-DILI patients,118 other-DILI patients and 183 healthy controls using the MassARRAY system.HLA-B high-resolution genotyping was performed for the 73 PM-DILI and 118 other-DILI patients.The Han-MHC database was selected as a population control for HLA-B analysis.P <6.25 x 103 after Bolferroni correction was considered significant.RESULTS The frequencies of rslll686806 in the HLA-A gene,rs1055348 in the HLA-B gene,and rs202047044 in the HLA-DRB1 gene were significantly higher in the PM-DILI group than in the control group [27.2% vs 11.6%,P=1.72×105,odds ratio(OR)=3.96,95% confidence interval(Cl):2.21-7.14;42.5% vs 8.6%,P=1.72×10-19 OR=13.62,95% CI:7.16-25.9;22.9% vs 8.1%,P=4.64×106,OR=4.1,95% CI:2.25-7.47].Only rs1055348 showed a significantly higher frequency in the PM-DILI group than in the other-DILI group(42.5% vs 13.6%,P=1.84×10-10,OR=10.06,95% Cl:5.06-20.0),which suggested that it is a specific risk factor for PM-DILI.rs1055348 may become a tag for HLA-B*35:01 with 100% sensitivity and 97.7% specificity in the PM-DILI group and 100% sensitivity and 98.1% specificity in the other-DILI group.Furthermore,HLA-B*35:01 was confirmed to be associated with PM-DILI with a frequency of 41.1% in the PM-DILI group compared with 11.9%(P=4.30×10-11,OR=11.11,95% CI:5.57-22.19) in the other-DILI group and 2.7%(P=6.22×10-166,OR=62.62,95% Cl:35.91-109.20) in the Han-MHC database.CONCLUSION rslll686806,rs1055348,and rs202047044 are associated with PM-DILI,of which,rs1055348 is specific to PM-DILI.As a tag for HLA-B*35:01,rs1055348 may become an alternative predictive biomarker of PM-DILI.

基于trnL-F序列探讨杠板归Polygonum perfoliatum的系统位置

杠板归(Polygonum perfoliatum L.)的系统位置一直存在争议,文中以塔黄为外类群,采用最大简约法对杠板归及其近缘类群的trnL-F序列进行了系统发育分析,结果表明:(1)杠板归和刺蓼为姊妹群,自展分析的支持率为99%,分子证据支持杠板归归入刺蓼组,而没有必要单立组或属。(2)刺蓼组、春蓼组和头状蓼组植物聚在一起,自展支持率为100%,说明它们之间有很近的亲缘关系。

Two new coumarin glucosides biosynthesized by transgenic hairy roots of Polygonum multiflorum

The glycosylation of hydroxylcoumarin was investigated by using suspension cultures of hairy roots of Polygonum multiflorum. Two new coumarin glucosides （3 and 4） were biosysthesized by regioselectively glycosylation of corresponding substrates （1 and 2） in the system. The structures of two products were identified as 7-hydroxy-4-methylcoumarin 5-O-β-D-glucopyranoside and 7- hydroxy-3,4-dimethylcoumarin 5-O-β-D-glucopyranoside on the ground of chemical and spectroscopic methods, respectively. 2007 Rong Min Yu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

Simultaneous determination of human plasma protein binding of bioactive favonoids in Polygonum orientale by equilibrium dialysis combined with UPLC–MS/MS

A simple and selective ultra performance liquid chromatography--electrospray ionization tandem mass spectrometry （UPLC-ESI-MS/MS） assay was developed for the determination of the human plasma protein binding of four bioactive ftavonoids （such as orientin and vitexin） in Polygonum orientale. Protein precipitation was used for sample preparation. Equilibrium dialysis technique was applied to determine the plasma protein binding under physiological conditions. The separation was achieved through a Waters C i s column with a mobile phase composed of 0.1% formic acid in acetonitrile and 0.1% aqueous formic acid using step gradient elution at a flow rate of 0.35 mL/min. A Waters ACQUITYTM TQD system was operated under the multiple reaction monitoring （MRM） mode of positive electrospray ionization. All of the recovery, precision, accuracy and stability of the method met the requirements. Good correlations （r 〉 0.99） of the four compounds were found, which suggested that these compounds can be simultaneously determined with acceptable accuracy. Results showed that the plasma protein bindings of the four bioactive flavonoids were in the range of 74-89% over the six concentrations studied. The binding parameters containing protein binding affinity, protein binding dissociation constant, and protein binding site were studied. The maximum ability to bind with protein was also determined in the assay in order to understand the drug-protein binding of each compound better.