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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...

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.

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.

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.

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 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.

The objective of the study was to investigate the activity of the ethyl acetate (EA) fraction of Euphorbia royleana latex on cellular and humoral-mediated immune responses and phagocytic function of the cells of the reticuloendothelial system in mice. Oral administration of EA at doses of 50, 100 and 200 mg/kg p.o. in mice with sheep red blood cells (SRBC) as an antigen-inhibited both the delayed-type hypersensitivity reaction and the production of circulating antibody titre. Reduction of CD4+ T cell counts in the peripheral whole blood and the neutrophil counts in pleural exudates of the animals treated with EA was observed by flowcytometric analysis. Process of phagocytosis was also inhibited in in vivo and in vitro experimental test models. The oral LD50 in both rats and mice was more than 2.5 g/kg body weight.

The aim of present study was to evaluate antioxidant, antimicrobial, and antitumor activities of methanol, hexane, and aqueous extracts of fresh Euphorbia royleana . Total phenolic and flavonoid contents were estimated as gallic acid and querectin equivalents, respectively. Antioxidant activity was assessed by scavenging of free 2,2′- diphenyl-1-picrylhydrazyl radicals and reduction of ferric ions, and it was observed that inhibition values increase linearly with increase in concentration of extract. The results of ferric reducing antioxidant power assay showed that hexane extract has maximum ferric reducing power (12.70 ± 0.49 mg gallic acid equivalents/g of plant extract). Maximum phenolic (47.47 ± 0.71 μg gallic acid equivalents/mg of plant extract) and flavonoid (63.68 ± 0.43 μg querectin equivalents/mg of plant extract) contents were also found in the hexane extract. Furthermore, we examined antimicrobial activity of the three extracts (methanol, hexane, aqueous) against a panel of microorganisms ( Escherichia coli, Bacillus subtillis, Pasteurella multocida, Aspergillus niger , and Fusarium solani ) by disc-diffusion assay, and found the hexane extract to be the best antimicrobial agent. Hexane extract was also observed as to be most effective in a potato disc assay. As hexane extract showed potent activity in all the investigated assays, it was targeted for cytotoxic assessment. Maximum cytotoxicity (61.66%) by hexane extract was found at 800 μg/mL. It is concluded that investigated extracts have potential for isolation of antioxidant and antimicrobial compounds for the pharmaceutical industry.

The latex of Euphorbia royleana which has high molluscicidal and anti-cholinesterase activity against Lymnaea acuminata reduced the levels of 5-hydroxytryptamine (5HT) and dopamine (DA) in the nervous tissue of L. acuminata. There was, however, no significant change in the level of 5-hydroxyindole acetic acid (5HIAA). The changes were found to be dependent on concentration of the latex extract. Similar changes were produced by both water and organic solvent extracts of the latex. The latex of E. royleana thus affects all the known neurotransmission mechanisms in the snail either separately or through a complex interaction between the different neurotransmitters. This may account for its high toxicity to snails.