051: Phytomedicine 2000 Mar;7(1):31-8

Antiamoebic and spasmolytic activities of extracts from some antidiarrhoeal traditional preparations used in Kinshasa, Congo.

Tona L, Kambu K, Ngimbi N, Mesia K, Penge O, Lusakibanza M, Cimanga K, De Bruyne

T, Apers S, Totte J, Pieters L, Vlietinck AJ.

Faculty of Pharmacy, University of Kinshasa, Democratic Republic of Congo.

Three major extracts from some traditional preparations, based on medicinal plants, used as antidiarrhoeal agents were investigated for their putative antiamoebic and spasmolytic activities in vitro. Results indicated that both biological activities are concentrated in the polyphenolic fraction, and not in the saponin or alkaloid containing fractions. The most active polyphenolic extracts were those from Euphorbia hirta whole plant, leaves of Alchornea cordifolia, Crossopteryx febrifuga, Nauclea latifolia, Psidium guajava, Tithonia diversifolia, stem bark of Harungana madagascariensis, Mangifera indica, Maprounea africana and Psidium guajava, inhibiting Entamoeba histolytica growth with MAC < 10 micrograms/ml. The same extracts, at a concentration of 80 micrograms/ml in an organ bath, also exhibited more than 70% inhibition of acetylcholine and/or KCl solution-induced contractions on isolated guinea-pig ileum.

052: J Ethnopharmacol 2000 May;70(2):119-25

Molluscicidal activity of some Saudi Arabian euphorbiales against the snail Biomphalaria pfeifferi.

Al-Zanbagi NA, Banaja AA, Barrett J.

Department of Biology, King Abdul-Aziz University Saudi Arabia, Jeddah.

The comparative susceptibility of the snail vector of intestinal schistosomiasis, Biomphalaria pfeifferi to the action of extracts from Saudi Arabian Euphorbiales has been determined. Methanol and chloroform extracts of the plants tested (Jatropha glauca, Euphorbia helioscopia and Euphorbia schimperiana) were the most promising from the molluscicidal point of view with LD(50) values in the range 10-100 ppm.

053: Phytochemistry 2000 Mar;53(6):639-44

Cucumisin-like protease from the latex of Euphorbia supina.

Arima K, Uchikoba T, Yonezawa H, Shimada M, Kaneda M.

Department of Chemistry, Faculty of Science, Kagoshima University, Japan.

A protease has been purified from the latex of Euphorbia supina Rafin by two steps of chromatography. The Mr was estimated by SDS-PAGE to be 80 kDa. Its activity was inhibited strongly by diisopropyl fluorophosphate, but not by EDTA, pepstatin, or cysteine protease inhibitors, indicating that the enzyme is a serine protease. The specificity of the protease is broad, but the preferential

cleavage sites were C-terminal sites of hydrophobic amino acid residues. The N-terminal sequence of the first fifteen residues was determined and six of the residues match those in cucumisin [EC 3.4.21.25], a protease from the sarcocarp of melon fruit (Cucumis melo L. var. Prince). The results indicate that the E. supina protease is a cucumisin-like serine protease.

054: Fitoterapia 2000 Apr;71(2):134-42

Polycyclic diterpenoids from Euphorbia characias.

Appendino G, Belloro E, Tron GC, Jakupovic J, Ballero M.

Dipartimento di Scienza e Tecnologia del Farmaco, Via Giuria 9, I-10125 Torino, Italy. appendin@pharm.unito.it

In addition to widespread flavonoids, a collection of Euphorbia characias from Sardinia afforded 13 oxygenated diterpenoids of the atisane, abietane, pimarane, and kaurane type. Four of these compounds (1, 3a, 7a,b) are new. The accumulation of substantial amounts of biologically active diterpenoids of limited availability, like ent-atisanes endowed with anti-HIV activity and ent-abietanolides active on the central nervous system, makes E. characias an interesting source of lead compounds for biomedical research.

055: J Pharm Pharmacol 2000 Jan;52(1):119-24

Inhibitory effect of euphol, a triterpene alcohol from the roots of Euphorbia kansui, on tumour promotion by 12-O-tetradecanoylphorbol-13-acetate in two-stage carcinogenesis in mouse skin.

Yasukawa K, Akihisa T, Yoshida ZY, Takido M.

College of Pharmacy, Nihon University, Chiba, Japan.

The anti-inflammatory activity of euphol, twelve other triterpene alcohols and sitosterol-beta-D-glucopyranoside, isolated from the dichloromethane extract of the roots of Euphorbia kansui, has been evaluated in mice with inflammation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). TPA (1.7 nmol; 1.0 microg/ear) was dissolved in acetone and 10 microL delivered to the inner and outer surfaces of the right ear of ICR mice. A triterpene alcohol, sterol glucoside or vehicle (20 microL; chloroform-methanol 1:1), was applied topically approximately 30 min before each TPA treatment. The ear thickness was measured before treatment and then oedema was measured 6 h after TPA treatment. For the two-stage carcinogenesis experiment, initiation was accomplished by administration of a single topical application of 7,12-dimethylbenz[a]anthracene (DMBA; 195 nmol; 50 microg/mouse) to the shaved backs of mice. Promotion was with 1.7 nmol (1.0 microg) TPA, applied twice weekly to the same shaved area, begun one week after the initiation. Euphol (2.0 micromol; 853 microg), or its vehicle (acetone-dimethylsulphoxide, 9:1; 100 microL), was applied topically 30 min before each TPA treatment. The number and diameter of skin tumours were measured every other week for 20 weeks. All the compounds were found to possess marked inhibitory activity and their 50% inhibitory dose for TPA-induced inflammation was 0.2-1.0 mg/ear. Topical application of euphol (2.0 micromol; 853 microg/mouse) markedly suppressed the tumour-promoting effect of TPA (1.7 nmol; 1.0 microg/mouse) in mouse skin initiated with DMBA.

056: J Nat Prod 2000 Feb;63(2):267-9

Nonpolar components of the latex of Euphorbia peplus.

Giner JL, Berkowitz JD, Andersson T.

Department of Chemistry, SUNY-ESF, Syracuse, New York 13210, USA. jlginer@syr.edu

The less polar fractions of the latex of Euphorbia peplus were found to contain obtusifoliol, cycloartenol, 24-methylenecycloartanol, lanosterol, and 24-methylenelanosterol in the free and esterified triterpene alcohol fractions; 9-cis-tricosene as the major component of the hydrocarbon fraction; and a new acyclic triterpene alcohol named peplusol (1). The structure of 1 was determined as the R-isomer of (all-E)-2-(5,9-dimethyl-1-methylene-4,8-decadienyl)-5,9, 13-trimethyl-4,8,12-tetradecatrien-1-ol by spectral and chemical methods.

057: J Nat Prod 2000 Jan;63(1):99-103

Bioactive steroids from the whole herb of Euphorbia chamaesyce.

Tanaka R, Kasubuchi K, Kita S, Tokuda H, Nishino H, Matsunaga S.

Department of Medicinal Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan. tanakar@oysun01.oups.ac.jp

Three new ergostane-type steroids, 3beta-hydroxy-4alpha, 14alpha-dimethyl-5alpha-ergosta-8,24(28)-dien-11 -one (1); 3beta, 11alpha-dihydroxy-4alpha,14alpha-dimethyl-5alpha -ergosta-8, 24(28)-dien-7-one (2); and 3beta,7alpha-dihydroxy-4alpha, 14alpha-dimethyl-5alpha-ergosta-8,24(28)-dien-11 -one (3), were isolated, together with two known triterpenoids, wrightial and lup-20(30)-ene-3beta,29-diol from the whole herb of Euphorbia chamaesyce. Compound 3 showed a potent inhibitory effect on Epstein-Barr virus early antigen activation induced by the tumor promoter 12-O-tetradecanoylphorbol 13-acetate (TPA).

058: Am J Bot 2000 Jan;87(1):48-55

Pollinator-mediated interactions between a pathogenic fungus, Uromyces pisi (Pucciniaceae), and its host plant, Euphorbia cyparissias (Euphorbiaceae).

Pfunder M, Roy BA.

Geobotanical Institute, Swiss Federal Institute of Technology (ETH) Zurich, Zurichbergstrasse 38,8044 Zurich, Switzerland.

The plant Euphorbia cyparissias is commonly infected by rust fungi of the species complex Uromyces pisi. When infected, E. cyparissias is unable to flower, but instead is induced by the fungus to form pseudoflowers. Pseudoflowers are rosettes of yellow leaves upon which the fungus presents its gametes in a sweet-smelling fungal nectar. We hypothesized that the fungi, as they are heterothallic, are dependent on insect visitation to cross-fertilize their mating types. We confirmed that insects are required with an insect exclusion experiment. We further hypothesized that pseudoflowers of U. pisi interact with uninfected true host flowers through insects during their period of co-"flowering" in early spring. We conducted artificial array experiments in the field to test whether the two species share insects and whether they influenced each other's insect visitation. Insects moved between true flowers and pseudoflowers, but true flowers received more visits over all. Pseudoflowers and true flowers did not influence each other's visitation rates in mixtures. However, shorter visits were observed on pseudoflowers in mixtures than monocultures, suggesting that true flowers might be competitors for pseudoflowers. Further experiments are needed to determine whether the similarity of pseudoflowers to true flowers is adaptive.

059: Arch Ophthalmol 2000 Jan;118(1):13-6

Comment in: Arch Ophthalmol. 2000 Aug;118(8):1141.

The spectrum of ocular inflammation caused by euphorbia plant sap.

Eke T, Al-Husainy S, Raynor MK.

Department of Ophthalmology, Leicester Royal Infirmary, United Kingdom.

OBJECTIVE: To report the spectrum of clinical findings in patients with ocular inflammation caused by plant sap from Euphorbia species.

DESIGN: Clinical case series.

SETTING: Ophthalmology emergency referrals in the United Kingdom.

PATIENTS: We examined 7 patients, all of whom gave a history of recent ocular exposure to the sap of Euphorbia species.

INTERVENTIONS: All patients were treated with antibiotic drops or ointment (chloramphenicol). Cycloplegic and steroid drops were also used for some patients. Patients were observed until all signs and symptoms had resolved.

MAIN OUTCOME MEASURES: Symptoms, visual acuity, and clinical signs of inflammation. All patients provided a specimen of the plant for formal identification.

RESULTS: Initial symptoms were generally burning or stinging pain with blurred vision. In most cases, visual acuity was reduced between 1 and 2 Snellen lines. In 1 patient with age-related maculopathy, acuity dropped from 20/80 to hand motions before recovering. Clinical findings varied from a mild epithelial keratoconjunctivitis to a severe keratitis with stromal edema, epithelial sloughing, and anterior uveitis. All signs and symptoms had resolved by 1 to 2 weeks.

CONCLUSIONS: These cases illustrate the range of severity of Euphorbia sap keratouveitis. The condition seems to be self-limiting when managed supportively. People who work with Euphorbia plant species should wear eye protection. Clinicians managing keratopathy caused by Euphorbia species should be aware of the danger of sight-threatening infection and uveitis, particularly during the first few days.

060: J Ethnopharmacol 1999 Dec 15;68(1-3):193-203

Antimalarial activity of 20 crude extracts from nine African medicinal plants used in Kinshasa, Congo.

Tona L, Ngimbi NP, Tsakala M, Mesia K, Cimanga K, Apers S, De Bruyne T, Pieters L, Totte J, Vlietinck AJ.

Faculty of Pharmacy, University of Kinshasa, Democratic Republic of the Congo.

Twenty extracts including ten EtOH and ten CH2Cl2 from different parts of nine African medicinal plants used in Congolese traditional medicine for the treatment of malaria, were submitted to a pharmacological test in order to evaluate their effect on P. falciparum growth in vitro. Of these plant species, 14 (70%) extracts including EtOH and CH2Cl2 from Cassia occidentalis leaves, Cryptolepis sanguinolenta root bark, Euphorbia hirta whole plant, Garcinia kola stem bark and seeds, Morinda lucida leaves and Phyllanthus niruri whole plant produced more than 60% inhibition of the parasite growth in vitro at a test concentration of 6 microg/ml. Extracts from E. hirta, C. sanguinolenta and M. morindoides showed a significant chemosuppression of parasitaemia in mice infected with P. berghei berghei at orally given doses of 100-400 mg/kg per day.

061: Planta 1999 Nov;210(1):85-96

Rubber particles from four different species, examined by transmission electron microscopy and electron-paramagnetic-resonance spin labeling, are found to consist of a homogeneous rubber core enclosed by a contiguous, monolayer biomembrane

Cornish K, Wood DF, Windle JJ.

USDA, ARS, Western Regional Research Center, 800 Buchanan Street, Albany, CA 94710, USA.

The physical characteristics of rubber particles from the four rubber (cis-1,4-polyisoprene) producing species Euphorbia lactiflua Phil., Ficus elastica Roxb., Hevea brasiliensis Mull. Arg., and Parthenium argentatum Gray, were investigated using transmission electron microscopy (TEM) and electron-paramagnetic-resonance (EPR) spin labeling spectroscopy. Transmission electron microscopy showed the rubber particles to be composed of a spherical, homogeneous, core of rubber enclosed by a contiguous, electron-dense, single-track surface layer. The biochemical composition of the surface layer and its single-track TEM suggested that a monolayer biomembrane was the surface structure most compatible with the hydrophobic rubber core. The EPR spectra for a series of positional isomers of doxyl stearic acid, used to label the surface layer of the rubber particles, exhibited flexibility gradients and evidence for lipid-protein interactions for all four rubber particle types that is consistent with a biomembrane-like surface. The EPR spectra confirmed that the surface biomembrane is a monolayer. Thus, rubber particles appear similar to oil bodies in their basic architecture. The EPR spectra also provided information on protein location and degree of biomembrane penetration that correlated with the known properties of the rubber-particle-bound proteins. The monolayer biomembrane serves as an interface between the hydrophobic rubber interior and the aqueous cytosol and prevents aggregation of the particles. An unexpected observation for the probes in pure polyisoprene was evidence of an intrinsic flexibility gradient associated with the stearic acid molecule itself.

062: J Nat Prod 1999 Oct;62(10):1399-404

Diterpenoids from euphorbia pithyusa subsp. cupanii

Appendino G, Belloro E, Tron GC, Jakupovic J, Ballero M.

Dipartimento di Scienza e Tecnologia del Farmaco, Universita di Torino, Via Giuria 9, 10125 Torino, Italy, Dipartimento di Scienze Botaniche, Universita di Cagliari, Viale San Ignazio 13, 09123 Cagliari, Italy, and Analyticon AG, Hermannswe.

The aerial parts of Euphorbia pithyusa subsp. cupanii collected in Sardinia afforded eleven novel diterpenoids belonging to the lathyrane (1a), premyrsinane (4a-g), and tigliane (5a-c) types. Compounds 4a-g and 5a are esters of two new parent alcohols, named premyrsinol and 4,12,20-trideoxyphorbol, respectively. Structures were elucidated by spectroscopic and chemical methods. Puzzling differences between the NMR data of lathyrol (1c) and its esters were rationalized in terms of flipping of the exomethylene around the mean plane of the macrocycle.

063: Klin Monatsbl Augenheilkd 1999 Sep;215(3):203-4

[Dermatitis and conjunctivitis after contact with Euphorbia myrsinites (wolf's

milk extract)--a case report]

[Article in German]

Eberle MM, Erb C, Flammer J, Meyer P.

Universitats-Augenklinik Basel.

BACKGROUND: Fresh sap of euphorbiaceae leads to a toxic burn of the skin and the eyes. Since years the sap of euphorbiaceae has been used in the treatment of different kinds of verrucas.

PATIENTS: After contact with the sap of Euphorbia myrsinites three children developed a toxic dermatitis. In addition, the youngest girl showed a conjunctivitis and an occlusion of the right eye. Phorbolesters are considered to be responsible for the toxicity of the euphorbiaceae. All three children have resulted in a restitutio ad integrum.

CONCLUSION: This case report is demonstrating the danger of toxic burn of this kind of plant.

064: J Environ Sci Health B 1999 Mar;34(2):289-303

The influence of environmental factors on the molluscicidal activity of Euphorbia milii latex.

Oliveira-Filho EC, De-Carvalho RR, Paumgartten FJ.

Laboratory of Environmental Toxicology, National School for Public Health, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.

The present study was undertaken to investigate the influence of biotic (snail size and presence of food during the test) and abiotic factors (temperature, water hardness and concentration of organic materials) on the molluscicidal activity of Euphorbia milii latex. Bioassays were conducted with B. glabrata (10 snails per concentration) and snail lethality was evaluated after 24 hr and 48 hr of exposure to lyophilized latex solutions. Neither the degree of water hardness, nor the presence of food during the test affected latex-induced snail mortality. The snail size had a minor influence on E. milii-induced snail lethality. Newly-hatched (shell diameter < or = 1 mm) as well as young (3-8 mm) snails were slightly less susceptible than older (10-25 mm) mollusks. On the other hand, the molluscicidal effect of E. milii latex was modified by environmental factors such as temperature (i.e., LC50 and LC90 values were halved for every 10 degrees C rise in temperature) and concentration of organic materials in the water (i.e. the higher the concentration of organic matter, the higher the LC50 value). The efficacy of E. milii latex as a molluscicide can be modified by factors such as water temperature and concentration of organic materials, and to a lesser extent by snail size.

065: Biochem Biophys Res Commun 1999 Aug 2;261(2):499-503

Piceatannol, a stilbene phytochemical, inhibits mitochondrial F0F1-ATPase activity by targeting the F1 complex.

Zheng J, Ramirez VD.

Department of Molecular and Integrative Physiology, University of Illinois at Urbana-Champaign, 524 Burrill Hall, Urbana, Illinois, 61801, USA.

Piceatannol is a stilbene phytochemical from the seeds of Euphorbia lagascae, previously identified as an antileukemic principle. Piceatannol is considered an inhibitor of several tyrosine kinases. We recently reported that resveratrol, another stilbene phytoalexin from grape seeds, was an inhibitor of ATP synthase. Here, we demonstrated that piceatannol potently inhibited the rat brain mitochondrial F0F1-ATPase activity in both solubilized and submitochondrial preparations (IC50 of 8-9 microM), while having relatively small effect on the Na(+), K(+)-ATPase activity of porcine cerebral cortex (no effect up to 7 microM). Piceatannol inhibited the ATPase activity of the purified rat liver F1 with IC50 of about 4 microM, while resveratrol was slightly less active (IC50 of about 14 microM). Our results indicate that piceatannol and resveratrol inhibit the F-type ATPase by targeting the F1 sector, which is located to the inner membrane of mitochondria and plasma membrane of normal endothelial cells and several cancer cell lines. This mechanism could potentially contribute to the multiple effects of these chemopreventive phytochemicals. Copyright 1999 Academic Press.

066: J Nat Prod 1999 Jul;62(7):1016-8

New diterpenoids from euphorbia teheranica

Ahmad VU, Jassbi AR.

HEJ Research Institute of Chemistry, University of Karachi, Karachi 75270, Pakistan.

Two novel pentacyclic diterpenoid esters of the cyclomyrsinane type (1, 2), and one tetracyclic diterpenoid ester of the myrsinane type (3) were isolated from the aerial parts of the plant Euphorbia teheranica. The structures of the novel compounds were determined by spectral data interpretation.

067: Phytochemistry 1999 Jul;51(5):673-7

Jatrophane diterpenoids from Euphorbia peplus.

Hohmann J, Vasas A, Gunther G, Dombi G, Blazso G, Falkay G, Mathe I, Jerkovich G.

Department of Pharmacognosy, Albert Szent-Gyorgyi Medical University, Szeged, Hungary.

From the pro-inflammatory active extract of Euphorbia peplus, a new diterpene polyester (1) based on the jatrophane skeleton was isolated together with the known compounds 2-5. The irritant activities of some jatrophane diterpenes (2, 3 and 6-9) were also investigated: only compound 2 was found to exert a weak pro-inflammatory activity on mouse ear.

068: Yakugaku Zasshi 1999 May;119(5):319-39

[Terpenoids and steroids from several euphorbiaceae and pinaceae plants]

[Article in Japanese]

Tanaka R, Matsunaga S.

Osaka University of Pharmaceutical Sciences, Japan.

During the course of a search for biologically active constituents from unexamined plant sources, several biogenetically interesting new di- and tri-terpenes and steroids were isolated from several weeds and shrubs of Euphorbiaceae and the bark, leaves and cones of several Pinaceae trees which had been treated as wastes in the forestry industry. Euphorbia supina contained 3,4-seco-5 alpha- and 5 beta-adian-4(23)-ene-3,5-diols and related oxides, oxygenated fern-8-en-3 beta-ols named supinenolones A-E and unusually migrated oxyfernanes having (9S)- and (9R)-7(8-->9)abeo-9-D:C-friedo-B':A'-neogammacerane skeletons named spirosupinane and neospirosupinane, while E. chamaesyce contained 3,4-seco-oleana-4(23), 18-dien-3-oic acid, 3,4-seco-8 beta H-ferna-4(23),9(11)-dien-3-oic acid and two oxygenated obtusifoliols. The bark of Phyllanthus flexuosus (Euphorbiaceae) contained 11 beta-hydroxy-D:A-friedo-olean-1-en-3-one, lup-20(29)-ene-3 beta, 15 alpha-diol, olean-12-ene-3 beta,15 alpha-diol and olean-12-ene-3 beta,15 alpha,24-triol together with trichadenic acid B for which we revised the structure to 3 beta-hydroxy-D:A-friedo-oleanan-27-oic acid. Two 26-nor-D:A-friedo-olean-14-enes were isolated from P. watsonii. Regarding Pinaceae trees, an unusually migrated abieslactone [(3R, 7S, 9R, 23R)-7-hydroxy-3-methoxy-8-oxo-7(8-->9)abeo-lanost-24-eno-26,23-lactone], named spiroveitchionolide, was isolated from the bark of Abies species, besides nine abieslactone analogues. Two pairs of unusually migrated serratanes, piceanonols A and B and jezananals A and B having novel skeletal systems of 14(13-->12) abeo- and 16(15-->14) abeo-serratanes named piceanane and jezanane, respectively, were also isolated from the stem bark of Picea species, besides three 14 beta,15 beta-epoxyserratanes and two 13 alpha,14 alpha-epoxyserratanes. The leaves of Larix kaempferi contained two deformed abietanes named karamatsuic acid (9,10-seco-9,10 alpha-epoxyabieta-8,11,13-trien-18-oic acid) and larikaempferic acid [9 alpha,13 alpha-epoxy-8-oxo-9(8-->7)abeo-7 beta-abietan-18-oic acid], as well as the cones to contain 8 alpha,12 alpha-epidioxy-15-hydroxyabiet-13-en-18-oic acid, three diepoxy-abietan-18-oic acids and two new dehydroabietic acid analogues. Several of the above compounds exhibited inhibitory effects against tumor-promoting and DNA topoisomerase II activities.

069: Phytochemistry 1999 May;51(2):289-95

Tumor promoting diterpenes from Euphorbia leuconeura L.

Vogg G, Mattes E, Rothenburger J, Hertkorn N, Achatz S, Sandermann H Jr.

Institut fur Biochemische Pflanzenpathologie, GSF-Forschungszentrum fur Umwelt und Gesundheit GmbH, Oberschleissheim, Germany.

Diterpene esters of the phorbol and ingenol types are known to be highly active tumor promoting agents that typically occur in members of the Euphorbiaceae. In the present work, Euphorbia leuconeura, a rare indoor plant, is analyzed for its tumor promoting potential. Latex as well as total leaf extracts exhibited Epstein-Barr-virus (EBV) inducing activity comparable to 12-O-tetradecanoyl-phorbol-13-O-acetate, a well known tumor promoter. The activity of individual fractions correlated with their ingenol ester content. Three ingenol esters with EBV inducing activity could be isolated and identified. They belong to the milliamine type of diterpene esters that contain aromatic peptidyl groups. Two of them (milliamines L and M) are already known from E. milii. The third compound is identified as an isomer of milliamine F with a novel 3,20-diester arrangement. The data show a close relationship between E. leuconeura and the more popular indoor plant E. milii whose latex is also used as a powerful molluscicide.

070: J Ethnopharmacol 1999 Apr;65(1):63-9

Euphorbia hirta leaf extracts increase urine output and electrolytes in rats.

Johnson PB, Abdurahman EM, Tiam EA, Abdu-Aguye I, Hussaini IM.

Department of Pharmacology, Ahmadu Bello University, Zaria, Nigeria.

Euphorbia hirta is locally used in Africa and Australia to treat numerous diseases, including hypertension and edema. The diuretic effect of the E. hirta leaf extracts were assessed in rats using acetazolamide and furosemide as standard diuretic drugs. The water and ethanol extracts (50 and 100 mg/kg) of the plant produced time-dependent increase in urine output. Electrolyte excretion was also significantly affected by the plant extracts. The water extract increased the urine excretion of Na+, K+ and HCO3-. In contrast, the ethanol extract increased the excretion of HCO3- decreased the loss of K+ and had little effect on renal removal of Na+. Acetazolamide, like the water extract, increased urine output and enhanced the excretion of Na+, K+ and HCO3-. The high-ceiling diuretic, furosemide, increased the renal excretion of Na+ and Cl-; but had no effect on K+ and HCO3- loss. This study suggests that the active component(s) in the water extract of E. hirta leaf had similar diuretic spectrum to that of acetazolamide. These results validate the traditional use of E. hirta as a diuretic agent by the Swahilis and Sukumas.

071: Phytomedicine 1999 Mar;6(1):59-66

Biological screening of traditional preparations from some medicinal plants used as antidiarrhoeal in Kinshasa, Congo.

Tona L, Kambu K, Mesia K, Cimanga K, Apers S, De Bruyne T, Pieters L, Totte J, Vlietinck AJ.

Faculty of Pharmacy, University of Kinshasa, Dem. Rep. of Congo.

Forty six aqueous extracts from 38 medicinal plant species belonging to different families were selected on the basis of their traditional medicinal use as antidiarrhoeic agents. They were submitted in a broad biological screening including antibacterial, antiamoebic and antispasmodic activities. The results of the testing have indicated that 37 extracts (80.43%), 33 (71.74%) and 32 (69.54%) exhibited some level of antibacterial, antiamoebic and antispasmodic activity respectively. Only 8 plant extracts (17.39%) would act as antidiarrhoeic agents by a triple pronounced antibacterial, antiamoebic and antispasmodic action. They include aqueous extracts from Euphorbia hirta whole plant, leaves of Psidium guajava and Tithonia diversifolia, root bark of Alchornea cordifolia, Heinsia pulchella, Paropsia brazzeana, Rauwolfia obscura and Voacanga africana.

072: Phytother Res 1999 Feb;13(1):31-6

Inhibitory effects of Sudanese plant extracts on HIV-1 replication and HIV-1 protease.

Hussein G, Miyashiro H, Nakamura N, Hattori M, Kawahata T, Otake T, Kakiuchi N, Shimotohno K.

Research Institute for Wakan-Yaku (Traditional Sino-Japanese Medicines), Toyama Medical and Pharmaceutical University, Japan.

Forty-eight methanol and aqueous extracts from Sudanese plants were screened for their inhibitory activity on viral replication. Nineteen extracts showed inhibitory effects on HIV-induced cytopathic effects (CPE) on MT-4 cells. The extracts were further screened against HIV-1 protease (PR) using an HPLC assay method. Of the tested extracts, the methanol extracts of Acacia nilotica (bark and pods), Euphorbia granulata (leaves), Maytenus senegalensis (stem-bark) and aqueous extracts of A. nilotica (pods) and M. senegalensis (stem-bark) showed considerable inhibitory effects against HIV-1 PR. Inhibitory principles were isolated from M. senegalensis and their activities were also discussed.

073: Planta Med 1998 Dec;64(8):754-6

Cytotoxicity and antiviral activity of the compounds from Euphorbia kansui.

Zheng WF, Cui Z, Zhu Q.

Eleven compounds including four triterpenes, one sterol, and six diterpenes from E kansui had been assayed for their cytotoxicity and activiral activity. The relations between structures and bioactivities have also been noted.

074: Mem Inst Oswaldo Cruz 1998;93 Suppl 1:235-7

Effects of Euphorbia milii latex on Schistosoma mansoni eggs, miracidia and cercariae.

De-Carvalho RR, Maldonado Junior A, Oliveira Filho EC, Ribeiro AC, Paumgartten

FJ, Rey L.

Laboratorio de Toxicologia Ambiental, Escola Nacional de Saude Publica, Fiocruz, Rio de Janeiro, Brasil.

075: Mycoses 1998 Dec;41(11-12):529-33

Euphorbia hirta leaves and Musa sapientum fruits in culture media for fungi.

Emele FE, Agbonlahor DE, Ahanotu C.

Medical Microbiology Department, Usman Danfodio University Teaching Hospital, Sokoto, Nigeria.

Two plant products, Euphorbia hirta leaves and fruits of Musa sapientum, were evaluated as principal ingredients for selective cultivation of fungi. Sapientum glucose agar supported the growth of both dermatophytic, yeast-like, and saprophytic fungi; growth on this medium compared favourably with growth on Sabouraud glucose agar, a standard mycological medium. Sporulation and pigment formation were stronger on sapientum glucose agar than on Sabouraud glucose agar, although fungal growth on the latter was more luxuriant. Addition of Euphorbia extract to mycological media remarkably enhanced fungal growth on the media, and concomitantly suppressed bacterial growth to a similar extent as did antibiotics. The results of this study suggest that Euphorbia sapientum glucose agar can safely be recommended as a cheap and efficient medium for routine isolation of fungi in both clinical and general mycological studies.

076: J Nat Prod 1999 Jan;62(1):176-8

A novel lathyrane diterpenoid from the roots of euphorbia lathyris

Hohmann J, Evanics F, Vasas A, Dombi G, Jerkovich G, Mathe I I.

Department of Pharmacognosy, Albert Szent-Gyorgyi Medical University, P.O. Box 121, H-6701 Szeged, Department of Pharmaceutical Analysis, Albert Szent-Gyorgyi Medical University, 4 Somogyi u., H-6720 Szeged, Hungary, and Spectr.

A new lathyrane diterpene (1) has been isolated and characterized from a CH2Cl2 extract of the roots of Euphorbia lathyris. Detailed spectral analysis revealed that the structure of 1, including relative stereochemistry, is that of a diester of a hitherto unknown, polyfunctional diterpene parent alcohol.

077: J Nat Prod 1999 Jan;62(1):110-3

Isoterracinolides A and B, novel bishomoditerpene lactones from euphorbia terracina

Marco JA, Sanz-Cervera JF, Yuste A, Jakupovic J.

Departamento de Quimica Organica, Universidad de Valencia, E-46100 Burjassot, Valencia, Spain, and Institut fur Organische Chemie, Technische Universitat Berlin, D-10623 Berlin, Germany.

An extract of Euphorbia terracina L. has yielded six acylated polyhydroxy terpenoid lactones (1-6), which all display the C22 17-ethyljatrophane carbon framework. Four of these (1-4) are delta lactones belonging to the previously described terracinolide type, and two of them (2, 3) are new. Two further new compounds have been named isoterracinolides A (5) and B (6) and exhibit an eight-membered lactone ring. Another isolated new compound is the jolkinolide-type, ent-abietane gamma lactone (7).

078: J Nat Prod 1999 Jan;62(1):107-9

Isolation and structure revision of pepluane diterpenoids from euphorbia peplus

Hohmann J, G nther G, Vasas A, Kalman A, Argay G.

Department of Pharmacognosy, Albert Szent-Gyorgyi Medical University, P.O. Box 121, H-6701 Szeged, Department of Pharmaceutical Analysis, Albert Szent-Gyorgyi Medical University, 4 Somogyi u., H-6720 Szeged, Hungary, and Instit.

A new pepluane diterpene polyester (2) was isolated from a CH2Cl2 extract of the whole, undried plant of Euphorbia peplus, together with the known compound 1. The structures were established by high-field spectroscopic methods, including 2D NMR techniques, and by X-ray crystallography, and the stereostructure of the first member of the pepluane diterpenoids (1) was revised.

079: J Nat Prod 1999 Jan;62(1):76-9

An expeditious procedure for the isolation of ingenol from the seeds of euphorbia lathyris

Appendino G, Tron GC, Cravotto G, Palmisano G, Jakupovic J.

Dipartimento di Scienza e Tecnologia del Farmaco, via Giuria 9, 10125 Torino, Italy, and Institut fur Organische Chemie, Technische Universitat Berlin, Strasse des 17. Juni 135, 10623 Berlin, Germany.

A short and practical process for the isolation of ingenol (1a) from an agricultural commodity (the seeds of Euphorbia lathyris) is described. Macrocyclic diterpene esters are obtained as byproducts, and the esterification pattern of the Euphorbia factors L2 (3), L3 (4a), and L8 (4b) was established by 2D NMR measurements. Full spectroscopic data for these compounds are reported.

080: Bioorg Med Chem Lett 1998 Oct 20;8(20):2829-32

In vitro inhibitory effects of DNA topoisomerase II by fernane-type triterpenoids isolated from a Euphorbia genus.

Wada S, Tanaka R, Iida A, Matsunaga S.

Osaka University of Pharmaceutical Sciences, Japan.

Several kinds of naturally occurring fernane-type triterpenoids isolated from a Euphorbia genus were tested on the inhibitory effects of DNA Topoisomerases I (Topo I) and II (Topo II) activities. A-ring cleaved 3,4-seco-8 beta H-ferna-4(23),9(11)-dien-3-oic acid and its 3-hydroxyl derivative were found to be selective inhibitors of Topo II activity without the stabilization of a DNA/Topo II cleavable complex.

081: Cutis 1998 Nov;62(5):221-2

Botanical briefs: leafy spurge--Euphorbia esula l.

McGovern TW, Barkley TM.

Department of Dermatology, Yale University School of Medicine, New Haven, Connecticut 06519, USA.

082: Med Res Rev 1998 Nov;18(6):375-82

Recent advances on bioactive natural products from Chinese medicinal plants.

Qin GW, Xu RS.

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, People's Republic of China. gwqin@server.shcnc.ac.cn

China has accumulated a rich body of empirical knowledge of the use of medicinal plants for the treatment of various diseases throughout its long history. Chemical studies on Chinese medicinal plants provide a valuable material base for the discovery and development of new drugs of natural origin. In this article recent chemical work on various Chinese medicinal plants is reviewed, including Mussaenda pubescens (Rubiaceae), Isatis indigotica (Cruciferae), Euphorbia fischeriana, and E. ebracteolata (Euphorbiaceae), and Stemona species (Stemonaceae). The structural diversity of the medicinal chemical constituents of the above plants is discussed.

083: Dakar Med 1997;42(2):169-71

[Application of phytotherapy in odontology: the case of Euphorbia balsamifera. Endodontic clinical trial]

[Article in French]

Yam AA, Gaye F, Dieme FA, Bassene E, Ba I.

Institut d'Odontologie-Stomatologie, Universite Cheikh Anta Diop, Dakar.

Phytotherapy is a medicinal and ancestral practice in Africa. It deals with all the fields of human pathology. We wanted to ascertain the efficacy of some plants used in odontology as Euphorbia balsamifera traditionally used as antalgic treatment of acute dental pulpitis. The latex of the plant was caught and treated as to get enough stable paste. We used that paste in the same conditions we use arsenical nerve caustics, a pulpal devitalizer widely used in dental offices. The study carried out on 37 teeth has shown that latex of Euphorbia balsamifera is an effective pulpal devitalizing in contact with the pulp. Its lifetime action was comparable to that of the pulpal nerve caustics. The active principles are not known, however the product seems attractive as a pulpal devitalizing agent.

084: Scand J Urol Nephrol 1998 Sep;32(5):331-4

Intravesical resiniferatoxin for the treatment of detrusor hyperreflexia refractory to capsaicin in patients with chronic spinal cord diseases.

Lazzeri M, Spinelli M, Beneforti P, Zanollo A, Turini D.

Department of Urology, University of Ferrara, Italy.

OBJECTIVE: Resiniferatoxin (RTX), a substance isolated from some species of Euphorbia, a cactus-like plant, shows pharmacological effects similar to those of capsaicin. We have studied the possibility of treating detrusor hyperreflexia refractory to intravesical capsaicin in patients with chronic spinal cord injuries, thereby providing insight into the mechanism of action of RTX on sensory neurons and its possible future pharmacological and clinical use.

MATERIALS AND METHODS: RTX saline solution (30 ml at a concentration of 10(-5) M) was instilled into the bladder of 7 patients with detrusor hyperreflexia, refractory to intravesical capsaicin therapy, and left in place for 30 min. Effects on bladder function were monitored during the treatment and at follow-up (15 days and 4 weeks later).

RESULTS: Fifteen days after RTX, the mean cystomanometric capacity increased significantly from 190 ml +/- 20 ml to 407.14 ml +/- 121.06 (p < 0.01), and it remained high four weeks later (421.66 +/- 74.40 p < 0.01). After 15 days, four patients had a pharmacologically induced detrusor areflexia. They emptied their bladders by clean intermittent catheterization. After four weeks, only two patients still had a pharmacologically induced detrusor areflexia. Clinically, three patients remained dry, and the other three reported a significant improvement in their incontinence and symptoms (frequency, urgency and nocturia).

CONCLUSIONS: By interfering with sensory unmyelinated fibers, intravesical RTX seems to be a promising treatment option for selected cases of detrusor hyperreflexia. The ideal dosage and treatment interval have not yet been established, and further studies are necessary to confirm our preliminary results.

085: Contact Dermatitis 1998 Oct;39(4):166-70

Immediate skin and mucosal symptoms from pot plants and vegetables in gardeners and greenhouse workers.

Paulsen E, Skov PS, Andersen KE.

Department of Dermatology, Odense University Hospital, Denmark.

Short-lived occupational skin symptoms of irritant or urticarial nature were commonly reported among 253 attendants in a clinical study on occupational dermatitis in Danish gardeners and greenhouse workers. Aimed prick or scratch-patch testing for immediate skin and mucosal symptoms was performed in 105 persons with plants as is. 35 persons (33%) had at least 1 positive reaction and a family history of, or personal, atopy was significantly more prevalent among these compared to attendants with negative reactions. Positive histamine release tests made immunologic etiology probable in Schlumbergera cacti, Stephanotis floribunda, Euphorbia pulcherrima and Gerbera reactions. Other new species implicated in immediate-type reactions included Ficus pumila, Gardenia jasminoides, Hibiscus rosa-sinensis, Campanula, Columnea, Epipremnum aureum, Pelargonium and Primula vulgaris. Because of the high prevalence of short-lived skin symptoms and because contact urticaria may present itself as a dermatitis, it is recommended that one supplement patch tests with tests for immediate reactions.

086: J Enzyme Inhib 1998 Aug;13(5):311-25

Inhibitors of plant copper amine oxidases.

Padiglia A, Medda R, Pedersen JZ, Lorrai A, Pec P, Frebort I, Floris G.

Department of Biochemistry and Human Physiology, University of Cagliari, Italy.

In this review, inhibitors of plant copper amine oxidases from Lens esculenta seedlings, Pisum sativum seedlings, and Euphorbia characias latex are described. Reversible competitive inhibitors and non-competitive inhibitors, irreversible active-site directed inhibitors and mechanism-based inactivators are reviewed in regard to their mechanisms of action.

087: J Nat Prod 1998 Oct;61(10):1198-201

Diterpene polyesters from euphorbia seguieriana

Oksuz S, Gurek F, Qiu SX, Cordell GA.

University of Istanbul, Faculty of Pharmacy, Department of Chemistry, 34452 Istanbul, Turkey, TUBITAK, Marmara Research Center, Department of Chemistry, P.O. Box 21, 41470 Gebze, Turkey, Program for Collaborative Research in the Pharmaceutic.

An Me2CO extract of Euphorbia seguieriana (Euphorbiaceae) afforded seven new diterpene polyesters (1-7). Five of them (1-5), having a new parent alcohol that was named 17-hydroxymyrsinol, were structurally related to myrsinol. The other two compounds (6, 7) were new derivatives of the known parent alcohols cyclomyrsinol and lathyrane. The structure elucidations of the new compounds by highfield spectroscopic methods, including 1D and 2D NMR techniques, are described.

088: Yao Xue Xue Bao 1996;31(7):524-9

[Studies on chemical constituents of roots of Euphorbia pekinensis]

[Article in Chinese]

Kong LY, Min ZD.

Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing.

Nine compounds were isolated from the roots of Euphorbia pekinensis Rupr., a traditional Chinese medicine. By combination of chemical methods and spectral analyses, the structures of the compounds were identified as lanosterol (I), octadecanyl-3-methoxy-4-hydroxybenzeneacrylate (II), beta-sitosterol (III), 7-hydroxycoumarin (IV), 2, 2'-dimethoxy-3, 3'-dihydroxy-5, 5'-oxygen-6, 6'-biphenylformic anhydride (V), d-pinoresinol (VI), quercetin (VII), 3, 4-dimethoxybenzoic acid (VIII) and 3, 4-dihydroxybenzoic acid (IX). II and V are new compounds which have not been reported in the literature. The other compounds were isolated for the first time from this plant. VI is a lignan which was first isolated from the plants of genus of Euphorbia.

089: Acta Microbiol Immunol Hung 1998;45(2):195-207

Saprophytic and cycloheximide resistant fungi isolated from golden hamster.

Bagy MM, el-Shanawany AA, Abdel-Mallek AY.

Department of Botany, Faculty of Science, Assiut University, Egypt.

Healthy hair samples from golden hamsters were examined for the presence of dermatophytes and non-dermatophytes using baiting technique and direct inoculation. Thirty-four species and 2 varieties attributed to 17 genera were recovered. Paecilomyces variotii (isolated from 84.4% of the examined hair) and Aspergillus niger (81.3%) were the more frequent isolates on Sabouraud's dextrose agar (SDA) without cycloheximide. Our results have clearly demonstrated that the hair of hamster was free from true dermatophytes. Using the dilution plate method many fungal species were isolated from cage material (7 genera and 10 species + 1 variety); from faeces (10 genera and 17 species); from standard chow (3 genera and 6 species) of hamster. P. variotii which was the most frequent fungus in the preceding 3 substrates was completely absent in the presence of cycloheximide in SDA. The present study has demonstrated for the first time the isolation of Trichophyton rubrum from hamster faeces. Also, several saprophytic and cycloheximide resistant fungi were isolated. In the air of hamster cage Cladosporium cladosporioides, Penicillium chrysogenum, Alternaria alternata and Scopulariopsis brevicaulis were the most dominant species on SDA with or without cycloheximide. Using the agar diffusion method, Aloe sap, onion oil, garlic bulb extract and aqueous leaf extracts of Andropogon citratus, Euphorbia sp. and Ruta graveolens were tested for their antifungal activity on 10 fungal species. It was observed that onion oil exhibited a high inhibitory effect against most of the tested fungi.

090: Plant Mol Biol 1998 Nov 1;38(4):531-8

Cloning and characterization of cold-regulated glycine-rich RNA-binding protein genes from leafy spurge (Euphorbia esula L.) and comparison to heterologous genomic clones.

Horvath DP, Olson PA.

U.S. Department of Agriculture, Agricultural Research Service, State University Station, Fargo, ND 58105-5674, USA.

Leafy spurge (Euphorbia esula) is a perennial weed which is capable of acclimating to sub-freezing temperatures. We have used the differential display technique to identify and clone a cDNA for a cold-regulated gene (cor20) which hybridizes to mRNAs that accumulate specifically during the cold acclamation process. The cor20 cDNA was used to isolate two different genomic clones. Both clones were similar but not identical to each other and the cDNA. Sequence analysis of the genomic clones indicated that they share considerable homology to a group of glycine-rich RNA-binding protein genes. Comparison of the promoter region from the three clones (Ccr1 from Arabidopsis. BnGRP10 from Brassica napus, and GRRBP2 from Euphorbia esula) have identified at least two conserved motifs. CAGC is most likely involved in cold regulation and AACCCYAGTTA, is conserved but has no known function. RNAs which hybridize to cor20 reach maximal expression in less than 2 days after exposure of the plant to temperatures of 5 degrees C, and remains at high levels in the plant for at least 30 days so long as the plant is left in the cold. These RNAs drop to control levels within 24 h when the plant is returned to normal growing temperatures. Transcripts which hybridize to cor20 do not accumulate under conditions of drought or heat stress. These transcripts are induced in response to low temperatures in roots, stems and leaves, but are expressed constitutively in tissue culture at control temperatures.

091: Acta Pharm Hung 1998 May;68(3):175-82

[Macrocyclic diterpene polyesters of the jatrophane type from Euphorbia esula]

[Article in Hungarian]

Hohmann J, Vasas A, Gunther G, Mathe I, Evanics F, Dombi G, Jerkovich G.

SZOTE Gyogynoveny- es Drogismereti Intezet, Szeged.

Three new jatrophane diterpenes, esulatin A, B and C (1-3) were isolated and characterized from the whole, undried plant of Euphorbia esula. By means of spectral analysis, the structures were established as penta- and heptaesters of hitherto unknown, polyfunctional diterpene parent alcohols. Esulatin A (1) and C (3) are the diterpenoids with the highest degree of esterification identified to date from the family Euphorbiaceae.

092: Plant Physiol 1998 Aug;117(4):1363-71

Characterization of Euphorbia characias latex amine oxidase.

Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Finazzi Agro A, Floris G.

Department of Biochemistry and Human Physiology, University of Cagliari, Cagliari, Italy.

A copper-containing amine oxidase from the latex of Euphorbia characias was purified to homogeneity and the copper-free enzyme obtained by a ligand-exchange procedure. The interactions of highly purified apo- and holoenzyme with several substrates, carbonyl reagents, and copper ligands were investigated by optical spectroscopy under both aerobic and anaerobic conditions. The extinction coefficients at 278 and 490 nm were determined as 3.78 x 10(5) M-1 cm-1 and 6000 M-1 cm-1, respectively. Active-site titration of highly purified enzyme with substrates and carbonyl reagents showed the presence of one cofactor at each enzyme subunit. In anaerobiosis the native enzyme oxidized one equivalent substrate and released one equivalent aldehyde per enzyme subunit. The apoenzyme gave exactly the same 1:1:1 stoichiometry in anaerobiosis and in aerobiosis. These findings demonstrate unequivocally that copper-free amine oxidase can oxidize substrates with a single half-catalytic cycle. The DNA-derived protein sequence shows a characteristic hexapeptide present in most 6-hydroxydopa quinone-containing amine oxidases. This hexapeptide contains the tyrosinyl residue that can be modified into the cofactor 6-hydroxydopa quinone.

093: J Cancer Res Clin Oncol 1998;124(6):301-6

Dietary cancer risk from conditional cancerogens in produce of livestock fed on species of spurge (Euphorbiaceae). III. Milk of lactating goats fed on the skin irritant herb Euphorbia peplus is polluted by tumor promoters of the ingenane diterpene ester type.

Zayed SM, Farghaly M, Taha H, Gminski R, Hecker E.

Laboratory of Organic Chemistry, National Research Center, Dokki, Cairo, Egypt.

Special procedures were developed to investigate poisonous milk of lactating goats fed experimentally on aerial parts of the herb Euphorbia peplus L. In extracts of the milk, weakly irritant in the mouse-ear assay, three diterpene ester toxins were detected by techniques of high-performance liquid chromatography. They are of the ingenane structural type: Euphorbia factor Pel (ingenol 20-acetate 3-angelate), Euphorbia factor Pe2 (20-deoxyingenol 3-angelate) and Euphorbia factor Pe4 (20-deoxyingenol-6alpha,7alpha-epoxide 3-angelate). From goats milk collected 15 days after cessation of the experimental feeding period, extracts were completely free of diterpene ester toxins. The toxins polluting the milk are identical to diterpene ester entities occurring in the aerial parts of E. peplus. Of these, Euphorbia factors Pel and Pe2 are known as promoters of tumors of mouse skin. Apart from the toxic Euphorbia factors, the non-toxic parent alcohol ingenol was also detected in the milk. It is absent in the plant, and may have been generated metabolically from a certain portion of the toxic diterpene esters picked up by the goats from their fodder. The results presented here provide, for the first time, data for a novel interpretation of the locally high incidence of esophageal cancer observed in certain areas in the Caspian littoral of Iran, associated with a greater consumption of goat's (and sheep's) milk.

094: J Ethnopharmacol 1998 Jun;61(2):101-10

Study of the anti-hyperglycemic effect of plants used as antidiabetics.

Alarcon-Aguilara FJ, Roman-Ramos R, Perez-Gutierrez S, Aguilar-Contreras A, Contreras-Weber CC, Flores-Saenz JL.

Departamento de Ciencias de la Salud, Universidad Autonoma Metropolitana Iztapalapa, Mexico, DF, Mexico.

The purpose of this research was to study the anti-hyperglycemic effect of 28 medicinal plants used in the treatment of diabetes mellitus. Each plant was processed in the traditional way and intragastrically administered to temporarily hyperglycemic rabbits. The results showed that eight out of the 28 studied plants significantly decrease the hyperglycemic peak and/or the area under the glucose tolerance curve. These plants were: Guazuma ulmifolia, Tournefortia hirsutissima, Lepechinia caulescens, Rhizophora mangle, Musa sapientum, Trigonella foenum graceum, Turnera diffusa, and Euphorbia prostrata. The results suggest the validity of their clinical use in diabetes mellitus control, after their toxicological investigation.

095: J Nat Prod 1998 Jun 26;61(6):749-56

Macrocyclic diterpenoids from Euphorbia semiperfoliata.

Appendino G, Jakupovic S, Tron GC, Jakupovic J, Milon V, Ballero M.

Dipartimento di Scienza e Tecnologia del Farmaco, via Giuria 9, 10125 Torino, Italy. appendin@pharm.unito.it

In addition to known compounds, the aerial parts of E. semiperfoliata afforded an abietanolide (3), 13 jatrophane polyesters (4-9, 12, 14-19), two 4-deoxyphorbol diesters (23, 24), and a pair of epimeric diterpenes (21, 22) with a novel carbon skeleton, which was named euphoperfoliane. Structures were determined by spectroscopic analysis, and the main conformational features of jatropha-6(17),11-dienes are discussed in detail. The obtained isolation yield of several jatrophanes was unprecedented within the spurges (Euphorbia spp.), making E. semiperfoliata a unique source of macrocyclic diterpenoids.

096: J Cancer Res Clin Oncol 1998;124(3-4):179-85

Dietary cancer risk from conditional cancerogens in produce of livestock fed on species of spurge (Euphorbiaceae). II. Pathophysiological investigations in lactating goats fed on the skin irritant herb Euphorbia peplus and in their milk-raised kids.

Nawito M, Ahmed YF, Zayed SM, Hecker E.

Department of Animal Reproduction, National Research Centre, Dokki, Cairo, Egypt.

Lactating goats were fed on aerial parts of the herb Euphorbia peplus L. admixed with their usual green fodder. During the experimental feeding period they showed symptoms of general poisoning. In necropsy the main toxic effects were seen in the heart, lung and liver. Histopathological examinations revealed that the primary toxic effects originated from degenerative changes in parenchymal and endothelial cells. Adverse symptoms in the liver and kidney were also reflected in an alteration of the levels of certain serum enzymes and of blood urea nitrogen. The milk of the goats fed on E. peplus, consumed by their young kids, caused poisoning and even death, with signs similar to those observed in the adult dams. These observations support the hypothesis that the poisoning observed in both milk-raised kids and mother goats is caused by diterpene ester type toxins present in the aerial parts of the herb contaminating the dams fodder. Generally, such skin irritant and hyperplasiogenic toxins are known to be highly active tumour promoters of skin and other organ, e.g. in mice. Lactating goats--as an important source of milk around the world--in a setting similar to that described, may provide a valid experimental etiological model for investigation of food polluted by tumour-promoting diterpene ester toxins.

097: J Cancer Res Clin Oncol 1998;124(3-4):131-40

Erratum in: J Cancer Res Clin Oncol 1998;124(6):351

Dietary cancer risk conditional cancerogens in produce of livestock fed on species of spurge (Euphorbiaceae). I. Skin irritant and tumor-promoting ingenane-type diterpene esters in E. peplus, one of several herbaceous Euphorbia species contaminating fodder of livestock.

Zayed SM, Farghaly M, Taha H, Gotta H, Hecker E.

Laboratory of Organic Chemistry, National Research Center, Dokki, Cairo, Egypt.

The hypothesis was proposed that there is a risk of dietary cancer from conditional cancerogens in produce of livestock polluted with irritants of the diterpene ester type, picked up by feeding on species of Euphorbiaceae (spurge). To challenge this, several herbaceous plants of the genus Euphorbia, widespread as weeds and contaminants of livestock fodder, were identified botanically and extracts of their aerial parts were tested for irritancy on the mouse ear. As compared to a standard probe of croton oil, the extracts of E. peplus, E. nubica and E. helioscopia displayed irritancy. The most active extract (that from E. peplus) was investigated by a fractionation procedure monitored by the mouse ear assay, and five molecularly uniform irritant Euphorbia factors Pe1-Pe5 were identified as diterpene ester-type toxins. Together these factors comprise at least 11 ppm in the aerial parts. They were characterized individually to carry the diterpene parent alcohols ingenol, 20-deoxyingenol, and 20-deoxyingenol-6 alpha, 7alpha-epoxide. The irritancy of the aerial plant parts was shown to be caused mainly by the Euphorbia factors Pe1 and Pe2 together. Upon chronic administration of these irritants and hyperplasiogens as principal cancerogenic risk factors in the mouse skin initiation/promotion bioassay, Pe1 and Pe2 were established as tumor promoters. These findings together support the initial hypothesis and suggest the need for further investigations to determine whether there is a consequent risk of dietary cancer.

098: J Ethnopharmacol 1998 Mar;60(2):163-72

Screening of Australian medicinal plants for antiviral activity.

Semple SJ, Reynolds GD, O'Leary MC, Flower RL.

School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, Australia.

Extracts of 40 different plant species used in the traditional medicine of the Australian Aboriginal people have been investigated for antiviral activity. The extracts have been tested for activity against one DNA virus, human cytomegalovirus (HCMV) and two RNA viruses, Ross River virus (RRV) and poliovirus type 1, at non-cytotoxic concentrations. The most active extracts were the aerial parts of Pterocaulon sphacelatum (Asteraceae) and roots of Dianella longifolia var. grandis (Liliaceae), which inhibited poliovirus at concentrations of 52 and 250 microg/ml, respectively. The extracts of Euphorbia australis (Euphorbiaceae) and Scaevola spinescens (Goodeniaceae) were the most active against HCMV. Extracts of Eremophila latrobei subsp. glabra (Myoporaceae) and Pittosporum phylliraeoides var. microcarpa (Pittosporaceae) exhibited antiviral activity against RRV.

099: J Pharm Pharmacol 1998 Feb;50(2):237-41

Comparative analysis of the vascular actions of diterpenes isolated from Euphorbia canariensis.

Miranda FJ, Alabadi JA, Orti M, Centeno JM, Pinon M, Yuste A, Sanz-Cervera JF, Marco JA, Alborch E.

Department of Physiology, University of Valencia, Hospital La Fe, Spain.

We have analysed the effects of 2,3-diepiingol 7,12-diacetate-8-isobutyrate (compound 1), ingenol-3-angelate-17-benzoate (compound 2), ingenol-3-angelate-17-benzoate-20-acetate (compound 3) and 3,5,7,8,9,15-hexahydroxyjatropha-6(17),11-dien-14-one-5,8-bi s(2-methylbutyrate)-7-(2-methylpropionate) (compound 4), four diterpenes isolated from E. canariensis, on the isometric tension developed by isolated rabbit basilar and carotid arteries. Concentration-response curves to these compounds were obtained cumulatively in both arteries at resting tension and active tone (KCl, 50 mM). At resting tension a concentration-dependent contraction was induced by the four compounds. In the basilar artery the order of potency was 3=1>2=4, without significant differences between Emax values. In the carotid artery the order of potency was 3>2=1=4 and there were no significant differences between the Emax (maximum effect) values of compounds 1-3, all of which were higher than that of compound 4. In pre-contracted basilar artery compounds 1-3 induced concentration-dependent relaxation and compound 4 was almost ineffective; the order of potency was 3>2=1 without significant differences between Emax values. In the carotid artery with active tone the four compounds tested induced further contractions; the order of potency was 3>2=4>1 without significant differences between Emax values. These results show that the four diterpenes are potent active substances in rabbit basilar and carotid arteries and that there are regional differences between their action. The four compounds tested contract basilar and carotid arteries at resting tension. Compounds 1-3 relax pre-contracted basilar artery but not carotid artery.

100: Mem Inst Oswaldo Cruz 1997 Sep-Oct;92(5):719-24

Evaluation of the molluscicidal properties of Euphorbia splendens var. hislopii (N.E.B.) latex: experimental test in an endemic area in the State of Minas Gerais, Brazil.

Mendes NM, Vasconcellos MC, Baptista DF, Rocha RS, Schall VT.

Centro de Pesquisas Rene Rachou-FIOCRUZ, Belo Horizonte, MG, Brasil.

Following the positive results obtained regarding the molluscicidal properties of the latex of Euphorbia splendens that were corroborated in laboratory and field tests under restricted conditions, a field study was conducted in experimental streams located in an endemic area. After recording the average annual fluctuations of vectors in three streams, a solution of E. splendens latex at 12 ppm was applied in stream A, a solution of niclosamide at 3 ppm that was applied in stream B and a third stream (C) remained untreated for negative control. Applications of E. splendens and niclosamide resulted in a mortality of 100% among the snails collected in the streams A and B. No dead snails were found in the negative control stream. A monthly follow-up survey conducted during three consecutive months confirmed the return of vectors to both experimental streams treated with latex and niclosamide. This fact has called for a need to repeat application in order to reach the snails that remained buried in the mud substrate or escaped to the water edge, as well as, newly hatched snails that did not respond to the concentration of these molluscicides. Adults snails collected a month following treatment led us to believe that they had migrate from untreated areas of the streams to those previously treated.

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