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.

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.

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.

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.

种植年限对头花蓼土壤微生物群落的影响

【目的】探明不同种植年限头花蓼土壤微生物(细菌和真菌)群落组成及物种多样性的变化趋势,从土壤微生物的角度探究其连作障碍机制,为贵州头花蓼产业的可持续发展提供理论依据。【方法】采用Illumina测序技术,以头花蓼与玉米轮作地块土壤为对照(CK),通过对头花蓼连续种植2年(T2)、3年(T3)和4年(T4)地块土壤微生物进行测序分析,研究种植年限对头花蓼土壤微生物群落的影响。【结果】随连作年限增加,细菌群落丰度呈上升趋势,丰度从1620.30升至1787.22,物种多样性逐渐趋于平稳;真菌群落丰度呈下降趋势,丰度从635.00降至612.89,物种多样性变化不大。细菌群落:门水平下,变形菌门与酸杆菌门为优势菌群,相对丰度总占比>64%;变形菌门相对丰度显著降低(从40.80%降至34.80%),酸杆菌门显著增加(从24.20%升至29.10%);变形菌门(40.80%、40.20%、37.60%和34.80%)、浮霉菌门(1.50%、1.50%、2.60%和2.50%)在不同连作年限间相对丰度存在显著差异;属水平下,uncultured_bacterium_c_Subgroup_6所占比例最大,为10.66%~20.50%。真菌群落:门水平下,子囊菌门和担子菌门为优势菌群,其相对丰度总占比>61%,较CK逐年下降;被孢霉门和壶菌门在连作第4年(T_(4))几乎完全消失。属水平下,被孢霉属占比最大,为2.66%~14.30%,在连作第3年(T3)出现多孢囊霉属真菌。【结论】连作加大了头花蓼土壤中微生物群落差异。随着连续种植年限增加,变形菌门细菌、被孢霉门被孢霉属真菌等相对丰度逐渐降低,酸杆菌门细菌、子囊菌门镰刀菌属真菌等相对丰度逐渐增加,可能是头花蓼连作障碍发生的原因之一。

PB-BBD响应面法优化头花蓼提取工艺及抗氧化活性研究

目的利用Plackett-Burman和Box-Behnken响应面法优化头花蓼的总黄酮和总多酚超声提取工艺并研究其抗氧化活性。方法以头花蓼总黄酮和总多酚的综合得率为指标,通过单因素实验确定各影响因素的范围,再利用Plackett-Burman实验筛选影响综合得率的显著因素,最后采用Box-Behnken响应面法进行工艺优化;并通过考察提取物对DPPH自由基、羟基自由基的清除率和对Fe3+的还原能力来评价头花蓼的抗氧化性活性。结果影响综合得率的显著因素为超声功率、超声温度和超声时间,最优提取工艺为超声功率160W、超声温度58℃、超声时间38min、乙醇浓度40%、液料比25∶1(mL∶g),头花蓼中总黄酮和总多酚的综合得率为68.79mg·g^(-1),与模型预测值的相对误差为4.15%;当浓度为5mg·mL^(-1)时,此工艺条件下头花蓼提取物对DPPH自由基和羟基自由基的清除率分别为81.66%、84.93%,总还原能力达到2.48。结论采用基于PB实验设计和BBD响应面法优化得到的头花蓼总黄酮和总多酚提取工艺简便、稳定、可行,且得到的头花蓼提取物具有较强的抗氧化活性。

基于网络药理学与分子对接探索头花蓼抗肺炎的作用机制

目的:运用网络药理学与分子对接探索头花蓼抗肺炎的作用机制。方法:通过查阅文献收集头花蓼的化学成分,在chemdraw软件绘制分子结构图,通过PharmMapper数据库选择(NF)≥0.9的靶点蛋白获取潜在化合物的靶点;运用GeneCards、OMIM、DRUGBANK数据库以获得肺炎核心靶点;使用Metascape平台将头花蓼活性成分靶点和肺炎核心靶点交集进行GO和KEGG富集分析;使用Cytoscape3.8.2软件构建成分-靶点-通路图,AutoDock Tools 1.5.7、Pymol软件进行分子对接。结果:头花蓼中筛选获得38个活性成分、116个成分靶点、6个核心靶点;KEGG富集分析结果主要集中在IL-17信号通路、MAPK信号通路、TNF信号通路等;分子对接结果显示ALB、EGFR、CASP3、MAPK1、MAPK14、SCR与头花蓼主要化学成分的结合活性较好。结论:头花蓼中的核心化合物槲皮素、木犀草素、儿茶素等,可能通过ALB、EGFR、CASP3、MAPK1、MAPK14、SCR等靶点作用于IL-17、MAPK、TNF信号通路,从而达到治疗肺炎的作用。

Antioxidant, anti-quorum sensing and anti-biofilm potential of ethanolic leaf extract of Phrynium capitatum and Dryptes indica

Objective: To investigate the antioxidant and anti-infective potential of Phrynium capitatum and Dryptes indica extract. Methods: The antioxidant potentials were determined by DPPH radical scavenging, reducing power, hydroxyl radical scavenging and total antioxidant assays. We further examined anti-quorum sensing activity and inhibition of synthesis of pathogenic factor of Chromobacterium violaceum and Pseudomonas aeruginosa PAO1. Bioactive compounds were determined using gas chromatography–mass spectrometry analysis. In silico analysis was conducted to determine the binding affinity of bioactive compounds of plant extracts for the quorum sensing regulatory receptor LasR. Results: DPPH assay showed that the ethanolic extract of Phrynium capitatum and Dryptes indica at 500 μg/mL showed (86.96 ± 4.07)% and (74.83 ± 3.47)% inhibition, respectively. Hydroxyl radical scavenging assay showed (73.17 ± 3.03)% and (62.63 ± 4.59)% activity, respectively. The ethanolic extract of Phrynium capitatum and Dryptes indica showed high level of attenuation of quorum sensing regulated pyocyanin production. Confocal laser scanning microscopic analysis revealed that the extracts had the potential to effectively inhibit biofilm formation of Pseudomonas aeruginosa. Molecular docking analysis showed a better binding affinity of bioactive compounds from the extracts for the structure of LasR protein of Pseudomonas aeruginosa. Conclusions: The ethanolic extracts of Phrynium capitatum and Dryptes indica possess antioxidant activity and the potential to inhibit the quorum sensing system and its regulatory virulence traits in Pseudomonas aeruginosa PAO1.

头花杜鹃、陇蜀杜鹃及杜鹃属植物叶绿体基因组比较分析

头花杜鹃(Rhododendron capitatum)和陇蜀杜鹃(R.przewalskii)是极具观赏价值的野生花卉和药用植物。为探讨头花杜鹃和陇蜀杜鹃叶绿体基因组的遗传结构及进化特征,该研究利用Illumina HiSeq 4000平台对头花杜鹃和陇蜀杜鹃的叶绿体全基因组进行测序,经组装和注释后,结合7个已发表的杜鹃属植物叶绿体全基因组进行比较基因组学分析和系统发育分析。结果表明:(1)头花杜鹃和陇蜀杜鹃叶绿体全基因组呈典型的环状四分体结构,均由一个大单拷贝区(105 990、109 191 bp)、一个小单拷贝区(2 617、2 606 bp)和一对反向重复区(45 825、47 516 bp)构成,全长分别为200 257、206 829 bp。(2)头花杜鹃和陇蜀杜鹃叶绿体基因组中共鉴定出263个SSR位点,大部分SSR偏好使用A/T碱基,密码子偏好使用A/U结尾。(3)杜鹃属植物叶绿体全基因组中普遍存在基因丢失以及基因组重排等结构变异现象。该研究丰富了杜鹃属植物的基因组资源,为头花杜鹃、陇蜀杜鹃的资源开发、遗传进化、育种及系统发育相关研究提供了理论参考。

Study on the Pharmacological Identification of Polygonum capitatum

[Objectives]This study was conducted to establish a microscopic identification method of Polygonum capitatum Buch.Ham.ex D.Don.[Methods]The cross sections were identified by microscopic identification.[Results]The stem cross section of P.capitatum is round-like,and shows pericyclic fibers forming a ring,strongly lignified,many vascular bundles,and a hollow pith part.There are many starch granules in the powder,and single granules are more common;and fibers are mostly bundled or scattered,lignified or non-lignified,and calcium oxalate cluster crystals are common.There are many pollen grains,obtuse triangular or round-like,and some of them have three germination apertures.They have fine thorn-like protrusions on the outer wall,the surface of which has reticulate carvings.[Conclusions]The results of microscopic identification are reliable and can be used as the basis for identification of P.capitatum.

A Research Summary on the Chemical Constituents and Pharmacological Effects of the National Medicine Polygonum capitatum

Polygonum capitatum Buch.Ham.ex D.Don is a commonly used medicine in Zhuang people’s settlements,which has antipyretic,wind and evil-dispelling,dehumidifying and analgesic effects.The research on the chemical composition of P.capitatum began in the 1980 s.Modern scientific research has shown that it has antibacterial,cooling and blood sugar lowering effect.In order to better develop and utilize P.capitatum,this paper reviewed the progress of the chemical composition and pharmacological research of P.capitatum.

Identification of Ethnic Medicine Polygonum capitatum by Thin Layer Chromatography

[Objectives]To establish a thin-layer chromatography identification method for the ethnic medicinal materials of Polygonum capitatum.[Methods]The thin layer chromatography(TLC)method was used to identify materials.[Results]The TLC identification showed that in the chromatogram of the test sample,there were spots of the same color in the corresponding position of the chromatogram of the reference medicinal material,and the reproducibility was good.[Conclusions]The TLC identification and the determination results of the inspection items can provide a basis for the quality control of the medicinal materials of P.capitatum.

创面护理用苗药头花蓼双层纳米纤维功能敷料的制备及性质研究

目的制备头花蓼双层纳米纤维功能敷料,并对其外观形貌、内部结构及其性能进行研究。方法通过考察头花蓼提取物的主要成分没食子酸和槲皮素的抑菌活性和促愈合效果,将头花蓼作为活性成分,运用静电纺丝技术制备头花蓼双层纳米纤维功能敷料。利用扫描电子显微镜、傅里叶变换红外光谱和X-射线衍射对敷料的微观形貌及内部结构进行表征。并对敷料的吸水性、水蒸气透过率、机械性能、体外药物释放行为以及促伤口愈合效果进行研究。结果头花蓼双层纳米纤维功能敷料断面显示清晰的双层结构,平均直径为(476±88)nm,孔隙率为95.77%,无串珠现象,具有良好的吸水性、透气性、防护性、适合创面护理使用的机械性能以及较好的促进伤口愈合能力。结论头花蓼双层纳米纤维功能敷料有望成为在创面护理领域除传统创面敷料以外的又一种选择。

苗药头花蓼生药的综合鉴定

目的探讨苗药头花蓼生药综合鉴定的方法。方法选取黔产苗药头花蓼药材10批次,制作头花蓼药材植物标本,对其根、茎、叶、花、果等形态特征进行性状鉴别;制作头花蓼药材粉末,分别采用氯化铁(FeCl_(3))显色反应、盐酸-镁粉反应、氯化铝(AlCl 3)显色反应及薄层色谱法进行理化鉴别;采用显微镜对其药材粉末进行显微鉴别;采用植物基因组DNA提取试剂盒进行DNA分子标记鉴定。结果头花蓼茎丛生,叶椭圆形、长2~5 cm、宽1~2 cm、叶先端急尖基部楔形,花序头状、单生或顶生、成对,总状花序直立、近球形,花被淡红色;苗药头花蓼醇提液在FeCl_(3)显色反应中显蓝色、久置变深蓝色,在盐酸-镁粉反应中显深红色,在AlCl 3显色反应中于360 nm紫外灯下显黄色荧光;头花蓼粉末显微鉴别具有花粉粒、晶鞘纤维、纤维素、导管、淀粉粒、木栓细胞等特征碎片;头花蓼药材在500 bp附近显示清晰明亮的单一条带,测序显示序列差异主要集中在ITS1和ITS2区。结论由性状鉴别、理化鉴别、粉末显微鉴别及DNA分子标记鉴定结果,阐明了原鉴定药材为蓼科蓼属植物头花蓼Polygonum capitatum Buch.-Ham.ex D.Don。

头状骨、钩骨骨折伴第3、4、5腕掌关节半脱位1例

患者,男,39岁,2022年9月16日不慎摔伤,右腕关节疼痛难忍,立即至山东中医药大学附属医院创伤骨科就诊。CT检查显示:右头状骨、钩骨骨质不连续,断端分离移位,其旁见多发斑点状游离骨样影。诊断为:右头状骨、钩骨骨折伴第3、4、5腕掌关节半脱位。2022年9月19日在臂丛神经阻滞麻醉下行切开复位内固定术。

头花蓼化学成分及药理作用机制研究进展

头花蓼为贵州传统苗药,具有清热利湿、利水通淋等功效。其主要化学成分为黄酮类、木脂素类及挥发油类,还含有萜类、鞣质类等成分。近年来,因头花蓼具有抗炎、抗菌、抗氧化及降血糖等多种药理作用而成为研究热点。研究头花蓼相关国内外文献,综述其化学成分及药理作用机制,以期对头花蓼的药理研究及临床应用提供参考。

头花蓼不同入药部位总黄酮代谢模式研究进展

头花蓼皆为地上全草入药,富含黄酮类成分,治疗泌尿道感染疗效显著。但是头花蓼茎、花、叶等部位总黄酮含量差异悬殊,其基因组研究资源十分缺乏。课题组经过10余年对转录组、代谢组及其网络药理学的研究积累,有助于探索头花蓼不同入药部位总黄酮代谢模式。本文从头花蓼黄酮类成分药效研究、药效成分、基因表达等研究层次方面进行介绍,为头花蓼黄酮类成分最佳临床入药部位的选择提供理论依据。

头花蓼纳米纤维功能敷料的药效评价

目的评价头花蓼纳米纤维功能敷料(P-PVP-PCL)的药效。方法利用静电纺丝技术制备P-PVP-PCL,观察其微观形貌;考察P-PVP-PCL的抑菌活性、抗氧化活性和对小鼠成纤维L929细胞存活率、黏附性及迁移率的影响。通过建立大鼠背部皮肤伤口模型,考察医用纱布敷料、空白纳米纤维敷料(PVP-PCL)和P-PVP-PCL对创面愈合率的影响,观察创面组织病变和胶原纤维沉积情况,以及创面组织中血小板内皮细胞黏附分子1(CD31)阳性血管数量和转化生长因子β(TGF-β)蛋白表达。结果制得的P-PVP-PCL表面光滑,断面处可见双层结构,对金黄色葡萄球菌和大肠埃希菌的抑制率分别为(98.88±0.66)%、(94.75±1.41)%,抗氧化活性为(83.69±1.56)%,且P-PVP-PCL组的细胞活性均显著高于对照组和PVP-PCL组(P<0.05)。与医用纱布敷料相比,P-PVP-PCL更有利于L929细胞黏附;在48 h时,该组的细胞划痕已基本愈合。与医用纱布敷料组比较,PVP-PCL组和P-PVP-PCL组的大鼠创面愈合率均显著升高(P<0.05)。干预第14天时,P-PVP-PCL组创面已基本愈合,创面组织中胶原纤维排列相对整齐、密度相对均匀;CD31阳性血管数量和TGF-β蛋白表达与干预第7天比较有下降趋势,其中CD31阳性血管数量显著低于医用纱布敷料组和PVP-PCL组(P<0.05),TGF-β蛋白表达显著高于医用纱布敷料组和PVP-PCL组(P<0.05)。结论P-PVP-PCL在体外具有良好的抗菌和抗氧化活性,能够促进L929细胞的增殖、黏附和迁移;在体内能够促进大鼠伤口愈合。

基于网络药理学、微阵列数据分析和分子对接探索头花蓼治疗幽门螺杆菌相关性胃炎的分子机制

目的探索头花蓼(Polygonum capitatum,PC)治疗幽门螺杆菌相关性胃炎(Helicobacter Pylori associated gastritis,HAG)的作用机制。方法运用数据库识别PC活性化合物的作用靶点及HAG相关基因,并取交集获得PC治疗HAG的潜在靶标;利用Cytoscape 3.6.0构建“药物-活性成分-靶点-疾病”网络图和PC治疗HAG潜在靶蛋白的PPI网络,采用多个拓扑指标筛选出网络中的重要节点,运用STRING数据库进行GO和KEGG富集分析,获得PC治疗HAG的潜在信号通路,利用分子对接观察PC活性成分与关键靶蛋白的结合能力;在此基础上,通过体内外实验对PC治疗HAG的相关靶标进行验证。结果通过数据库识别出PC活性化合物及靶标,构建“药物-活性成分-靶点-疾病”网络图和潜在靶蛋白的PPI网络,多个拓扑指标筛选出52个hub genes,进一步的生物信息学分析和高通量测序显示,PC通过Akt/NF-κB/NLRP3通路对HAG发挥作用。基于此,通过实验发现PC作用于HAG GES-1细胞和HAG SD大鼠后,能够减少其IL-18和IL-1β的分泌,上调Akt及其磷酸化水平,减少NF-κB表达,抑制NLRP3炎症小体的活化,从而改善HAG炎症反应。结论PC可通过激活Akt及其磷酸化水平,抑制NF-κB和NLRP3炎症小体相关因子的表达,对HAG发挥治疗作用。本研究为阐释PC治疗HAG的作用机制提供了理论依据。