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Aeonium is a genus of succulents belonging to the Crassulaceae family. Their importance in traditional medicine has stimulated both pharmacological and chemical research. In this study, we optimized extraction, separation, and analytical conditions using a high performance liquid chromatographic method coupled with electrospray ionization mass spectrometry by the negative mode (HPLC-ESI-MS) in order to, for the first time, determine thirty-four compounds from Aeonium arboreum leaves. Twenty-one of them are assigned among which are sixteen flavonoids and five phenolic acids. FRAP, TAC, DPPH, and ABTS•+ radical scavenging were used to evaluate antioxidant activity. The obtained IC50 values ranged from 0.031 to 0.043 mg.mL−1 for DPPH and between 0.048 and 0.09 mg·mL−1 for ABTS•+. Antimicrobial activity was also assessed. The obtained minimum inhibitory concentrations (MIC) of these extracts ranged from 12.5 to 50 µg·mL−1 against Micrococcus luteus, Listeria ivanovii, Staphylococcus aureus, Salmonella enterica, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger, and Fusarium oxysporum, and from 25 to 50 µg·mL−1 against Candida albicans. Therefore, these extracts can be considered as a potential source of biological active compounds.

Over the last few decades, Rumex species have been recognized as a promising source of new compounds with numerous pharmacological activities. Therefore, the antioxidant activity of Rumex tingitanus (R. tingitanus) leaves extracts was evaluated in vitro and then confirmed in vivo as well as the antidepressant-like and toxicological effects of the extracts. The ethyl acetate fraction (Rt EtOAcF) followed by hydroalcoholic extract (Rt EtOH-H2O) showed a remarkable in vitro antioxidant activity. The hydroalcoholic extract (Rt EtOH-H2O) showed significant hepatoprotective activity against carbon tetrachloride- (CCl4-) induced liver toxicity which is seen from inhibition of the malondialdehyde (MDA) accumulation and enhancement of the liver antioxidant enzymes activities. The Rt EtOH-H2O and Rt EtOAcF extracts were able to reduce the immobility time in mice and then elicited a significant antidepressant-like effect. The ethyl acetate fraction (Rt EtOAcF) was purified and resulted in the identification of a new antioxidant component called 4′-p-acetylcoumaroyl luteolin. The Rt EtOAcF and the 4′-p-acetylcoumaroyl luteolin revealed a strong antioxidant activity using DPPH test with IC50 of 11.7 ± 0.2 and 20.74 ± 0.6 μg/ml, respectively, and AAI of 3.39 and 1.92 better than that of BHT, used as control.

BACKGROUND The molluscicidal and larvicidal activities of the medicinal plant Citrullus colocynthis leaf extracts and its main cucurbitacins were tested against the mollusc gastropod Galba truncatula, the intermediate host of Fasciola hepatica. RESULTS Our findings proved for the first time that the molluscicidal activity was correlated with the presence of terpenoids. A significant molluscicidal value was found in the ethyl acetate extract (LC50 = 12.6 mg L−1). Further fractionation of this extract led to the isolation of two main compounds identified to cucurbitacin E 1 and 2-O-β-d-glucocucurbitacin E 2. Their molluscicidal activities were also investigated and they possessed close activities with LC50 = 9.55 and 10.61 mg L−1 for compounds 2 and 1, respectively. CONCLUSION The ethyl acetate extract and both pure compounds proved the highest larvicidal activities, with a deterioration rate exceeding 89.2% (89.2–100%) and with no toxic effects against associated fauna. © 2016 Society of Chemical Industry

The hexane extract of Echinops spinosissimus Turra subsp. spinosus flower heads was analyzed for its fatty acid and sterol composition. Its physicochemical characteristics were also studied. The saponification, iodine and peroxide values were determined as 255 mg KOH/g, 42.57 g I2 /100 g and 110 m equiv. O2 /kg of oil, respectively. The oleic (C18:1; 61.14%), palmitic (C16:0; 21.36%) and linoleic (C18:2; 10.45%) acids were the dominant fatty acids. This extract was also found to contain high levels of β-sitosterol and stigmasterol (44.97% and 34.95% of total sterols, respectively). On the other hand, the identification of terpenoid compounds was investigated by using GC/MS, which revealed fourteen major terpenoids mainly taraxasterol, lupeol, pseudotaraxasterol, lup-22(29)-en-3-yl acetate, taraxasteryl acetate, α-amyrin, β-amyrin, pseudotaraxasteryl acetate, hop-20(29)-en3-β-ol, α-amirenone, along with β-sitosterol and stigmasterol. Moreover, we have evaluated the in vitro antibacterial and antifungal activities of the unsaponifiable matter and a fraction isolated from this extract. These activities were conducted using the diffusion disc methods and broth microdilution assay. The resulted fraction from this extract showed the highest antibacterial activity with significant minimum inhibitory concentrations (MIC) values 125.0 μg/ml against Staphylococcus aureus, Micrococcus luteus and Bacillus cereus. However, it did exhibit no substantial antifungal activity.

International audience; Context and objective: Diplotaxis harra (Forssk.) Boiss. (Brassicaceae) is traditionally used as an antidiabetic, anti-inflammatory or anticancer agent. In these pathologies, the glycogen synthase kinase 3 b (GSK3b) is overactivated and represents an interesting therapeutic target. Several flavonoids can inhibit GSK3b and the purpose of this study was to search for the compounds in Diplotaxis harra which are able to modulate GSK3b. Materials and methods: Methanol extracts from D. harra flowers were prepared and the bio-guided fractionation of their active compounds was performed using inflammatory [protease-activated receptor 2 (PAR2)-stimulated IEC6 cells] and cancer (human Caco-2 cell line) intestinal cells. 50–100 lg/mL of fractions or compounds purified by HPLC were incubated with cells whose inhibited form of GSK3b (Pser9 GSK3b) and survival were analyzed by Western blot at 1 h and colorimetric assay at 24 h, respectively. LC-UV-MS profiles and MS-MS spectra were used for the characterization of extracts and flavonoids-enriched fractions, and the identification of pure flavonoids was achieved by MS and NMR analysis. Results: The methanol extract from D. harra flowers and its flavonoid-enriched fraction inhibit GSK3b in PAR2-stimulated IEC6 cells. GSK3b inhibition by the flavonoid-enriched D. harra fraction was dependent on PKC activation. The flavonoid-enriched D. harra fraction and its purified compound isorhamnetin-3,7- di-O-glucoside induced a 20% decrease of PAR2-stimulated IEC6 and Caco-2 cell survival. Importantly, normal cells (non-stimulated IEC6 cells) were spared by these treatments. Conclusion: This work indicates that flavonoids from D. harra display cytotoxic activity against inflammatory and cancer intestinal cells which could depend on GSK3b inhibition.

This study describes the antimicrobial and antioxidant activities of the extracts of Hammada scoparia (H. scoparia) and its major alkaloids. Total phenolic content showed that the hydroethanolic extract has the highest phenolic concentration (75.32 mg GAE/g) followed by methanolic extract (59.75 mg GAE/g) and the dichloromethane one with a concentration of 35.23 mg GAE/g. The antioxidant activities exhibited by the hydroethanolic extract and the organic ones were assessed by three methods 2,2-diphenyl-1-picrylhydrazyl (DPPH), β-carotene–linoleic acid system, and reducing activity. The hydroethanolic extract showed the highest scavenging activity (EC50 = 24 μg/mL) and a strong β-carotene–linoleate inhibition, better than the activities of the organic extracts. All the extracts, except of the hexane one, showed antibacterial activity against both Gram-positive and Gram-negative microorganisms with diameter inhibition zones ranged from 8 to 30 mm. The fractionation of the crude extract of H. scoparia afforded two major compounds, carnegine (1) and N-methylisosalsoline (2). The study of their antimicrobial activity showed that the carnegine was more active with minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) ranging from 0.125 to 0.5 mg/mL and 0.25–2 mg/mL, respectively. The time-kill curves of carnegine showed a potent and rapid bactericidal activity. The investigation of the antioxidant activity of these two alkaloids showed that, contrarily to the carnegine, the N-methylisosalsoline exhibited an antioxidant activity. The structure–activity relationship of these alkaloids was discussed.

Objective To investigate the potential of anemonin and Clematis flammula (C. flammula) extracts against infective organisms. Methods The molluscicidal activities of anemonin and C. flammula extracts against Galba truncatula Mull. (Lymnaeidae) and Fasciola hepatica larval stages contaminating this snail in Tunisia were assessed by testing six groups of snails in 250 mL of extracts and aqueous dechlorinated solutions with different concentrations (ranging from 2.5 to 20.0 mg/L) for 48 h. Besides, the antifungal potential of C. flammula leaves and flowers was evaluated by using the diffusion agar and broth dilution methods against four fungal strains: Aspergillus niger, Pythium catenulatum, Rhizoctonia solani and Fusarium phyllophilum. Results As a result, hexane and ethyl acetate flower extracts exhibited significant molluscicidal activities with LC50 median lethal concentrations values of 11.87 and 11.65 mg/L, respectively while LC50 value of anemonin was 9.64 mg/L after 48 h exposure. The flower extracts showed a larvicidal effect with a deterioration rate exceeding 35.39% where flower ethyl acetate residue gave a deterioration rate of cercariae close to 97%. Moreover, C. flammula extracts were not noxious to the associated fauna survival. All extracts inhibited the growth of P. catenulatum, the leaves and flowers methanolic extracts had the more important fungicide action with minimum inhibitory concentrations of 1.56 and 3.12 mg/mL together with minimum fungistatic concentrations of 3.12 and 6.25 mg/mL respectively. Only flower extracts were active against Rhizoctonia solani with minimum inhibitory concentrations varying between 0.70 and 1.56 mg/mL and 6.25 mg/mL of minimum fungistatic concentration. Phytochemical tests showed that the antifungal activity may be attributed to the presence of the flavonoids/saponins in the methanolic extracts and the molluscicide effects could be due to the richness of hexane and ethyl acetate extracts on sterols and triterpenoids. Conclusions This study emphasizes the important molluscicidal and antiparasitic effects of flower ethyl acetate extracts and anemonin compound as well as the considerable antifungal activities of methanolic extracts. These results improve the therapeutic virtues of C. flammula aerial part extracts.

The essential oils of flowers and remaining parts of the plant Senecio gallicus (Asteraceae), growing wild in Sfax (Tunisia), were obtained by hydrodistillation over a period of two years (2012 and 2013). Their analysis by Gas Chromatography-Mass Spectrometry (GC-MS), led to a total number of 36 components, belonging to different classes of chemical compounds. Oils compositions were characterized by the abundance of monoterpenes hydrocarbons, the major compounds present in flowers for the two years of study were respectively the sabinene (49.45% and 28.86%), the α-pinene (9.67% and 9.1%), and the β-myrcene (9.88% and 10.97%). These compounds were also dominant in the essential oils of the plant without flowers where they represent (65.34% and 55%) for the sabinene, (4.14% and 7.3%) for α-pinene, and (6.86% and 0%) for β-myrcene. Obtained essential oils were tested for many biological activities and showed a moderate effect against the fungus Trichoderma reesei and bacteria such as Bacillus sp and Staphylococcus aureus. This study of the Senecio gallicus essential oils represents the first one in Tunisia.

Fasciolose é uma parasitose generalizada que ocorre em animais de fazendas em muitos países em desenvolvimento. Por esta razão, é necessária a busca de novas substâncias contra as doenças parasitárias causadas por vermes. De fato, uma grande variedade de plantas terrestres foi objeto de testes farmacológicos e químicos a fim de descobrir o seu potencial para utilização em terapêutica humana. As atividades moluscicida e larvicida de Atriplex inflata foram testadas contra estágios larvários de Galba truncatula e Fasciola hepatica infectando este caracol na Tunísia. Testes fitoquímicos foram realizados com extratos a fim de estabelecer uma relação significativa com as atividades moluscicida e larvicida. A atividade moluscicida foi avaliada submetendo os caracóis a soluções aquosas. Conforme o caso, hexano, acetato de etilo, metanol e metanol-água (8:2, v-v) foram utilizados como solventes de extração. Como resultado, hexano e extratos de acetato apresentaram atividades potentes de acordo com a Organização Mundial de Saúde, resultando em LC50 = 7,59 mg/L e 6,69 mg/L para extratos de hexano de folhas e frutos, respectivamente. Extratos de acetato de etilo resultaram em LC50 = 5,90 mg/L e 7,32 mg/L para as folhas e frutos sucessivamente. Atividades moluscicidas das substâncias sob a forma de pó foram menos potentes em caracóis, mas ativas de acordo com a Organização Mundial de Saúde. Hexano e extratos de acetato de folhas e frutos apresentaram atividade larvicida potente, com uma taxa de atraso superior a 45,50% (45,50-98,92%). Testes fitoquímicos mostraram que estas atividades podem ser atribuídas à presença de triterpenóides e/ou esteróis. Fasciolosis is a widespread parasitosis of farm live-stock in many developing countries. For this reason, it is necessary to search for new substances against parasitic diseases caused by flukes. Indeed, a wide variety of terrestrial plants have been subjected to chemical and pharmacological screening in order to discover their potential for human medicinal use. The molluscicidal and larvicidal activities of Atriplex inflata were tested on Galba truncatula and Fasciola hepatica larval stages infecting this snail in Tunisia. Phytochemical tests were conducted on extracts in order to establish a meaningful relationship with molluscicidal and larvicidal activities. The molluscicidal activity was evaluated by subjecting snails to sample aqueous solutions. Accordingly, hexane, ethyl acetate, methanol and methanol-water (8:2, v-v) were used as extraction solvents. As a result, hexane and ethyl acetate extracts showed potent activity, according to the World Health Organization, giving LC50 = 7.59 mg/L and 6.69 mg/L for hexane extracts of leaves and fruits, respectively. Ethyl acetate extracts gave LC50 = 5.90 mg/L and 7.32 mg/L for leaves and fruits, successively. Molluscicidal activities of powders were less potent on snails, but active according to the World Health Organization. Hexane and ethyl acetate extracts from leaves and fruits gave potent larvicidal activities with a delay rate exceeding 45.50% (45.50- 98.92%). Phytochemical tests showed that these activities may be attributed to the presence of triterpenoids and/or sterols.

International audience; In search for compounds able to reduce cell adhesion-mediated drug resistance (CAM-DR), we studied effects of Hammada scoparia extracts on leukemic cells adherent or in suspension. We show that H. scoparia flavonoidic fraction and its compound rutin induce apoptosis specifically in adherent leukemic cells and abolish CAM-DR. Importantly, rutin inhibited survival of adherent leukemic progenitors (CD34(+)38(-)123(+)) but spared normal progenitors (CD34(+)38(-)). The pro-apoptotic effects of rutin were correlated with a decrease of active GSK3 beta and inhibitors of GSK3 beta reproduced rutin-induced cytotoxicity. This study uncovers the potential of H. scoparia flavonoids and rutin to overcome CAM-DR in acute myeloid leukemia. (C) 2010 Elsevier Ltd. All rights reserved.

The persistence of fascioliasis in many developing countries urges the search for simple, cheap, and effective substances. In this view, plants provide interesting molluscicidal activities thanks to the secondary metabolites they produce. The genus Solanum is known for its potent effect on vector snails.The molluscicidal activity of Solanum elaeagnifolium Cav. (Solanaceae) seeds against Galba truncatula Müll. (Lymnaeidae), intermediate host of Fasciola hepatica L. (Fasciolidae), was evaluated.Solanum elaeagnifolium seeds were powdered and successively extracted using n-hexane, methylene chloride, acetone, and methanol, for 20 h each. After filtration, solvents were evaporated. An acid-base treatment was conducted on seed methanolic extract to isolate total alkaloids and β-solamarine. Total saponins fraction was obtained after successive macerations and evaporations. The molluscicidal activity was evaluated by subjecting snails, in groups of 10, for 48 h to 500 mL of extracts, fractions, and pure product aqueous solutions, each containing amounts, ranging from 1 to 50 mg of plant material in 5 mg increments.The methanolic extract of seeds, β-solamarine isolated for the first time from this plant and total saponins fraction showed very potent activities on snails, giving respective median lethal concentrations (LC50) of 1.18, 0.49, and 0.94 mg/L. Total alkaloids fraction obtained from the methanolic extract was less active giving an LC50 value of 14.67 mg/L.This study emphasizes that glycoalkaloids and saponins of Solanum elaeagnifolium are potent molluscicidal agents. Seed methanolic extract, β-solamarine, and total saponins fraction may be used as molluscicides.

In this study, we investigated the protective effects of Peganum harmala seeds extract (CPH) against chronic ethanol treatment. Hepatotoxicity was induced in male Wistar rats by administrating ethanol 35% (4 g/kg/day) for 6 weeks. CPH was co-administered with ethanol, by intraperitonial (IP) injection, at a dose of 10 mg/kg bw/day. Control rats were injected by saline solution (NaCl 9‰). Chronic ethanol administration intensified lipid peroxidation monitored by an increase of TBARS level in liver. Ethanol treatment caused also a drastic alteration in antioxidant defence system; hepatic superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) activities. A co-administration of CPH during ethanol treatment inhibited lipid peroxidation and improved antioxidants activities. However, treatment with P. harmala extract protects efficiently the hepatic function of alcoholic rats by the considerable decrease of aminotransferase contents in serum of ethanol-treated rats.

The present study describes the phytochemical profile and the protective effects of Ceratonia siliqua pods essential oil (CsEO), a food and medicinal plant widely distributed in Tunisia. Twenty five different components were identified in the CsEO. Among them, the major detected components were: Nonadecane, Heneicosane , Naphthalene, 1,2-Benzenedicarboxylic acid dibutylester, Heptadecane, Hexadecanoic acid, Octadecanoic acid, 1,2-Benzenedicarboxylic acid, Phenyl ethyl tiglate, Eicosene, Farnesol 3, Camphor, Nerolidol and n-Eicosane. The antimicrobial activity of CsEO was evaluated against a panel of 13 bacteria and 8 fungal strains using agar diffusion and broth microdilution methods. Results have shown that CsEO exhibited moderate to strong antimicrobial activity against the tested species. In addition, the inhibitory effect of this CsEO was evaluated in vivo against a foodborne pathogens Listeria monocytogenes, experimentally inoculated in minced beef meat (2×10(2) CFU/g of meat) amended with different concentrations of the CsEO and stored at 7 °C for 10 days. The antibacterial activity of CsEO in minced beef meat was clearly evident and its presence led to a strong inhibitory effect against the pathogens at 7 °C. On the other hand, the cytotoxic effects of the essential oil against two tumoral human cell lines HeLa and MCF-7 were examined by MTT assay. The CsEO showed an inhibition of both cell lines with significantly stronger activity against HeLa cells. The IC(50) values were 210 and 800 μg/ml for HeLa and MCF-7 cells, respectively. Overall, results presented here suggest that the EO of C. siliqua possesses antimicrobial and cytotoxic properties, and is therefore a potential source of active ingredients for food and pharmaceutical industry. Tunisian Ministry of Higher Education, Scientific Research

Molluscicidal activity of Solanum nigrum var. villosum (morelle velue) extracts and their fractions were tested against the mollusca gastropoda Galba truncatula intermediate host of Fasciola hepatica. The results indicated that the hydro-methanol (MeOH-H2O) immature fruit extract possess the highest molluscicidal activity (LC50 = 3.96 mg/L) against Galba truncatula compared with other tested compounds. After acido-basic treatment, the methanolic extract fraction isolated from the immature fruits and the richest in alkaloids was the most toxic (LC50 = 1.65 mg/L). The fractions richest in saponosides obtained from the hydromethanolic and methanolic extracts of immature fruits showed interesting molluscicidal activities (LC50 = 6.15 mg/L and LC50 = 7.91 mg/L, respectively). The observed molluscicide activity could be attributed to the presence of alkaloids or saponosides. So, the immature fruits of Solanum nigrum var. villosum could be substrates of choice for molluscicide activity. In addition, total alkaloids and saponosides present in this plant deserve further investigations in order to identify the active principles and demonstrate their activities on mollusks in their natural habitat. According to the World Health Organization’s guidelines on screening for plant molluscicides, use of these fractions may add to the arsenal of methods to control snail transmitting fasciolosis in tropical and Third World countries where fasciolosis is a common disease.