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.

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.

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.

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.

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.

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.

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.

小飞扬草(Euphorbia thymifolia L.)中镉的亚细胞分布及化学形态

采用差速离心法和逐步提取法,分析Cd超积累植物小飞扬草根、茎、叶中Cd的亚细胞分布和化学形态。培养液中Cd浓度5mg/L和10mg/L条件下,在小飞扬草根、茎、叶中,细胞壁和细胞膜是Cd主要的结合场所,含量分别占总量的47.1%～49.0%、39.7%～41.4%、42.9%～56.2%,其次是胞液组分,含量分别占37.5%～41.4%、28.2%～40.7%、35.2%～46.8%,细胞器组分中Cd含量较少。Cd在小飞扬草根、茎、叶中均以氯化钠提取态为主,含量分别占70.5%～84.8%、72.4%～83.0%、50.0%～74.8%。根部各提取态含量依次为CNaCl>CHAC>CEtOH>CHCl>CW>CR,茎、叶中各提取态含量依次为CNaCl>CHCl>CHAC>CEtOH>CW>CR。在小飞扬草中,Cd与细胞壁和细胞膜中的果胶酸和蛋白质等物质结合固定,而进入细胞的Cd大部分与有机酸络合而隔离于液泡内,这可能是小飞扬草忍耐并超积累Cd的机制。

A new aryl glycoside from Euphorbia helioscopia L.

A new aryl glycoside, 3″-O-galloyl-benzyl-O-α-L-rharnnopyranosyl-（1 → 6）-β-D-glucopyranoside, was isolated from Euphorbia helioscopia L., and its structure was elucidated on the basis of various spectroscopic data analysis.

A new lathyrane diterpene glycoside from Euphorbia helioscopia L.

A new lathyrane diterpene glycoside,named 3β,7β,15β-trihydroxy-14-oxolathyra-5E,12E-dienyl-16-O-β-D-glucopyranoside, was isolated from Euphorbia helioscopia L.Its structure was established by spectroscopic techniques including 2D NMR.

Occurrence and Control of Brown Patch in Energy Oil Plants Euphorbia lathyris L.

[ Objective] The purpose was to study the occurrence law and control effect of brown patch of E. lathyris. [ Method ] The pathogen of brown patch in E. lathyris was isolated and identified in Xingyi of Guizhou Province in 2008 -2009, and disease symptom observation and field fungicide efficacy test were conducted. [ Result ] The pathogen of brown patch in E. lathyris was fungus in Pseudoc ercospora sp., its suitable growth temperature was 20 -35 ℃, its occurrence peak was from June to September, and its field incidence were 30% -60%. Field efficacy test showed that 5 kinds of fungicides such as Thiophanate-methyl, Mancozeb, etc. had certain control effect on the disease, the relative control effect was 54. 3% -82.5%, in which mancozeb had better control effect, while Thiediazole copper had worse control effect. [Conclusion] The study would provide theoretical reference for further research on the cultivation of E. lathyris with hiah vield and aualitv and control of brown hatch.

Acid Value Determination and Pre-Esterification of Crude Euphorbia lathyris L. Oil

There were various problems in the determination of oil acid value of the national standard method, and this paper developed a low cost, simple and effective way to determine the acid value of oil and grease. Furthermore, the esterification of high acid Euphorbia lathyris L. oil (ELO) with methanol could be efficiently catalyzed by hydrochloric acid to produce biodiesel, and the influencing factors such as the amount of catalyst, reaction time, reaction temperature and molar ratio of oil to methanol were also studied. Under the optimized conditions with the oil to methanol molar ratio of 1:30 and a reaction temperature of 70℃, 95.8% oil conversion was obtained within 40 min in the presence of only 2.0 wt% of catalyst. Therefore, the low-cost non-edible Euphorbia lathyris L. oil as a raw material had good potential for the synthesis of biodiesel in industry.

Antimicrobial activity of Tunisian Euphorbia paralias L.

Objective: To examine the potential antimicrobial activity of Euphorbia paralias L. (Euphorbiaeae) leaves and stems extracts. Methods: The antimicrobial activity was tested against six microbial strains:Escherichia coli ATCC 8739, Bacillus subtilis ATCC 6633, Salmonella enterica CIP 8039, Staphy-lococcus aureus ATCC 6538, Pseudomonas aeruginosa ATCC 9027 and Candida albicans ATCC 90028 by two different methods, the disk method and the dilution method. Results: Our results showed the important antimicrobial activity of the chloroform extract of the stems towards the majority of the strains by using both methods. Bacillus subtilis was the most sensitive strain (MIC=MBC=15μg/mL). Conclusion: Thus, some extracts of Euphorbia paralias can be used in the treatment of infectious diseases caused by microbes.

Pharmacognostic Identification of Euphorbia maculata L.and Its Related Species

[Objectives]To make pharmacognostic identification of Euphorbia maculata L.and its related species.[Methods]The classical pharmacognostic identification method was adopted.[Results]The four main medicinal materials are very similar,the fluff can be seen in E.maculata and Euphorbia thymifolia L.,but not in Euphorbia prostrata Ait.and Euphorbia taihsiensis(Chaw et Koutnik)Oudejians;the tissue structure is basically the same;except for E.taihsiensis without non-glandular hairs,the powder has secretory cells,laticifers,cells,calcium oxalate crystals,fibers,vessels,and seed coat fragments.Through ultrasonic extraction with 80%ethanol,extraction with isobutanol,extending with chloroform∶ethyl acetate∶formic acid(5∶3∶0.3),developing color with 3%aluminum trichloride ethanol solution,under ultraviolet light(365 nm),the fluorescent spots of the same color appeared on the corresponding position of the chromatogram of the reference substance(quercetin,kaempferol).[Conclusions]It is not easy to distinguish the four medicinal materials by character identification and microscopic identification,while the thin-layer chromatography(TLC)is more reliable.

NaCl胁迫下地被菊光合生理特性及水分利用率的变化

为研究地被菊(Rudbeckia hirta L.)的抗盐能力,采用不同浓度的NaCl(0、50、100、250、400mmol/L)胁迫处理地被菊幼苗,20d后测定其光合生理特性及水分利用率的变化。结果表明,地被菊在不同浓度NaCl胁迫下,随着胁迫浓度的加大,净光合速率(Pn)、蒸腾速率(Tr)、气孔导度(Gs)呈下降趋势,而胞间CO2浓度(Ci)先下降后升高;水分利用率在NaCl浓度≤250mmol/L时升高,在400mmol/L时降低。叶绿素a、叶绿素b含量下降,但叶绿素a/叶绿素b比值上升。

狼毒化学成分基于Mpro靶点的虚拟筛选及抗SARS-CoV-2活性分析

目的 对瑞香狼毒和狼毒大戟中的化学成分进行基于新型冠状病毒(Severe Acute Respiratory Syndrome-coronavirus-2,SARS-CoV-2)3CL水解酶(Mpro)的抑制剂虚拟筛选以及体外活性验证以为发现抗新型冠状病毒疾病(Corona Virus Disease 2019,COVID-19)治疗药物提供参考。方法 以瑞香狼毒和狼毒大戟中的天然产物为研究对象,以Mpro为靶点,以Mpro晶体结构(PDB ID:6LU7)中的配体小分子N3为阳性对照,采用AutoDock Vina进行分子对接,对结合亲和力和结合构象进行分析并进行基于SARS-CoV-2 Mpro蛋白的体外抑制活性测试。结果 与N3(亲和力为-7.7 kcal/Mol)相比,双黄酮类化合物狼毒素和异狼毒素呈现了最高的Mpro靶点亲和力(-9.7 kcal/Mol),且优于利托那韦、更昔洛韦、利巴韦林、氯喹、达芦那韦、阿巴卡韦等已知抗病毒药物以及其他天然产物的亲和力。对接构象分析发现二者均能有效占据Mpro蛋白结合位点并形成若干重要的氢键结合,其中以异狼毒素为最优,这对于二者与Mpro靶点的结合以及Mpro靶点抑制构象的稳定起着重要作用。异狼毒素在50μM浓度下显示出优于狼毒素的较好的Mpro体外抑制活性。结论 狼毒素和异狼毒素具有基于Mpro靶点抑制SARS-CoV-2病毒的潜在活性,可作为结构优化和抗SARS-CoV-2体内外活性研究的先导化合物。

金刚纂内生真菌Irpex sp.的次生代谢产物研究

通过硅胶柱层析和半制备型高效液相色谱等分析方法对金刚纂(Euphorbia neriifolia L.)内生真菌Irpex sp.的液体发酵产物进行提取与分离,共得到9个化合物,分别为IrpexIacteC(1)、IrpexIacteD(2)、5-(4-Oxopentyl)furan-2-carbaldehyde(3)、22-tetraen-3-one(4)、IrlactinL(5)、IrlactinK(6)、IrlactinI(7)、Davotremulane B(8)、(+)-(1R,6S,7S)-Tremul-2-ene-12(11)-lactone(9),其中,3个为呋喃衍生物,5个为倍半萜化合物,1个为甾醇类化合物;化合物3,4,8,9为首次从耙齿菌属Irpex sp.中分离得到.