Effect of Elephantopus scaber L.Extract on Acute Pleurisy in Rats

[Objectives]To study the anti-inflammatory effect of Elephantopus scaber L.extract on acute pleurisy induced by carrageenan in rats,and to explore its anti-inflammatory mechanism.[Methods]The active sites of E.scaber L.were extracted by ethanol reflux method.The extracts of different concentrations of E.scaber L.were used as the study object,and dexamethasone was used as the positive control drug.The anti-inflammatory effects of E.scaber L.extracts were studied by measuring the levels of malondialdehyde(MDA),prostaglandin E_(2)(PGE_(2)),tumor necrosis factor(TNF-α),interleukin-1β(IL-1β)in pleural fluid and serum nitric oxide(NO),MDA,PEG_(2),TNF-α,IL-1βin rats with acute pleurisy induced by carrageenan.[Results]E.scaber L.extracts in three doses could reduce the levels of inflammatory factors in pleural fluid and serum,and inhibit acute pleurisy in rats.It was speculated that the anti-inflammatory mechanism was related to the inhibition of the release of inflammatory factors and the antioxidant effect of extracts of three doses of E.scaber L.[Conclusions]This experiment provides a basis for the development and application of E.scaber L.

Sesquiterpene Lactones from Elephantopus scaber

A new germacranolide sesquiterpene lactone, isoscabertopin, was isolated from Elephantopus scaber together with the known scabertopin. Their structures were determined by spectroscopic methods.

Antineoplastic effects of deoxyelephantopin,a sesquiterpene lactone from Elephantopusscaber, on lung adenocarcinoma (A549) cells

OBJECTIVE： Deoxyelephantopin, a sesquiterpene lactone from Elephantopus scaber, showed inhibition of the growth of various tumor cells in vitro. In the present study, we investigated the cytotoxicity and apoptosis-inducing capacity of deoxyelephantopin on lung adenocarcinoma （A549） cells. METHODS： The cytotoxic effect of deoxyelephantopin on A549 cells and normal lymphocytes was evaluated using 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide （MTT） assay and 50% inhibitory concentration （IC50） value was determined. The self-renewal and proliferating potential of A549 cells after treatment with deoxyelephantopin were examined by colony formation assay. Cellular morphology of deoxyelephantopin-treated cells was observed using phase- contrast microscopy. The induction of apoptosis was evaluated using acddine orange and ethidium bromide staining, Hoechst 33342 staining, terminal deoxynucleotidyl transferase-mediated dUTP biotin nick end-labeling （TUNEL） assay, DNA fragmentation analysis and Annexin V-fluorescein isothiocyanate staining by flow cytometry. Activation of caspases was detected using fluorogenic substrate specific to caspases 2, 3, 8 and 9 and flow cytometric analysis. The total cellular DNA content and expression of cleaved poly （ADP-ribose） polymerase was also analyzed. RESULTS： Deoxyelephantopin exhibited cytotoxicity to A549 cells （IC50 = 12.287 μg/mL）, however, there was no toxicity towards normal human lymphocytes. Deoxyelephantopin suppressed the colony-forming ability of A549 cells in a dose-dependent manner. Acridine orange, ethidium bromide and Hoechst 33342 staining showed cell shrinkage, chromosomal condensation and nuclear fragmentation, indicating induction of apoptosis. Deoxyelephantopin increased apoptosis of A549 cells, as evidenced by more TUNEL-positive cells. DNA fragmentation and Annexin V staining revealed late-stage apoptotic cell population. Deoxyelephantopin inhibited A549 cell growth by cell cycle arrest at G2/M phase and induced apoptosis through both extrinsic and intrinsic pathways. CONCLUSION： These results suggest that deoxyelephantopin has great potential as a new chemotherapeutic agent to be developed further for the treatment of lung cancer.

A review of research on the chemical constituents and pharmacological effects of Elephantopus tomentosus L.

Elephantopus tomentosus,belonging to the genus Elephantopus,is widely distributed in the coastal areas of southern China and tropical regions,used locally as traditional folk medicine.Previous phytochemistry studies on Elephantopus tomentosus led to the isolation of sesquiterpenoids,triterpenoids,flavonoids and other compounds.Research has shown that these compounds possess multiple biological activities,which have attracted great attention of researchers worldwide.This study reviews the chemical constituents and biological activities of the Elephantopus tomentosus in order to better explore and utilize Elephantopus tomentosus.

Effect of Elephantopus scaber Linn on community acquired pneumonia through TLR4/NF-κB signaling pathway

Objective:To observe the effect of Elephantopus scaber Linn on community-acquired pneumonia and its relationship with the expression of TLR4/NF-κB pathway and the downstream inflammatory cytokines IL-6,IL-8,TNF-α.and to explore its molecular mechanism for the treatment of community-acquired pneumonia,so as to provide new ideas and theoretical basis for the treatment of community-acquired pneumonia.Methods:140 patients with community-acquired pneumonia were randomly divided into observation group and control group,with 70 cases in each group.Observation group:Elephantopus scaber Linn+NS atomized inhalation+intravenous injection of ceftazidine;Control group:intravenous injection of ceftazidine;Meanwhile,70 healthy subjects were selected as the healthy control group.The expressions of TLR4,NF-kB,IL-6,IL-8 and TNF-αin serum of observation group,control group before and after treatment and healthy control group were detected by enzyme linked immunosorbent assay(ELISA),and the efficacy of Elephantopus scaber Linn in the treatment of community acquired pneumonia was observed.Results:Compared with the control group,the observation group was significantly better than the control group in recovery rate,total effective rate,number of days for the disappearance of symptoms such as fever,cough,expectoration,with statistical significance(P<0.05);Compared with the healthy control group,the serum TLR4,NF-κB,IL-6,IL-8,TNF-αwere significantly different(P<0.05)between the observation group and the control group;Serum TLR4,NF-κB,IL-6,IL-8,TNF-αwere significantly different(P<0.05)in the observation group before and after treatment with Elephantopus scaber Linn;Compared with the control group after treatment,there were significantly different(P<0.05)in serum TLR4,NF-κB,IL-6,IL-8 and TNF-αin the observation group after treatment.Conclusion:Serum TLR4,NF-κB,IL-6,IL-8,TNF-αwere highly expressed in patients with community-acquired pneumonia,Elephantopus scaber Linn can decreased the expression of TLR4 and NF-κB in blood,and its downstream inflammatory factors also decreased significantly.There were significantly different(P<0.05)in blood TLR4 and NF-κB between the observation group and the control group after treatment.It is suggested that Elephantopus scaber Linn may inhibit TLR4/NF-kB signal pathway to exert anti-inflammatory effect.Elephantopus scaber Linn has a definite effect and can significantly improve the clinical symptoms,and effectively shorten the treatment cycle.

Isolation and identification of chemical constituents from Elephantopus scaber Linn.

Elephantopus scaber L.,as a popular Chinese medicinal herb of the Compositae family,is widely distributed in America,Africa and Asia.In the present study,five compounds were isolated from the 70%EtOH extract of the whole herb from Elephantopus scaber L.,including two lignans and three flavones.Their chemical structures were identified based on NMR spectroscopic analysis and comparison with the data reported in literature.It is noteworthy that compounds 1-5 were isolated from Elephantopus scaber L.for the first time and their chemotaxonomic significance was discussed.

Phenolic compounds from Elephantopus scaber L.

Eight compounds,(+)-syringaresinol(1),apigenin(2),3,5-dimethoxy-4-hydxyphenylpropanol(3),3,4,5-trimethoxy benzoic acid,(4)ferulaic acid(5),trans-p-hydroxycinnamic methyl ester(6),4-hydroxy-3-methoxybenz-oic acid(7)and p-methoxy benzoic acid(8)were isolated from the 70%ethanol extract of the whole herb of Elephantopus scaber L.The structures of all compounds were identified by spectral data analysis.All compounds were obtained for the first time from Elephantopus scaber L..

Research review on the main chemical constituents and pharmacological effects of Elephantopus scaber L.

Elephantopus scaber L.belongs to Elephantopus plant of Compositae,is widely used as the common Chinese herbal medicine in folk.Phytochemical investigations of the E.scaber have resulted in the isolation of triterpennoids,sesquiterpene lactones,sesquiterpene phenols,steroids,flavones,anthraquinones,peptides,lipid compounds and aryl compounds.It possesses the effects of antibacterial,clearing away heat and detoxification,detumescence and diuresis,and is used for treating lung cancer,cervical cancer,liver cancer,nasopharyngeal cancer,breast cancer,anemia and diarrhea.The research progress in the chemical constituents ofE scaber and pharmacological effects are reviewed for better explore and utilize theE scaber resource.

Virtual screening of active ingredients,potential targets and pathways from Elephantopus scaber L.against liver cancer based on network pharmacology

Elephantopus scaber L.,belonging to Elephantopus plant of Compositae,is widely used as the common Chinese herbal medicine in folk.According to the phytochemical investigations,E.scaber is used to treat several cancers,anemia and diarrhea on account of the property of the complex components and multi-targets.However,the underlying molecular mechanisms of herb remain unclear.In this report,network pharmacology method is used to analyze the relation among the small-molecule compounds of E.scaber,target proteins,biological pathways and liver cancer.The potential active compounds from the E.scaber,potential target proteins and the key pathways were predicted by network pharmacology models.We believe that our present study is useful to find novel lead compounds for liver cancer.

Virtual screening of the active compounds and potential targets of Elephantopus tomentosus L. for the treatment of liver cancer based on a network pharmacology approach

Liver cancer is the leading cause of cancer-related death.As the clinical treatment for this disease is not satisfactory,it is urgent to discover new medications to treat liver cancer.Elephantopus tomentosus L.is a traditional whole grass herb,which contains sesquiterpene lactones,triterpenoids,aldehyde caffeic with good anti-tumor effect.In this study,molecular docking and network analysis were carried out to identify the active compounds,and predict the potential targets of E.tomentosus for the treatment of liver cancer.These attempts may provide insights for finding novel lead compounds for the treatment of liver cancer.

双标多测法同时测定地胆草中11种成分的含量

目的建立双标多测法同时测定地胆草中新绿原酸、绿原酸、隐绿原酸、木犀草苷-7-O-葡萄糖醛酸苷、异绿原酸B、异绿原酸A、异绿原酸C、去氧地胆草素、异去氧地胆草素、异地胆草种内酯、地胆草种内酯的含量。方法分析采用Waters Symmetry C_(18)、Phenomenex C_(18)、Agilent ZORBAX Eclipse Plus C_(18)色谱柱(4.6 mm×250 mm,5.0μm);流动相乙腈-0.1%磷酸,梯度洗脱;体积流量1.0 mL/min;柱温35℃;检测波长220、326 nm。以绿原酸为内标,计算新绿原酸、隐绿原酸、木犀草苷-7-O-葡萄糖醛酸苷、异绿原酸B、异绿原酸A、异绿原酸C相对校正因子;以异去氧地胆草素为内标,计算去氧地胆草素、地胆草种内酯、异地胆草种内酯相对校正因子,测定其含量。再进行聚类分析、主成分分析、正交偏最小二乘法-判别分析。结果11种成分在各自范围内线性关系良好(r≥0.9990),平均加样回收率95.3%~103.4%,RSD 0.32%~3.45%。双标多测法所得结果与外标法接近。异绿原酸A、异绿原酸C、异绿原酸B、绿原酸、木犀草苷-7-O-葡萄糖醛酸苷、隐绿原酸为质量差异成分。结论该方法稳定可靠,可用于地胆草的质量控制。

白花地胆草化学成分分离鉴定

目的:研究菊科地胆草属植物白花地胆草Elephantopus tomentosus L.的化学成分。方法:采用硅胶、MCI、Sephadex LH-20葡聚糖凝胶柱色谱、半制备高效液相和重结晶等方法对白花地胆草全草的醇提物进行分离纯化,并通过核磁共振波谱和质谱技术,结合文献数据进行结构鉴定。结果:从白花地胆草中分离得到16个化合物,分别鉴定为:乙酰异乔木萜醇(1)、camarolide(2)、桦木醇(3)、桦木酮酸(4)、乌索酸内酯(5)、齐墩果-9(11),12-二烯-3β-醇(6)、22-氧代-20-蒲公英赛烯-3β-醇(7)、3β-羟基-11-氧代-乌苏烷-12-烯(8)、elephanmollen(9)、桦木酸(10)、木栓酮(11)、表木栓醇(12)、豆甾醇(13)、去氢松香酸(14)、euglobal-G1(15)、6-甲基-5-羟基-7,4′-二甲氧基黄酮(16)。结论:其中,化合物1~8、14~16为首次从地胆草属植物中分离得到。

基于网络药理学和分子对接技术探究地胆草治疗溃疡性结肠炎的作用机制

基于网络药理学和分子对接技术,研究地胆草治疗溃疡性结肠炎(ulcerative colitis,UC)的分子机制。根据文献调研确定地胆草的化学成分,利用SwissADME数据库筛选活性成分、SwissTargetPrediction数据库预测其作用靶点。通过GeneCards、Disgenet、PharmGKB和TTD数据库获取UC的相关靶点,并进行拓扑分析,采用Metascape数据库对候选靶点进行GO(gene ontology)功能和KEGG(Kyoto encyclopedia of genes and genomes)生物通路富集分析,最后结合RCSB PDB数据库及Chemdraw、PyMoL、AutoDock 4.2.6对核心成分和关键靶点进行分子对接验证并进行可视化分析。从地胆草中筛选出34个调控UC的潜在靶点,对关键靶点作GO功能和KEGG通路富集分析,显示地胆草可能通过对系统过程的调节、外部刺激反应的负面调节、凋亡信号通路的调节以及机械刺激的反应等生物学过程调节MAPK3、PIK3CA、STAT3和JAK2等关键靶点的表达,从而参与调控癌症信号通路、PI3K-Akt信号通路、NF-κB信号通路、幽门螺旋杆菌感染的上皮细胞信号传导和钙信号传导通路等多个KEGG信号通路,从而达到治疗UC的目的。分子对接结果显示,各活性成分与关键靶点的亲和力较好。研究认为地胆草治疗UC的作用机制可能与抑制MAPK3、PIK3CA、STAT3等靶点的表达,缓解结肠组织炎症反应有关。

UPLC-MS/MS同时测定地胆草中黄酮类成分含量

地胆草中黄酮成分经乙醇溶液提取后,通过大孔树脂纯化,以Waters BEH C18柱分离。以1%甲酸的水溶液和1%甲酸的乙腈溶液为流动相,流速为0.2m L·min^(-1),柱温为30℃,进样体积为1μL。采用UPLC/MS/MS电喷雾电离,多反应监测模式检测,以保留时间和子离子比定性,外标法定量。在该色谱条件下,地胆草中的5种黄酮类成分能得到较好的分离并检测。结果表明,地胆草中木犀草素平均含量为8.75g·kg^(^(-1)),山奈酚平均含量为0.86g·kg^(-1),儿茶素平均含量为4.29g·kg^(-1),芹菜素平均含量为2.43g·kg^(-1),芦丁平均含量为10.71g·kg^(-1)。地胆草中黄酮类化合物种类丰富,含量较高,该研究为地胆草黄酮类化合物的含量测定及中草药地胆草的进一步开发应用提供理论依据。

地胆草化学成分的研究

采用硅胶、葡聚糖凝胶SephadexLH-20和十八烷基硅烷键合硅胶(ODS)等多种色谱技术,对地胆草根部的化学成分进行分离纯化,从地胆草醇提物的乙酸乙酯萃取部位中分离了9个化合物,通过理化性质和波谱数据鉴定化合物1-9的化学结构分别为:大黄素甲醚(1),异香草酸(2),香豆酸(3),对羟基苯甲酸(4),阿魏酸(5),3-甲氧基-4-羟基-桂皮醛(6),豆甾醇-3-O-β-D-葡萄糖(7),豆甾醇(8),吲唑(9).化合物1、2、4、5、6、9为首次从该种植物中分离得到,其中化合物9为一新的天然产物.

地胆草三萜成分的研究

目的分离鉴定地胆草的化学成分,为PC-12细胞活性筛选提供样品。方法用体积分数80%工业酒精提取,硅胶柱色谱分离纯化,根据理化性质和光谱分析确定结构。结果分得8个三萜类成分,分别为无羁萜酮(friedlin,E-6),表无羁萜醇(epifriedlinol,E-7),羽扇豆醇(lupeol,E-8),羽扇豆醇乙酸酯(lupeol acetate,E-9),乌苏酸(ursolic acid,E-10),乌苏-12-烯-3β-十七酸酯(ursa-12-ene-3β-heptadecanoate,E-11),桦木酸(betulinic acid,E-12),30-羟基羽扇豆醇(30-hydroxylupeol,E-13)。结论化合物E-11为一个新的天然产物;化合物E-6,E-10,E-12,E-13为首次从该属植物中得到。

地胆草与白花地胆草脂溶性成分的GC-MS分析及抑菌活性研究

采用溶剂萃取法提取地胆草(Elephantopusscaber Linn.)和白花地胆草(Elephantopustomentosus Linn.)的脂溶性成分,经GC-MS分析,从地胆草中鉴定出44种化学成分,占总脂溶性成分的93.72%;从白花地胆草中鉴定出25种化学成分,占总脂溶性成分的82.08%。地胆草和白花地胆草在萜类成分含量具有显著性差异。通过滤纸片琼脂扩散法测试其抗菌活性,结果表明地胆草与白花地胆草的脂溶性成分对耐甲氧西林金黄色葡萄球菌(MRSA)和金黄色葡萄球菌均有抑制活性,且白花地胆草的抑菌活性强于地胆草。

中药材苦地胆的DNA指纹鉴定

采用分子生物技术包括任意引物聚合酶链式反应(AP-PCR)和随意引物扩增的多态性DNA(RAPD)方法扩增菊科植物地胆草、白花地胆草和假地胆草以及商品药材苦地胆的基因组DNA,获得清晰可靠的DNA指纹图谱。根据琼脂糖凝胶上显示的DNA带型差异可鉴别苦地胆和其混淆品,同时,根据DNA指纹图谱的相似度指数值计算,证实福建、台湾、香港、澳门商品药材苦地胆的基原为菊科植物地胆草Elephantopus scaber L.。

地胆草的化学成分研究

对地胆草全草的化学成分进行研究。采用硅胶柱色谱、SephadexLH-20以及半制备型高效液相色谱技术进行分离纯化，通过1D、2DNMR，MS等方法鉴定化合物的结构。结果从地胆草95％乙醇提取物中分离并鉴定了9个化合物，分别为1-[（2R＊，3．S＊）-3-ethoxy-2，3-dihydro-6-hydroxy-2一（1-methylethenyl）-1-benzofuran-5-y1]ethanone（1）、7-hydroxy-6．acetyl-2．methylchromone（2）、matriisobenzofrrran（3）、桦木酸（betulinicacid，4）、木犀草素（1uteolin，S）、木犀草素-7-D-β-D-葡萄糖苷（1uteolin-7-01B-D—ghcoside，6）、对香豆酸（P-coumaricacid，7）、3，4-二羟基苯甲醛（3，4-dihydroxybenzaldehyde，8）、豆甾醇-3-O-β-D-葡萄糖苷（stigmasterol-3-O-β-D—ghcoside，9）。其中化合物1—3均为首次从该属植物中分离得到，化合物3在国内未见从其它植物中分离报道。

地胆草倍半萜内酯化合物体外抗肿瘤作用的研究

采用四甲基偶氮唑盐比色法和琼脂糖凝胶电泳法等研究地胆草倍半萜内酯化合物scabertopin（1）和isodeoxyelephantopin（2）在体外对SMMC-7721、Hela和Caco-2三种肿瘤细胞增殖的影响。发现这两个化合物在1～100 μM浓度内对三种肿瘤细胞增殖有显著的抑制作用，且呈一定剂量依赖关系。二者抑制SMMC-7721细胞增殖的IC50值分别为29.27和9.54 μM；抑制Hela细胞增殖的IC50值分别为22.19和25.39 μM；抑制Caco-2细胞增殖的IC50值分别为35.99和25.76 μM。时效性实验还显示2对Hela细胞增殖的抑制作用呈时间依赖关系。2浓度 100 μM作用Hela细胞48 h琼脂糖凝胶电泳显示明显的细胞凋亡“梯状”条带（DNA ladder），提示isodeoxyelephantopin抑制Hela细胞作用是通过诱导其凋亡。