A Review on Bioactive Compounds Isolated from Euphorbia hirta L.

Euphorbia hirta L. is an annual medicinal herb throughout many tropical continents used to cure various diseases. Several studies have isolated many bioactive compounds from E. hirta. This study aimed at providing a collection of bioactive constituents in E. hirta. This review summarizes the extraction solvent, the structures and the properties of 38 bioactive phytochemicals isolated from E. hirta. It could help to understand the relationship existing between phytochemicals and their activities.

Studies on the Chemical Constituents of Euphorbia hirta

[Objective] The aim was to study the chemical constituents of Euphorbia hirta. [Method] The constituents were isolated and purified by various chromatography methods including normal phase and reverse phase silica gel as well as Sephadex LH-20 gel column, and then elucidated by spectroscopic analysis such as MS and NMR etc. Compounds 1, 4, 5 and 6 were evaluated for their immunostimulatory activity against splenic cell of mouse by FCM. [Result] Six compounds were isolated from Euphorbia hirt, and identified as diisobutyl-O-phthalate （compond 1）, diethylhexyl phthalate （compond 2）, hispidulin （compond 3）, acetyl peroxide （compond 4）, quercetein （compond 5） and gallic acid （compond 6）. All compounds were inactive against splenic cell of mouse. [Conclusion] Compounds 1, 2 and 3 were isolated from this plant for the first time, and compound 4 was the first naturally occurring compound. This study provided reference for isolating bioactive substances from Euphorbia hirta.

Antioxidant and hepatoprotective potentials of novel endophytic fungus Achaetomium sp.,from Euphorbia hirta

Objective: To isolate, identify and evaluate the antioxidant, antimicrobial, hepatoprotective potentials, total phenolic content, flavonoid content, tannin content of ethyl acetate extract of endophytic fungus Achaetomium sp., isolated from Euphorbia hirta. Methods: Hepatoprotectivity of ethyl acetate extract of Achaetomium sp., was evaluated by CCl4 induced toxicity in Hep G2 cells and subsequently analyzed for cell viability using MTT assay. It also demonstrates antioxidant and antimicrobial potentials by DPPH radical scavenging assay and well diffusion assay respectively. Quantification of total phenolic content, tannin content and flavonoid content were assessed by spectroscopic methods. Results: Phenols, flavonoids and tannins were the phytochemicals present in ethyl acetate extract of Achaetomium sp., with rich phenolic content exhibited potent hepatoprotective, antimicrobial and antioxidant activities. The hepatoprotective activity was recorded as of 72.13%±2.948% of cell viability at a concentration of 150 μg/m L, whereas the standard silymarin showed 93.260%±0.784%. It was observed to be dose dependent, when CCl4 exposed Hep G2 cells were treated with different concentrations of ethyl acetate extract. Antibacterial activity showed significant inhibition against Staphylococcus aureus, Pseudomonas aeroginosa, and Klebsiella pneumonia. The antioxidant activity ranged from 66.890%±1.385% to 87.340%±0.289% with(44.02±1.57) μg of total phenolics,(54.54±1.82) μg of flavonoid content and(18.790±1.018) μg of tannin content. Ascorbic acid, BHT(butylated hydroxyl toluene) Gallic acid and Pyrogallol were used as standards which showed 98.370%±0.763%; 97.080%±0.636%; 94.890%±1.103% and 96.980%±0.098% reducing potential respectively. Conclusions: The results reveal that the metabolites produced by endophytic fungi isolated from Euphorbia hirta could be novel natural products that could lead to new drug discovery.

Antioxidant activity and phytochemical screening of the methanol extracts of Euphorbia hirta L

Objective:To assess antioxidant activities of different parts of Euphorbia hirta（E.hirta）,and to search for new sources of safe and inexpensive antioxidants.Methods:Samples of leaves,stems, flowers and roots from E.hirta were tested for total phenolic content,and flavonoids content and in vitro antioxidant activity by diphenyl-1-picrylhydrazyl（DPPH） assay and reducing power was measured using cyanoferrate method.Results:The leaves extract exhibited a maximum DPPH scavenging activity of（72.96±0.78）%followed by the flowers,roots and stems whose scavenging activities were（52.45±0.66）%,（48.59±0.97）%,and（44.42±0.94）%,respectively.The standard butylated hydroxytoluene（BHT） was（75.13±0.75）%.The IC50,for leaves,flowers,roots,stems and BHT were 0.803,0.972,0.989,1.358 and 0.794 mg/mL,respectively.The reducing power of the leaves extract was comparable with that of ascorbic acid and found to be dose dependent. Leaves extract had the highest total phenolic content[（206.17±1.95） mg GAE/g],followed by flowers,roots and stems extracts which were（117.08±3.10） mg GAE/g,（83.15±1.19） mg GAE/g,and （65.70±1.72） mg GAE/g,respectively.On the other hand,total flavonoids content also from leave had the highest value[（37.970±0.003） mg CEQ/g],followed by flowers,roots and stems extracts which were（35.200±0.002） mg CEQ/g,（24.350±0.006） mg CEQ/g,and（24.120±0.004） mg CEQ/ g,respectively.HPTLC bioautography analysis of phenolic and antioxidant substance revealed phenolic compounds.Phytochemical screening of E.hirta leaf extract revealed the presence of reducing sugars,terpenoids,alkaloids,steroids,tannins,flavanoids and phenolic compounds. Conclusions:These results suggeste that E.hirta have strong antioxidant potential.Further study is necessary for isolation and characterization of the active antioxidant agents,which can be used to treat various oxidative stress-related diseases.

A transmission electron microscopy study of the diversity of Candida albicans cells induced by Euphorbia hirta L.leaf extract in vitro

Objective:To determine the major changes in the microstructure of Candida albicans(C. albicans) after treatment with Euphorbia hirta(E.hirta) L.leaf extract.Methods:Transmission electron microscopy was used to study the ultrastructural changes caused by E.hirta extract on C. albicans cells al various exposure time.Results:It was found that the main abnormalities were the alterations in morphology,lysis and complete collapse of the yeast cells after 36 h of exposure to the extract.Whereas the control cultures showed a typical morphology of Candida with a uniform central density,typically structured nucleus,and a cytoplasm with several elements of endomembrane system and enveloped by a regular,intact cell wall.Conclusions:The significant antifungal activity shown by this methanol extract of E.hirta L.suggests its potential against infections caused by C.albicans.The extract may be developed as an anticandidal agent.

Mosquito larvicidal and pupicidal activity of Euphorbia hirta Linn.(Family:Euphorbiaceae) and Bacillus sphaericus against Anopheles stephensi Liston.(Diptera:Culicidae)

Objective:To explore the larvicidal and pupicidal activity of Euphorbia hirta（E.hirta） leaf extract and Bacillus sphaericus（B.sphaericus） against the malarial vector.Anopheles siephensi（An. stephensi）.Methods:The larvicidal and pupicidal activity was assayed against An.stephensi at various concentrations ranging from（75-375 ppm） under the laboratory as well as field conditions. The LC50 and LC90 value of the E.hirta leaf extract was determined by probit analysis.Results: The plant extract showed larvicidal effects after 24 h of exposure;however,the highest larval mortality was found in the methanol extract of E.hirta against the first to fourth instars larvae and pupae of values LC50=137.40,172.65,217.81,269.37 and 332.39 ppm;B.sphaericus against the first to fourth instars larvae and pupae of values LC50= 44.29,55.83,68.51,82.19 and 95.55 ppm, respectively.Moreover,combined treatment of values of LC50= 79.13,80.42,86.01,93.00 and 98.12 ppm,respectively.No mortality was observed in the control.Conclusions:These results suggest methanol leaf extracts of E.hirta and B.sphaericus have potential to be used as an ideal ecofriendly approach for the control of the malarial vector.An.stephensi as target species of vector control programs.This study provides the first report on the combined mosquito larvicidal and pupicidal activity of this plant crude extract and bacterial toxin against An.stephensi mosquitoes.

Cytotoxicity and genotoxicity assessment of Euphorbia hirta in MCF-7cell line model using comet assay

Objective:To evaluate the cytotoxicity and genotoxicity activity of Euphorbia hirta(E.hirta)in MCF-7 cell line model using comet assay.Methods:The cytotoxicity of E.hirta extract was investigated by employing brine shrimp lethality assay and the genotoxicity of E.hirta was assessed by using Comet assay.Results:Both toxicity tests exhibited significant toxicity result.In the comet assay,the E.hirta extract exhibited genotoxicity effects against MCF-7 DNA in a time-dependent manner by increasing mean percentage of DNA damage.The extract of E.hirta showed significant toxicity against brine shrimp with an LC_(50)value of 620.382μg/mL(24 h).Comparison with positive control potassium dichroniate signifies that cytotoxicity exhibited by the methanol extract might have moderate activity.Conclusion:The present work confirmed the cytotoxicity and genotoxicity of E.hirta.However,the observed toxicity of E.hta extracts needs to be confirmed in additional studies.

Galactagogue Effect of <i>Euphorbia hirta</i>(Euphorbiaceae) Aqueous Leaf Extract on Milk Production in Female Wistar Rats

Background: Populations of Gontougo (C?te d’Ivoire) commonly used Euphorbia hirta (Euphorbiaceae) leaves as galactagogue to boost milk production in lactating women. Our study was carried to verify this traditional belief via evaluations of milk production, serum prolactin levels, body weight and mammary lobuloalveolar proliferation induced by the aqueous leaf extract of this medicinal plant in Wistar rats. Methods: 6 groups of 6 virgin rats and 6 groups of 6 lactating rats were used. Each lactating rat was isolated with its six pups. These groups of animals were treated orally with distilled water, Metoclopramide (Metocl 5 mg/kg) and E. hirta aqueous leaf extract (EHae 100, 200, 400 and 600 mg/kg) daily during 17 days of lactation. The indirect method which assimilates the weight gain of untreated pups to the quantity of milk produced by lactating rats was used. At the end of the treatment, histological sections of the abdominal mammary glands of lactating rats were observed. Results: EHae administration induced an increase of milk production in lactating rats. This action of EHae was stronger at the dose of 200 mg/kg. Milk production of the treated rats at a dose of 200 mg/kg was 118.14 ± 1 g. The quantity of milk produced by the control female rats was 83.83 ± 0.88 g. Compared with the control, EHae 200 mg/kg significantly increased milk production (40.92%) (P Conclusion: EHae showed a galactagogue activity illustrated by increases of milk production, PRL secretions and the development of the lobuloalveolar system of the mammary glands in treated female rats. This galactagogue property could partly justify the traditional use of this plant to boost milk production in lactating women.

Evaluation of Anxiolytic and Sedative-Like Activities of Methanolic Extract of <i>Euphorbia hirta</i>Leaves in Mice

In indigenous or folk medicine, Euphorbia hirta is a very popular herb and used as a palliative to treat various ailments including intestinal parasites, diarrhoea, vomiting, amoebic dysentery, asthma, bronchitis, emphysema, coughs, kidney stones, menstrual problems etc. The objective of this study is to evaluate the anxiolytic and sedative-like effects of the methanol extract from the leaves of Euphorbia hirta (Euphorbiaceae). Methanolic extract of Euphorbia hirta was evaluated for its CNS depression effect using mice behavioral models such as, elevated plus maze and hole board test for its anxiolytic potential where hole cross and pentobarbital-induced sleeping time tests were performed for its sedative properties, respectively. The test group received three different doses of the MEHL (100 mg/kg, 200 mg/kg and 300 mg/kg) orally. The positive control group received diazepam (1 mg/kg) orally where the negative control group received distilled water (10 ml/kg) orally. In elevated plus maze test, the extract exhibited significant (p d the number of open arm entry and time spent in open arm by mice compared to control group. In addition, the number of head dips and hole crosses significantly (p < 0.05) decreased by mice in hole board and hole cross tests respectively, compared to control group. Moreover, mice treated with MEHL significantly decrease the onset of sleep and increase the duration of sleep in pentobarbital-induced sleeping time test in mice compared to control group. The data obtained from the present study clearly demonstrate that the methanolic extract of Euphorbia hirta has potential anxiolytic and sedative-like activity in the animal behavioral models. And the findings represent a rational explanation for its use in traditional medicine for the management of neurological disorder.

<i>In Vitro</i>Sickling Inhibitory Effects and Anti-Sickle Erythrocytes Hemolysis of <i>Dicliptera colorata</i>C. B. Clarke, <i>Euphorbia hirta</i>L. and <i>Sorghum bicolor</i>(L.) Moench

Diclipteracolorata C. B. Clarke, Euphorbia hirta L. and Sorghum bicolor (L.) Moench are reported among plant species used in Congolese traditional medicine to treat Sickle Cell Disease. These medicinal plants have been investigated for their inhibitory effect on the induced sickling process of red blood cells using Emmel’s test. Aqueous plant extracts showed good antisickling activity as revealed by the observed normal biconcave form of sickle red blood cells in anoxic conditions. The calculated radius of treated red blood cells by Euphorbia hirta L., Diclipteracolorata C. B. Clarke and Sorghum biocolor (L.) Moench extracts are 3.31 ± 0.55;3.34 ± 0.53;3.17 ± 0.52, respectively. Euphorbia hirta L. is the most active with a normalization rate, more than 70%. The chemical screening performed on these plants showed the presence of anthocyanins which were then extracted. The test carried out with anthocyanin extracts showed that these phenolic compounds have a good antisickling activity and, additionally, possess an anti-hemolytic effect on SS blood. This suggests that the evidenced biological activity of these plants would be due to anthocyanins. The results hence obtained justify the use of these plants in Congolese traditional medicine.

紫外分光光度法测定飞扬草中总黄酮、总酚的含量

为建立飞扬草提取物中总黄酮和总酚的测定方法。本实验以芦丁和没食子酸为对照品,样品分别采用NaNO_(2)-Al(NO_(3))_(3)-NaOH显色法和福林酚试剂显色法进行处理,通过紫外分光光度法测定飞扬草中总黄酮和总酚的含量。结果表明在9.7~58.2μg/mL范围内芦丁的质量与其吸光度值呈良好的线性关系(y=0.0113x-0.0067,R^(2)=0.9993);在1.12~6.72μg/mL范围内没食子酸的质量与其吸光度值呈良好的线性关系(y=0.2273x+0.0109,R^(2)=0.9991)。该方法简便、准确,具有良好的精密度、稳定性、重复性,可用于飞扬草中总黄酮、总酚的含量测定。

大、小飞扬草的化学成分、药理活性及临床应用进展

目的大飞扬草和小飞扬草的名称相近,但药材原植物来源不同,外观性状具有显著差异。为了解二者异同之处,本文对大飞扬草和小飞扬草的化学成分、药理活性及临床应用进展进行总结综述。方法通过查阅国内外五十余篇相关文献,对大飞扬草和小飞扬草的化学成分、药理活性及临床应用进行归纳总结。结论大飞扬草中主要含有黄酮类、香豆素类、木脂素类、三萜类、甾体类、单宁类、生物碱以及其他化学成分;小飞扬草中主要含有黄酮类、香豆素类、木脂素类、三萜类、甾体类、单宁类、生物碱以及其他化学成分。大飞扬草具有解热、镇痛、抗炎、抗氧化、抗过敏、抗哮喘、抗糖尿病、利尿、降血压、抗焦虑、止泻、抑菌、抗病毒、抗疟、杀虫等药理活性;小飞扬草具有抗炎、镇痛、降血糖、抑菌、抗病毒等药理活性。大飞扬草临床外用可治疗皮肤疾病,内服可以治疗肠胃疾病;小飞扬草除与大飞扬草联合使用外,未见单独使用案例。通过比较二者的化学成分、药理活性及临床应用,发现大飞扬草和小飞扬草的化学成分相似,大飞扬草的药理活性及临床应用较为广泛。据此建议在二者药理活性相同的方面,小飞扬草可作为大飞扬草的药品替代品进行使用。

飞扬草的化学成分研究(Ⅱ)

目的研究飞扬草Euphorbia hirta地上部分70%丙酮提取物的化学成分。方法飞扬草地上部分70%丙酮提取物利用正反相硅胶和Sephadex LH-20等多种色谱方法交替使用进行分离纯化,利用MS、NMR等现代光谱技术确定化合物结构。结果从飞扬草地上部分的70%丙酮提取物中共分离得到12个化合物,分别鉴定为:β-谷甾醇(1)、蒲公英赛酮(2)、(23E)-25-甲氧基环木菠萝烯-3-醇(3)、23-环木菠萝烯-3β,25-二醇(4)、环阿尔廷-25-烯-3β,24ξ-二醇(5)、羊毛甾醇(6)、山柰酚-3-鼠李糖苷(7)、邻苯二甲酸二丁酯(8)、邻苯二甲酸二异丁酯(9)、黑麦草内酯(10)、3,4-二羟基苯甲酸(11)、没食子酸(12)。结论化合物3～5,10～11为首次从该植物中分离得到。

大飞扬总黄酮提取工艺优化及抗氧化活性测定

大飞扬为大戟科(Euphorbiaceae)大戟属(Euphorbia)植物飞扬草(E.hirta),主要化学成分为黄酮类、丹宁类、三萜类、二萜类,具有清热解毒、利湿止痒、通乳等功效。目前对大飞扬的研究主要集中在化学成分及药理活性的研究,对黄酮类成分提取工艺优化报道较少。为优化大飞扬总黄酮的提取工艺,该文以采自海南儋州的野生大飞扬干燥全草为材料,以总黄酮产率为评价指标,在单因素试验的基础上,进一步通过正交试验设计对大飞扬总黄酮的提取工艺进行优化,同时采用清除DPPH自由基及ABTS法对其抗氧化活性进行测定。结果表明:大飞扬总黄酮最佳提取工艺为药材粉碎过4号筛(65目),以85%乙醇超声提取4次;大飞扬总黄酮对DPPH和ABTS自由基均有较好的清除率作用,其IC50值分别为56.1和60.7μg/mL。大飞扬黄酮类成分大多具有酚羟基基团,如异鼠李素、槲皮素等,具有较好的抗氧化活性。该文结果为大飞扬中黄酮类成分工业化生产提供了依据,也为进一步开发利用大飞扬药材奠定了基础。

飞扬草中酚类成分的分离与鉴定

为研究飞扬草中的酚类化学成分,利用溶剂提取法,正、反相硅胶柱和半制备高效液相色谱法对其进行了分离纯化,并根据理化性质和波谱技术对其进行了结构鉴定.从飞扬草乙酸乙酯提取物中分离得到了12个酚类化合物,分别鉴定为木犀草素(1)、槲皮素(2)、3'-甲基杨梅黄酮(3)、松脂酚(4)、4-ketopinoresinol(5)、3,4-二羟基苯甲酸(6)、咖啡酸(7)、香草酸(8)、丁香酸(9)、没食子酸乙酯(10)、橙黄胡椒酰胺乙酸酯(11)、橙黄胡椒酰胺(12),其中化合物3、5、8、10~12为首次从飞扬草中分离得到.

飞扬草提取物的抗菌性能研究

从飞扬草中提取防腐抑菌液并测定了防腐抑菌效果。结果表明,飞扬草提取液对常见食品腐败菌确有较强的抑菌作用,其抑制腐败菌大肠杆菌、金黄色葡萄球菌、苏云金芽孢杆菌的最低体积分数为0.156%,抑制根霉菌和青霉菌的体积分数为0.625%,抑制枯草芽孢杆菌、曲霉菌、酵母菌的最低体积分数分别为0.078%、0.313%、1.25%;在相同时间内,飞扬草提取液含量越高,抑菌率就越高,同一含量液提取的作用时间越长,抑菌率也就越高,热处理对其抑菌效果有加强作用。

温度、光照和水分对飞扬草种子萌发和幼苗生长的影响

为明确热带常见杂草飞扬草(Euphorbia hirta)的种子萌发特性,本研究运用培养皿滤纸法和盆栽法,分别研究温度、光照和水分条件对飞扬草种子萌发和幼苗生长的影响。结果表明,飞扬草种子在20~40℃范围内均可萌发,其中30℃为种子萌发的最适温度(萌发率和萌发指数均最大),25℃时幼苗生长最好(根长/苗长为1.031)。恒温条件(25℃)下,光照8~24h时的种子萌发率无显著差异(平均值94.07%)、光/暗0h/24h时萌发率降至52%(P<0.05),萌发指数随光照时间缩短先增大后降低,光/暗16h/8h时最大(93.93),0h/24h最低(30.59);有光照时幼苗的根长均显著大于苗长,无光照时苗长显著大于根长(P<0.05)。变温条件(光/暗,35℃/25℃)下,光照时长对飞扬草种子萌发率和幼苗苗长无显著影响(P>0.05),随光照时长缩短萌发指数和幼苗根长均显著减低(P<0.05)。综合各指标,12~16h光照为飞扬草种子萌发和幼苗生长的最佳光照条件。25℃、光/暗12h/12h条件下,飞扬草在土壤最大持水量60%时的种子出苗率达39%、幼苗根长苗长比为1.10∶1。

皖南歙县药用植物分布新记录

目的摸清皖南野生药用植物分布的新种类,为后期安徽省药用植物资源种类的统计奠定基础。方法采用野外调查、文献查阅和标本鉴定的研究方法。结果皖南有4种药用植物分布新记录,新记录种分别是锦葵科植物白背黄花稔Sida rhombifolia Linn.、景天科植物土佐景天Sedum tosaense Makino、大戟科植物飞扬草Euphorbia hirta Linn.和荨麻科植物小叶冷水花Pilea microphylla(Linn.)Liebm.。结论这4种药用植物标本可为其在安徽的分布提供依据,可丰富安徽药用植物资源的种类。

飞扬草总多酚提取及其对羟基自由基的抑制作用

采用乙醇浸提法对飞扬草多酚进行提取,并开展了飞扬草多酚对羟基自由基抑制活性的研究。本文分析了乙醇体积分数、温度、时间、料液比对多酚提取的影响,并通过正交实验进行了优化。确定出最佳参数为:50%乙醇,浸提温度60℃,时间2.5 h,料液比1∶30。在此条件下浸提,多酚质量分数可达31.331 mg/g。抗氧化性研究表明,飞扬草提取液能清除·OH自由基,在多酚质量浓度为3.759 mg/mL时,清除率约为50%,说明清除能力较强,这为飞扬草药用开发和利用奠定了理论基础。

飞扬草中一个木脂素苷的结构研究

从大戟属植物飞扬草(Euphorbia hirta)地上部分的乙醇提取物中分离得到一个木脂素苷,经IR,NMR和HRESIMS等波谱技术鉴定为化合物tibeticoside A(1).该化合物为首次从大戟属植物中分离得到。