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.

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.

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..

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.

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.

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。

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。

遮光与定植方式对地胆草生长及产量的影响

目的：了解地胆草在不同光照条件下的生长与产量表现,为地胆草的人工种植提供参考。方法：以全光照的露地栽培为对照,对遮光率分别为42%、50%、60%、69%、85%的遮光处理下穴播、苗植两种方式种植的地胆草生长状况及产量进行了研究。结果：适度遮光促进地胆草株高、叶片数、根系长度的增加并提高根冠比;随遮光率的增加,地胆草由定植到抽薹盛期、开花盛期所需时间减少;单位面积地胆草种子产量、全草产量、根头产量均为全光照的最高,并随遮光率增加而下降,各处理单位面积种子产量在8.46-31.10 kg/667 m^2之间,全草干品产量在327.28-800.95 kg/667 m^2之间,根头干品产量在30.65-70.72 kg/667 m^2之间。结论：地胆草对光照的适应能力较强,属偏喜阳,但可耐受较大程度的荫蔽;人工种植地胆草以穴播方式为好,在热带经济林下间种建议荫蔽度不超过60%为宜。

地胆草中去氧地胆草内酯的定性和定量方法研究

目的建立地胆草中有效成分去氧地胆草内酯的定性和定量分析方法。方法采用薄层色谱法进行定性鉴别,薄层板为硅胶G板,展开剂为石油醚(60~90℃)-乙酸乙酯(2∶3),展开后喷以10%香草醛硫酸溶液,105℃加热至斑点清晰;采用反相高效液相色谱法测定含量,色谱柱为Kromasil C18色谱柱(250 mm×4.6 mm,5μm),流动相为乙腈-水(35∶65),流速:1.0mL·min-1,检测波长208 nm,柱温:30℃。结果供试品色谱中,在与对照药材色谱和对照品色谱相应的位置上,显相同颜色的斑点;去氧地胆草内酯在0.005 915~0.059 15 g·L-1范围内线性关系良好(r=1.000),平均回收率(n=6)为98.75%,样品含量范围为0.072%~0.15%。结论所建立的方法简单灵敏,准确可靠,重复性好,可用于地胆草的质量控制。

民族药地胆草的生药学鉴定

采用原植物、性状、显微、薄层鉴别方法对民族药地胆草进行系统的生药学鉴定,为其鉴别及应用提供科学依据。结果表明:通过原植物、性状鉴别、显微鉴别、薄层色谱鉴别能够很好的鉴定原植物。

地胆草总黄酮提取工艺的研究

地胆草中的黄酮类成分具有丰富的药理作用,为了最大限度的提取出地胆草中的黄酮类成分,特采用醇提法对地胆草总黄酮的提取工艺进行研究,借用单因素试验考察乙醇浓度、料液比、醇提时间、醇提温度对地胆草总黄酮提取率的影响,然后选取乙醇浓度、料液比、醇提时间和醇提温度4个因素进行正交试验。结果表明,提取时间对地胆草总黄酮的提取具有明显影响,醇提法提取地胆草总黄酮的最佳工艺条件为:80%乙醇、料液比为1∶40、醇提时间为2.5h、提取温度为80℃,提取率为1.75%,该研究为地胆草资源的合理开发及应用提供了理论依据。

盆栽地胆草播种方式及肥效试验研究初报

移栽野生地胆草,收集成熟种子,通过不同播种方式盆栽播种,观测种子发芽情况。再通过盆栽肥效试验,确定野生地胆草生长的营养需求。结果表明,浅播种子发芽快,且后期生长好;肥效试验表明,盆栽地胆草每株每周施100 mL 0.1%浓度的复合肥水肥时长势好。

地胆根的镇咳、祛痰和平喘作用

用动物实验方法,研究地胆根乙醇提取液治疗支气管炎,咳、痰、喘三种症状的效果及其药理作用.给豚鼠腹腔泣射地胆根乙醇提取液,能显著地增大方波刺激迷走神经的引咳阈值;给小白鼠灌胃,能非常显著增加其呼吸道的酚红排泌量;给豚鼠离体气管滴入提取液,对气管有非常显著的扩张效应;该提取液能延长豚鼠的引喘潜伏期,对蛙口腔粘膜上皮的纤毛运动有一定的加快作用.地胆根乙醇提取液有明显的镇咳、祛痰和平喘作用.

地胆草的化学成分研究

目的:研究地胆草的化学成分。方法:采用硅胶柱层析、ODS反向柱色谱、Sephadex LH-20凝胶柱色谱以及制备型高效液相色谱等色谱手段进行分离纯化,并通过波谱数据和理化常数鉴定化合物结构。结果:从地胆草中分离得到15个化合物,分别鉴定为:地胆草种内酯(1)、异地胆草种内酯(2)、去氧地胆草内酯(3)、异去氧地胆草内酯(4)、(2R,6R,7R,8S)-8-tigloyloxy-1(10),4,11(13)-germacratrien-2,14,6,12-diolide(5)、(2S,6R,7R,8S)-8-tigloyloxy-1(10),4,11(13)-germacratrien-2,14,6,12-diolide(6)、乌苏酸(7)、羽扇豆醇(8)、苜蓿素(9)、槲皮素(10)、绿原酸(11)、新绿原酸(12)、3,4-O-二咖啡酰基奎宁酸(13)、3,5-O-二咖啡酰基奎宁酸(14)、bis(2-ethylhexyl)phthalate(15)。结论:其中,化合物5、6、10、12、15为首次从该植物中分离得到。

地胆草总黄酮水提工艺优化

以总黄酮提取率为评价指标,采用水提法提取地胆草总黄酮,在单因素实验的基础上,通过正交实验优化提取工艺。结果表明,水提温度对总黄酮提取率的影响最显著,其次是水提时间和料液比;最优提取工艺条件为:料液比1∶40(g∶mL)、水提温度90℃、水提时间2.0h,在此条件下,地胆草总黄酮提取率达到18.6%。

南药木麻黄和地胆草对肉鸡生长性能和免疫器官发育的影响

为研究饲料中添加南药木麻黄和地胆草对肉鸡生长性能、免疫器官发育的影响,试验选用240羽1日龄AA肉鸡,随机分为4组,试验组(Ⅰ组、Ⅱ组、Ⅲ组)分别在日粮中添加1%的木麻黄和地胆草常规粉、超微粉、水提物(木麻黄和地胆草的质量比为7︰3),对照组(Ⅳ组)饲喂基础日粮。分别在0、14、28、42日龄空腹称体质量,称余料质量,计算料重比和平均日增质量,并颈静脉放血处死,称量免疫器官质量,计算免疫器官指数。结果显示:试验过程中,与对照组相比,试验Ⅱ组平均日增质量显著增加19.05%、料重比显著降低3.20%;在肉鸡14日龄时,试验Ⅱ组脾脏指数显著提高,胸腺指数显著降低,整体上添加木麻黄和地胆草对免疫器官指数影响不明显。综上,在饲料中添加木麻黄和地胆草超微粉能够显著提高肉鸡的生长性能。

白花地胆草酚类成分的研究

目的 研究白花地胆草Elephantopus tomentosus L.酚类成分。方法 采用硅胶、ODS、Sephadex LH-20、半制备HPLC对白花地胆草95%乙醇提取物进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果 从中分离得到15个化合物,分别鉴定为丁香酚苷(1)、3-O-β-D-吡喃葡萄糖-7-羟基苯甲酸苄酯(2)、4-咖啡酰-3-芥子酰奎宁酸甲酯(3)、3,5-O-二咖啡酰奎宁酸乙酯(4)、3-O-咖啡酰奎宁酸乙酯(5)、绿原酸甲酯(6)、木犀草素(7)、山柰酚3-O-(3″,6″-二-O-E-p-香豆酰)-β-D-吡喃葡萄糖苷(8)、邻羟基苯甲酸(9)、反式对羟基肉桂酸(10)、顺式对羟基肉桂酸(11)、对羟基苯甲酸(12)、原儿茶酸(13)、没食子酸乙酯(14)和咖啡酸(15)。结论 化合物1~5、8~14为首次从地胆草属植物中分离得到,化合物6为首次从该植物中发现。