Search

Three new ingol diterpenoids, 8,12-O-diacetylingol-7-benzoyl-3-tiglate (1), 12-O-acetylingol-3,7-dibenzoyl-8-tiglate (2) and 3,12-O-diacetyl-7-O-benzoylingol-8-tiglate (3), were isolated from the aerial parts of Euphorbia royleana, together with three known ingol derivatives (4-6). Their structures were elucidated by the extensive HR-MS, 1H NMR, 13C NMR, HSQC, HMBC, 1H-1H COSY, ROESY and CD analyses. The cytotoxic activities of 1-3 were evaluated by MTT methods.

Background: Natural products have been shown to be reliable sources of anticancer medicines although there is still a consistent demand for new therapeutic natural products for cancer treatment with minimal side-effects.Materials and Methods: In this study, six plant extracts (Grevillea robusta; Euphorbia millii; Euphorbia royleana; Aloe grandidentata; Bauhinia corniculate; and Cassia fistula) were screened for the presence of phytochemical metabolites as saponins, tannins, cardiac glycosides, alkaloids, flavonoids, anthraquinones and sterols, using qualitative tests. Antiproliferative screening assay was performed on a panel of three cancer cell-lines (HepG-2, HCT-116 and MCF-7) using MTT assay, and cytotoxicity was determined using WI-38 human fibroblast cell- line.Results: Some plant extracts reduced cellular growth for the selected cancerous cell-lines. For example, E. royleana and A. grandidentata extracts reduced HepG-2 cellular growth with IC50 of 0.42 and 0.53μg/mL, respectively. Moreover, A. grandidentata and C. fistula reduced cellular growth of MCF-7 with IC50 of 0.37 and 0.67 μg/mL, respectively. Conclusion: E. royleana, A. grandidentata and C. fistula showed significant anti-proliferative activity against HepG-2 and MCF-7 cell-lines with non-cytotoxic nature. This suggests their potential role as anticancer agents against these types of cancer. The presence of flavonoids, sterols and anthraquinones may suggest their enhanced anti-proliferative activities. Therefore, this study has shed light on the possible use of these extracts as potential sources of natural products-based therapy for cancer.

Oxidative stress is associated with streptozotocin induced diabetes. The present study was conducted to investigate the anti-oxidant, anti-diabetic and genotoxic effects of Euphorbia royleana Boiss...

The present study was carried out to identify the 20 medicinally important species of family Euphorbiaceae by the aid of scanning electron microscopy (SEM) of the foliar anatomical characteristics. Both qualitative and quantitative measurements for the anatomical characters like epidermal cells, stomata, trichomes, and subsidiary cells on both abaxial(ab) and adaxial(ad) epidermis were recorded. Remarkable variations in these anatomical features had been observed among the studied Euphorbiaceae species. Most species had epidermal cells irregular or polygonal in shape, only five species had hexagonal cells, that is, Euphorbia neriifolia L., Euphorbia prostate Aiton, Jatropha integerrima Jacq., Vernicia fordii (Hemsl.), and Euphorbia royleana Boiss. Stomata were abundant on abaxial epidermis as compared to adaxial epidermis. E. prostate Aiton, Euphorbia pulcherrima Willd. Ex Klotzsch and Phyllanthus emblica L. possessed anomocytic stomata, and Euphorbia helioscopia L., Euphorbia cotinifolia L., E. neriifolia L., and Ricinus communis L. possessed anisocytic stomata, while rest of the species had paracytic stomata. Trichomes were present in very few species including Euphorbia hirta L., E. prostate Aiton, E. pulcherrima Willd. Ex Klotzsch, and Putranjiva roxburghii Wall. Similarly, variations were also reported by quantitative features such as E. helioscopia L. can be distinguished from E. hirta on the basis of length of epidermal cells, that is, 103.4 ± 0.15 and 74.9 ± 0.55 μm, respectively. Moreover, E. pulcherrima Willd. Ex Klotzsch had trichomes with the length of 408 ± 0.55 μm and P. roxburghii Wall. had trichome with the length of 314.2 ± 1.35 μm, respectively. These findings confirmed that taxonomic utility of the anatomical traits for the identification of studied Euphorbiaceae taxa.

The bark extract of Euphorbia royleana as a green corrosion inhibitor was studied in 1M HCl using weight-loss method and potential measurement. The results show that the bark extract of Euphorbia royleana is an effective anti-corrosion inhibitor of mild steel in acidic media. The corrosion rate decreases with the time of immersion. Weight loss experiment shows that the loss in weight decreases with the time of immersion and inhibition efficiency increases with the concentration of extract. It was observed that maximum inhibition efficiency is 99.60% in 100% concentration of extract. Potential measurement study shows that bark extracts act as a mixed type of inhibitor i.e. inhibits both anodically as well as cathodically.

Two ingenane- (1 and 2), two ent-atisane- (3 and 4), two ent-kaurane- (5 and 6), two ent-abietane- (7 and 8), and one ent-isopimarane-type (9) diterpenoid and 12 known analogues have been isolated from the methanolic extract of the stems of Euphorbia royleana. Their structures, including absolute configurations, were determined by extensive spectroscopic methods and ECD data analysis. The nitric oxide inhibitory activities of those diterpenoids were examined biologically in lipopolysaccharide-stimulated BV-2 cells, with compounds 1, 2, 5–7, 10, and 12 having IC50 values lower than 40 μM. Molecular docking was used to investigated the possible mechanism of compounds 1, 2, 5–7, 10, and 12.

In this study toxicity of Euphorbia royleana latex and stem bark extract was evaluated in a static bioassay test for the fry and fingerlings of freshwater fish Channa punctatus. For fry the LC50 values for Euphorbia royleana latex were 12.66, 6.27, 4.04 and 3.05 mg/L whereas for stem bark extract the LC50 values were 113.77, 89.16, 71.99 and 56.59 mg/L for 24, 48, 72 and 96 h, respectively. It seems that toxicity of latex was more pronounced as compared to stem bark extract. The LC50 values for latex for fingerlings were 22.58, 18.14, 14.99 and 12.34 mg/L whereas for stem bark extract the LC50 values were 614.35, 585.06, 535.93 and 475.37 mg/L for 24, 48, 72 and 96 h, respectively. The activities of the latex and stem bark extract were time- and dose-dependant. The present study clearly indicates that Euphorbia royleana extracts should be applied with great precautions nearby the aquatic reservoirs as it is toxic to growing stages of the fish.

Phytochemical investigation on the 95% EtOH extract of the Traditional Chinese Medicine (TCM) Euphorbia royleana (Ba-wang-bian in Chinese) led to the isolation of 11 diterpenoids (1–11) and two triterpenoids (12 and 13). Among them, compounds 1 and 2 were new ingenane and ingol diterpenoids, respectively. Their structures were elucidated by a combination of spectroscopic analyses (1 D and 2 D NMR, HRMS, ECD, UV, and IR data) and chemical methods. Compounds 12 and 13 exhibited moderate cytotoxicities in vitro against human lung cancer cell line A549 with IC50 values of 14.84 ± 0.56 and 27.11 ± 1.65 µM, respectively.

The present study had been conducted in Swathi village of Nawalparasi district, which is rich in traditional knowledge. The primary aim of the study was to document medicinal plants used to cure various ailments in Tharu community in Swathi village. Data was collected through semi-structured interviews, household survey, and focus group discussion. Altogether 105 plant species of medicinal values were recorded belonging to 94 genera and 50 families, among which Fabaceae accounts as the most dominant species, i.e., 12 species. Most of the species found in the study area found in wild of which herbs account as the most used lifeform. Leaves were the widely used plant part practiced to treat human ailments. These plant species were evaluated in terms of parts use category, habit category, mode of use category, disease use category, medicinal use pattern and multiple uses, number of use reports, and number of taxa uses to treat different ailments. These medicinal plants were documented with their scientific name, local name, family, and lifeform of plants. Especially local faith healers, Guruwas, and elderly people had rich knowledge about the traditional use of medicinal plants. Women of the study area had rich knowledge on the use of plants for different purposes. Respiratory diseases and fever ailments have the highest ICF (0.80), whereas ureno-genital disorders have the lowest (0.25) ICF. Euphorbia royleana, Cuscuta reflexa, Bryophyllum pinnatum, and Artemisia indica have the highest FL (100% each) being used for respiratory disease and fever, others (jaundice), and gastrointestinal disorders, respectively. Further biological studies should also be conducted on the reported medicinal plant species of the study area to utilize them in drug development. Further studies are needed to evaluate the efficacies and possible side effects of the traditional medicinal plants before they are recommended for their wider use in both the study area and elsewhere in the country.

Background Canine mammary gland tumors (cMGTs) are the most common neoplasms in intact female canines and viewed as a suitable model for studying human breast cancers. Euphorbia royleana has been reported to have a variety of antitumor efficacies. We have prepared the crude extracts of E. royleana in ethanol and hexane solvents to evaluate the anti-tumor effects for cMGT in vitro and in vivo. Results The results showed that E. royleana could inhibit cell proliferation and colony formation in cMGT cells. The suppression of tumor cell growth resulted from necrosis and cell cycle arrest. Moreover, autophagy appears to play a critical role in E. royleana-mediated cell death by triggering cell apoptosis. The in vivo results also revealed that E. royleana treatment could reduce the size of solid tumors while exhibiting low toxicity in cMGT-bearing nude mice. Conclusions The anti-tumor mechanisms of E. royleana were firstly verified to show it would cause autophagic cell death, apoptosis, and cell cycle arrest in canine mammary tumor cells. The in vitro and in vivo findings in the present study revealed E. royleana has potential anticancer effects for the treatment of canine mammary gland tumors.

Background: We aimed to evaluate effect of Euphorbia royleana exposure on histocytology of corpuscles of Stannius in fish, Heteropneustes fossilis. Methods: Fish were subjected to 2.47 mg/L and 0.618 mg/L of E. royleana for short-term and long-term exposure, respectively. Blood samples were collected on 24, 48, 72 and 96 h in short-term and after 7, 14, 21, and 28 d in long-term experiment and analyzed for serum calcium levels. Corpuscles of Stannius were fixed on these intervals. Results: Serum calcium levels of H. fossilis decline progressively from 48 h until 96 h following the E. royleana exposures. Serum calcium levels decreased on 7 d. This decrease continued until close of the experiment. After 96 h treatment, AF–positive cells of CS exhibit increased granulation. Nuclear volume of these cells exhibited no change throughout short-term treatment. Increased nuclear volume of AF– negative cells of CS is noticed at 96 h. Nuclear volume of AF-positive cells decreases after 14 d and onwards. The AF–positive cells exhibit increased granulation following 21 d exposure. After 28 d these changes are intensified and few degenerating cells have been encountered. AF–negative cells of CS increase in their nuclear volume 21 d onwards. Conclusion: The botanical pesticide induced severe changes in the corpuscles of Stannius of catfish. This gland controls the calcium level in fish and thus the use of E. royleana should not be done near water reservoirs.

Eight previously undescribed diterpenoids, euphoroyleans A−H, including two cembranes, three ingenanes, two ent-atisanes, and one ent-kaurane, along with 22 known analogues were isolated from the whole plants of Euphorbia royleana. The structures of euphoroyleans A−H, including the absolute configurations, were elucidated by extensive spectroscopic analyses, chemical transformation, and single crystal X-ray diffractions. All the isolates were screened for their chemoreversal abilities on P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) cancer cell line HepG2/DOX, and eight compounds exhibited significant activities. Among them, ingol-3,7,12-triacetate-8-benzoate, the most active MDR modulator with no obvious cytotoxicity, could enhance the efficacy of anticancer drug DOX to ca. 105 folds at 10 μM, being stronger than the positive drug verapamil. Mechanistic study revealed that ingol-3,7,12-triacetate-8-benzoate could inhibit the transport activity of P-gp rather than its expression, and the possible recognition mechanism between compounds and P-gp was predicted by molecular docking.

Fiber reinforced polymer composites are used for building and structural applications due to their high strength. In conventional composites both the binder and the reinforcing fibers are synthetic or either one of the material is natural. In the present study coagulum of Euphorbia royleana has been used for replacing polyester resinas binder in polyester banana composite. Euphorbia coagulum (driedlatex) is rich in resinous mass (60-80%), which are terpenes and polyisoprene (10-20%). Effect of varying percentage of coagulum content on various physico-mechanical properties of polyester-banana composites has been studied. Since banana fiber is sensitive to water due to presence of polar group, banana composite undergoes delamination and deterioration under humid condition. Alkali treated banana fiber along with coagulum content has improved overall mechanical properties and reduction in water absorption. The best physico-mechanical properties have been achieved on replacing 40% of polyester resin by coagulu...

Many natural compounds produced within plants like alkaloids, flavonoids, and terpenoids are reported to have possible anti-HIV potential which can target reverse transcriptase or protease and inhibit replication. Many flavonoids like swertifrancheside, glycyrrhizin, and chrysin are known to be effective against HIV infection. Plants like Acer okamotoanum, Aegle marmelos, Argemone mexicana, Andrographis paniculata, Asparagus racemosus, Azadirachta indica, Bulbine alooides, Canna indica, Coleus forskohlii, Garcinia speciosa, Geum japonicum, Humulus lupulus, Magnolia spp., Musa acuminata, Ocimum sanctum, Polyalthia suberosa, Rubia cordifolia, Syzygium cumini, Terminalia chebula, and Tinospora cordifolia revealed promising anti-HIV activities, and their potential against AIDS is being explored. Antiviral activities of different trees are described, which include Artocarpus integrifolia, Aegle marmelos, Caesalpinia pulcherrima, Gleditsia triacanthos, Euphorbia royleana, Jatropha curcas, Heterophragma adenophyllum, Mimusops elengi, Platanus orientalis, Syzygium cumini, and Tamarix aphylla.

Presently composites made up of either both the binder and the reinforcing fibers are synthetic or either one of the material is natural or synthetic. In the present study coagulum (dried latex) of Euphorbia royleana has been used for replacing polyester resin as a natural binder in polyester banana fiber composite. The influence of different volume fraction of the coagulum in the composite is studied. It is observed that with the increase in the coagulum fraction, the flexural property of the polyester banana fiber composite increases. The flexural strength increase by 25% and flexural modulus by 15% at 40% of coagulum weight fraction. This study presents the possibility of preparation of composites using coagulum of Euphorbia latex. The developed composite may be used in partition walls, roof tiles, interior linings of automobiles, etc as wood substitute.

The aim of the present study was to determine changes in blood electrolytes (calcium and phosphate) in the freshwater catfish Heteropneustes fossilis following short- and long-term exposure to latex of Euphorbia royleana. To investigate the effects of short-term exposure, fish were exposed to 80% of the 96-h LC(50) of E. royleana latex (2.47 mg/L) for 96 h. To assess the effects of long-term exposure, fish were exposed to 20% of the 96-h LC(50) of E. royleana latex (0.618 mg/L) for 28 days. Fish were killed after 24, 48, 72 and 96 h (short-term experiments) or after 7, 14, 21 and 28 days (long-term experiments). Blood samples were collected and sera were analyzed to determine calcium and inorganic phosphate levels. Serum calcium levels decreased progressively in H. fossilis after 48 h exposure to E. royleana latex. This decrease persisted until the end of the experiment (96 h). Serum inorganic phosphate levels in treated fish decreased progressively from 72 h. After 7 days exposure to E. royleana latex, decreased serum calcium levels were noted in H. fossilis that persisted until the end of the experiment. Serum phosphate levels were decreased in H. fossilis on days 21 and 28 of exposure to E. royleana latex. It is concluded that E. royleana latex alters the blood electrolyte content of the fish. The change in these electrolytes, particularly calcium levels, may cause disturbances in the normal vital physiological functions of the fish, its growth rate, and even its ability to survive in nature.

The latex of four plants viz. Euphorbia royleana, Jatropha gossypifolia (Euphorbiaceae), Nerium indicum and Thevetia peruviana (Apocynaceae) caused significant reduction in acid/alkaline phosphatase activity and anti-acetylcholinesterase activity in nervous tissue of freshwater air breathing fish Channa marulius. The reduction in the activity of both phosphatases and AChE were time as well as dose dependent.

Exposure of fish over 96 h to 40 and 80% of LC 50 (24 h) of aqueous latex extracts of Euphorbia royleana and Jatropha gossypifolia of family Euphorbiaceae significantly altered the level of total protein, total free amino acids, nucleic acids, pyruvate, lactate, glycogen and as well as protease activity also in muscle, liver and gonadal tissue of the fish Channa punctatus . The alterations in all the biochemical parameters were significantly dose-dependent. Withdrawal study also shows that there is a partial recovery in the levels of glycogen, pyruvate, lactate and nucleic acids, but nearly complete recovery in total protein, total free amino acids level and protease activity in all the three tissues of the fish after the 7th day of the withdrawal of treatment, which supports the view that the plant product is safer in use as pesticides for control of common weed fishes in culture ponds.

The hydrosoluble fraction of Euphorbia royleana latex (AER), administered by gavage at doses of 50–200 mg/kg, showed dose-dependent anti-inflammatory and anti-arthritic effects in different acute and chronic test models in rats and mice. It reduced the exudate volume and the migration of leukocytes and showed a poor inhibitory effect on the granuloma formation induced by cotton pellets, while it had a low ulcerogenic score. The oral LD50 was more than 1500 mg/kg in both rats and mice.

Ethnopharmacological relevance Poisonous plants comprise the third largest category of poisons known around the world. Other than affecting the humans directly, they are the major cause of economic losses in the livestock industry since the advent of civilisation. Aim of the present study was to collect and systematically document the traditional knowledge of poisonous plants of Udhampur District for the benefit of humanity before it is entombed forever. Material and methods Direct interviews of the informants were conducted and the plants identified as poisonous by them were collected, identified and herbarium sheets were prepared. The data collected through interviews was analysed with two quantitative tools viz. the factor informant consensus and fidelity level. Results A total of 90 toxic plants were listed from the study site. Most dominant toxic families were Fabaceae, Asteraceae, Solanaceae, Apocynaceae and Euphorbiaceae. Most of the poisonous plants were herbs (57.1%) and the whole plant toxicity was reported to be the highest (32.4%) followed by leaves (23.1%). According to the factor informant consensus, gastrointestinal category had the greatest agreement closely followed by the death category. The most important species on the basis of fidelity level for gastrointestinal category were Cannabis sativa, Cassia occidentalis, Cuscuta reflexa, Euphorbia helioscopia and Euphorbia hirta, for death category were Anagalis arvensis, Embelia robusta and Prunus persica, for dermatological category Euphorbia royleana, Leucaena leucocephala, Parthenium hysterophorus and Urtica dioica, and for sexual illness category were Calotropis procera and Carica papaya. Conclusion Further phytochemical and pharmacological studies are required to ascertain the toxic components of the poisonous plants, so that they may be utilised for the betterment of future generations.

The antiinflammatory activity of the ethyl acetate extract (EA) from the residue of an 85% alcohol extract of the latex of plant Euphorbia royleana was tested in mice and rats. In acute tests EA displayed marked antiinflammatory activity. Significant antiarthritic activity was observed in subacute and chronic models of formaldehyde-induced arthritis, adjuvant-induced developing and established arthritis. It produced inhibition of the exudate volume and the leucocyte migration in rats and vascular permeability in mice. EA showed a poor inhibitory effect on the granuloma formation by cotton pellet and croton oil. In in vitro studies EA inhibited the spontaneous contractions of the isolated pregnant rat uterus and oxytocin-induced contractions of virgin rat uterus. It had a very low ulcerogenic potential. The oral LD 50 in both rats and mice was more than 2500 mg/kg.

Heteropneustes fossilis were subjected to high and low doses of the latex of Euphorbia royleana for short-term and long-term exposures, respectively. The blood was analyzed for plasma calcium levels, and the ultimobranchial glands fixed and examined. Serum calcium levels declined after 48 h following short-term exposure, and this decrease continued until the end of the experiment. The ultimobranchial cells exhibited a decrease in the cytoplasmic staining response after 96 h following treatment, and the nuclear volumes slightly decreased. Chronically exposed fish also exhibited a decline in serum calcium levels, but much later, on day 7, again progressively declining until the close of the experiment. Up to day 14 following treatment there was no change in histological structure of the ultimobranchial glands, but then there was a decrease in nuclear volume and the cytoplasm displayed a weak staining response. There was some vacuolization and degeneration. Keywords: Botanicals, calcitonin, calcium, teleost

The latex of four plants belonging to the family Euphorbiaceae viz. Jatropha gossypifolia, Euphorbia royleana, Euphorbia antisyphlitica and Euphorbia lactea cristata caused significant reductions in the acid and alkaline phosphatase activity in nervous tissue of the snail Lymnaea acuminata. The reduction in the activity of both the phosphatases was time and dose dependent; the order of effectiveness was as follows: Euphorbia lactea cristata > Euphorbia antisyphlitica > Euphorbia royleana > Jatropha gossypifolia. It has been suggested that the inhibition of these enzymes might be through activation of Protein Kinase C.

Mortality to fish Channa punctatus caused by the latices of four species of terrestrial plants belonging to family Euphorbiaceae and Apocynaceae have been reported. It was found that extremely dilute aqueous solutions of the latex were effective in killing the fishes. The ranking of toxicity of four plants was Nerium indicum > Euphorbia royleana > Thevetia peruviana > Jatropha gossypifolia. It has been suggested that these plant products cannot be used directly in freshwater ecosystem unless their detailed toxicity has been studied on the beneficial freshwater animals. Die akute Toxizitat von Pestiziden pflanzlichen Ursprunges fur den Suswasserfisch Channa punctatus Berichtet wird uber die Mortalitat von Channa punctatus, verursacht durch die Safte aus vier terrestrischen Pflanzenarten der Familien Euphorbiaceae und Apocynaceae. Selbst extreme wassrige Verdunnungen der Pflanzensafte erwiesen sich als effektiv toxisch fur die Fischart. Die Reihenfolge der Toxizitat ergibt sich zu Nerium indicum > Euphorbia royleana > Thevetia peruviana > Jatropha gossypifolia. Es wird vorgeschlagen, diese pflanzlichen Produkte nicht in Suswassersystemen anzuwenden, bevor nicht ihre Toxizitat gegen Suswasserorganismen naher untersucht ist.

Ten new ingol lathyrane-type diterpenes (1-10) and two known ingenol derivatives (11 and 12) were isolated from the aerial parts of Euphorbia royleana. The structures of 1-10 were elucidated on the basis of spectroscopic methods including 2D NMR analysis, and the structure of compound 1 was confirmed by single-crystal X-ray crystallography. Antiangiogenic effects of all compounds except for 5 were tested using a zebrafish model, with compounds 11 and 12 being active in this bioassay.

The ethyl acetate fraction (EA) from the residue of an 85% ethanol extract of the latex of Euphorbia royleana (Euphorbiaceae) was investigated for antipyretic and analgesic properties. The results showed a dose related peripheral analgesic effect. The fraction assayed exhibited a significant antipyretic effect in hyperthermic rats and rabbits. The oral LD50 was more than 2 g/kg in rats and mice. © 1997 John Wiley & Sons, Ltd.

Different dilutions of aqueous and methanolic extracts of lattices of Nerium indicum (Apocynaceae) and Euphorbia royleana (Euphorbiaceae) were administered for 24h and 48h to the Culex quinquesfasciatus (Diptera: Culicidae) larvae in order to test their lethality. The larvicidal activity of lattices of both plants, were time and dose dependent respectively. There was a significant negative correlation between LC values and exposure periods. The result also indicates that the different dilutions of the lattices of both plants also significantly delayed the post-embryonic development of Culex larvae. Methanolic extract of N. indicum is 1.8 times more toxic than aqueous extract while in case of E. royleana, the methanolic extract was 16 times more toxic in comparison to aqueous. Key Words: Nigerian Journal of Natural Products and Medicine Vol.7 2003: 61-64

Different dilutions of aqueous and methanolic extracts of lattices of Nerium indicum (Apocynaceae) and Euphorbia royleana (Euphorbiaceae) were administered for 24h and 48h to the Culex quinquesfasciatus (Diptera: Culicidae) larvae in order to test their lethality. The larvicidal activity of lattices of both plants, were time and dose dependent respectively. There was a significant negative correlation between LC values and exposure periods. The result also indicates that the different dilutions of the lattices of both plants also significantly delayed the post-embryonic development of Culex larvae. Methanolic extract of N. indicum is 1.8 times more toxic than aqueous extract while in case of E. royleana , the methanolic extract was 16 times more toxic in comparison to aqueous. Key Words: Nigerian Journal of Natural Products and Medicine Vol.7 2003: 61-64