Euphorbia tirucalli L.: Review on morphology, medicinal uses, phytochemistry and pharmacological activities

The intention of current review is to make available up-to-date information on morphology, ecological biodiversity, medicinal uses, phytochemistry and pharmacological activities on different parts of Euphorbia tirucalli (E. tirucalli). This plant has a number of medicinal uses. Latex of E. tirucalli is vesicant and rubefacient which is used for rheumatism, warts, cough, asthma, ear-ache, tooth-ache and neuralgia. It acts as a purgative in small doses while in big doses it is bitter irritant and emetic. Milky juice is alexiteric, carminative and purgative. It is useful in whooping cough, gonorrhea, asthma, leprosy, dropsy, dyspepsia, enlargement of spleen, colic, jaundice and stone in bladder. The fresh milky juice is good alternative in syphilis and a good application in neuralgia. A decoction of branches is used in gastralgia and colic. Bark is used in treatment of fractures. Poultices prepared from the stem are useful to repair the broken bones. Boiled root liquid acts as an emetic in cases of snake-bite and for infertility in women. The wood is used for rafters, toys and veneering purposes. It is also useful against leprosy and foot paralysis subsequent to childbirth. E. tirucalli is reported to have euphol, β-sitosterol, euphorbol hexacosonate, cycloeuphordenol, cyclotirucanenol, tirucalicine, tri-methyl ellagic acid, gallic acids, terpenic alcohol, isoeuphorol, taraxasterol, tirucallol, euphorone, euphorcinol, euphorbins, 12-deoxy-4β-hydroxyphorbol-13-phenyl acetate-20-acetate, 12, 20-dideoxyphorbol-13-isobutyrate, glut-5-en-3-β-ol, 3,3′-di-O-methylellagic acid, euphorbin-A (polyphenol), tirucallin-A (7) (tannin), tirucallin-B (11), euphorbin-F (14) (dimers), cycloartenol, 24-methylenecycloartenol, ingenol triacetate, 12-deoxy-4β-hydroxyphorbol-13-phenyl acetate-20-acetate, taraxerone, euphorginol, taraxerol, campesterol, stigmasterol, palmitic acid, linoleic acid, β-amyrin, etc. active phytoconstituents. E. tirucalli have possessed activity in human-lymphocytes, analgesic, anthelmintics, antiarthritic, antibacterial/antifungal/antimicrobial, anti-HIV, anti-inflammatory, antioxidant, antiviral, biodiesel production, CNS depressant/neuropathic pain, cytotoxicity/anticancer, genotoxic/mutagenic, hepatoprotective, insect repellants, immunomodulatory, larvicidal, molluscicidal/ovicidal/piscicidal, myelopoiesis, proteolytic/chitinolytics pharmacological activities. There is a need to isolate dynamic constituents, their biological trial, molecular mechanisms, experimental protection and legalization of therapeutic uses of E. tirucalli. The collected information will be helpful to locate up study protocol for recent drugs and Ayurvedic formulation expansion in curative and treat a variety of ailments.

GC-MS analysis of some volatile constituents extracted from stem of Euphorbia tirucalli Linn

Euphorbia tirucalli Linn. is traditionally used as medicine especially in the treatment of diseases caused by bacterial pathogens. The objectives of the present study were to identify the bioactive compounds in the stem of Euphorbia tirucalli Linn. using the gas chromatography-mass spectrometry (GCMS) analysis, and to investigate their potentials as an alternative for antimicrobial activity. Two-microliters of dried powdered of Euphorbia tirucalli Linn. stem were mixed with methanol followed by injection into splitless mode of GC-MS. Separation was achieved by Elite-5MS fused capillary column. The mass spectra were compared with the spectra of known components stored in the NIST and WILEY databases for compound identification. Forty-six chemical constituents were identified. The major constituents were lanosta-8,24-dien-3-ol, (3β)- (13.60%), (23S)-ethylcholest-5-en-(3β)-ol (7.02%), linoleic acid (2.96%) and viminalol (2.57%). Most of the active compounds present in the stem of Euphorbia tirucalli Linn. have previously been shown to exhibit antimicrobial properties.

The Antibacterial Properties of Euphorbia Tirucalli Stem Extracts against Dental Caries-Related

Euphorbia tirucalli are reported to possess antibacterial activity against various microorganisms. This in vitro study aimed to evaluate the antibacterial properties of Euphorbia tirucalli stems extracts (methanol, ethanol and aqueous extracts) against dental caries-related bacteria, i.e. Streptococcus mutans (S. mutans) and Streptococcus sobrinus (S. sobrinus). The antibacterial properties were determined using agar-well diffusion method at different extract concentrations (10, 20 and 30 mg/ml). Commercially available amoxicillin (10 µg) was used as positive control while the appropriate solvent served as negative control. The methanolic and ethanolic extracts of Euphorbia tirucalli stem were found to be effective against S. mutans and S. sobrinus. However, the aqueous extract of Euphorbia tirucalli stem showed no activity against both bacterial strains. The differences in the antibacterial properties in different extracts of Euphorbia tirucalli may be due to the differences in phytochemical constituents.

Euphorbia tirucalli L.: Review on morphology, medicinal uses, phytochemistry and pharmacological activities

The intention of current review is to make available up-to-date information on morphology, ecological biodiversity, medicinal uses, phytochemistry and pharmacolog-ical activities on different parts of Euphorbia tirucalli (E. tirucalli). This plant has a number of medicinal uses. Latex of E. tirucalli is vesicant and rubefacient which is used for rheumatism, warts, cough, asthma, ear-ache, tooth-ache and neuralgia. It acts as a purgative in small doses while in big doses it is bitter irritant and emetic. Milky juice is alexiteric, carminative and purgative. It is useful in whooping cough, gonorrhea, asthma, leprosy, dropsy, dyspepsia, enlargement of spleen, colic, jaundice and stone in bladder. The fresh milky juice is good alternative in syphilis and a good application in neuralgia. A decoction of branches is used in gastralgia and colic. Bark is used in treatment of fractures. Poultices prepared from the stem are useful to repair the broken bones. Boiled root liquid acts as an emetic in cases of snake-bite and for infertility in women. The wood is used for rafters, toys and veneering purposes. It is also useful against leprosy and foot paralysis subsequent to childbirth. E. tirucalli is reported to have euphol, β-sitosterol, euphorbol hexacosonate, cycloeuphordenol, cyclotirucanenol, tirucalicine, tri-methyl ellagic acid, gallic acids, terpenic alcohol, isoeuphorol, taraxasterol, tirucallol, euphor-one, euphorcinol, euphorbins, 12-deoxy-4β-hydroxyphorbol-13-phenyl acetate-20-acetate, 12, 20-dideoxyphorbol-13-isobutyrate, glut-5-en-3-β-ol, 3,3′-di-O-methylellagic acid, euphorbin-A (polyphenol), tirucallin-A (7) (tannin), tirucallin-B (11), euphorbin-F (14) (dimers), cycloartenol, 24-methylenecycloartenol, ingenol triacetate, 12-deoxy-4β-hydroxyphorbol-13-phenyl acetate-20-acetate, taraxerone, euphorginol, taraxerol, cam-pesterol, stigmasterol, palmitic acid, linoleic acid,β-amyrin, etc. active phytoconstituents. E. tirucalli have possessed activity in human-lymphocytes, analgesic, anthelmintics, antiarthritic, antibacterial/antifungal/antimicrobial, anti-HIV, anti-inflammatory, antioxi-dant, antiviral, biodiesel production, CNS depressant/neuropathic pain, cytotoxicity/anticancer, genotoxic/mutagenic, hepatoprotective, insect repellants, immunomodulatory, larvicidal, molluscicidal/ovicidal/piscicidal, myelopoiesis, proteolytic/chitinolytics phar-macological activities. There is a need to isolate dynamic constituents, their biological trial, molecular mechanisms, experimental protection and legalization of therapeutic uses of E. tirucalli. The collected information will be helpful to locate up study protocol for recent drugs and Ayurvedic formulation expansion in curative and treat a variety of ailments.

EFFECTS OF TOPICAL TREATMENT WITH EUPHORBIA TIRUCALLI LATEX ON THE SURVIVAL AND INTESTINAL ADHESIONS IN RATS WITH EXPERIMENTAL PERITONITIS / EFEITOS DO TRATAMENTO TÓPICO COM O LÁTEX DA EUPHORBIA TIRUCALLI NA SOBREVIDA E NAS ADERÊNCIAS INTESTINAIS DE RATOS COM PERITONITE EXPERIMENTAL

Background: The use of plants of the family Euphorbiaceae, particularly Euphorbia tirucalli (avelós) has been popularly widespread for treating a variety of diseases of infectious, tumoral, and inflammatory. Aim: To demonstrated antimicrobial and immunomodulatory effects of these extracts, evaluating the effect of a topical treatment with an aqueous solution of avelós latex on the survival and on intestinal adhesions in rats with experimental peritonitis. Methods: Peritonitis was induced in 24 Wistar rats, that were randomized into four groups of six as follows: (1) Control group (n=6), no treatment; (2) Antibiotic group (n=6), treatment with a single intramuscular dose of antibiotic Unasyn; (3) Saline group (n=6), the abdominal cavity was washed with 0.9% saline; and (4) E.tirucalli group (n=6), the abdominal cavity was washed with E. tirucalli at a concentration of 12 mg/ml. The animals that died were necropsied, and the time of death was recorded. The survivors were killed on postoperative day 11, and necropsy was subsequently performed for evaluation of the intestinal adhesions. Results: Significant differences were observed in the control and antibiotic groups (p<0.01) with respect to the survival hours when compared with the saline and E. tirucalli groups. There was no significant difference (p>0.05) in the survival of animals in the saline andE. tirucalli groups; however, one animal died in the saline group. Necropsy of the animals in the saline and E. tirucalligroups showed strong adhesions resistant to manipulation, between the intestinal loops and abdominal wall. The remaining groups did not show any adhesions. Conclusions: Topical treatment with E. tirucalli latex stimulated an increased formation of intestinal adhesions and prevented the death of all animals with peritonitis.

Racional: O uso de plantas da família Euphorbiaceae, principalmente a Euphorbia tirucalli (avelós), tem sido popularmente difundido para o tratamento de uma variedade de doenças de natureza infecciosa, tumoral e inflamatória. Objetivo: Avaliar o efeito do tratamento tópico com a solução aquosa do látex do avelós na sobrevida e nas aderências intestinas de ratos com peritonite experimental. Métodos: Foi induzido peritonite em 24 ratos Wistar e randomizados em quatro grupos de seis, assim distribuídos: 1) Controle - (n=6), nenhum tratamento; 2) Antibiótico - (n=6), tratamento com dose única intramuscular de antibiótico Unasyn (Pfizer - São Paulo); 3) Salina - (n=6), lavagem da cavidade abdominal com solução fisiológica 0,9%; 4) E.Tirucalli - (n=6), lavagem da cavidade abdominal com E. tirucalli na concentração de 12 mg/ml. Os animais que morreram foram submetidos à necropsia e o horário do óbito anotado. Os sobreviventes foram submetidos à eutanásia no 11odia de pós-operatório e, posteriormente, realizou-se a necropsia para avaliação da formação de aderências. Resultados: Os grupos controle e antibiótico obtiveram diferença significativa (p<0,01) com relação às horas de vida entre os grupos salina e E. tirucalli. Não houve diferença significativa (p>0,05) na sobrevida dos animais dos grupos salina e E. tirucalli, no entanto, houve um óbito no grupo salina. A necropsia dos animais dos grupos salina e E. tirucalli mostrou aderências firmes e resistentes à manipulação entre alças intestinais e parede abdominal. Os demais grupos não tiveram formação de aderências. Conclusão: O tratamento tópico com o látex da E. tirucalli estimulou maior formação de aderências intestinais e evitou o óbito de todos animais com peritonite até o período avaliado.

Angiogenic activity of latex from Euphorbia tirucalliLinnaeus 1753 (Plantae, Euphorbiaceae) / Atividade angiogênica do látex da Euphorbia tirucalliLinnaeus 1753 (Plantae, Euphorbiaceae)

AbstractTo assess the pro-angiogenic activity of Euphorbia tirucalli, commonly known as “avelós” plant, we performed a series of tests by applying an aqueous E. tirucalli latex solution (10 mg/mL) to the chorioallantoic membranes (CAMs) of 80 fertilized chicken eggs incubated in a temperature- and humidity-controlled automatic incubator. The results indicated that the aqueous latex solution increased vascular network formation compared to that with the negative control (p < 0.05) and the inhibitor control (p < 0.05). This suggests that under the experimental conditions tested, the aqueous latex solution induced an inflammatory response leading to neoangiogenesis.

ResumoCom o objetivo de analisar a atividade angiogênica apresentada pela Euphorbia tirucalli, popularmente conhecida comumente como “avelós”, foram realizados ensaios utilizando solução aquosa de látex na concentração de 10 mg/ml, aplicada em membrana corioalantóide (MCA) de 80 ovos férteis de galinha, incubado em estufa automática com temperatura e umidade controladas. Os resultados apontaram que a ação da solução aquosa provocou aumento da percentagem da rede vascular formada em relação aos controles negativo (p<0,05) e inibidor (p<0,05), indicando que nas condições deste experimento, foi responsável pela ativação da resposta inflamatória e crescimento de novos vasos sanguíneos.

Análise fitoquímica e atividade fotoprotetora de extrato etanólico de Euphorbia tirucalli Linneau (Euphorbiaceae) / Phytochemical analysis and photoprotective activity of theethanolic extract of Euphorbia tirucalli Linneau (Euphorbiaceae)

RESUMO Euphorbia tirucalli Linneau, conhecida popularmente como "avelós", "cachorro pelado" ou "pau-pelado", é utilizada na medicina popular para o tratamento de câncer, antibiótico e antivirótico. As plantas medicinais são, frequentemente, utilizadas com o intuito de substituir ou auxiliar as terapias convencionais no tratamento de várias doenças, inclusive para evitar os malefícios causados por radiações ultravioletas. Com isso, o objetivo desta pesquisa foi avaliar o potencial fotoprotetor e a triagem fitoquímica do extrato etanólico das partes aéreas de avelós. A atividade fotoprotetora foi avaliada por meio de ensaios in vitro segundo o método adaptado de Mansur, utilizando extrato etanólico das partes aéreas. Os resultados obtidos mostraram que o estudo fitoquímico evidenciou a presença de açúcares redutores, alcaloides, fenóis, flavonoides, taninos, saponinas, esteroides e triterpenóides na fração etanólica. O extrato apresentou capacidade antioxidante (EC50) de 16,98 ± 0,35 µg.mL-1, teor de compostos fenólicos de 96,18 ± 1,33 mg EqAG/g e flavonoides de 63,57 ± 2,74 mg EqC/g que podem favorecer a atividade fotoprotetora. Avaliando o fator de proteção solar, pode-se observar que todas as concentrações testadas (0,01 a 0,1 µg.mL-1) apresentaram potencial de fotoproteção da radiação ultravioleta com variação de FPS de 6,05 a 19,84, respectivamente. Esses resultados sugerem que o extrato etanólico de Euphorbia tirucalli Linneau apresenta possível efeito fotoprotetor

ABSTRACT Euphorbia tirucalli Linneau, popularly known as "avelos", "naked cock" or "naked dog", is used in popular medicinein order to treat cancer, antibiotic and antiviral diseases. Herbal medicines are often employed in order to assist or replace conventional therapies for the treatment of several diseases, including the prevention of the damage caused by ultraviolet radiation. Thus, the aim of this research was to evaluate the photoprotective potential and phytochemical screening of the ethanol extract of the aerial parts of avelos. The photoprotective activity was assessed by in vitrotrials according to the method adapted from Mansur, using the ethanol extract of the aerial parts. The results showed that the phytochemical study revealed the presence of reducing sugars, alkaloids, phenols, flavonoids, tannins, saponins, steroids and triterpenoids in ethanolic fraction. The extract showed antioxidant activity (EC50) of 16,98 ± 0,35 µg.mL-1, phenolic contents of 96,18 ± 1,33 mg EqAG/g and 63,57 ± 2,74 flavonoids from mg EqC/g that can advantage the photoprotective activity. Assessing the sun protection factor, it can be observed that all the tested concentrations (0,01 to 0,1 µg.mL-1) showed potential for photoprotection from ultraviolet radiation with a range of 6,05 to 19,84 FPS, respectively. These results suggest that the ethanol extract of Euphorbia tirucalli Linneau presents possible photoprotective effect

Antifungal activity against Cryptococcus neoformans strains and genotoxicity assessment in human leukocyte cells of Euphorbia tirucalli L.

In the last times, focus on plant research has increased all over the world. Euphorbia tirucalli L., a plant known popularly as Aveloz, and originally used in Africa, has been drawing attention for its use in the United States and Latin America, both for use as an ornamental plant and as a medicinal plant. E. tirucalli L. is a member of the family Euphorbiaceae and contains many diterpenoids and triterpenoids, in particular phorbol esters, apparently the main constituent of this plant, which are assumed to be responsible for their activities in vivo and in vitro. The in vitro antifungal activities of Euphorbia tirucalli (L.) against opportunistic yeasts were studied using microbroth dilution assay. The results showed that aqueous extract and latex preparation were effective against ten clinical strains of Cryptococcus neoformans in vitro (Latex and extract MIC range of 3.2 - > 411 µg/mL). Aiming the safe use in humans, the genotoxic effects of E. tirucalli were evaluated in human leukocytes cells. Our data show that both aqueous extract and latex preparation have no genotoxic effect in human leukocytes cells in vitro. Although the results cannot be extrapolated by itself for use in vivo, they suggest a good perspective for a therapeutic application in future. In conclusion, our results show that the aqueous extract and latex preparation from E. tirucalli L. are antifungal agents effectives against several strains of C. neoformans and do not provoke DNA damage in human leukocyte cells, considering the concentrations tested.

The crude latex of Euphorbia tirucalli modulates the cytokine response of leukocytes, especially CD4+ T lymphocytes

The plants of the Euphorbiaceae family, especially those of the genus Euphorbia, are frequently used by Brazilian folk communities to treat a wide variety of infectious, tumoral and inflammatory illnesses. Among the species of this genus, Euphorbia tirucalli L. is widely used in some Brazilian regions, such as the Jequitinhonha River Valley. There is evidence that the latex produced by E. tirucalli has antiviral and antitumor activities, but little is known about the mechanisms involved in these effects. It is likely that the mechanism for such activities involves leukocyte activation and cytokine production. In this work, we aimed to evaluate the production of type 1 (TNF-α and IFN-γ) and type 2 (IL-4 and IL-10) cytokines by circulating leukocyte subsets submitted to brief stimulation with the crude latex of E. tirucalli. Peripheral blood leukocytes of twenty healthy subjects were submitted to 4 h incubation with crude E. tirucalli latex diluted in dimethylsulfoxide. After the incubation period, the cells were stained with FITC-conjugated monoclonal antibodies specific to the cell surface receptors CD4, CD8 and CD14, and to PE-conjugated monoclonal antibodies specific to the cytokines TNF-α, IFN-γ, IL-4 and IL-10. The acquisition and analysis of data were performed by flow cytometry. The results showed a significant increase (p<0.05) in the percentage of CD4+ T lymphocytes positive for the type 1 cytokines TNF-α and IFN-γ. Neutrophils and CD8+ T lymphocytes showed a mixed profile of cytokine production, characterized by an increase in the percentage of cells expressing IFN-γ, TNF-α, and IL-10. The data indicate a predominant type 1 cytokine response. The findings presented suggest that the effect popularly attributed to E. tirucalli usage may be attributed to its effect on the production of TNF-α and IFN-γ. However, the relationship between the in vitro and in vivo effects of E. tirucalli needs to be investigated.

Physical chemical and citotoxic evaluation of highly diluted solutions of Euphorbia tirucalli L. prepared through the fifty milesimal homeopathic method / Avaliação físico-química e citotóxica de soluções altamente diluídas de euphorbia tirucalli l. Preparada pelo método cinqüenta milesimal (lm) / Evaluación físico-química y citotóxica de soluciones altamente diluídas de Euphorbia tirucalli L. preparadas por el método homeopático cincuenta milesimal (LM)

Motivação: Embora Hahnemann tenha descrito o método LM na 6ª. Edição do Organon da Arte de Curar, poucas pesquisas tem sido feitas sobre as propriedades físico-químicas destas preparações. Além disso, ainda não existem evidências que apontem para a correlação entre propriedades físico-químicas e os efeitos biológicos das altas diluições. Objetivos: determinar características físico-químicas das preparações LM tais como condutividade elétrica, pH e índice de refração, bem como o efeito biológico em modelos experimentais. Materiais e Métodos: foi analisada uma série de diluições desde 1 lm até 10 lm de Euphorbia tirucalli L., preparada a partir do látex e do suco da planta. Para considerar as características sazonais desta planta, usamos 2 populações diferentes, colhidas uma em Junho de 2007 e outra em Maio de 2008. Além disso, o efeito citotóxico da Euphorbia tirucalli L. 5 lm foi testado em células humanas cancerosas (MCF7) através de ensaio MTT. Conclusões: Algumas diferenças entre as duas populações foram observadas. No entanto, nenhuma correlação clara pode ser observada entre as propriedades físico-químicas e a atividade biológica.

Background: although Hahnemann described the fifty-milesimal (LM) method in the 6th edition of the Organon of the Medical Art, very little research has been carried out on the physical chemical properties of these homeopathic preparations. Furthermore, there is still no evidence allowing for the correlation between the alleged physical chemical properties and the biological effects of high dilutions. Aims: to evaluate physical chemical characteristics of LM preparations including electrical conductivity, pH and refraction index, and their effect on biological experimental models. Materials and methods: preparations tested for physical chemical analysis were dilutions 1 lm to 10 lm of Euphorbia tirucalli L. prepared from the latex and the juice of the plant. To rule the seasonal characteristics of this plant, 2 different populations were used, one collected in June 2007 and the other in May 2008. Furthermore, the cytotoxic effect of Euphorbia tirucalli 5 lm was tested on human breast cancer cells (MCF7) through MTT assay. Conclusions: Some differences among the two collections were observed. However, any clear correlation could be observed between physical chemical properties and biological activity.

Motivación: Aunque Hahnemann describió el métodocincuenta milesimal (LM) en la 6 ª edición del Organon del Arte Médica, muy poca investigación se ha realizado sobre las propiedades físico-químicas de estos preparados homeopáticos. Por otra parte, todavía no hay pruebas que permitan la correlación entre las presuntas propiedades físico-químicas y los efectos biológicos, de las altas diluciones. Objetivos: evaluar las características físico-químicas de los preparados LM, incluyendo conductividad eléctrica, pH y el índice de refracción, y su efecto en modelos biológicos experimentales. Materiales y métodos: las muestras para el análisis físico-químico fueron diluciones 1 a 10 lm de Euphorbia tirucalli L. preparadas a partir del látex y el jugo de la planta. Para descartar las características sazonales de esta planta, dos poblaciones diferentes fueron utilizadas, una recogida en junio de 2007 y otro en mayo de 2008. Además, el efecto citotóxico de Euphorbia tirucalli 5 lm fue probado en células humanas de cáncer de mama (MCF7) a través del ensayo MTT. Conclusiones: Algunas diferencias entre las dos colecciones se observaron. Sin embargo, ninguna correlación clara se observó entre las propiedades físicas- químicas y actividad biológica.