Effect of the Harvest Season of Anthyllis henoniana Stems on Antioxidant and Antimicrobial Activities: Phytochemical Profiling of Their Ethyl Acetate Extracts.

Anthyllis henoniana stems were harvested in two seasons: winter and spring (February and May 2021). In this study, we investigated the antioxidant (DPPH, ABTS, FRAP and TAC) and antimicrobial activities, total phenolic contents and total flavonoid contents of the obtained extracts (hexane, ethyl acetate and methanol). The results showed that ethyl acetate extract from stems harvested in winter exhibited the highest antioxidant activity, while ethyl acetate extract from the stems harvested in spring showed the most potent antibacterial and antifungal activities. To explain these differences, we investigated the phytochemical composition of these two extracts using liquid chromatography coupled with mass spectrometry. Therefore, 45 compounds were detected, from which we identified 20 compounds (flavonoids, triterpenoids, chalcones and phenolic acids); some were specific to the harvest month while others were common for both periods. Some of the major compounds detected in ethyl acetate (spring) were dihydrochalcone (Kanzonol Y, 8.2%) and flavanone (sophoraflavanone G, 5.9%), previously recognized for their antimicrobial effects. We therefore concluded that the difference in activities observed for the two harvest periods depends on the chemical composition of the extracts and the relative abundance of each compound.

Antioxidant and Antimicrobial Activities of Erodium arborescens Aerial Part Extracts and Characterization by LC-HESI-MS2 of Its Acetone Extract.

The phytochemical analysis of antioxidant and antibacterial activities of Erodium arborescens aerial part extracts constitute the focus of this research. The chemical composition of an acetone extract was investigated using LC-HESI-MS2, which revealed the presence of 70 compounds. The major identified components were tannin derivatives. Total polyphenol and total flavonoid contents were assessed in plant extracts (hexane, ethyl acetate, acetone and methanol). The results showed that the acetone extract exhibited the highest contents of polyphenols and flavonoids, 895.54 and 36.39 mg QE/g DE, respectively. Furthermore, when compared to other extracts, Erodium arborescens acetone extract was endowed with the highest antioxidant activity with 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC) tests. In addition, the four extracts of Erodium arborescens showed variable degrees of antimicrobial activity against the tested strains, and the interesting activity was obtained with acetone and methanol extracts.

HESI-MS/MS Analysis of Phenolic Compounds from Calendula aegyptiaca Fruits Extracts and Evaluation of Their Antioxidant Activities.

Considering medicinal plants as an inexhaustible source of active ingredients that may be easily isolated using simple and inexpensive techniques, phytotherapy is becoming increasingly popular. Various experimental approaches and analytical methods have been used to demonstrate that the genus Calendula (Asteraceae) has a particular richness in active ingredients, especially phenolic compounds, which justifies the growing interest in scientific studies on this genus' species. From a chemical and biological viewpoint, Calendula aegyptiaca is a little-studied plant. For the first time, high-performance liquid chromatography combined with negative electrospray ionization mass spectrometry (HPLC-HESI-MS) was used to analyze methanolic extracts of Calendula aegyptiaca (C. aegyptiaca) fruits. Thirty-five molecules were identified. Flavonoids (47.87%), phenolic acids (5.18%), and saponins (6.47%) formed the majority of these chemicals. Rutin, caffeic acid hexoside, and Soyasaponin ßg' were the most abundant molecules in the fruit methanolic extract, accounting for 17.49% of total flavonoids, 2.32 % of total phenolic acids, and 0.95% of total saponins, respectively. The antioxidant activity of the fruit extracts of C. aegyptiaca was investigated using FRAP, TAC, and DPPH as well as flavonoids and total phenols content. Because the phenolic components were more extractable using polar solvents, the antioxidant activity of the methanolic extract was found to be higher than that of the dichloromethane and hexane extracts. The IC50 value for DPPH of methanolic extract was found to be 0.041 mg·mL-1. Our findings showed that C. aegyptiaca is an important source of physiologically active compounds.

ESI-MS/MS Analysis of Phenolic Compounds from Aeonium arboreum Leaf Extracts and Evaluation of their Antioxidant and Antimicrobial Activities.

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.

Characterization of polysaccharides isolated from Periploca angustifolia and its antioxidant activity and renoprotective potential against cadmium induced toxicity in HEK293 cells and rat kidney.

Periploca angustifolia has numerous biological properties and also used against various diseases. In our study, this plant has been used for biotechnological production of polysaccharides. The prevention action of polysaccharides isolated from P. angustifolia (PAPS) against Cd-caused oxidative stress in HEK293 cells and kidneys of rats was tested. PAPS were characterized by HPLC, FT-IT, DRX, 1D-and 2D-MNR. PAPS present strong capacity to slow the rate of lipid peroxidation and protein glycation in vitro. In addition, the results indicated that the Cd treatment caused a significant decrease in HEK293 cells viability which wasattenuated by PAPS pre-treatment. Furthermore, our findings revealed that Cd injection increased the levels of urea and creatinine in the serum. The increased levels of protein oxidation and lipid peroxidation along with decreased activities of SOD, CAT and GPx were significantly (p < 0.01) ameliorated by PAPS pre-treatment. Finally, histopathological studies also supported the prevention action of PAPS.

Tunisian Clematis flammula Essential Oil Enhances Wound Healing: GC-MS Analysis, Biochemical and Histological Assessment.

The aerial part of Clematis flammula (Ranunculaceae) has been traditionally used in the treatment of skin diseases including mycotic infection in the Tunisian traditional medicine. The study was undertaken to extract and determine the essential oil chemical composition of Clematis flammula aerial parts and to assess the potential of anemonin in wound healing on mechanically wounded wistar rats. The essential oil was obtained by hydrodistillation and analyzed by GC-MS. Anemonin was isolated and then incorporated as active in a cream for which the cytotoxicity was evaluated by methyl thiazolyl tetrazolium (MTT)-based colorimetric assay. Then, its potential in wound healing on mechanically wounded wistar rats was assessed. The GC-MS analysis showed that the major compound was protoanemonin (86.74%) which spontaneously dimerised in part to form the anemonin. The wound healing activity of anemonin cream exhibited a non toxic potential of anemonin at a concentration of 25 µg/mL with a cell migration efficiency that reaches more than 80% after 48 hours of treatment. Wound healing efficiency was evaluated by monitoring morphological and skin histological analyses. Comparable wound surface reduction of the group treated by anemonin cream (p ≥ 0.05) when compared to the reference treated group. The skin histological analysis showed the completely wound closure. Antioxidant activity was assessed by the malondialdehyde (MDA) rates and antioxidant enzymes (glutathione peroxidase (GPx) and catalase) determination. The results provided strong support for the effective wound healing activity of anemonin cream, making it a promising candidate as a therapeutic agent in tissue repairing processes.

Phytochemical Screening and Antidiabetic, Antihyperlipidemic, and Antioxidant Properties of Anthyllis henoniana (Coss.) Flowers Extracts in an Alloxan-Induced Rats Model of Diabetes.

BACKGROUND: This study investigates the biological activities of Anthyllis henoniana flowers extracts. MATERIALS AND METHODS: Antioxidant activity and the in vitro inhibitory effect of key digesting enzymes related to postprandial hyperglycemia were determined. Diabetic rats were orally and daily given the best extract from flowers of Anthyllis henoniana at a dose of acarbose for one month. RESULTS: Among the extracts, the ethyl acetate one displayed remarkable antioxidant activity including DPPH (IC50 = 2.34 mg/mL) and was more effective in inhibiting α-glucosidase (IC50 = 17 µg/mL) than α-amylase (IC50 = 920 µg /mL) activities. In vivo, the results proved that ethyl acetate extract at doses of 400 mg/kg bw decreased significantly the blood glucose level and lipid profile levels and increased the activities of antioxidant enzymes. These protective impacts of Anthyllis henoniana ethyl acetate flowers extract were confirmed by histological results. CONCLUSION: This study demonstrates, for the first time, that Anthyllis henoniana flowers ethyl acetate extract is effective in inhibiting hyperglycemia and oxidative stress caused by diabetes.

Antioxidant, Hepatoprotective, and Antidepression Effects of Rumex tingitanus Extracts and Identification of a Novel Bioactive Compound.

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.

Antifungal, molluscicidal and larvicidal assessment of anemonin and Clematis flammula L. extracts against mollusc Galba truncatula, intermediate host of Fasciola hepatica in Tunisia.

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 Müll. (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.

A study of the molluscicidal and larvicidal activities of Citrullus colocynthis (L.) leaf extract and its main cucurbitacins against the mollusc Galba truncatula, intermediate host of Fasciola hepatica.

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-ß-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.

Anti-inflammatory and anticancer effects of flavonol glycosides from Diplotaxis harra through GSK3ß regulation in intestinal cells.

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 ß (GSK3ß) is overactivated and represents an interesting therapeutic target. Several flavonoids can inhibit GSK3ß and the purpose of this study was to search for the compounds in Diplotaxis harra which are able to modulate GSK3ß. 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 µg/mL of fractions or compounds purified by HPLC were incubated with cells whose inhibited form of GSK3ß (Pser9 GSK3ß) 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 GSK3ß in PAR2-stimulated IEC6 cells. GSK3ß 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 GSK3ß inhibition.

Antimicrobial activity and bioguided fractionation of Rumex tingitanus extracts for meat preservation.

This study was undertaken to investigate the antibacterial and antifungal activities of Rumex tingitanus leaves extracts as well as the identification of bioactive components and their performance in meat preservation. Total phenolics and flavonoids showed the highest content of phenolics and flavonoids in the ethyl acetate fraction (Rt EtOAcF). For antimicrobial efficacy, leaves extract and derived fraction were tested for their capacity to inhibit bacterial and fungal proliferation in vitro and in vivo. The ethyl acetate fraction showed the most potent antibacterial and antifungal activities compared to the others extracts. Thus, the efficacy of this extract to inhibit the proliferation of Listeria monocytogenes in minced beef meat model was examined. This fraction eradicates the L. monocytogenes population in meat in a concentration- and time-dependent manner. A bio-guided purification of the Rt EtOAc fraction resulted in the isolation of the compound responsible for the observed antimicrobial activity. This compound was identified as luteolin by analysis of spectroscopic data. CHEMICAL COMPOUNDS ISOLATED IN THIS ARTICLE: Luteolin (PubChem CID: 5280445); p-iodonitrotetrazolium chloride (PubChem CID: 64957); Amphotericin B (PubChem CID: 5280965); Gentamicin and (PubChem CID: 6419933); Hexane (PubChem CID: 8058); Methanol (PubChem CID: 887); Ethanol (PubChem CID: 702); Dimethylsulfoxide (PubChem CID: 679); Quercetin (PubChem CID: 5280343); Gallic acid (PubChem CID: 370).

Antibacterial Activity of Onopordum Espinae: Identification of Hispidulin and Dehydromelitensin-8-(4ꞌ-Hydroxy-Methacrylate).

Hexane, ethyl acetate and methanol extracts of Onopordum espinae leaves were investigated for their antibacterial activities against Bacillus cereus, Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, and Salmonella enteritidis. Hexane and ethyl acetate extracts were toxic to Gram-positive bacteria with inhibition zone diameters ranging between 12 and 30 mm. Two products, hispidulin 1, and dehydromelitensin-8-(4ꞌ-hydroxy-methacrylate) 2 were isolated from the ethyl acetate extract of leaves and identified by 2D-NMR for the first time from this species. Ethyl acetate extractꞌs total flavonoid content was the highest, as 78.73 mg quercetin equivalents (QE)/g. The methanol extract showed the highest total phenolic content as 243.43 mg gallic acid equivalents (GAE)/g and gave the most important 2,2-diphenyl-1-picrylhydrazyl (DPPH)scavenging activity (EC50 = 86 µg/mL).

Hexane Extract of Echinops spinosissimus Turra subsp. spinosus from Tunisia: A Potential Source of Acetylated Sterols - Investigation of its Biological Activities.

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 ß-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, ß-amyrin, pseudotaraxasteryl acetate, hop-20(29)-en3-ß-ol, α-amirenone, along with ß-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.

PAR2-dependent activation of GSK3ß regulates the survival of colon stem/progenitor cells.

Protease-activated receptors PAR1 and PAR2 play an important role in the control of epithelial cell proliferation and migration. However, the survival of normal and tumor intestinal stem/progenitor cells promoted by proinflammatory mediators may be critical in oncogenesis. The glycogen synthase kinase-3ß (GSK3ß) pathway is overactivated in colon cancer cells and promotes their survival and drug resistance. We thus aimed to determine PAR1 and PAR2 effects on normal and tumor intestinal stem/progenitor cells and whether they involved GSK3ß. First, PAR1 and PAR2 were identified in colon stem/progenitor cells by immunofluorescence. In three-dimensional cultures of murine crypt units or single tumor Caco-2 cells, PAR2 activation decreased numbers and size of normal or cancerous spheroids, and PAR2-deficient spheroids showed increased proliferation, indicating that PAR2 represses proliferation. PAR2-stimulated normal cells were more resistant to stress (serum starvation or spheroid passaging), suggesting prosurvival effects of PAR2 Accordingly, active caspase-3 was strongly increased in PAR2-deficient normal spheroids. PAR2 but not PAR1 triggered GSK3ß activation through serine-9 dephosphorylation in normal and tumor cells. The PAR2-triggered GSK3ß activation implicates an arrestin/PP2A/GSK3ß complex that is dependent on the Rho kinase activity. Loss of PAR2 was associated with high levels of GSK3ß nonactive form, strengthening the role of PAR2 in GSK3ß activation. GSK3 pharmacological inhibition impaired the survival of PAR2-stimulated spheroids and serum-starved cells. Altogether our data identify PAR2/GSK3ß as a novel pathway that plays a critical role in the regulation of stem/progenitor cell survival and proliferation in normal colon crypts and colon cancer.

Barium chloride induces redox status unbalance, upregulates cytokine genes expression and confers hepatotoxicity in rats-alleviation by pomegranate peel.

The present study was performed to establish the therapeutic efficacy of pomegranate peel against barium chloride induced liver injury. Adult rats were divided into four groups of six animals each: group I, serving as controls, received distilled water; group II received by their drinking water 67 ppm of BaCl2; group III received both 67 ppm of BaCl2 by the same way than group II and 5 % of pomegranate peel (PP) via diet; group IV received 5 % of PP. Analysis by HPLC/MS of PP showed its rich composition in flavonoids such as gallic acid, castalin, hyperin, quercitrin, syringic acid, and quercetin. The protective effects of pomegranate peel against hepatotoxicity induced by barium chloride were assessed using biochemical parameters and histological studies. Exposure of rats to barium caused oxidative stress in the liver as evidenced by an increase in malondialdehyde (MDA), lipid hydroperoxides (LOOHs), H2O2 and advanced oxidation protein product (AOPP) levels, and lactate dehydrogenase (LDH), gamma glutamyl transpeptidase (GGT), alanine aminotransferase (AST) and aspartate aminotransferase (ALT) activities, a decrease in catalase (CAT) and glutathione peroxidase (GPx) activities, glutathion (GSH), non-protein thiol (NPSH), vitamin C levels, and Mn-SOD gene expression. Liver total MT levels, MT-1, and MT-2 and pro-inflammatory cytokine genes expression like TNF-α, IL-1ß and IL-6 were increased. Pomegranate peel, supplemented in the diet of barium-treated rats, showed an improvement of all the parameters indicated above.The present work provided ethnopharmacological relevance of pomegranate peel against the toxic effects of barium, suggesting its beneficial role as a potential antioxidant.

Molluscicidal activity of Solanum elaeagnifolium seeds against Galba truncatula intermediate host of Fasciola hepatica: Identification of ß-solamarine.

CONTEXT: 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. OBJECTIVE: The molluscicidal activity of Solanum elaeagnifolium Cav. (Solanaceae) seeds against Galba truncatula Müll. (Lymnaeidae), intermediate host of Fasciola hepatica L. (Fasciolidae), was evaluated. MATERIALS AND METHODS: 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 ß-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. RESULTS: The methanolic extract of seeds, ß-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. DISCUSSION AND CONCLUSION: This study emphasizes that glycoalkaloids and saponins of Solanum elaeagnifolium are potent molluscicidal agents. Seed methanolic extract, ß-solamarine, and total saponins fraction may be used as molluscicides.

MOLLUSCICIDAL AND LARVICIDAL ACTIVITIES OF Atriplex inflata AERIAL PARTS AGAINST THE MOLLUSK Galba truncatula, INTERMEDIATE HOST OF Fasciola hepatica / Atividade moluscicida e larvicida das partes aéreas de Atriplex inflata contra o molusco Galba truncatula, hospedeiro intermediário da Fasciola hepatica

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.

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.

Cucurbitacins from the Leaves of Citrullus colocynthis (L.) Schrad.

Two new tetracyclic cucurbitane-type triterpene glycosides were isolated from an ethyl acetate extract of Citrullus colocynthis leaves together with four known cucurbitacins. Their structures were established on the basis of their spectroscopic data (mainly NMR and mass spectrometry). Evaluation of the in vitro cytotoxic activity of the isolated compounds against two human colon cancer cell lines (HT29 and Caco-2) and one normal rat intestine epithelial cell line (IEC6), revealed that one of the isolated compounds presented interesting specific cytotoxic activity towards colorectal cell lines.

Synthesis of C3/C1-Substituted Tetrahydroisoquinolines.

A broad biological screening of the natural alkaloid N-methylisosalsoline (2) extracted from Hammada scoparia leaves against a panel of human and parasitic proteases revealed an interesting activity profile of 2 towards human 20S proteasome. This outcome suggests that the 1,2,3,4-tetrahydroisoquinoline skeleton may be exploited as a template for the development of novel anticancer agents. In this article, we report the synthesis and chemical characterization of a new series of isosalsoline-type alkaloids (10-11) with variations at N2 and C3 positions with respect to the natural Compound 2, obtained by a synthetic strategy that involves the Bischler-Napieralski cyclization. The substrate for the condensation to the tetrahydroisoquinoline system, i.e., a functionalized ß-arylethyl amine, was obtained through an original double reduction of nitroalkene. The synthetic strategy can be directed to the construction of highly substituted and functionalized 1,2,3,4-tetrahydroisoquinolines.