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Sample records for biologically active methyl

  1. Estimation of the fraction of biologically active methyl tert-butyl ether degraders in a heterogeneous biomass sample

    DEFF Research Database (Denmark)

    Waul, Christopher Kevin; Arvin, Erik; Schmidt, Jens Ejbye

    2008-01-01

    The fraction of biologically active methyl tert-butyl ether degraders in reactors is just as important for prediction of removal rates as knowledge of the kinetic parameters. The fraction of biologically active methyl tert-butyl ether degraders in a heterogeneous biomass sample, taken from a packed...

  2. Physical properties and biological activities of hesperetin and naringenin in complex with methylated β-cyclodextrin

    Directory of Open Access Journals (Sweden)

    Waratchada Sangpheak

    2015-12-01

    Full Text Available The aim of this work is to improve physical properties and biological activities of the two flavanones hesperetin and naringenin by complexation with β-cyclodextrin (β-CD and its methylated derivatives (2,6-di-O-methyl-β-cyclodextrin, DM-β-CD and randomly methylated-β-CD, RAMEB. The free energies of inclusion complexes between hesperetin with cyclodextrins (β-CD and DM-β-CD were theoretically investigated by molecular dynamics simulation. The free energy values obtained suggested a more stable inclusion complex with DM-β-CD. The vdW force is the main guest–host interaction when hesperetin binds with CDs. The phase solubility diagram showed the formation of a soluble complex of AL type, with higher increase in solubility and stability when hesperetin and naringenin were complexed with RAMEB. Solid complexes were prepared by freeze-drying, and the data from differential scanning calorimetry (DSC confirmed the formation of inclusion complexes. The data obtained by the dissolution method showed that complexation with RAMEB resulted in a better release of both flavanones to aqueous solution. The flavanones-β-CD/DM-β-CD complexes demonstrated a similar or a slight increase in anti-inflammatory activity and cytotoxicity towards three different cancer cell lines. The overall results suggested that solubilities and bioactivities of both flavanones were increased by complexation with methylated β-CDs.

  3. Biological activities of essential oils of Endlicheria citriodora, a methyl geranate-rich lauraceae

    Energy Technology Data Exchange (ETDEWEB)

    Yamaguchi, Klenicy K.L.; Veiga-Junior, Valdir F., E-mail: valdirveiga@ufam.edu.br [Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal do Amazonas, Manaus - AM (Brazil); Pedrosa, Tatiana do Nascimento; Vasconcellos, Marne Carvalho de; Lima, Emerson Silva [Faculdade de Ciencias Farmaceuticas, Universidade Federal do Amazonas, Manaus, AM (Brazil)

    2013-09-01

    The essential oils of branches and leaves of Endlicheria citiodora were obtained by hydrodistillation and analysed using GC-FID, GC-MS and both NMR {sup 13}C and {sup 1}H, resulting in the identification of methyl geranate as major constituent (93%) in both oils. Cytotoxicity, tyrosinase-inhibition and antioxidant activities were studied and characterized. High antioxidant potential (15.52 and 13.53 {mu}g/mL), low cytotoxicity and tyrosinase inhibition (53.85%) were observed. This is the first paper reporting the biological activities and composition of the essential oils of this species. (author)

  4. The in vitro biological activities of synthetic 18-O-methyl mycalamide B, 10-epi-18-O-methyl mycalamide B and pederin.

    Science.gov (United States)

    Richter, A; Kocienski, P; Raubo, P; Davies, D E

    1997-04-01

    Mycalamides A and B, which were originally isolated from a marine sponge, show close structural similarity to the insect toxin pederin, and exhibit potent cytotoxicity and antitumour activity. Detailed investigation of the clinical potential of these compounds has been hampered because they are available in only minute quantities from natural sources. We now describe the biological activities of 18-O-methyl mycalamide B, 10-epi-18-O-methyl mycalamide and pederin, all prepared by total synthesis. The activities of 18-O-methyl mycalamide B and pederin were virtually indistinguishable when evaluated in DNA or protein synthesis assays, and in cytotoxicity assays using human carcinoma cell lines (IC50s 0.2-0.6 nM). In all assays, 10-epi-18-O-methyl mycalamide B was 10(3) times less toxic than its diastereoisomer, demonstrating that the cytotoxicity of 18-O-methyl mycalamide B is inseparable from its ability to inhibit protein synthesis. Short-term exposure of squamous carcinoma cells to 18-O-methyl mycalamide B or pederin caused an irreversible inhibition of cellular proliferation and induced cellular necrosis. In contrast, the antiproliferative effects of the compounds on human fibroblasts were reversible and there was no evidence of necrosis. Demonstration that 18-O-methyl mycalamide B and the synthetically less complex molecule, pederin, show some tumour cell toxicity indicates that this novel class of compounds should be subjected to preclinical evaluation.

  5. Synthesis and Biological Activity of 3-Methyl-1H-pyrazole-4-carboxylic Ester Derivatives

    Institute of Scientific and Technical Information of China (English)

    ZHAO Wei-Guang; LI Zheng-Ming; YUAN Ping-Wei; WANG Wen-Yan

    2001-01-01

    In search of novel pyrazole derivatives with bioactivity,a se-ries of 3-methyl- 1H-pyrazole-4-caboxylic ester derivatives were synthesized via α-oxoketene dithioacetals as starting ma-terial.The structures of al1 compounds prepared were con-firmed by 1HNMR, IR, MS and elemental analyses.Prelimi-nary bioassays indicated that some compounds showed fungici-dal activity against wheat rust,phoma asparagi and antiviral activity against TMV.

  6. Biological Activity of Methyl tert-butyl Ether in Relation to Soil Microorganisms has a Negative Environmental Impact

    Directory of Open Access Journals (Sweden)

    Gholam H.S. Bonjar

    2005-01-01

    Full Text Available Fuel oxygenates are added to gasoline to enhance combustion efficiency of automobiles and reduce air pollution. Methyl tert-butyl ether (MTBE is the most commonly used oxygenate because of its low cost, high-octane level and ease of blending with gasoline. However, due to its water solubility, high mobility and low biodegradability it leaches in soil subsurface at the speed of groundwater. Amending gasoline with MTBE has made a widespread contamination of groundwater, surface waters in coastal environments and at low levels in well water. Although current public concern about MTBE contamination is widely discussed, but its adverse effects on soil micro flora is not yet understood. Soil Streptomycetes are beneficial to soil productivity and are of the major contributors to the biological buffering of soils having antagonistic activity against wide spectrum of pathogenic bacteria and fungi. Streptomyceticidal activity of Methyl tert-butyl ether (MTBE is being reported here. Adverse effect of MTBE against four soil-inhabitant Streptomyces spp. isolates and two plant root-pathogens was investigated. To elucidate antimicrobial activity of MTBE, it was tested against four soil isolates of Streptomyces; a plant bacterial-pathogen, Erwinia carotovora and a plant root fungal-pathogen, Fusarium solani. MTBE did not reveal any growth inhibitory-activity against E. carotovora and F. solani but showed strong inhibitory effect against Streptomyces spp. isolates. The Minimum Inhibitory Concentration (MIC was 1/800 of the original MTBE. Fuel leaks and spills can adversely suppress or eliminate the Streptomyces role in the soil causing alteration in the balance of soil micro flora. This change will lead to domination of microorganisms with adverse biological or ecological effects. Fortunately, major oil companies have decided to phase out MTBE from automobile fuels because of its adverse effect on environment and human health.

  7. Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro

    Institute of Scientific and Technical Information of China (English)

    Xu ZHANG; Yang ZHOU; Yu SHEN; Li-li DU; Jun-hua CHEN; Ying LENG; Jian-hua SHEN

    2009-01-01

    Aim: To design and synthese a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors, featuring the (phenylsul-fonamido-methyl)pyridine and (phenyisulfonamido-methyl)thiazole framework. Methods: Our initial lead 4-(phenylsulfonamido-methyl)benzamides were modified. Inhibition of human and mouse 11β-HSD1 enzy-matic activities by the new compounds was determined by a scintillation proximity assay (SPA) using microsomes containing 11β-HSD1.Results: Sixteen new compounds (6a-6h, 7a-7h) were designed, synthesized and bioassayed. In dose-response studies, several com-pounds showed strong inhibitory activities with IC_(50) values at nanomolar or low nanomolar concentrations. Structure-activity relation-ships are also discussed with respect to molecular docking results. Conclusion: This study provides two promising new templates for 11β-HSD1 inhibitors.

  8. Synthesis, Dimeric Crystal Structure, and Biological Activities of N-(4-Methyl-6-oxo-1,6-dihydro-pyrimidin-2-yl)-N-(2-trifluoromethyl-phenyl)-guanidine

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    The title compound, N-(4-methyl-6-oxo-1,6-dihydro-pyrimidin-2-yl)-N′-(2-trifluoromethyl-phenyl)-guanidine, was synthesized and its structure was confirmed by using IR, MS, 1H NMR, and elemental analysis. The single crystal structure of the title compound was determined by X-ray diffraction. The preliminary biological test showed that the synthesized compound has a weak herbicidal activity.

  9. Relationship between the biological activities of methylated derivatives of (-)-epigallocatechin-3-O-gallate (EGCG) and their cell surface binding activities.

    Science.gov (United States)

    Yano, Satomi; Fujimura, Yoshinori; Umeda, Daisuke; Miyase, Toshio; Yamada, Koji; Tachibana, Hirofumi

    2007-08-22

    It was previously reported that (-)-epigallocatechin-3-O-gallate (EGCG) suppresses the expression of the high-affinity IgE receptor FcepsilonRI in human basophilic cells and that this suppressive effect is associated with EGCG binding to the cell surface. This study examined the effects of five methylated derivatives of EGCG, (-)-epigallocatechin-3-O-(3-O-methyl)gallate (EGCG 3' 'Me), (-)-epigallocatechin-3-O-(4-O-methyl)gallate (EGCG 4' 'Me), (-)-4'-O-methyl-epigallocatechin-3-O-gallate (EGCG 4'Me), (-)-epigallocatechin-3-O-(3,4-O-methyl)gallate (EGCG 3' '4' 'diMe), and (-)-4'-O-methyl-epigallocatechin-3-O-(4-O-methyl)gallate (EGCG 4'4' 'diMe) on FcepsilonRI expression and ERK1/2 phosphorylation, and each of their cell surface binding activities was measured. Of these five methylated derivatives, three that are methylated at the 3' '- and/or 4' '-position, EGCG 3' 'Me, EGCG 4' 'Me, and EGCG 3' '4' 'diMe, suppressed FcepsilonRI expression and ERK1/2 phosphorylation, although the suppressive effects were lower than that of EGCG. EGCG 4'Me and EGCG 4'4' 'diMe, both of which are methylated at the 4'-position, did not demonstrate a suppressive effect. Furthermore, it was found that EGCG 3' 'Me, EGCG 4' 'Me, EGCG 3' '4' 'diMe, and EGCG 4'Me, which are methylated at the 3' '- and/or 4' '-positions or the 4'-position, could bind to the cell surface even though their binding activities were lower than that of EGCG. Only EGCG 4'4' 'diMe, which is methylated at both the 4'- and 4' '-positions, could not bind. These results suggest that the trihydroxyl structure of the B ring is essential for EGCG to exert the suppressive effects and that the hydroxyl groups on both the 4'-position in the B ring and the 4' '-position in the gallate are crucial for the cell surface binding activity of EGCG.

  10. Biological Activity of Methyl tert-butyl Ether in Relation to Soil Microorganisms has a Negative Environmental Impact

    OpenAIRE

    Gholam H.S. Bonjar

    2005-01-01

    Fuel oxygenates are added to gasoline to enhance combustion efficiency of automobiles and reduce air pollution. Methyl tert-butyl ether (MTBE) is the most commonly used oxygenate because of its low cost, high-octane level and ease of blending with gasoline. However, due to its water solubility, high mobility and low biodegradability it leaches in soil subsurface at the speed of groundwater. Amending gasoline with MTBE has made a widespread contamination of groundwater, surface waters in coast...

  11. Synthesis, spectral characterization, molecular modeling, biological activity and potentiometric studies of 4-amino-5-mercapto-3-methyl-S-triazole Schiff's base complexes

    Science.gov (United States)

    Alaghaz, Abdel-Nasser M. A.; Zayed, Mohamed E.; Alharbi, Suliman A.

    2015-03-01

    The Schiff's base derived from condensation of s-triazole (4-amino-5-mercapto-3-methyl-S-triazole) with pyridine-2-aldehyde and their corresponding Mn(II), Co(II), Ni(II), Cu(II) and Zn(II) complexes have been synthesized. The isolated solid complexes were characterized by elemental analyses, molar conductance, spectral (IR, UV-Vis, 1H NMR, mass), magnetic moment and thermal measurements. The IR spectral data suggest that the ligand coordinate in a tridentate manner (SNN) via the one thiol (SH), one pyridine ring and the azomethine (Cdbnd N) groups. The data show that the complexes have composition of ML2 type. The activation of thermodynamic parameters are calculated using Coats-Redfern, Horowitz-Metzger (HM), and Piloyan-Novikova (PN). The octahedral geometry of the complexes is confirmed using DFT method from DMOL3 calculations and ligand field parameters. Protonation constants of Schiff base and stability constants of their binary metal complexes have been determined potentiometrically in 50% DMSO-water media at 25 °C and ionic strength 0.10 M potassium nitrate. The biological activity of these compounds against various fungi has been investigated.

  12. Reaction of Ketene Dithioacetals with Pyrazolylcarbohydrazide:Synthesis and Biological Activities of Ethyl 5-Amino-1-(5'-methyl-1'-t-butyl-4'-pyrazolyl)carbonyl-3-methylthio-1H-pyrazole-4-carboxylate

    Institute of Scientific and Technical Information of China (English)

    LI Ming李明; WEN Li-Rong文丽荣; FU Wei-Jun付维军; ZHAO Gui-Long赵桂龙; HU Fang-Zhong胡方中; YANG Hua-Zheng杨华铮

    2004-01-01

    The title compound, C16-H23N5O3S, ethyl 5-amino-1-(5'-methyl-1'-t-butyl-4'-pyrazolyl)carbonyl-3-methylthio1H-pyrazole-4-carboxylate (5) has been synthesized by the treatment of ethyl 2-cyano-3,3-dimethylthioacrylate with 1-t-butyl-5-methyl-4-hydrazinocarbonylpyrazole (4) in refluxed ethanol. The possible mechanism of the above reaction was also discussed. The results of biological test show that the title compound has fungicidal and plant growth regulation activities.

  13. Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.

    Science.gov (United States)

    Wang, Le; Wang, Gary T; Wang, Xilu; Tong, Yunsong; Sullivan, Gerry; Park, David; Leonard, Nicholas M; Li, Qun; Cohen, Jerry; Gu, Wen-Zhen; Zhang, Haiying; Bauch, Joy L; Jakob, Clarissa G; Hutchins, Charles W; Stoll, Vincent S; Marsh, Kennan; Rosenberg, Saul H; Sham, Hing L; Lin, Nan-Horng

    2004-01-29

    A novel series of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles have been synthesized as selective farnesyltransferase inhibitors using structure-based design. X-ray cocrystal structures of compound 20-FTase-HFP and A313326-FTase-HFP confirmed our initial design. The decreased interaction between the aryl groups and Ser 48 in GGTase-I binding site could be one possible reason to explain the improved selectivity for this new series of FTase inhibitors. Medicinal chemistry efforts led to the discovery of compound 64 with potent cellular activity (EC(50) = 3.5 nM) and outstanding pharmacokinetic profiles in dog (96% bioavailable, 18.4 h oral t(1/2), and 0.19 L/(h x kg) plasma clearance).

  14. The radical mechanism of biological methane synthesis by methyl-coenzyme M reductase

    Energy Technology Data Exchange (ETDEWEB)

    Wongnate, T.; Sliwa, D.; Ginovska, B.; Smith, D.; Wolf, M. W.; Lehnert, N.; Raugei, S.; Ragsdale, S. W.

    2016-05-19

    Methyl-coenzyme M reductase (MCR), the rate-limiting enzyme in methanogenesis and anaerobic methane oxidation, is responsible for the production of over one billion tons of methane per year. The mechanism of methane synthesis is unknown, with the two leading proposals involving either a methyl-nickel(III) (Mechanism I) or methyl radical/Ni(II)-thiolate (Mechanism II) intermediate(s). When the reaction between the active Ni(I) enzyme with substrates was studied by transient kinetic, spectroscopic and computational methods, formation of an EPR-silent Ni(II)-thiolate intermediate was positively identified by magnetic circular dichroism spectroscopy. There was no evidence for an EPR-active methyl-Ni(III) species. Temperature-dependent transient kinetic studies revealed that the activation energy for the initial catalytic step closely matched the value computed by density functional theory for Mechanism II. Thus, our results demonstrate that biological methane synthesis occurs by generation of a methyl radical.

  15. Relationship between structure, conformational flexibility, and biological activity of agonists and antagonists at the N-methyl-D-aspartic acid subtype of excitatory amino acid receptors

    DEFF Research Database (Denmark)

    Madsen, U; Brehm, L; Schaumburg, Kjeld;

    1990-01-01

    The relationship between conformational flexibility and agonist or antagonist actions at the N-Methyl-D-aspartic acid (NMDA) subtype of central L-glutamic acid (GLU) receptors of a series of racemic piperidinedicarboxylic acids (PDAs) was studied. The conformational analyses were based on 1H NMR...... receptors. Each of the three cyclic acidic amino acids showing NMDA agonist activities was found to exist as an equilibrium mixture of two conformers in aqueous solution. In contrast, the NMDA antagonists cis-2,3-PDA and cis-2,4-PDA as well as the inactive compounds trans-2,5-PDA and cis-2,6-PDA were shown...

  16. Biological activities of Zn(II)-S-methyl-cysteine complex as antiradical, inhibitor of acid phosphatase enzyme and in vivo antidepressant effects.

    Science.gov (United States)

    Escudero, Graciela E; Martini, Nancy; Jori, Khalil; Jori, Nadir; Maresca, Nahuel R; Laino, Carlos H; Naso, Luciana G; Williams, Patricia A M; Ferrer, Evelina G

    2016-12-01

    The antidepressant effect of simple Zn(II) salts has been proved in several animal models of depression. In this study, a coordination metal complex of Zn(II) having a sulfur containing ligand is tested as antidepressant for the first time. Forced swimming test method on male Wistar rats shows a decrease in the immobility and an increase in the swimming behavior after treatment with [Zn(S-Met)2] (S-Met=S-methyl-l-cysteine) being more effective and remarkable than ZnCl2. The thiobarbituric acid and the pyranine consumption (hydroxyl and peroxyl radicals, respectively) methods were applied to evaluate the antioxidant activity of S-Met and [Zn(S-Met)2] showing evidence of attenuation of hydroxyl but not peroxyl radicals activities. UV-vis studies on the inhibition of acid phosphatase enzyme (AcP) demonstrated that S-methyl-l-cysteine did not produce any effect but, in contrast, [Zn(S-Met)2] complex behaved as a moderate inhibitor. Finally, bioavailability studies were performed by fluorescence spectroscopy denoting the ability of the albumin to transport the complex.

  17. Biological meaning of the methyl eugenol to fruit flies

    Energy Technology Data Exchange (ETDEWEB)

    Tachi, S.; Subahar, S

    1998-12-16

    The objective of this research is to test a hypothesis whether methyl eugenol has a benefit in sexual selection of fruit flies and to find at what age the male flies respond to methyl eugenol. This test was conducted using carambola fruit fly (Bractocera carambolae) at Inter University Center for Life Science of ITB. The results of the tests are summarized as follows ; 1. Males started to respond to methyl eugenol at the age of 11 days old and the maximum number of males were recorded on 14 and 15 days old. 2. Most of the carambola fruit fly start to respond to methyl eugenol before they become sexually mature. 3. A very small percentage of newly emerged males (less than 1%) survive to mate with females during treatment with methyl eugenol. Methyl eugenol has benefit in sexual selection of carabola fruit fly, i.e., males responded to methyl eugenol before they engage in sexual activities, while females responded to methyl eugenol only when males started their mating activities. (author)

  18. Synthesis, Crystal Structure and Biological Activities of 3-[2-(4-Fluoro-phenyl)-ethyl]-5-methyl-4-hydroxyl-4-methyl-7-methylsulfanyl-3,4-dihydro-pyrido[4,3-d]pyrimidine-8-carbonitrile

    Institute of Scientific and Technical Information of China (English)

    MO Wen-Yan; HE Hong-Wu

    2007-01-01

    The title compound, 3-[2-(4-fluoro-phenyl)-ethyl]-5-methyl-4-hydroxyl-4-methyl-7-methylsulfanyl-3,4-dihydro-pyrido[4,3-d]pyrimidine-8-carbonitrile, has been prepared and detemined by single-crystal X-ray diffraction. The crystal belongs to the triclinic system, space group P1- with a = 6.8754(8), b = 10.2617(12), c = 13.3491(16)(A), α = 93.163(2), β = 96.704(2), γ =102.421(2)°, V= 910.35(19) (A)3, Z = 2, Mr = 370.44, Dc = 1.351 g/cm3,μ = 0.203 mm-1, F(000) =388, the final R = 0.0573 and wR = 0.1497. X-ray analysis reveals that the pyridine and pyrimidine rings are almost coplanar.

  19. Emerging Molecular and Biological Functions of MBD2, a Reader of DNA Methylation

    Directory of Open Access Journals (Sweden)

    Kathleen H Wood

    2016-05-01

    Full Text Available DNA methylation is an epigenetic mark that is essential for many biological processes and is linked to diseases such as cancer. Methylation is usually associated with transcriptional silencing, but new research has challenged this model. Both transcriptional activation and repression have recently been found to be associated with DNA methylation in a context-specific manner. How DNA methylation patterns are interpreted into different functional output remains poorly understood. One mechanism involves the protein ‘readers’ of methylation, which includes the methyl-CpG binding domain (MBD family of proteins. This review examines the molecular and biological functions of MBD2, which binds to CpG methylation and is an integral part of the nucleosome remodeling and histone deacetylation (NuRD complex. MBD2 has been linked to immune system function and tumorigenesis, yet little is known about its functions in vivo. Recent studies have found the MBD2 protein is ubiquitously expressed, with relatively high levels in the lung, liver and colon. Mbd2 null mice surprisingly show relatively mild phenotypes compared to mice with loss of function of other MBD proteins. This evidence has previously been interpreted as functional redundancy between the MBD proteins. Here we examine and contextualize research that suggests MBD2 has unique properties and functions among the MBD proteins. These functions translate to recently described roles in the development and differentiation of multiple cell lineages, including pluripotent stem cells and various cell types of the immune system, as well as in tumorigenesis. We also consider possible models for the dynamic interactions between MBD2 and NuRD in different tissues in vivo. The functions of MBD2 may have direct therapeutic implications for several areas of human disease, including autoimmune conditions and cancer, in addition to providing insights into the actions of NuRD and chromatin regulation.

  20. [Biological activity of Spirulina].

    Science.gov (United States)

    Blinkova, L P; Gorobets, O B; Baturo, A P

    2001-01-01

    In this review information of Spirulina platensis (SP), a blue-green alga (photosynthesizing cyanobacterium) having diverse biological activity is presented. Due to high content of highly valuable proteins, indispensable amino acids, vitamins, beta-carotene and other pigments, mineral substances, indispensable fatty acids and polysaccharides, PS has been found suitable for use as bioactive additive. SP produces an immunostimulating effect by enhancing the resistance of humans, mammals, chickens and fish to infections, the capacity of influencing hemopoiesis, stimulating the production of antibodies and cytokines. Under the influence of SP macrophages, T and B cells are activated. SP sulfolipids have proved to be effective against HIV. Preparations obtained from SP biomass have also been found active against herpesvirus, cytomegalovirus, influenza virus, etc. SP extracts are capable in inhibiting cancerogenesis. SP preparations are regarded as functional products contributing to the preservation of the resident intestinal microflora, especially lactic acid bacilli and bifidobacteria, and to a decrease in the level of Candida albicans. The biological activity of SP with respect to microorganisms holds good promise for using these microalgae as components of culture media.

  1. Synthesis, Crystal Structure and Biological Activities of 1-((5-(4-(4-Chlorophenoxy)-2-chlorophenyl)-2,2,3-trimethyloxazolidin-5-yl)methyl)-1H-1,2,4-triazole

    Institute of Scientific and Technical Information of China (English)

    XU Liang-Zhong; BI Wen-Zhao; YANG Zhi; MENG Fan-Lei; ZHU Qi

    2008-01-01

    The title compound 1-((5-(4-(4-chlorophenoxy)-2-chlorophenyl)-2,2,3-trimethyl-oxazolidin-5-yl)methyl)-1H-1,2,4-triazole (C21H22Cl2N4O2) has been synthesized and characterized by elemental analysis, IR, 1H NMR, MS and single-crystal X-ray diffraction. The crystal belongs to the triclinic system, space group P1 with a = 6.891(2), b = 9.074(2), c = 18.258(4)(A), α = 99.292(4), β = 95.105(4), γ = 108.068(3)°, C21H22Cl2N4O2, Mr = 433.33, V = 1059.3(4) (A)3, Z = 2, Dc = 1.359 g/cm3, F(000) = 452, μ = 0.331 mm-1, the final R = 0.0448 and wR = 0.0994 for 3727 unique reflections. The dihedral angle between the oxazolidine ring taking an envelope conformation with a local pseudo-mirror and the triazole ring is 27.7(9)°. Weak intermolecular C-H…N hydrogen bonds and π-π interactions exist between the triazole rings of neighboring molecules, forming a three-dimensional network, which stabilizes the crystal structure. The primary biological test shows the target compound has certain fungicidal activity.

  2. Histone tails regulate DNA methylation by allosterically activating de novo methyltransferase

    Institute of Scientific and Technical Information of China (English)

    Bin-Zhong Li; Guo-Liang Xu; Zheng Huang; Qing-Yan Cui; Xue-Hui Song; Lin Du; Albert Jeltsch; Ping Chen; Guohong Li; En Li

    2011-01-01

    Cytosine methylation of genomic DNA controls gene expression and maintains genome stability. How a specific DNA sequence is targeted for methylation by a methyltransferase is largely unknown. Here, we show that histone H3 tails lacking lysine 4 (K4) methylation function as an allosteric activator for methyltransferase Dnmt3a by binding to its plant homeodomain (PHD). In vitro, histone H3 peptides stimulated the methylation activity of Dnmt3a up to 8-fold, in a manner reversely correlated with the level of K4 methylation. The biological significance of allosteric regulation was manifested by molecular modeling and identification of key residues in both the PHD and the catalytic domain of Dnmt3a whose mutations impaired the stimulation of methylation activity by H3 peptides but not the binding of H3 peptides. Significantly, these mutant Dnmt3a proteins were almost inactive in DNA methylation when expressed in mouse embryonic stem cells while their recruitment to genomic targets was unaltered. We therefore propose a two-step mechanism for de novo DNA methylation - first recruitment of the methyltransferase probably assisted by a chromatin- or DNA-binding factor, and then allosteric activation depending on the interaction between Dnmt3a and the histone tails - the latter might serve as a checkpoint for the methylation activity.

  3. Biological Activities of Hydrazone Derivatives

    Directory of Open Access Journals (Sweden)

    S. Güniz Küçükgüzel

    2007-08-01

    Full Text Available There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH- proton constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

  4. Biological methylation of inorganic mercury by Saccharomyces cerevisiae - a possible environmental process

    Energy Technology Data Exchange (ETDEWEB)

    Reisinger, K.; Stoeppler, M.; Nuernberg, H.W.

    1983-11-01

    The biological methylation of inorganic mercury by S-adenosylmethione (SAM) was investigated by incubation experiments with Saccharomyces cerevisae (''bakers' yeast''). The methyl donor (methionine) and the acceptor (Hg/sup 2 +/ as HgCl/sub 2/) were also applied in their labelled form (double labelling). Methylmercury as a result of a possibly biological methyl group transfer could not be detected. As reaction product only small amounts (0.01per mille yield) of elemental mercury (Hg/sup 0/) were found, while the overwhelming amount of HgCl/sub 2/ had not reacted.

  5. Biological activities of alginate.

    Science.gov (United States)

    Ueno, Mikinori; Oda, Tatsuya

    2014-01-01

    To gain insight into the structure-activity relationship of alginate, we examined the effect of alginates with varying molecular weights and M/G ratio on murine macrophage cell line, RAW264.7 cells in terms of induction of tumor necrosis factor-α (TNF-α) secretion. Among the alginates tested, alginate with the highest molecular weight (MW 38,000, M/G 2.24) showed the most potent TNF-α-inducing activity. Alginates having higher M/G ratio tended to show higher activity. These results suggest that molecular size and M/G ratio are important structural parameters influencing the TNF-α-inducing activity. Interestingly, enzymatic depolymerization of alginate with bacterial alginate lyase resulted in dramatic increase in the TNF-α-inducing activity. The higher activity of enzymatically digested alginate oligomers to induce nitric oxide production from RAW264.7 cells than alginate polymer was also observed. On the other hand, alginate polymer and oligomer showed nearly equal hydroxyl radical scavenging activities.

  6. Recursively partitioned mixture model clustering of DNA methylation data using biologically informed correlation structures.

    Science.gov (United States)

    Koestler, Devin C; Christensen, Brock C; Marsit, Carmen J; Kelsey, Karl T; Houseman, E Andres

    2013-03-05

    DNA methylation is a well-recognized epigenetic mechanism that has been the subject of a growing body of literature typically focused on the identification and study of profiles of DNA methylation and their association with human diseases and exposures. In recent years, a number of unsupervised clustering algorithms, both parametric and non-parametric, have been proposed for clustering large-scale DNA methylation data. However, most of these approaches do not incorporate known biological relationships of measured features, and in some cases, rely on unrealistic assumptions regarding the nature of DNA methylation. Here, we propose a modified version of a recursively partitioned mixture model (RPMM) that integrates information related to the proximity of CpG loci within the genome to inform correlation structures from which subsequent clustering analysis is based. Using simulations and four methylation data sets, we demonstrate that integrating biologically informative correlation structures within RPMM resulted in improved goodness-of-fit, clustering consistency, and the ability to detect biologically meaningful clusters compared to methods which ignore such correlation. Integrating biologically-informed correlation structures to enhance modeling techniques is motivated by the rapid increase in resolution of DNA methylation microarrays and the increasing understanding of the biology of this epigenetic mechanism.

  7. Mercury methylation and bacterial activity associated to tropical phytoplankton

    Energy Technology Data Exchange (ETDEWEB)

    Coelho-Souza, Sergio A. [Laboratorio de Tracadores Wolfgang Pfeiffer, SL 62, Instituto de Biofisica Carlos Chagas Filho, Bloco G, Ilha do Fundao, Universidade Federal do Rio de Janeiro (IBCCF/UFRJ), RJ, CEP 21949-900 (Brazil); Guimaraes, Jean R.D. [Laboratorio de Tracadores Wolfgang Pfeiffer, SL 62, Instituto de Biofisica Carlos Chagas Filho, Bloco G, Ilha do Fundao, Universidade Federal do Rio de Janeiro (IBCCF/UFRJ), RJ, CEP 21949-900 (Brazil)]. E-mail: jeanrdg@biof.ufrj.br; Mauro, Jane B.N. [Laboratorio de Tracadores Wolfgang Pfeiffer, SL 62, Instituto de Biofisica Carlos Chagas Filho, Bloco G, Ilha do Fundao, Universidade Federal do Rio de Janeiro (IBCCF/UFRJ), RJ, CEP 21949-900 (Brazil); Miranda, Marcio R. [Laboratorio de Tracadores Wolfgang Pfeiffer, SL 62, Instituto de Biofisica Carlos Chagas Filho, Bloco G, Ilha do Fundao, Universidade Federal do Rio de Janeiro (IBCCF/UFRJ), RJ, CEP 21949-900 (Brazil); Azevedo, Sandra M.F.O. [Laboratorio de Ecofisiologia e Toxicologia de Cianobacterias, IBCCF/UFRJ, RJ (Brazil)

    2006-07-01

    The methylated form of mercury (Hg), methylmercury (MeHg), is one of the most toxic pollutants. Biotic and/or abiotic methylation, often associated to sulfate-reducing bacteria metabolism, occurs in aquatic environments and in many tropical areas, mostly in the periphyton associated to floating macrophyte roots. Data about mercury methylation by phytoplankton are scarce and the aim of this study was to verify the biotic influence in the methylation process in Microcystis aeruginosa and Sineccocystis sp. laboratory strains and in natural populations of phytoplankton from two different aquatic systems, the mesotrophic Ribeirao das Lajes reservoir and hypereutrophic oligohaline Jacarepagua lagoon, Rio de Janeiro state, Brazil. Adapted radiochemical techniques were used to measure sulfate-reduction, mercury methylation and bacterial activity in phytoplankton samples. Methyl-{sup 203}Hg formation from added inorganic {sup 203}Hg and {sup 3}H-Leucine uptake were measured by liquid scintillation as well as sulfate-reduction, estimated as H{sub 2} {sup 35}S produced from added Na{sub 2} {sup 35}SO{sub 4}. There was no significant difference in low methylation potentials (0.37%) among the two cyanobacterium species studied in laboratory conditions. At Ribeirao das Lajes reservoir, there was no significant difference in methylation, bacterial activity and sulfate-reduction of surface sediment between the sampling points. Methylation in sediments (3-4%) was higher than in phytoplankton (1.5%), the opposite being true for bacterial activity (sediment mean 6.6 against 150.3 nmol gdw{sup -1} h{sup -1} for phytoplankton samples). At Jacarepagua lagoon, an expressive bacterial activity (477.1 x 10{sup 3} nmol gdw{sup -1} h{sup -1} at a concentration of 1000 nM leucine) and sulfate-reduction ({approx}21% H{sub 2} {sup 35}S trapped) associated to phytoplankton (mostly cyanobacteria M. aeruginosa) was observed, but mercury methylation was not detected.

  8. Synthesis and antitumor activity of 9-methyl-10-hydroxycamptothecin

    Institute of Scientific and Technical Information of China (English)

    Sheng Wang; Yu Yan Li; Qi Dong You

    2008-01-01

    A novel camptothecin analogue, 9-methyl-10-hydroxycamptothecin (4), was unexpectedly synthesized from 10-hydroxycamptothecin in two steps. The key step included an efficient Mannich-type reaction. The overall yield was 47.2%. An ether analogue of 4, 9-methyl-10-benzylaminomethoxycamptothecin (5), was also prepared. These new camptothecin analogues were evaluated for in vitro cytotoxicity against four human cancer cell lines, and exhibited more potent antitumor activities than contrals camptothecin and topotecan against several cancer cells.

  9. Synthesis, Characterization, and Biological Activity of N1-Methyl-2-(1H-1,2,3-Benzotriazol-1-y1-3-Oxobutan-ethioamide Complexes with Some Divalent Metal (II Ions

    Directory of Open Access Journals (Sweden)

    Nouria A. Al-Awadi

    2008-01-01

    Full Text Available A new series of Zn2+, Cu2+, Ni2+, and Co2+ complexes of N1-methyl-2-(1H-1,2,3-benzotriazol-1-yl-3-oxobutanethioamide (MBOBT, HL, has been synthesized and characterized by different spectral and magnetic measurements and elemental analysis. IR spectral data indicates that (MBOBT exists only in the thione form in the solid state while 13C NMR spectrum indicates its existence in thione and thiole tautomeric forms. The IR spectra of all complexes indicate that (MBOBT acts as a monobasic bidentate ligand coordinating to the metal(II ions via the keto-oxygen and thiolato-sulphur atoms. The electronic spectral studies showed that (MBOBT bonded to all metal ions through sulphur and nitrogen atoms based on the positions and intensity of their charge transfer bands. Furthermore, the spectra reflect four coordinate tetrahedral zinc(II, tetragonally distorted copper(II, square planar nickel(II, and cobalt(II complexes. Thermal decomposition study of the complexes was monitored by TG and DTG analyses under N2 atmosphere. The decomposition course and steps were analyzed and the activation parameters of the nonisothermal decomposition are determined. The isolated metal chelates have been screened for their antimicrobial activities and the findings have been reported and discussed in relation to their structures.

  10. Imidazole: Having Versatile Biological Activities

    Directory of Open Access Journals (Sweden)

    Amita Verma

    2013-01-01

    Full Text Available Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. There are several methods used for the synthesis of imidazole-containing compounds, and also their various structure reactions offer enormous scope in the field of medicinal chemistry. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. This paper aims to review the biological activities of imidazole during the past years.

  11. Dynamic Enhancer Methylation--A Previously Unrecognized Switch for Tissue-Type Plasminogen Activator Expression.

    Directory of Open Access Journals (Sweden)

    Mia Magnusson

    Full Text Available Tissue-type plasminogen activator (t-PA, which is synthesized in the endothelial cells lining the blood vessel walls, is a key player in the fibrinolytic system protecting the circulation against occluding thrombus formation. Although classical gene regulation has been quite extensively studied in order to understand the mechanisms behind t-PA regulation, epigenetics, including DNA methylation, still is a largely unexplored field. The aim of this study was to establish the methylation pattern in the t-PA promoter and enhancer in non-cultured compared to cultured human umbilical vein endothelial cells (HUVECs, and to simultaneously examine the level of t-PA gene expression. Bisulphite sequencing was used to evaluate the methylation status, and real-time RT-PCR to determine the gene expression level. While the t-PA promoter was stably unmethylated, we surprisingly observed a rapid reduction in the amount of methylation in the enhancer during cell culturing. This demethylation was in strong negative correlation with a pronounced (by a factor of approximately 25 increase in t-PA gene expression levels. In this study, we show that the methylation level in the t-PA enhancer appears to act as a previously unrecognized switch controlling t-PA expression. Our findings, which suggest that DNA methylation is quite dynamic, have implications also for the interpretation of cell culture experiments in general, as well as in a wider biological context.

  12. A single amino acid substitution confers enhanced methylation activity of mammalian Dnmt3b on chromatin DNA.

    Science.gov (United States)

    Shen, Li; Gao, Ge; Zhang, Ying; Zhang, He; Ye, Zhiqiang; Huang, Shichao; Huang, Jinyan; Kang, Jiuhong

    2010-10-01

    Dnmt3a and Dnmt3b are paralogous enzymes responsible for de novo DNA methylation but with distinguished biological functions. In mice, disruption of Dnmt3b but not Dnmt3a causes global DNA hypomethylation, especially in repetitive sequences, which comprise the large majority of methylated DNA in the genome. By measuring DNA methylation activity of Dnmt3a and Dnmt3b homologues from five species, we found that mammalian Dnmt3b possessed significantly higher methylation activity on chromatin DNA than Dnmt3a and non-mammalian Dnmt3b. Sequence comparison and mutagenesis experiments identified a single amino acid substitution (I662N) in mammalian Dnmt3b as being crucial for its high chromatin DNA methylation activity. Further mechanistic studies demonstrated this substitution markedly enhanced the binding of Dnmt3b to nucleosomes and hence increased the chromatin DNA methylation activity. Moreover, this substitution was crucial for Dnmt3b to efficiently methylate repetitive sequences, which increased dramatically in mammalian genomes. Consistent with our observation that Dnmt3b evolved more rapidly than Dnmt3a during the emergence of mammals, these results demonstrated that the I662N substitution in mammalian Dnmt3b conferred enhanced chromatin DNA methylation activity and contributed to functional adaptation in the epigenetic system.

  13. Synthesis, spectroscopic characterization, DNA interaction and biological activities of Mn(II), Co(II), Ni(II) and Cu(II) complexes with [(1H-1,2,4-triazole-3-ylimino)methyl]naphthalene-2-ol

    Science.gov (United States)

    Gaber, Mohamed; El-Wakiel, Nadia A.; El-Ghamry, Hoda; Fathalla, Shaimaa K.

    2014-11-01

    Manganese(II), cobalt(II), nickel(II) and copper(II) complexes of [(1H-1,2,4-triazole-3-ylimino)methyl]naphthalene-2-ol have been synthesized. The structure of complexes have been characterized by elemental analysis, molar conductance, magnetic moment measurements and spectral (IR, 1H NMR, EI-mass, UV-Vis and ESR), and thermal studies. The results showed that the chloro and nitrato Cu(II) complexes have octahedral geometry while Ni(II), Co(II) and Mn(II) complexes in addition to acetato Cu(II) complex have tetrahedral geometry. The possible structures of the metal complexes have been computed using the molecular mechanic calculations using the hyper chem. 8.03 molecular modeling program to confirm the proposed structures. The kinetic and thermodynamic parameters of the thermal decomposition steps were calculated from the TG curves. The binding modes of the complexes with DNA have been investigated by UV-Vis absorption titration. The results showed that the mode of binding of the complexes to DNA is intercalative or non-intercalative binding modes. Schiff base and its metal complexes have been screened for their in vitro antimicrobial activities against Gram positive bacteria (Staphylococcus aureus), Gram negative bacteria (Escherichia coli and Pesudomonas aeruginosa), fungi (Asperigllus flavus and Mucer) and yeast (Candida albicans and Malassezia furfur).

  14. Cu(II complexes of an ionic liquid-based Schiff base [1-{2-(2-hydroxy benzylidene amino ethyl}-3-methyl­imidazolium]Pf6: Synthesis, characterization and biological activities

    Directory of Open Access Journals (Sweden)

    Saha Sanjoy

    2015-01-01

    Full Text Available Two Cu(II complexes of an ionic liquid based Schiff base 1-{2-(2-hydroxybenzylideneamino ethyl}-3-methylimidazolium hexaflurophosphate, were prepared and characterized by different analytical and spectroscopic methods such as elemental analysis, magnetic susceptibility, UV-Vis, IR, NMR and mass spectroscopy. The Schiff base ligand was found to act as a potential bidentate chelating ligand with N, O donor sites and formed 1:2 metal chelates with Cu(II salts. The synthesized Cu(II complexes were tested for biological activity.

  15. Activity of pectin methyl esterase during blanching of peaches

    NARCIS (Netherlands)

    Tijskens, L.M.M.; Rodis, P.S.; Hertog, M.L.A.T.M.; Proxenia, N.; Dijk, van C.

    1999-01-01

    The activity of pectin methyl esterase (PE) in peaches during blanching treatments was modelled and analyzed. It was postulated that the enzyme exists in two configurations, one bound and one soluble. The bound configuration can be converted into the soluble configuration. These two configurations h

  16. Metabolic effects of azoxystrobin and kresoxim-methyl against Fusarium kyushuense examined using the Biolog FF MicroPlate.

    Science.gov (United States)

    Wang, Hancheng; Wang, Jin; Chen, Qingyuan; Wang, Maosheng; Hsiang, Tom; Shang, Shenghua; Yu, Zhihe

    2016-06-01

    Azoxystrobin and kresoxim-methyl are strobilurin fungicides, and are effective in controlling many plant diseases, including Fusarium wilt. The mode of action of this kind of chemical is inhibition of respiration. This research investigated the sensitivities of Fusarium kyushuense to azoxystrobin and kresoxim-methyl, and to the alternative oxidase inhibitor salicylhydroxamic acid (SHAM). The Biolog FF MicroPlate is designed to examine substrate utilization and metabolic profiling of micro-organisms, and was used here to study the activity of azoxystrobin, kresoxim-methyl and SHAM against F. kyushuense. Results presented that azoxystrobin and kresoxim-methyl strongly inhibited conidial germination and mycelial growth of F. kyushuense, with EC50 values of 1.60 and 1.79μgml(-1), and 6.25 and 11.43μgml(-1), respectively; while not for SHAM. In the absence of fungicide, F. kyushuense was able to metabolize 91.6% of the tested carbon substrates, including 69 effectively and 18 moderately. SHAM did not inhibit carbon substrate utilization. Under the selective pressure of azoxystrobin and kresoxim-methyl during mycelial growth (up to 100μgml(-1)) and conidial germination (up to 10μgml(-1)), F. kyushuense was unable to metabolize many substrates in the Biolog FF MicroPlate; while especially for carbon substrates in glycolysis and tricarboxylic acid cycle, with notable exceptions such as β-hydroxybutyric acid, y-hydroxybutyric acid, α-ketoglutaric acid, α-d-glucose-1-phosphate, d-saccharic acid and succinic acid in the mycelial growth stage, and β-hydroxybutyric acid, y-hydroxybutyric acid, α-ketoglutaric acid, tween-80, arbutin, dextrin, glycerol and glycogen in the conidial germination stage. This is a new finding for some effect of azoxystrobin and kresoxim-methyl on carbon substrate utilization related to glycolysis and tricarboxylic acid cycle and other carbons, and may lead to future applications of Biolog FF MicroPlate for metabolic effects of other

  17. Molecular characteristics versus biological activity

    Science.gov (United States)

    Applegate, Vernon C.; Smith, Manning A.; Willeford, Bennett R.

    1967-01-01

    The molecular characteristics of mononitrophenols containing halogens not only play a key role in their biological activity but provide a novel example of selective toxicity among vertebrate animals. It has been reported that efforts to control the parasitic sea lamprey in the Great Lakes are directed at present to the applications of a selective toxicant to streams inhabited by lamprey larvae. Since 1961, the larvicide that has been used almost exclusively in the control program has been 3-trifluoromethyl-4-nitrophenol (TFM). However, this is only one of about 15 closely related compounds, all halogen-containing mononitrophenols, that display a selectively toxic action upon lampreys. Although not all of the halogenated mononitrophenols are selectively toxic to lampreys (in fact, fewer than half of those tested), no other group of related compounds has displayed any useful larvicidal activity except for the substituted nitrosalicylanilides.

  18. Synthesis and characterization of selected methyl 5-methoxy-2-methyl-1-benzofuran-3-carboxylate derivatives with potential antimicrobial activity.

    Science.gov (United States)

    Krawiecka, Mariola; Kuran, Bozena; Kossakowski, Jerzy; Wolska, Irena; Kierzkowska, Marta; Młynarczyk, Grazyna

    2012-01-01

    Halogen and aminoalkyl derivatives of methyl 5-methoxy-2-methyl-1-benzofuran-3-carboxylate were prepared using 5-hydroxy-2-methyl-3-benzofuranocarboxylic acid as starting material. (1)H-NMR spectra were obtained for all of the synthesized structures, and for compounds 1 and 2 X-ray crystal structures were obtained too. All derivatives were tested for antimicrobial activity against a selection of Gram-positive cocci, Gram-negative rods and yeasts.

  19. Effect of salinity on mercury methylating benthic microbes and their activities in Great Salt Lake, Utah.

    Science.gov (United States)

    Boyd, Eric S; Yu, Ri-Qing; Barkay, Tamar; Hamilton, Trinity L; Baxter, Bonnie K; Naftz, David L; Marvin-DiPasquale, Mark

    2017-03-01

    Surface water and biota from Great Salt Lake (GSL) contain some of the highest documented concentrations of total mercury (THg) and methylmercury (MeHg) in the United States. In order to identify potential biological sources of MeHg and controls on its production in this ecosystem, THg and MeHg concentrations, rates of Hg(II)-methylation and MeHg degradation, and abundances and compositions of archaeal and bacterial 16 rRNA gene transcripts were determined in sediment along a salinity gradient in GSL. Rates of Hg(II)-methylation were inversely correlated with salinity and were at or below the limits of detection in sediment sampled from areas with hypersaline surface water. The highest rates of Hg(II)-methylation were measured in sediment with low porewater salinity, suggesting that benthic microbial communities inhabiting less saline environments are supplying the majority of MeHg in the GSL ecosystem. The abundance of 16S rRNA gene transcripts affiliated with the sulfate reducer Desulfobacterium sp. was positively correlated with MeHg concentrations and Hg(II)-methylation rates in sediment, indicating a potential role for this taxon in Hg(II)-methylation in low salinity areas of GSL. Reactive inorganic Hg(II) (a proxy used for Hg(II) available for methylation) and MeHg concentrations were inversely correlated with salinity. Thus, constraints imposed by salinity on Hg(II)-methylating populations and the availability of Hg(II) for methylation are inferred to result in higher MeHg production potentials in lower salinity environments. Benthic microbial MeHg degradation was also most active in lower salinity environments. Collectively, these results suggest an important role for sediment anoxia and microbial sulfate reducers in the production of MeHg in low salinity GSL sub-habitats and may indicate a role for salinity in constraining Hg(II)-methylation and MeHg degradation activities by influencing the availability of Hg(II) for methylation.

  20. SYNTHESIS AND BIOLOGICAL STUDIES OF CHERIMOLACYCLOPEPTIDE E AND ITS N- METHYLATED ANALOG

    Directory of Open Access Journals (Sweden)

    Himaja M

    2011-12-01

    Full Text Available The N-methyl derivative of Cherimolacyclopeptide E cyclo[Phe-(DimethylTyr-Pro-Gly-Leu-Gly] was synthesized using solution phase peptide synthesis. The synthesized compound was characterized by spectral data and was evaluated for anthelmintic and insecticidal activities. The compound exhibited potent anthelmintic activity as compared to the standard drug mebendazole.

  1. Biodegradation of triclosan and formation of methyl-triclosan in activated sludge under aerobic conditions

    DEFF Research Database (Denmark)

    Chen, Xijuan; Nielsen, Jeppe Lund; Furgal, Karolina;

    2011-01-01

    Triclosan is an antimicrobial agent which is widely used in household and personal care products. Widespread use of this compound has led to the elevated concentrations of triclosan in wastewater, wastewater treatment plants (WWTPs) and receiving waters. Removal of triclosan and formation...... of triclosan- methyl was investigated in activated sludge from a standard activated sludge WWTP equipped with enhanced biological phosphorus removal. The removal was found to occur mainly under aerobic conditions while under anoxic (nitrate reducing) and anaerobic conditions rather low removal rates were...... determined. In a laboratory-scale activated sludge reactor 75% of the triclosan was removed under aerobic conditions within 150 h, while no removal was observed under anaerobic or anoxic conditions. One percent of the triclosan was converted to triclosan-methyl under aerobic conditions, less under anoxic...

  2. 3-甲基-4-氨基-5-乙氧羰基甲硫基三唑席夫碱的合成及生物活性%Synthesis and Biological Activity of Schiff Base Derivatives 3-Methyl-4-amino-5-ethoxycarbonylmethylthio-1,2,4-triazole

    Institute of Scientific and Technical Information of China (English)

    杨清翠; 孙晓红; 刘源发; 靳如意; 马海霞

    2013-01-01

    以3-甲基-4-氨基-5-巯基-1,2,4-三唑为原料,在乙醇/氢氧化钠体系中与氯乙酸乙酯反应合成了3-甲基-4-氨基-5-乙氧羰基甲硫基-1,2,4-三唑,再与取代芳醛合成了6种(A1~A6)新型乙氧羰基三唑席夫碱化合物,化合物结构经元素分析,IR,1H NMR,MS等确证.对烟草赤星病、马铃薯干腐病、小麦赤霉病、西瓜枯萎病4种植物病原菌的初步生物活性测试结果表明,化合物A3的抑菌活性优于或相当于对照原药三唑酮.%New Shiff bases A1 ~ A6 were synthesized by 3-methyl-4-amino-5-ethoxycarbonylmethylthio-1,2,4-triazole with substituted aromatic aldehydes.The intermediate 3-methyl-4-amino-5-ethoxycarbonyl-methylthio-1,2,4-triazole was synthesized by 3-methyl-4-amino-5-mercapto-1,2,4-triazole with chloroacetic acid ethyl ester in ethanol /sodium hydroxide.The structures were confirmed by 1H NMR,IR,MS.The biological activities of prepared Schiff bases to four vegetable pathogens have been tested,and the results showed that A3 is better than or equivalent to triadimefon.

  3. Biological Activity of Masked Endotoxin

    Science.gov (United States)

    Schwarz, Harald; Gornicec, Jan; Neuper, Theresa; Parigiani, Maria Alejandra; Wallner, Michael; Duschl, Albert; Horejs-Hoeck, Jutta

    2017-01-01

    Low endotoxin recovery (LER) is a recently discovered phenomenon describing the inability of limulus amebocyte lysate (LAL)-based assays to detect lipopolysaccharide (LPS) because of a “masking effect” caused by chelators or detergents commonly used in buffer formulations for medical products and recombinant proteins. This study investigates the masking capacities of different buffer formulations and whether masked endotoxin is biologically active. We show that both naturally occurring endotoxin as well as control standard endotoxin can be affected by LER. Furthermore, whereas masked endotoxin cannot be detected in Factor C based assays, it is still detectable in a cell-based TLR4-NF-κB-luciferase reporter gene assay. Moreover, in primary human monocytes, masked LPS induces the expression of pro-inflammatory cytokines and surface activation markers even at very low concentrations. We therefore conclude that masked LPS is a potent trigger of immune responses, which emphasizes the potential danger of masked LPS, as it may pose a health threat in pharmaceutical products or compromise experimental results. PMID:28317862

  4. A review exploring biological activities of hydrazones

    Directory of Open Access Journals (Sweden)

    Garima Verma

    2014-01-01

    Full Text Available The development of novel compounds, hydrazones has shown that they possess a wide variety of biological activities viz. antimicrobial, anticonvulsant, antidepressant, anti-inflammatory, analgesic, antiplatelet, antimalarial, anticancer, antifungal, antitubercular, antiviral, cardio protective etc., Hydrazones/azomethines/imines possess-NHN = CH- and constitute an important class of compounds for new drug development. A number of researchers have synthesized and evaluated the biological activities of hydrazones. This review aims at highlighting the diverse biological activities of hydrazones.

  5. Laser Irradiation-Induced DNA Methylation Changes Are Heritable and Accompanied with Transpositional Activation of mPing in Rice

    Science.gov (United States)

    Li, Siyuan; Xia, Qiong; Wang, Fang; Yu, Xiaoming; Ma, Jian; Kou, Hongping; Lin, Xiuyun; Gao, Xiang; Liu, Bao

    2017-01-01

    DNA methylation is an integral component of the epigenetic code in most higher eukaryotes. Exploring the extent to which DNA methylation can be altered under a specific condition and its heritability is important for elucidating the biological functions of this epigenetic modification. Here, we conducted MSAP analysis of rice plants with altered phenotypes subsequent to a low-dose Nd3+YAG laser irradiation. We found that all four methylation patterns at the 5′-CCGG sites that are analyzable by MSAP showed substantial changes in the immediately treated M0 plants. Interestingly, the frequencies of hypo- and hypermethylation were of similar extents, which largely offset each other and render the total methylation levels unchanged. Further analysis revealed that the altered methylation patterns were meiotically heritable to at least the M2 generation but accompanied with further changes in each generation. The methylation changes and their heritability of the metastable epigenetic state were verified by bisulfite sequencing of portion of the retrotranspon, Tos17, an established locus for assessing DNA methylation liability in rice. Real-time PCR assay indicated that the expression of various methylation-related chromatin genes was perturbed, and a Pearson correlation analysis showed that many of these genes, especially two AGOs (AGO4-1 and AGO4-2), were significantly correlated with the methylation pattern alterations. In addition, excisions of a MITE transposon, mPing, occurred rampantly in the laser irradiated plants and their progenies. Together, our results indicate that heritable DNA methylation changes can be readily induced by low-dose laser irradiation, and which can be accompanied by transpostional activation of transposable elements.

  6. Loss of ATRX, associated with DNA methylation pattern of chromosome end, impacted biological behaviors of astrocytic tumors.

    Science.gov (United States)

    Cai, Jinquan; Chen, Jing; Zhang, Wei; Yang, Pei; Zhang, Chuanbao; Li, Mingyang; Yao, Kun; Wang, Hongjun; Li, Qingbin; Jiang, Chuanlu; Jiang, Tao

    2015-07-20

    Loss of ATRX leads to epigenetic alterations, including abnormal levels of DNA methylation at repetitive elements such as telomeres in murine cells. We conducted an extensive DNA methylation and mRNA expression profile study on a cohort of 82 patients with astrocytic tumors to study whether ATRX expression was associated with DNA methylation level in astrocytic tumors and in which cellular functions it participated. We observed that astrocytic tumors with lower ATRX expression harbored higher DNA methylation level at chromatin end and astrocytic tumors with ATRX-low had distinct gene expression profile and DNA methylation profile compared with ATRX-high tumors. Then, we uncovered that several ATRX associated biological functions in the DNA methylation and mRNA expression profile (GEP), including apoptotic process, DNA-dependent positive regulation of transcription, chromatin modification, and observed that ATRX expression was companied by MGMT methylation and expression. We also found that loss of ATRX caused by siRNA induced apoptotic cells increasing, reduced tumor cell proliferation and repressed the cell migration in glioma cells. Our results showed ATRX-related regulatory functions of the combined profiles from DNA methylation and mRNA expression in astrocytic tumors, and delineated that loss of ATRX impacted biological behaviors of astrocytic tumor cells, providing important resources for future dissection of ATRX role in glioma.

  7. High-resolution melt analysis of DNA methylation to discriminate semen in biological stains.

    Science.gov (United States)

    Antunes, Joana; Silva, Deborah S B S; Balamurugan, Kuppareddi; Duncan, George; Alho, Clarice S; McCord, Bruce

    2016-02-01

    The goal of this study was to develop a method for the detection of semen in biological stains using high-resolution melt (HRM) analysis and DNA methylation. To perform this task, we used an epigenetic locus that targets a tissue-specific differentially methylated region for semen. This specific locus, ZC3H12D, contains methylated CpG sites that are hypomethylated in semen and hypermethylated in blood and saliva. Using this procedure, DNA from forensic stains can be isolated, processed using bisulfite-modified polymerase chain reaction (PCR), and detected by real-time PCR with HRM capability. The method described in this article is robust; we were able to obtain results from samples with as little as 1 ng of genomic DNA. Samples inhibited by humic acid still produced reliable results. Furthermore, the procedure is specific and will not amplify non-bisulfite-modified DNA. Because this process can be performed using real-time PCR and is quantitative, it fits nicely within the workflow of current forensic DNA laboratories. As a result, it should prove to be a useful technique for processing trace evidence samples for serological analysis.

  8. DNMT3B isoforms without catalytic activity stimulate gene body methylation as accessory proteins in somatic cells.

    Science.gov (United States)

    Duymich, Christopher E; Charlet, Jessica; Yang, Xiaojing; Jones, Peter A; Liang, Gangning

    2016-04-28

    Promoter DNA methylation is a key epigenetic mechanism for stable gene silencing, but is correlated with expression when located in gene bodies. Maintenance and de novo DNA methylation by catalytically active DNA methyltransferases (DNMT1 and DNMT3A/B) require accessory proteins such as UHRF1 and DNMT3L. DNMT3B isoforms are widely expressed, although some do not have active catalytic domains and their expression can be altered during cell development and tumourigenesis, questioning their biological roles. Here, we show that DNMT3B isoforms stimulate gene body methylation and re-methylation after methylation-inhibitor treatment. This occurs independently of the isoforms' catalytic activity, demonstrating a similar functional role to the accessory protein DNMT3L, which is only expressed in undifferentiated cells and recruits DNMT3A to initiate DNA methylation. This unexpected role for DNMT3B suggests that it might substitute for the absent accessory protein DNMT3L to recruit DNMT3A in somatic cells.

  9. Spectroscopic (FT-IR, FT-Raman, UV, 1H and 13C NMR) profiling and computational studies on methyl 5-methoxy-1H-indole-2-carboxylate: A potential precursor to biologically active molecules

    Science.gov (United States)

    Almutairi, Maha S.; Xavier, S.; Sathish, M.; Ghabbour, Hazem A.; Sebastian, S.; Periandy, S.; Al-Wabli, Reem I.; Attia, Mohamed I.

    2017-04-01

    Methyl 5-methoxy-1H-indole-2-carboxylate (MMIC) was prepared via esterification of commercially available 5-methoxyindole-2-carboxylic acid. The title molecule MMIC was characterised using FT-IR and FT-Raman in the ranges of 4000-500 and 4000-50 cm-1, respectively. The fundamental modes of the vibrations were assigned and the UV-visible spectrum of the MMIC molecule was recorded in the range of 200-400 nm to explore its electronic nature. The HOMO-LUMO energy distribution was calculated and the bonding and anti-bonding structures of the title molecule were studied and analysed using the natural bond orbital (NBO) approach. The reactivity of the MMIC molecule was also investigated and both the positive and negative centres of the molecule were identified using chemical descriptors and molecular electrostatic potential (MEP) analysis. The chemical shifts of the 1H and 13C NMR spectra were noted and the magnetic field environment of the MMIC molecule are discussed. The non-linear optical (NLO) properties of the title molecule were studied based on its calculated values of polarisability and hyperpolarisability. All computations were obtained by DFT methods using the 6-311++G (d,p) basis set.

  10. Degradation of aqueous methyl tert-butyl ether by photochemical, biological, and their combined processes

    Directory of Open Access Journals (Sweden)

    Azadeh Asadi

    2006-01-01

    Full Text Available The degradation of aqueous methyl tert-butyl ether (MTBE at relatively high concentrations was investigated by various photo-induced oxidation processes such as UV/H2O2 and UV/TiO2 as well as biological processes and their combination. It was shown that the degradation of MTBE by UV/H2O2 and TiO2 photocatalytic followed a first-order model with apparent rate constant of 1.31×10−1 and 1.21×10−2 min-1, respectively. It was observed that UV/H2O2/TiO2 process did not have any advantages over each of the other processes alone. The biodegradation of methyl tert-butyl ether (MTBE was evaluated using aerobic mixed culture with three different approaches, including ultimate biological oxygen demand (BODU assessment, nonacclimated, and acclimated mixed cultures. The apparent rate constant for the biodegradation of MTBE by nonacclimated mixed culture was 4.36×10−2 day-1. It was shown that the acclimatization of the mixed cultures enhanced the rate of biodegradation of MTBE to 3.24×10−1mg L-1h-1. Finally, the effects of the photocatalytic pretreatment of aqueous MTBE on its subsequent biological treatment were studied. It was observed that the rate of bioreaction was not enhanced and the photocatalytic pretreatment had adverse effects on its biological treatment so that the apparent rate constant decreased to 2.83×10−1 mg L-1h-1.

  11. Sphaeropsidones, phytotoxic dimedone methyl ethers produced by Diplodia cupressi: a structure-activity relationship study.

    Science.gov (United States)

    Evidente, Antonio; Maddau, Lucia; Scanu, Bruno; Andolfi, Anna; Masi, Marco; Motta, Andrea; Tuzi, Angela

    2011-04-25

    Sphaeropsidone and episphaeropsidone are two phytotoxic dimedone methyl ethers produced by Diplodia cupressi, the causal agent of a canker disease of cypress in the Mediterranean area. In this study, eight derivatives obtained by chemical modifications and two natural analogues were assayed for phytotoxic and antifungal activities, and a structure-activity relationship was examined. Each compound was tested on nonhost plants and on five fungal pathogenic species belonging to the genus Phytophthora. The results provide insights into structure-activity relationships within these compounds. It was found that the hydroxy group at C-5, the absolute C-5 configuration, the epoxy group, and the C-2 carbonyl group appear to be structural features important in conferring biological activity. The conversion of sphaeropsidone into the corresponding 1,4-dione derivative led to a compound showing greater antifungal activity than its precursor. This finding could be useful in devising new natural fungicides for practical application in agriculture.

  12. Synthesis,Crystal Structure and Biological Activities of O,O-Dialkyl α-[1-(2-Chlorothiazol-5-ylmethyl)-5-methyl1H-1,2,3-triazol-4-ylcarbonyloxy]alkylphosphonates

    Institute of Scientific and Technical Information of China (English)

    CHEN Xiao-Bao; SHI De-Qing; ZHU Xiao-Fei

    2007-01-01

    In order to search for novel agrochemicals with high activity and low toxicity,a series of phosphonate derivatives containing 1,2,3-triazole and thiazole rings were designed and synthesized using 2-chloro-5-(chloromethyl)thiazole as the starting material.Their structures were confirmed by IR,1H NMR,31P NMR,EI-MS or ESI-MS and elemental analyses.The crystal structure of 7a was determined by single crystal X-ray diffraction.Prelimihary bioassays indicated that most of the target compounds did not display insecticidal activities,but a fraction of them possessed herbicidal and fungicidal activities to some extent.

  13. Syntheses, Structure and Biological Activities of 2-(1H-Benzo[1,2,3]triazole-1-yl)-1-(3-methyl-4-bromobiphenyl)-2-( 1H-1,2,4-triazole-1-yl) ethanone

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    @@ Introduction 1,2,4-Triazole derivatives represent an interesting class of heterocyclic compounds[1] and have become the most rapidly expanding group of antifungal compoundswith the advantages of toxicity, high oral bioavailability, and broad spectrum of activity against several fungi, including most yeasts and folanentous fungi[2-4].

  14. Evaluation of larvicidal activity and ecotoxicity of linalool, methyl cinnamate and methyl cinnamate/linalool in combination against Aedes aegypti.

    Science.gov (United States)

    Fujiwara, Gislene M; Annies, Vinícius; de Oliveira, Camila F; Lara, Ricardo A; Gabriel, Maria M; Betim, Fernando C M; Nadal, Jéssica M; Farago, Paulo V; Dias, Josiane F G; Miguel, Obdulio G; Miguel, Marilis D; Marques, Francisco A; Zanin, Sandra M W

    2017-05-01

    The frequent use of synthetic pesticides to control Aedes aegypti population can lead to environmental and/or human contamination and the emergence of resistant insects. Linalool and methyl cinnamate are presented as an alternative to the synthetic pesticides, since they can exhibit larvicidal, repellent and/or insecticidal activity and are considered safe for use. The aim of this study was to evaluate the larvicidal activity of methyl cinnamate, linalool and methyl cinnamate/linalool in combination (MC-L) (1:4 ratio, respectively) against Aedes aegypti. The in vitro preliminary toxicity through brine shrimp lethality assay and hemolytic activity, and the phytotoxic potential were also investigated to assess the safety of their use as larvicide. Methyl cinnamate showed significant larvicidal activity when compared to linalool (LC50 values of 35.4µg/mL and 275.2µg/mL, respectively) and to MC-L (LC50 138.0µg/mL). Larvae morphological changes subjected to the specified treatments were observed, as the flooding of tracheal system and midgut damage, hindering the larval development and survival. Preliminary in vitro toxicity through brine shrimp showed the high bioactivity of the substances (methyl cinnamate LC50 35.5µg/mL; linalool LC50 96.1µg/mL) and the mixture (MC-L LC50 57.7µg/mL). The results showed that, despite the higher larvicidal activity of methyl cinnamate, the use of MC-L as a larvicide seems to be more appropriate due to its significant larvicidal activity and low toxicity.

  15. DNA methylation fingerprint of neuroblastoma reveals new biological and clinical insights

    Science.gov (United States)

    Gómez, Soledad; Castellano, Giancarlo; Mayol, Gemma; Queiros, Ana; Martín-Subero, José I.; Lavarino, Cinzia

    2015-01-01

    Neuroblastoma (NB) is one of the most frequently occurring extracranial solid tumors of childhood (Maris et al., 2007 [1]; Brodeur, 2003 [2]). Probability of cure varies according to patient's age, extent of disease and tumor biology (Maris et al., 2007 [1]; Brodeur, 2003 [2]; Cohn et al., 2009 [3]). However, the etiology of this developmental tumor is unknown. Recent evidence has shown that pediatric solid tumors, including NB, harbor a paucity of recurrent genetic mutations, with a significant proportion of recurrent events converging on epigenetic mechanisms (Cheung et al., 2012 [4]; Molenaar et al., 2012 [5]; Pugh et al., 2013 [6]; Sausen et al., 2013 [7]. We have analyzed the DNA methylome of neuroblastoma using high-density microarrays (Infinium Human Methylation 450k BeadChip) to define the epigenetic landscape of this pediatric tumor and its potential clinicopathological impact. Here, we provide the detail of methods and quality control parameters of the microarray data used for the study. Methylation data has been deposited at NCBI Gene Expression Omnibus data repository, accession number GSE54719; superseries record GSE54721. PMID:26484286

  16. Biological activity of liposomal vanillin.

    Science.gov (United States)

    Castan, Leniher; Del Toro, Grisel; Fernández, Adolfo A; González, Manuel; Ortíz, Emilia; Lobo, Daliana

    2013-06-01

    This article presents a study of vanillin encapsulation inside multilamellar liposomes, with emphasis on the evaluation of antioxidant activity, the hemolytic effect, and the antisickling properties of these products. Egg phosphatidylcholine-cholesterol and egg phosphatidylcholine-cholesterol-1-O-decylglycerol liposomes were prepared by mechanical dispersion, all with vanillin included. Vesicles were characterized by determination of encapsulation efficiency and vanillin retention capacity. Antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. The hemolytic effect of liposomes was also evaluated by spectrophotometry, as well as the antisickling activity by the Huck test using optical microscopy. Results showed that the lipid composition of liposomes did not significantly affect the encapsulation efficiency. Stable vesicles were obtained with a high retention percentage of vanillin. Liposomes exhibited a high capture of the DPPH radical compared to free vanillin and 1-O-decylglycerol (C10) in solution. Vesicles caused no significant hemolisys in normal erythrocytes, nor in those coming from patients with sickle cell anemia. Vanillin encapsulated in liposomes retained its antisickling activity, with a greater effect for C10-containing vesicles. Our results show that vanillin encapsulation in liposomes is a way to enhance the pharmacologic properties of this molecule using a suitable vehicle.

  17. Potentiation of insulin release in response to amino acid methyl esters correlates to activation of islet glutamate dehydrogenase activity

    DEFF Research Database (Denmark)

    Kofod, Hans; Lernmark, A; Hedeskov, C J

    1986-01-01

    Column perifusion of mouse pancreatic islets was used to study the ability of amino acids and their methyl esters to influence insulin release and activate islet glutamate dehydrogenase activity. In the absence of L-glutamine, L-serine and the methyl ester of L-phenylalanine, but neither L...... glutamate dehydrogenase activity showed that only the two methyl esters of L-phenylalanine and L-serine activated the enzyme. It is concluded that the mechanism by which methyl esters of amino acids potentiate insulin release is most likely to be mediated by the activation of pancreatic beta-cell glutamate...

  18. Biologically active sesquiterpene coumarins from Ferula species.

    Science.gov (United States)

    Nazari, Zeinab Esmail; Iranshahi, Mehrdad

    2011-03-01

    Extracts from different species of the genus Ferula (Apiaceae) have had various biomedical applications for many centuries. Many biological features of this genus such as cytotoxicity, antibacterial, antiviral, P-glycoprotein (P-gp) inhibitory and antiinflammatory activity have been attributed to sesquiterpene coumarins; structures containing a common coumarin group and a sesquiterpene moiety. This both highlights the importance of sesquiterpene coumarins as biologically active natural products and necessitates further studies on these compounds. Taking into account the versatile biological properties of compounds isolated from Ferula and the unprecedented interest in the application of natural products as a new generation of therapeutics, the present review will discuss reports on biological activities of sesquiterpene coumarins of the genus Ferula, from 1990 onwards.

  19. Marine Pyridoacridine Alkaloids: Biosynthesis and Biological Activities.

    Science.gov (United States)

    Ibrahim, Sabrin R M; Mohamed, Gamal A

    2016-01-01

    Pyridoacridines are a class of strictly marine-derived alkaloids that constitute one of the largest chemical families of marine alkaloids. During the last few years, both natural pyridoacridines and their analogues have constituted excellent targets for synthetic works. They have been the subject of intense study due to their significant biological activities; cytotoxic, antibacterial, antifungal, antiviral, insecticidal, anti-HIV, and anti-parasitic activities. In the present review, 95 pyridoacridine alkaloids isolated from marine organisms are discussed in term of their occurrence, biosynthesis, biological activities, and structural assignment.

  20. Marine Biology Activities. Ocean Related Curriculum Activities.

    Science.gov (United States)

    Pauls, John

    The ocean affects all of our lives. Therefore, awareness of and information about the interconnections between humans and oceans are prerequisites to making sound decisions for the future. Project ORCA (Ocean Related Curriculum Activities) has developed interdisciplinary curriculum materials designed to meet the needs of students and teachers…

  1. Biological activity of acetylated phenolic compounds.

    Science.gov (United States)

    Fragopoulou, Elizabeth; Nomikos, Tzortzis; Karantonis, Haralabos C; Apostolakis, Constantinos; Pliakis, Emmanuel; Samiotaki, Martina; Panayotou, George; Antonopoulou, Smaragdi

    2007-01-10

    In recent years an effort has been made to isolate and identify biologically active compounds that are included in the Mediterranean diet. The existence of naturally occurring acetylated phenolics, as well as studies with synthetic ones, provide evidence that acetyl groups could be correlated with their biological activity. Platelet activating factor (PAF) is implicated in atherosclerosis, whereas its inhibitors seem to play a protective role against cardiovascular disease. The aim of this study was to examine the biological activity of resveratrol and tyrosol and their acetylated derivatives as inhibitors of PAF-induced washed rabbit platelet aggregation. Acetylation of resveratrol and tyrosol was performed, and separation was achieved by HPLC. Acetylated derivatives were identified by negative mass spectrometry. The data showed that tyrosol and its monoacetylated derivatives act as PAF inhibitors, whereas diacetylated derivatives induce platelet aggregation. Resveratrol and its mono- and triacetylated derivatives exert similar inhibitory activity, whereas the diacetylated ones are more potent inhibitors. In conclusion, acetylated phenolics exert the same or even higher antithrombotic activity compared to the biological activity of the initial one.

  2. Late-stage functionalization of biologically active heterocycles through photoredox catalysis.

    Science.gov (United States)

    Dirocco, Daniel A; Dykstra, Kevin; Krska, Shane; Vachal, Petr; Conway, Donald V; Tudge, Matthew

    2014-05-05

    The direct CH functionalization of heterocycles has become an increasingly valuable tool in modern drug discovery. However, the introduction of small alkyl groups, such as methyl, by this method has not been realized in the context of complex molecule synthesis since existing methods rely on the use of strong oxidants and elevated temperatures to generate the requisite radical species. Herein, we report the use of stable organic peroxides activated by visible-light photoredox catalysis to achieve the direct methyl-, ethyl-, and cyclopropylation of a variety of biologically active heterocycles. The simple protocol, mild reaction conditions, and unique tolerability of this method make it an important tool for drug discovery.

  3. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    Cédric Charrier; Joëlle Roche; Jean-Pierre Gesson; Philippe Bertrand

    2009-07-01

    New substituted trichostatic acid derivatives have been synthesized and evaluated for their biological activities towards the H661 non-small lung cancer cell line. These syntheses were achieved by alkylation of propiophenones to introduce the side chain with a terminal precursor of hydroxamic acid and aminobenzamide derivatives. The first fluorinated derivatives of trichostatic acid are described, such as 6-fluoro trichostatin A, with antiproliferative activities in the micromolar range and with histone deacetylase inhibitory activity.

  4. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112.

    Science.gov (United States)

    Chen, Liwei; Pernazza, Daniele; Scott, Latanya M; Lawrence, Harshani R; Ren, Yuan; Luo, Yunting; Wu, Xin; Sung, Shen-Shu; Guida, Wayne C; Sebti, Said M; Lawrence, Nicholas J; Wu, Jie

    2010-09-15

    The protein tyrosine phosphatase (PTP) Shp2 (PTPN11) is an attractive target for anticancer drug discovery because it mediates growth factor signaling and its gain-of-function mutants are causally linked to leukemias. We previously synthesized SPI-112 from a lead compound of Shp2 inhibitor, NSC-117199. In this study, we demonstrated that SPI-112 bound to Shp2 by surface plasmon resonance (SPR) and displayed competitive inhibitor kinetics to Shp2. Like some other compounds in the PTP inhibitor discovery efforts, SPI-112 was not cell permeable, precluding its use in biological studies. To overcome the cell permeation issue, we prepared a methyl ester SPI-112 analog (SPI-112Me) that is predicted to be hydrolyzed to SPI-112 upon entry into cells. Fluorescence uptake assay and confocal imaging suggested that SPI-112Me was taken up by cells. Incubation of cells with SPI-112Me inhibited epidermal growth factor (EGF)-stimulated Shp2 PTP activity and Shp2-mediated paxillin dephosphorylation, Erk1/2 activation, and cell migration. SPI-112Me treatment also inhibited Erk1/2 activation by a Gab1-Shp2 chimera. Treatment of Shp2(E76K) mutant-transformed TF-1 myeloid cells with SPI-112Me resulted in inhibition of Shp2(E76K)-dependent cell survival, which is associated with inhibition of Shp2(E76K) PTP activity, Shp2(E76K)-induced Erk1/2 activation, and Bcl-XL expression. Furthermore, SPI-112Me enhanced interferon-gamma (IFN-gamma)-stimulated STAT1 tyrosine phosphorylation, ISRE-luciferase reporter activity, p21 expression, and the anti-proliferative effect. Thus, the SPI-112 methyl ester analog was able to inhibit cellular Shp2 PTP activity.

  5. Biologically active secondary metabolites from Asphodelus microcarpus.

    Science.gov (United States)

    Ghoneim, Mohammed M; Ma, Guoyi; El-Hela, Atef A; Mohammad, Abd-Elsalam I; Kottob, Saeid; El-Ghaly, Sayed; Cutler, Stephen J; Ross, Samir A

    2013-08-01

    Bioassay guided fractionation of the ethanolic extract of Asphodelus microcarpus Salzm.et Vivi (Asphodelaceae) resulted in the isolation of one new metabolite, 1,6-dimethoxy-3-methyl-2-naphthoic acid (1) as well as nine known compounds: asphodelin (2), chrysophanol (3), 8-methoxychrysophanol (4), emodin (5), 2-acetyl-1,8-dimethoxy-3-methylnaphthalene (6), 10-(chrysophanol-7'-yl)-10-hydroxychrysophanol-9-anthrone (7), aloesaponol-III-8-methyl ether (8), ramosin (9) and aestivin (10). The compounds were identified by 1D and 2D NMR and HRESIMS. Compounds 3, 6 and 10 were isolated for the first time from this species. Compounds 3 and 4 showed moderate to weak antileishmanial activity with IC50 values of 14.3 and 35.1 microg/mL, respectively. Compound 4 exhibited moderate antifungal activity against Cryptococcus neoformans with an IC50 value of 15.0 microg/mL, while compounds 5, 7 and 10 showed good to potent activity against methicillin resistant Staphylococcus aureus (MRSA) with IC50 values of 6.6, 9.4 microg/mL and 1.4 microg/mL respectively. Compounds 5, 8 and 9 displayed good activity against S. aureus with IC50 values of 3.2, 7.3 and 8.5 microg/mL, respectively. Compounds 7 and 9 exhibited a potent cytotoxic activity against leukemia LH60 and K562 cell lines. Compound 10 showed potent antimalarial activities against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum with IC50 values in the range of 0.8-0.7 microg/mL without showing any cytotoxicity to mammalian cells.

  6. Reactions of 3-Formylchromone with Active Methylene and Methyl Compounds and Some Subsequent Reactions of the Resulting Condensation Products

    Directory of Open Access Journals (Sweden)

    M. Lácova

    2005-08-01

    Full Text Available This review presents a survey of the condensations of 3-formylchromone with various active methylene and methyl compounds, e.g. malonic or barbituric acid derivatives, five-membered heterocycles, etc. The utilisation of the condensation products for the synthesis of different heterocyclic systems, which is based on the ability of the γ-pyrone ring to be opened by the nucleophilic attack is also reviewed. Finally, the applications of microwave irradiation as an unconventional method of reaction activation in the synthesis of condensation products is described and the biological activity of some chromone derivatives is noted.

  7. Microbial and enzymatic activity of soil contaminated with a mixture of diflufenican + mesosulfuron-methyl + iodosulfuron-methyl-sodium.

    Science.gov (United States)

    Baćmaga, Małgorzata; Borowik, Agata; Kucharski, Jan; Tomkiel, Monika; Wyszkowska, Jadwiga

    2015-01-01

    The aim of this study was to determine the effect of three active substances, diflufenican, mesosulfuron-methyl and iodosulfuron-methyl-sodium, applied in combination, on soil microbial counts, the structure of soil microbial communities, activity of soil enzymes and their resistance to the tested product, the biochemical indicator of soil fertility, and spring wheat yield. Soil samples with the granulometric composition of sandy loam with pHKCl 7.0 were used in a pot experiment. The herbicide was applied to soil at seven doses: 0.057 (dose recommended by the manufacturer), 1.140, 2.280, 4.560, 9.120, 18.240 and 36.480 mg kg(-1) soil DM. Uncontaminated soil served as the control treatment. It was found that a mixture of the tested active substances increased the counts of total oligotrophic bacteria and spore-forming oligotrophic bacteria, organotrophic bacteria and actinomycetes, decreased the counts of Azotobacter and fungi, and modified the structure of soil microbial communities. The highest values of the colony development (CD) index and the ecophysiological (EP) index were observed in fungi and organotrophic bacteria, respectively. The herbicide applied in the recommended dose stimulated the activity of catalase, urease and acid phosphatase, but it had no effect on the activity of dehydrogenases, alkaline phosphatase, arylsulfatase and β-glucosidase. The highest dose of the analyzed substances (36.480 mg kg(-1)) significantly inhibited the activity of dehydrogenases, acid phosphatase, alkaline phosphatase and arylsulfatase. The values of the biochemical soil fertility indicator (BA21) decreased in response to high doses of the herbicide. Urease was most resistant and dehydrogenases were least resistant to soil contamination with a mixture of diflufenican + mesosulfuron-methyl + iodosulfuron-methyl-sodium. The analyzed herbicide had an adverse influence on spring wheat yield, and doses of 18.240 and 36.480 mg kg(-1) led to eventual death of plants.

  8. DNA methylation-based measures of biological age: meta-analysis predicting time to death

    Science.gov (United States)

    Chen, Brian H.; Marioni, Riccardo E.; Colicino, Elena; Peters, Marjolein J.; Ward-Caviness, Cavin K.; Tsai, Pei-Chien; Roetker, Nicholas S.; Just, Allan C.; Demerath, Ellen W.; Guan, Weihua; Bressler, Jan; Fornage, Myriam; Studenski, Stephanie; Vandiver, Amy R.; Moore, Ann Zenobia; Tanaka, Toshiko; Kiel, Douglas P.; Liang, Liming; Vokonas, Pantel; Schwartz, Joel; Lunetta, Kathryn L.; Murabito, Joanne M.; Bandinelli, Stefania; Hernandez, Dena G.; Melzer, David; Nalls, Michael; Pilling, Luke C.; Price, Timothy R.; Singleton, Andrew B.; Gieger, Christian; Holle, Rolf; Kretschmer, Anja; Kronenberg, Florian; Kunze, Sonja; Linseisen, Jakob; Meisinger, Christine; Rathmann, Wolfgang; Waldenberger, Melanie; Visscher, Peter M.; Shah, Sonia; Wray, Naomi R.; McRae, Allan F.; Franco, Oscar H.; Hofman, Albert; Uitterlinden, André G.; Absher, Devin; Assimes, Themistocles; Levine, Morgan E.; Lu, Ake T.; Tsao, Philip S.; Hou, Lifang; Manson, JoAnn E.; Carty, Cara L.; LaCroix, Andrea Z.; Reiner, Alexander P.; Spector, Tim D.; Feinberg, Andrew P.; Levy, Daniel; Baccarelli, Andrea; van Meurs, Joyce; Bell, Jordana T.; Peters, Annette; Deary, Ian J.; Pankow, James S.; Ferrucci, Luigi; Horvath, Steve

    2016-01-01

    Estimates of biological age based on DNA methylation patterns, often referred to as “epigenetic age”, “DNAm age”, have been shown to be robust biomarkers of age in humans. We previously demonstrated that independent of chronological age, epigenetic age assessed in blood predicted all-cause mortality in four human cohorts. Here, we expanded our original observation to 13 different cohorts for a total sample size of 13,089 individuals, including three racial/ethnic groups. In addition, we examined whether incorporating information on blood cell composition into the epigenetic age metrics improves their predictive power for mortality. All considered measures of epigenetic age acceleration were predictive of mortality (p≤8.2×10−9), independent of chronological age, even after adjusting for additional risk factors (p<5.4×10−4), and within the racial/ethnic groups that we examined (non-Hispanic whites, Hispanics, African Americans). Epigenetic age estimates that incorporated information on blood cell composition led to the smallest p-values for time to death (p=7.5×10−43). Overall, this study a) strengthens the evidence that epigenetic age predicts all-cause mortality above and beyond chronological age and traditional risk factors, and b) demonstrates that epigenetic age estimates that incorporate information on blood cell counts lead to highly significant associations with all-cause mortality. PMID:27690265

  9. Biologically Active Substances from Higher Fungi

    Institute of Scientific and Technical Information of China (English)

    Liu Jikai

    2007-01-01

    As a part of our search for naturally occurring bioactive metabolites of mushrooms, we have investigated the chemical constituents of more than 100 Basidiomycetes and Ascomycetes fungi, and isolated over 300 including 150 new terpenoids,phenolics and nitrogen-containing compounds. The isolation, structural elucidation and biologically activity of the natural products from the higher fungi are briefly discussed.

  10. Biological activities of Curcuma longa L.

    OpenAIRE

    Araújo CAC; LL Leon

    2001-01-01

    There are several data in the literature indicating a great variety of pharmacological activities of Curcuma longa L. (Zingiberaceae), which exhibit anti-inflammatory, anti-human immunodeficiency virus, anti-bacteria, antioxidant effects and nematocidal activities. Curcumin is a major component in Curcuma longa L., being responsible for its biological actions. Other extracts of this plant has been showing potency too. In vitro, curcumin exhibits anti-parasitic, antispasmodic, anti-inflammator...

  11. DAGESTAN HAWTHORN - A VALUABLE SOURCE OF BIOLOGICALLY ACTIVE SUBSTANCES

    Directory of Open Access Journals (Sweden)

    Omarieva L. V.

    2016-02-01

    Full Text Available The article deals with hawthorn Dagestan. It is noted that the more than 100 species are found 14 species in Dagestan. The most common of them are studied as a source of biologically active substances and nutrients, and they can be used as food additives for various purposes. The content of biologically active substances and nutrients are defined. The high content of phenolic substances in C. pentagyna Waldst. et Kit, which play an important role in the formation of immunity and possessing P-vitamin activity is defined. Amino acid and fatty acid composition of the fruit of the hawthorn Crataegus pentagyna Waldst. et Kit, as the most valuable for using as food additives is defined by ionexchange and gas-liquid chromatography. Sixteen amino acids were identified and quantified in the protein component of hawthorn fruit. The high content of essential amino acids such as lysine, threonine, valine, methionine, leucine, isoleucine, phenylalanine. The amount of essential amino acids is 296.1 mg / 100 g. Chromatographic separation of fatty acid methyl esters has enabled us to establish the presence of the following fatty acids: palmitic, oleic, stearic, linoleic and linolenic, including established the presence of essential fatty acids - the family of alpha-linolenic acid OMEGA -3 and linoleic acid family of OMEGA -6

  12. Stereoselective Syntheses and Biological Properties of (E)-α-(Methoxyimino)-2-[1-(aryloxy)methyl]-benzeneacetates

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    (E)-α-(Methoxyimino)-2-[1-(aryloxy)methyl]-benzeneacetates, the analogues of Kresoxim-methyl, were stereoselectively synthesized with the coupling reaction of 2-methylphenyldiazonium chloride and methyl 2-hydroxyiminoacetate in the presence of CuSO4/Na2SO3 as a key step, and it was first found that the coupling reaction could give the key intermediate material(E)- and(Z)-methyl 2-(hydroxyimino)-2-o-tolylacetate with a molar ratio of 14∶1. The(E)-configurations of all these compounds were assigned on the basis of their 2D-NOESY spectra of 1H NMR. The preliminary bioassays indicate that most of the compounds show an activity against a wide variety of fungi.

  13. Loranthus micranthus Linn.: Biological Activities and Phytochemistry

    Directory of Open Access Journals (Sweden)

    Soheil Zorofchian Moghadamtousi

    2013-01-01

    Full Text Available Loranthus micranthus Linn. is a medicinal plant from the Loranthaceae family commonly known as an eastern Nigeria species of the African mistletoe and is widely used in folkloric medicine to cure various ailments and diseases. It is semiparasitic plant because of growing on various host trees and shrubs and absorbing mineral nutrition and water from respective host. Hence, the phytochemicals and biological activities of L. micranthus demonstrated strong host and harvesting period dependency. The leaves have been proved to possess immunomodulatory, antidiabetic, antimicrobial, antihypertensive, antioxidant, antidiarrhoeal, and hypolipidemic activities. This review summarizes the information and findings concerning the current knowledge on the biological activities, pharmacological properties, toxicity, and chemical constituents of Loranthus micranthus.

  14. Biologically active substances of stone crop fruits

    Directory of Open Access Journals (Sweden)

    Margarita Makarkina

    2014-04-01

    Full Text Available Stone fruit crops are successfully cultivated in many regions of Russia. Their fruits contain a great diversity of biologically active and mineral substances. The stone fruit varietal collection of the All Russia Research Institute of Fruit Crop Breeding has been estimated on the content of biologically active substances (ascorbic acid and phenolic compounds in fruits: 80 sour cherry varieties, 28 sweet cherry varieties, 29 plum varieties and 24 apricot varieties. High cultivar variability of the content of ascorbic acid and P-active sub-stances in fruits has been determined in each crop. The best genotypes have been singled out according to each biochemical component and a complex of characters.

  15. Glycosides from Marine Sponges (Porifera, Demospongiae: Structures, Taxonomical Distribution, Biological Activities and Biological Roles

    Directory of Open Access Journals (Sweden)

    Valentin A. Stonik

    2012-08-01

    Full Text Available Literature data about glycosides from sponges (Porifera, Demospongiae are reviewed. Structural diversity, biological activities, taxonomic distribution and biological functions of these natural products are discussed.

  16. Glycosides from marine sponges (Porifera, Demospongiae): structures, taxonomical distribution, biological activities and biological roles.

    Science.gov (United States)

    Kalinin, Vladimir I; Ivanchina, Natalia V; Krasokhin, Vladimir B; Makarieva, Tatyana N; Stonik, Valentin A

    2012-08-01

    Literature data about glycosides from sponges (Porifera, Demospongiae) are reviewed. Structural diversity, biological activities, taxonomic distribution and biological functions of these natural products are discussed.

  17. Using synthetic biology to increase nitrogenase activity

    OpenAIRE

    Li, Xin-Xin; Liu, Qi; Liu, Xiao-Meng; Shi, Hao-Wen; Chen, San-feng

    2016-01-01

    Background Nitrogen fixation has been established in protokaryotic model Escherichia coli by transferring a minimal nif gene cluster composed of 9 genes (nifB, nifH, nifD, nifK, nifE, nifN, nifX, hesA and nifV) from Paenibacillus sp. WLY78. However, the nitrogenase activity in the recombinant E. coli 78-7 is only 10 % of that observed in wild-type Paenibacillus. Thus, it is necessary to increase nitrogenase activity through synthetic biology. Results In order to increase nitrogenase activity ...

  18. Estrogenic flavonoids: structural requirements for biological activity.

    Science.gov (United States)

    Miksicek, R J

    1995-01-01

    A systematic survey of polycyclic phenols has been performed to identify members of this chemical group with estrogenic activity. Twelve compounds were found to be able to stimulate the transcriptional activity of the human estrogen receptor expressed in cultured cells by transient transfection. These natural estrogens belong to several distinct, but chemically related classes including chalcones, flavanones, flavones, flavonols, and isoflavones. Selected examples of estrogenic flavonoids were further analyzed to determine their biological potencies and their relative affinities for binding to the estrogen receptor. These data are interpreted with respect to the molecular structure of polycyclic phenols required for hormonal activity as nonsteroidal estrogens.

  19. A methylation-stimulated DNA machine: an autonomous isothermal route to methyltransferase activity and inhibition analysis.

    Science.gov (United States)

    Zhu, Changfeng; Wen, Yanqin; Peng, Hongzhen; Long, Yitao; He, Yao; Huang, Qing; Li, Di; Fan, Chunhai

    2011-04-01

    The operation of DNA nanomachines is generally triggered by either conformational changes of DNA nanostructure or external environmental stimuli. In the present study, we demonstrate an alternative driving force, DNA methylation, to stimulate DNA machine operation. DNA methylation changes neither DNA sequence and conformation nor external environment, however, blocks its cleavage by corresponding methylation-sensitive restriction endonuclease. We thus designed a strand displacement amplification DNA machine, which could be stimulated upon DNA methylation and then autonomously generates accumulated amounts of peroxidase-mimicking DNAzyme signaling machine products in an isothermal manner. The machine product DNAzyme could catalyze the H(2)O(2)-mediated oxidation of 2,2'-azino-bis(3-ethylbenzo thiazoline-6-sulfonic acid) (ABTS(2-)) to a colored product ABTS(·-). This methylation-stimulated DNA machine was further used as a colorimetric assay for analysis of methyltransferases activities and screening of methylation inhibitors. As compared with classical methylation assay, this facile isothermal DNA machine avoids the introduction of methylation-specific polymerase chain reaction and radioactive labels, which might be employed as an effective tool for DNA methylation analysis.

  20. A DNA methylation-based definition of biologically distinct breast cancer subtypes.

    Science.gov (United States)

    Stefansson, Olafur A; Moran, Sebastian; Gomez, Antonio; Sayols, Sergi; Arribas-Jorba, Carlos; Sandoval, Juan; Hilmarsdottir, Holmfridur; Olafsdottir, Elinborg; Tryggvadottir, Laufey; Jonasson, Jon G; Eyfjord, Jorunn; Esteller, Manel

    2015-03-01

    In cancer, epigenetic states are deregulated and thought to be of significance in cancer development and progression. We explored DNA methylation-based signatures in association with breast cancer subtypes to assess their impact on clinical presentation and patient prognosis. DNA methylation was analyzed using Infinium 450K arrays in 40 tumors and 17 normal breast samples, together with DNA copy number changes and subtype-specific markers by tissue microarrays. The identified methylation signatures were validated against a cohort of 212 tumors annotated for breast cancer subtypes by the PAM50 method (The Cancer Genome Atlas). Selected markers were pyrosequenced in an independent validation cohort of 310 tumors and analyzed with respect to survival, clinical stage and grade. The results demonstrate that DNA methylation patterns linked to the luminal-B subtype are characterized by CpG island promoter methylation events. In contrast, a large fraction of basal-like tumors are characterized by hypomethylation events occurring within the gene body. Based on these hallmark signatures, we defined two DNA methylation-based subtypes, Epi-LumB and Epi-Basal, and show that they are associated with unfavorable clinical parameters and reduced survival. Our data show that distinct mechanisms leading to changes in CpG methylation states are operative in different breast cancer subtypes. Importantly, we show that a few selected proxy markers can be used to detect the distinct DNA methylation-based subtypes thereby providing valuable information on disease prognosis.

  1. Isoflavones: estrogenic activity, biological effect and bioavailability.

    Science.gov (United States)

    Vitale, Daniela Cristina; Piazza, Cateno; Melilli, Barbara; Drago, Filippo; Salomone, Salvatore

    2013-03-01

    Isoflavones are phytoestrogens with potent estrogenic activity; genistein, daidzein and glycitein are the most active isoflavones found in soy beans. Phytoestrogens have similarity in structure with the human female hormone 17-β-estradiol, which can bind to both alpha and beta estrogen receptors, and mimic the action of estrogens on target organs, thereby exerting many health benefits when used in some hormone-dependent diseases. Numerous clinical studies claim benefits of genistein and daidzein in chemoprevention of breast and prostate cancer, cardiovascular disease and osteoporosis as well as in relieving postmenopausal symptoms. The ability of isoflavones to prevent cancer and other chronic diseases largely depends on pharmacokinetic properties of these compounds, in particular absorption and distribution to the target tissue. The chemical form in which isoflavones occur is important because it influences their bioavailability and, therefore, their biological activity. Glucose-conjugated isoflavones are highly polar, water-soluble compounds. They are hardly absorbed by the intestinal epithelium and have weaker biological activities than the corresponding aglycone. Different microbial families of colon can transform glycosylated isoflavones into aglycones. Clinical studies show important differences between the aglycone and conjugated forms of genistein and daidzein. The evaluation of isoflavone metabolism and bioavailability is crucial to understanding their biological effects. Lipid-based formulations such as drug incorporation into oils, emulsions and self-microemulsifying formulations have been introduced to increase bioavailability. Complexation with cyclodextrin also represent a valid method to improve the physicochemical characteristics of these substances in order to be absorbed and distributed to target tissues. We review and discuss pharmacokinetic issues that critically influence the biological activity of isoflavones.

  2. The mechanism of methylated seed oil on enhancing biological efficacy of topramezone on weeds.

    Science.gov (United States)

    Zhang, Jinwei; Jaeck, Ortrud; Menegat, Alexander; Zhang, Zongjian; Gerhards, Roland; Ni, Hanwen

    2013-01-01

    Methylated seed oil (MSO) is a recommended adjuvant for the newly registered herbicide topramezone in China and also in other countries of the world, but the mechanism of MSO enhancing topramezone efficacy is still not clear. Greenhouse and laboratory experiments were conducted to determine the effects of MSO on efficacy, solution property, droplet spread and evaporation, active ingredient deposition, foliar absorption and translocation of topramezone applied to giant foxtail (Setaria faberi Herrm.) and velvetleaf (Abutilon theophrasti Medic.). Experimental results showed that 0.3% MSO enhanced the efficacy of topramezone by 1.5-fold on giant foxtail and by 1.0-fold on velvetleaf. When this herbicide was mixed with MSO, its solution surface tension and leaf contact angle decreased significantly, its spread areas on weed leaf surfaces increased significantly, its wetting time was shortened on giant foxtail but not changed on velvetleaf, and less of its active ingredient crystal was observed on the treated weed leaf surfaces. MSO increased the absorption of topramezone by 68.9% for giant foxtail and by 45.9% for velvetleaf 24 hours after treatment. It also apparently promoted the translocation of this herbicide in these two weeds.

  3. The mechanism of methylated seed oil on enhancing biological efficacy of topramezone on weeds.

    Directory of Open Access Journals (Sweden)

    Jinwei Zhang

    Full Text Available Methylated seed oil (MSO is a recommended adjuvant for the newly registered herbicide topramezone in China and also in other countries of the world, but the mechanism of MSO enhancing topramezone efficacy is still not clear. Greenhouse and laboratory experiments were conducted to determine the effects of MSO on efficacy, solution property, droplet spread and evaporation, active ingredient deposition, foliar absorption and translocation of topramezone applied to giant foxtail (Setaria faberi Herrm. and velvetleaf (Abutilon theophrasti Medic.. Experimental results showed that 0.3% MSO enhanced the efficacy of topramezone by 1.5-fold on giant foxtail and by 1.0-fold on velvetleaf. When this herbicide was mixed with MSO, its solution surface tension and leaf contact angle decreased significantly, its spread areas on weed leaf surfaces increased significantly, its wetting time was shortened on giant foxtail but not changed on velvetleaf, and less of its active ingredient crystal was observed on the treated weed leaf surfaces. MSO increased the absorption of topramezone by 68.9% for giant foxtail and by 45.9% for velvetleaf 24 hours after treatment. It also apparently promoted the translocation of this herbicide in these two weeds.

  4. Quantitative global and gene-specific promoter methylation in relation to biological properties of neuroblastomas

    Directory of Open Access Journals (Sweden)

    Kiss Nimrod B

    2012-09-01

    Full Text Available Abstract Background In this study we aimed to quantify tumor suppressor gene (TSG promoter methylation densities levels in primary neuroblastoma tumors and cell lines. A subset of these TSGs is associated with a CpG island methylator phenotype (CIMP in other tumor types. Methods The study panel consisted of 38 primary tumors, 7 established cell lines and 4 healthy references. Promoter methylation was determined by bisulphate Pyrosequencing for 14 TSGs; and LINE-1 repeat element methylation was used as an indicator of global methylation levels. Results Overall mean TSG Z-scores were significantly increased in cases with adverse outcome, but were unrelated to global LINE-1 methylation. CIMP with hypermethylation of three or more gene promoters was observed in 6/38 tumors and 7/7 cell lines. Hypermethylation of one or more TSG (comprising TSGs BLU, CASP8, DCR2, CDH1, RASSF1A and RASSF2 was evident in 30/38 tumors. By contrast only very low levels of promoter methylation were recorded for APC, DAPK1, NORE1A, P14, P16, TP73, PTEN and RARB. Similar involvements of methylation instability were revealed between cell line models and neuroblastoma tumors. Separate analysis of two proposed CASP8 regulatory regions revealed frequent and significant involvement of CpG sites between exon 4 and 5, but modest involvement of the exon 1 region. Conclusions/significance The results highlight the involvement of TSG methylation instability in neuroblastoma tumors and cell lines using quantitative methods, support the use of DNA methylation analyses as a prognostic tool for this tumor type, and underscore the relevance of developing demethylating therapies for its treatment.

  5. Identifying carcinogenic activity of methylated and non-methylated polycyclic aromatic hydrocarbons (PAHs) through electronic and topological indices

    CERN Document Server

    Braga, R S; Barone, P M V B

    2000-01-01

    Polycyclic aromatic hydrocarbons (PAHs) are a class of planar molecules, abundant in urban environment, which can induce chemical carcinogenesis. Their carcinogenic power varies in a large range, from very strong carcinogens to inactive ones. In a previous study, we proposed a methodology to identify the PAHs carcinogenic activity exploring electronic and topological indices. In the present work, we show that it is possible to simplify that methodology and expand its applicability to include methylated PAHs compounds. Using very simple rules, we can predict their carcinogenic activity with high accuracy (approx 89%).

  6. Spilanthol: occurrence, extraction, chemistry and biological activities

    Directory of Open Access Journals (Sweden)

    Alan F. Barbosa

    2016-02-01

    Full Text Available Abstract Spilanthol (C14H23NO, 221.339 g/mol is a bioactive compound that is found in many different plants that are used as traditional remedies throughout the world. It is present in Heliopsis longipes and several species in the genus Acmella, including A. oleracea L., also known as paracress and jambu. Its leaves and flowers have sensory properties (pungency, tingling, numbing, mouth-watering that make it a popular spice and ingredient in several Brazilian dishes. Spilanthol can exert a variety of biological and pharmacological effects including analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial, antilarvicidal and insecticidal activities. So, the aim of this review is to present a literature review on the spilanthol that describes its occurrence, chemistry, extraction and biological activities.

  7. Monitoring Biological Activity at Geothermal Power Plants

    Energy Technology Data Exchange (ETDEWEB)

    Peter Pryfogle

    2005-09-01

    The economic impact of microbial growth in geothermal power plants has been estimated to be as high as $500,000 annually for a 100 MWe plant. Many methods are available to monitor biological activity at these facilities; however, very few plants have any on-line monitoring program in place. Metal coupon, selective culturing (MPN), total organic carbon (TOC), adenosine triphosphate (ATP), respirometry, phospholipid fatty acid (PLFA), and denaturing gradient gel electrophoresis (DGGE) characterizations have been conducted using water samples collected from geothermal plants located in California and Utah. In addition, the on-line performance of a commercial electrochemical monitor, the BIoGEORGE?, has been evaluated during extended deployments at geothermal facilities. This report provides a review of these techniques, presents data on their application from laboratory and field studies, and discusses their value in characterizing and monitoring biological activities at geothermal power plants.

  8. Biological Activities of Polyphenols from Grapes

    OpenAIRE

    Hua-Bin Li; Ya-Jun Guo; Gui-Fang Deng; En-Qin Xia

    2010-01-01

    The dietary consumption of grape and its products is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds in grape. Anthocyanins, flavanols, flavonols and resveratrol are the most important grape polyphenols because they possess many biological activities, such as antioxidant, cardioprotective, anticancer, anti-inflammation, antiaging and antimicrobial proper...

  9. Synthesis of a high specific activity methyl sulfone tritium isotopologue of fevipiprant (NVP-QAW039).

    Science.gov (United States)

    Luu, Van T; Goujon, Jean-Yves; Meisterhans, Christian; Frommherz, Matthias; Bauer, Carsten

    2015-05-15

    The synthesis of a triple tritiated isotopologue of the CRTh2 antagonist NVP-QAW039 (fevipiprant) with a specific activity >3 TBq/mmol is described. Key to the high specific activity is the methylation of a bench-stable dimeric disulfide precursor that is in situ reduced to the corresponding thiol monomer and methylated with [(3)H3]MeONos having per se a high specific activity. The high specific activity of the tritiated active pharmaceutical ingredient obtained by a build-up approach is discussed in the light of the specific activity usually to be expected if hydrogen tritium exchange methods were applied.

  10. Design and biological properties of iodine-123 labeled. beta. -methyl-branched fatty acids

    Energy Technology Data Exchange (ETDEWEB)

    Knapp, F.F. Jr.; Goodman, M.M.

    1984-01-01

    The synthetic strategy, synthesis, preclinical evaluation and potential clinical applications of 3-methyl-branched radioiodinated iodophenyl- and iodovinyl-substituted fatty acids are reviewed for use as myocardial imaging agents. 50 references, 6 figures. (ACR)

  11. Biologic activity of digoxin-specific antisera.

    Science.gov (United States)

    Watson, J F; Butler, V P

    1972-03-01

    Digoxin-specific antibodies are capable of removing essentially all intracellular digoxin from rat renal cortical slices or from human erythrocytes. In removing digoxin from erythrocytes, these antibodies are capable of reversing an effect of the drug on cellular potassium transport. This study provides direct evidence that antibodies are capable of removing, and thereby reversing the biological effect of, physiologically active low molecular weight substances after they have been taken up by mammalian cells. This biologic property of digoxin-specific antibodies suggests that autidigoxin sera may prove useful in the reversal of digoxin toxicity. Rapid and essentially quantitative removal of digoxin from red cells by antibody is not accompanied by an immediate restoration of patassium influx to normal levels. Identification of the mechanism of this phenomenon may provide useful information concerning the mode of action not only of digoxin, but also of the cation transport system of human erythrocytes.

  12. Biological Activities of Royal Jelly - Review

    Directory of Open Access Journals (Sweden)

    Crenguţa I. Pavel

    2011-10-01

    Full Text Available Royal jelly is a secretion product of the cephalic glands of nurse bees that has been used for centuries for itsextraordinary properties and health effects. This bibliographic study aims to review many of the scientific findingsand research that prove many of the remarkable various actions, effects and some uses of royal jelly. There are takeninto consideration numerous biological properties and effects of royal jelly: antioxidant, neurotrophic, hipoglicemiant, hipocholesterolemiant and hepatoprotective, hypotensive and blood pressure regulatory, antitumor, antibiotic, anti-inflammatory, immunomodulatory and anti-allergic, general tonic and antiaging. Royal jelly is one ofthe most studied bee products, but there still remains much to reveal about its biochemistry and biological activity infuture research for our health and life benefit.

  13. Biological roles of the O-methyl phosphoramidate capsule modification in Campylobacter jejuni.

    Directory of Open Access Journals (Sweden)

    Lieke B van Alphen

    Full Text Available Campylobacter jejuni is a major cause of bacterial gastroenteritis worldwide, and the capsular polysaccharide (CPS of this organism is required for persistence and disease. C. jejuni produces over 47 different capsular structures, including a unique O-methyl phosphoramidate (MeOPN modification present on most C. jejuni isolates. Although the MeOPN structure is rare in nature it has structural similarity to some synthetic pesticides. In this study, we have demonstrated, by whole genome comparisons and high resolution magic angle spinning NMR, that MeOPN modifications are common to several Campylobacter species. Using MeOPN biosynthesis and transferase mutants generated in C. jejuni strain 81-176, we observed that loss of MeOPN from the cell surface correlated with increased invasion of Caco-2 epithelial cells and reduced resistance to killing by human serum. In C. jejuni, the observed serum mediated killing was determined to result primarily from activation of the classical complement pathway. The C. jejuni MeOPN transferase mutant showed similar levels of colonization relative to the wild-type in chickens, but showed a five-fold drop in colonization when co-infected with the wild-type in piglets. In Galleria mellonella waxmoth larvae, the MeOPN transferase mutant was able to kill the insects at wild-type levels. Furthermore, injection of the larvae with MeOPN-linked monosaccharides or CPS purified from the wild-type strain did not result in larval killing, indicating that MeOPN does not have inherent insecticidal activity.

  14. Biological activities of Curcuma longa L.

    Directory of Open Access Journals (Sweden)

    CAC Araújo

    2001-07-01

    Full Text Available There are several data in the literature indicating a great variety of pharmacological activities of Curcuma longa L. (Zingiberaceae, which exhibit anti-inflammatory, anti-human immunodeficiency virus, anti-bacteria, antioxidant effects and nematocidal activities. Curcumin is a major component in Curcuma longa L., being responsible for its biological actions. Other extracts of this plant has been showing potency too. In vitro, curcumin exhibits anti-parasitic, antispasmodic, anti-inflammatory and gastrointestinal effects; and also inhibits carcinogenesis and cancer growth. In vivo, there are experiments showing the anti-parasitic, anti-inflammatory potency of curcumin and extracts of C. longa L. by parenteral and oral application in animal models. In this present work we make an overview of the pharmacological activities of C. longa L., showing its importance.

  15. BDNF Methylation and Maternal Brain Activity in a Violence-Related Sample.

    Directory of Open Access Journals (Sweden)

    Dominik A Moser

    Full Text Available It is known that increased circulating glucocorticoids in the wake of excessive, chronic, repetitive stress increases anxiety and impairs Brain-Derived Neurotrophic Factor (BDNF signaling. Recent studies of BDNF gene methylation in relation to maternal care have linked high BDNF methylation levels in the blood of adults to lower quality of received maternal care measured via self-report. Yet the specific mechanisms by which these phenomena occur remain to be established. The present study examines the link between methylation of the BDNF gene promoter region and patterns of neural activity that are associated with maternal response to stressful versus non-stressful child stimuli within a sample that includes mothers with interpersonal violence-related PTSD (IPV-PTSD. 46 mothers underwent fMRI. The contrast of neural activity when watching children-including their own-was then correlated to BDNF methylation. Consistent with the existing literature, the present study found that maternal BDNF methylation was associated with higher levels of maternal anxiety and greater childhood exposure to domestic violence. fMRI results showed a positive correlation of BDNF methylation with maternal brain activity in the anterior cingulate (ACC, and ventromedial prefrontal cortex (vmPFC, regions generally credited with a regulatory function toward brain areas that are generating emotions. Furthermore we found a negative correlation of BDNF methylation with the activity of the right hippocampus. Since our stimuli focus on stressful parenting conditions, these data suggest that the correlation between vmPFC/ACC activity and BDNF methylation may be linked to mothers who are at a disadvantage with respect to emotion regulation when facing stressful parenting situations. Overall, this study provides evidence that epigenetic signatures of stress-related genes can be linked to functional brain regions regulating parenting stress, thus advancing our understanding of

  16. Biological Activities of Polyphenols from Grapes

    Directory of Open Access Journals (Sweden)

    Hua-Bin Li

    2010-02-01

    Full Text Available The dietary consumption of grape and its products is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds in grape. Anthocyanins, flavanols, flavonols and resveratrol are the most important grape polyphenols because they possess many biological activities, such as antioxidant, cardioprotective, anticancer, anti-inflammation, antiaging and antimicrobial properties. This review summarizes current knowledge on the bioactivities of grape phenolics. The extraction, isolation and identification methods of polyphenols from grape as well as their bioavailability and potential toxicity also are included.

  17. Reconstructing Causal Biological Networks through Active Learning.

    Directory of Open Access Journals (Sweden)

    Hyunghoon Cho

    Full Text Available Reverse-engineering of biological networks is a central problem in systems biology. The use of intervention data, such as gene knockouts or knockdowns, is typically used for teasing apart causal relationships among genes. Under time or resource constraints, one needs to carefully choose which intervention experiments to carry out. Previous approaches for selecting most informative interventions have largely been focused on discrete Bayesian networks. However, continuous Bayesian networks are of great practical interest, especially in the study of complex biological systems and their quantitative properties. In this work, we present an efficient, information-theoretic active learning algorithm for Gaussian Bayesian networks (GBNs, which serve as important models for gene regulatory networks. In addition to providing linear-algebraic insights unique to GBNs, leading to significant runtime improvements, we demonstrate the effectiveness of our method on data simulated with GBNs and the DREAM4 network inference challenge data sets. Our method generally leads to faster recovery of underlying network structure and faster convergence to final distribution of confidence scores over candidate graph structures using the full data, in comparison to random selection of intervention experiments.

  18. Biologically Active Metabolites Synthesized by Microalgae

    Directory of Open Access Journals (Sweden)

    Michele Greque de Morais

    2015-01-01

    Full Text Available Microalgae are microorganisms that have different morphological, physiological, and genetic traits that confer the ability to produce different biologically active metabolites. Microalgal biotechnology has become a subject of study for various fields, due to the varied bioproducts that can be obtained from these microorganisms. When microalgal cultivation processes are better understood, microalgae can become an environmentally friendly and economically viable source of compounds of interest, because production can be optimized in a controlled culture. The bioactive compounds derived from microalgae have anti-inflammatory, antimicrobial, and antioxidant activities, among others. Furthermore, these microorganisms have the ability to promote health and reduce the risk of the development of degenerative diseases. In this context, the aim of this review is to discuss bioactive metabolites produced by microalgae for possible applications in the life sciences.

  19. Layered metal laurates as active catalysts in the methyl/ethyl esterification reactions of lauric acid

    Energy Technology Data Exchange (ETDEWEB)

    Lisboa, Fabio da Silva; Cordeiro, Claudiney S.; Wypych, Fernando, E-mail: wypych@ufpr.br [Centro de Pesquisas em Quimica Aplicada (CEPESQ), Departamento de Quimica, Universidade Federal do Parana, Curitiba, PR (Brazil); Gardolinski, Jose Eduardo F. da Costa [Laboratorio de Analise de Minerais e Rochas (LAMIR), Departamento de Geologia, Universidade Federal do Parana, Curitiba, PR (Brazil)

    2012-07-01

    In this work we report the synthesis, characterization and investigation of the catalytic activity of layered copper(II), manganese(II), lanthanum(III) and nickel(II) laurates in the methyl and ethyl esterification reactions of lauric acid. In the methyl esterification, conversions between 80 and 90% were observed for all catalysts, while for the ethyl esterification only manganese laurate showed reasonable catalytic activity, with conversions close to 75%. Reuse of copper and lanthanum laurates in three cycles of reaction was also investigated and both catalysts preserved the structure and retained catalytic activity close to that observed for the first reaction cycle. (author)

  20. Litchi Flavonoids: Isolation, Identification and Biological Activity

    Directory of Open Access Journals (Sweden)

    Yueming Jiang

    2007-04-01

    Full Text Available The current status of the isolation, identification, biological activity, utilization and development prospects of flavonoids found in litchi fruit pericarp (LFP tissues is reviewed. LFP tissues account for approximately 15% by weight of the whole fresh fruit and are comprised of significant amount of flavonoids. The major flavonoids in ripe LFP include flavonols and anthocyanins. The major flavanols in the LFP are reported to be procyanidin B4, procyanidin B2 and epicatechin, while cyanindin-3-rutinside, cyanidin-3-glucoside, quercetin-3-rutinosde and quercetin-3-glucoside are identified as the important anthocyanins. Litchi flavanols and anthocyanins exhibit good potential antioxidant activity. The hydroxyl radical and superoxide anion scavenging activities of procyanidin B2 are greater than those of procyanidin B4 and epicatechin, while epicatechin has the highest α,α-diphenyl-β-picrylhydrazyl radical (DPPH· scavenging activity. In addition to the antioxidant activity, LFP extract displays a dose- and time-dependent inhibitory effect on human breast cancer, which could be attributed, in part, to its inhibition of proliferation and induction of apoptosis in cancer cells through upregulation and down-regulation of multiple genes. Furthermore, various anticancer activities are observed for epicatechin, procyanidin B2, procyanidin B4 and the ethyl acetate fraction of LFP tissue extracts. Procyanidin B4 and the ethyl acetate fraction show a stronger inhibitory effect on HELF than MCF-7 proliferation, while epicatechin and procyanidin B2 have lower cytotoxicities towards MCF-7 and HELF than paclitaxel. It is therefore suggested that flavonoids from LFP might be potentially useful components for functional foods and/or anti-breast cancer drugs.

  1. ACTIVE AND PARTICIPATORY METHODS IN BIOLOGY: MODELING

    Directory of Open Access Journals (Sweden)

    Brînduşa-Antonela SBÎRCEA

    2011-01-01

    Full Text Available By using active and participatory methods it is hoped that pupils will not only come to a deeper understanding of the issues involved, but also that their motivation will be heightened. Pupil involvement in their learning is essential. Moreover, by using a variety of teaching techniques, we can help students make sense of the world in different ways, increasing the likelihood that they will develop a conceptual understanding. The teacher must be a good facilitator, monitoring and supporting group dynamics. Modeling is an instructional strategy in which the teacher demonstrates a new concept or approach to learning and pupils learn by observing. In the teaching of biology the didactic materials are fundamental tools in the teaching-learning process. Reading about scientific concepts or having a teacher explain them is not enough. Research has shown that modeling can be used across disciplines and in all grade and ability level classrooms. Using this type of instruction, teachers encourage learning.

  2. Biologically Active and Antimicrobial Peptides from Plants

    Directory of Open Access Journals (Sweden)

    Carlos E. Salas

    2015-01-01

    Full Text Available Bioactive peptides are part of an innate response elicited by most living forms. In plants, they are produced ubiquitously in roots, seeds, flowers, stems, and leaves, highlighting their physiological importance. While most of the bioactive peptides produced in plants possess microbicide properties, there is evidence that they are also involved in cellular signaling. Structurally, there is an overall similarity when comparing them with those derived from animal or insect sources. The biological action of bioactive peptides initiates with the binding to the target membrane followed in most cases by membrane permeabilization and rupture. Here we present an overview of what is currently known about bioactive peptides from plants, focusing on their antimicrobial activity and their role in the plant signaling network and offering perspectives on their potential application.

  3. 5'-Cytosine-phosphoguanine (CpG) methylation impacts the activity of natural and engineered meganucleases.

    Science.gov (United States)

    Valton, Julien; Daboussi, Fayza; Leduc, Sophie; Molina, Rafael; Redondo, Pilar; Macmaster, Rachel; Montoya, Guillermo; Duchateau, Philippe

    2012-08-31

    In this study, we asked whether CpG methylation could influence the DNA binding affinity and activity of meganucleases used for genome engineering applications. A combination of biochemical and structural approaches enabled us to demonstrate that CpG methylation decreases I-CreI DNA binding affinity and inhibits its endonuclease activity in vitro. This inhibition depends on the position of the methylated cytosine within the DNA target and was almost total when it is located inside the central tetrabase. Crystal structures of I-CreI bound to methylated cognate target DNA suggested a molecular basis for such inhibition, although the precise mechanism still has to be specified. Finally, we demonstrated that the efficacy of engineered meganucleases can be diminished by CpG methylation of the targeted endogenous site, and we proposed a rational design of the meganuclease DNA binding domain to alleviate such an effect. We conclude that although activity and sequence specificity of engineered meganucleases are crucial parameters, target DNA epigenetic modifications need to be considered for successful gene editions.

  4. Biological active compounds from Georgian Galanthus shaoricus.

    Science.gov (United States)

    Jokhadze, M; Kuchukhidze, J; Chincharadze, D; Murtazashvili, T

    2011-10-01

    Amaryllidaceae alkaloids exhibit antitumour, antiviral and anticholinergic activities. Some of them have been used in the treatment of myasthenia gravis, myopathy and diseases of the nervous system. In this study, the characterization of these compounds from Amaryllidaceae plants along with some biological activities and some regulations to conserve the native flora will be reviewed. Plants materials: Galanthus shaoricus Kem.-Nath., were collected in 2007-2008 during the flowering period in Georgia. The preparation of extracts and fractions were obtained using methanolic maceration. Crude alkaloidal extracts were typically purified by liquid-liquid partitioning of their basic forms in chloroform. Lycorine, galantamine and tazettine has been found as one of the major alkaloid from Amaryllidaceae plants. Galanthus shaoricus have shown good antimalarial and cytotoxic activity in a dose-dependent manner. Methanolic extracts from bulbs demonstrated significant growth inhibition on human Hela and HCT-116 cells lines with IC50 (μg/mL) 16.3±1.8; 22.1±2.9 (aerial parts) and 12.8±1.7; 16.5±1.9 (Bulbs), respectively. Concerning the Amaryllidaceae alkaloids, lycorine with IC50 (μM) 0.8±0.5 and 2.6±0.2, haemantaimene (IC50=1.1±0.7 and 2.7±0.8 μM), hamaine (IC50=3.4±1.0 and 6.2 ±1.4 μM), homolycorine (IC50=1.4±0.9 and 3.3±1.0 μM), hipeastrine (IC50=2.8±1.0 and 7.5±1.8 μM) were found to be responsible for the cytotoxic activity on HCT-116 and Hela cell lines, respectively.

  5. Sulfation and biological activities of konjac glucomannan.

    Science.gov (United States)

    Bo, Surina; Muschin, Tegshi; Kanamoto, Taisei; Nakashima, Hideki; Yoshida, Takashi

    2013-05-15

    The sulfation of konjac glucomannan and its anti-HIV and blood anticoagulant activities were investigated. Konjac glucomannan is a polysaccharide occurring naturally in konjac plant tubers and has high molecular weights. Solubility in water is very low, and the aqueous solutions at low concentrations have high viscosity. Before sulfation, hydrolysis by diluted sulfuric acid was carried out to decrease the molecular weights of M¯n=19.2 × 10(4)-0.2 × 10(4). Sulfation with piperidine-N-sulfonic acid or SO3-pyridine complex gave sulfated konjac glucomannans with molecular weights of M¯n=1.0 × 10(4)-0.4 × 10(4) and degrees of sulfation (DS) of 1.3-1.4. It was found that the sulfated konjac glucomannans had potent anti-HIV activity at a 50% effective concentration, (EC50) of 1.2-1.3 μg/ml, which was almost as high as that of an AIDS drug, ddC, whose EC50=3.2 μg/ml, and moderate blood anticoagulant activity, AA=0.8-22.7 units/mg, compared to those of standard sulfated polysaccharides, curdlan (10 units/mg) and dextran (22.7 units/mg) sulfates. Structural analysis of sulfated konjac glucomannans with negatively charged sulfated groups was performed by high resolution NMR, and the interaction between poly-l-lysine with positively charged amino groups as a model compound of proteins and peptides was measured by surface plasmon resonance measurement, suggesting that the sulfated konjac glucomannans had a high binding stability on immobilized poly-l-lysine. The binding of sulfated konjac glucomannan was concentration-dependent, and the biological activity of the sulfated konjac glucomannans may be due to electrostatic interaction between the sulfate and amino groups.

  6. The Optimum Reaction Time, Activation Energy and Frequency Factor of Methyl Ricinoleate Nitration

    OpenAIRE

    Abdullah, Abdullah; Triyono, Triyono; Trisunaryanti, Wega; Haryadi, Winarto

    2013-01-01

    Determination of the optimum reaction time, activation energy (Ea) and frequency factor (A) of methyl ricinoleate nitration has been done. The nitration was conducted with the mole ratio of methyl ricinoleate to HNO3 of 1:15. The reaction was conducted at temperatures of 29 and 64 °C with a variation of reaction time for 10, 20, 30, 60, 90, 120, and 150 min. Determination of activation energy and frequency factor was performed in a temperature of 29, 33, 38, 44, 49, 57 and 64 °C. The results ...

  7. Activity of Acetolactate Synthase from Maize (Zea mays L. ) as Influenced by Chlorsulfuron and Tribenuron-methyl

    Institute of Scientific and Technical Information of China (English)

    FAN Zhi-jin; CHEN Jun-peng; HU Ji-ye; QIAN Chuan-fan; LI Zheng-ming

    2003-01-01

    Study on relative sensitivity of maize (Zea mays L. ) Nongda108 and Nongda3138 to sulfonylurea herbicide chlorsulfuron and tribenuron-methyl using maize taproot length by sand bioassy indicated that, Nongda3138 had higher tolerance to chlorsulfuron and tribenuron-methyl than Nongda108 did. Chlorsulfuron had stronger growth inhibition to maize Nongda108 and Nongda3138 than tribenuron-methyl did. Study on target enzyme of sulfonylurea herbicide acetolactate synthase (ALS) showed that, chlorsulfuron and tribenuron-methyl inhibited ALS in vitro strongly, and non-competitively. In the same concentration of inhibitors,chlorsuifuron had stronger ALS activity inhibition than tribenuron-methyl did. Lower level of chlorsulfuron and tribenuron-methyl has no ALS activity inhibition in vivo, the ALS inhibition only occurred in the condition of high concentration of chlorsulfuron and tribenuron-methyl in vivo.

  8. Study of TAMe (p-tosyl-L-arginine methyl ester) esterase activity of bovine plasma.

    Science.gov (United States)

    Claxton, J; Black, W D; Gentry, P A

    1978-07-01

    The TAMe (p-tosyl-L-arginine methyl ester) esterase activity of mature and immature bovine plasma was studied and compared with the activity of this enzyme in human plasma. Kaolin activation of 2 minutes was required to produce maximal activation in cattle, as compared with 1 minute activation in man. The kaolin-activated TAMe esterase values in bovine plasma were approximately one-half the values found in human plasma. The activity of this enzyme was statistically greater in immature than in mature cattle (P less than 0.05) at kaolin activation times of 1, 2, 15, and 20 minutes.

  9. Synthesis and Herbicidal Activities of Potassium Methyl 1-(Substituted Phenoxyacetoxy)alkylphosphonate

    Institute of Scientific and Technical Information of China (English)

    WANG Tao; WANG Wei; PENG Hao; HE Hong-wu

    2013-01-01

    A series of potassium methyl 1-(substituted phenoxyacetoxy)alkylphosphonates(9a-9o) was designed and synthesized.The results of preliminary bioassays indicate that most of the title compounds possess excellent pre-emergence and post-emergence herbicidal activities against Brassica napus,Amaranthus mangostanus,Medicago sativa,Echinochloa crusgalli,and Digitaria sanguinalis at a dosage of 1500 g/ha(1 ha=10000 m2).Especially,potassium methyl 1-(2,4-dichlorophenoxyacetoxy)-1-(4-methylphenyl)methylphosphonate(9g) and potassium methyl 1-(2,4-dichlorophenoxyacetoxy)-1-(furan-2-yl)methylphosphonate(9j) show the best herbicidal activity against five tested weeds with more than 85% inhibitory rate in pre-emergence.

  10. DNA Methylation Pyrosequencing Assay Is Applicable for the Assessment of Epigenetic Active Environmental or Clinical Relevant Chemicals

    Directory of Open Access Journals (Sweden)

    Ana-Maria Florea

    2013-01-01

    Full Text Available Exposure of cells and organisms to stressors might result in epigenetic changes. Here it is shown that investigation of DNA methylation using pyrosequencing is an alternative for in vitro and in vivo toxicological testing of epigenetic effects induced by chemicals and drugs. An in vitro evaluation of global and CpG site specific DNA methylation upon treatment of cells with chemicals/drugs is shown. Bisulfite genomic sequencing of methylation controls showed high methylation of LINE1 in methylation positive control and low methylation in the negative controls. The CpG sites within the LINE1 element are methylated at different levels. In vitro cell cultures show a methylation level ranging from 56% to 49%. Cultures of drug resistant tumor cells show significant hypomethylation as compared with the originating nonresistant tumor cells. The in vitro testing of epigenetically active chemicals (5-methyl-2’-deoxycytidine and trichostatin A revealed a significant change of LINE1 methylation status upon treatment, while specific CpG sites were more prone to demethylation than others (focal methylation. In conclusion, DNA methylation using pyrosequencing might be used not only for testing epigenetic toxins/drugs but also in risk assessment of drugs, food, and environmental relevant pollutants.

  11. A biologically active fructan from the roots of Arctium lappa L., var. Herkules.

    Science.gov (United States)

    Kardosová, A; Ebringerová, A; Alföldi, J; Nosál'ová, G; Franová, S; Hríbalová, V

    2003-11-01

    From the roots of Arctium lappa L., var. Herkules a low-molecular-weight fructofuranan of the inulin-type has been isolated by water extraction and ethanol precipitation, followed by ion-exchange chromatography and gel filtration of the crude precipitate. The methods employed in structural determination were methylation analysis and 1H and 13C NMR spectral measurements. In tests for antitussive activity in cats the fructan was found to be equally active as some non-narcotic, synthetic preparations used in clinical practice to treat coughing, and in mitogenic and comitogenic tests its biological response was comparable to that of the commercial Zymosan immunomodulator.

  12. BIOLOGICALLY ACTIVE SUBSTANCES OF SPIRIT PRODUCTION WASTE

    Directory of Open Access Journals (Sweden)

    A. S. Kayshev

    2014-01-01

    Full Text Available A content of biologically active compounds (BAC with signified pharmacological activity in distillers grains was proved. It is prospective for applications of these grains as a raw material resource of pharmaceuticals. A composition of BAC distillers grains received from wheat, corn, barley, millet at different spirit enterprises which use hydro fermentative grain processing. Considering polydispersity of distillers grains they were separated on solid and liquid phases preliminary. Physical and chemical characteristics of distillers grains' liquid base were identified. Elementary composition of distillers grains is signified by active accumulation of biogenic elements (phosphorus, potassium, magnesium, calcium, sodium, iron and low content of heavy metals. The solid phase of distillers grains accumulates carbon, hydrogen and nitrogen in high concentration. The liquid phase of distillers grains contains: proteins and amino acids (20-46%, reducing sugars (5,6%-17,5%, galacturonides (0,8-1,4%, ascorbic acid (6,2-11,4 mg%. The solid base of distillers grains contains: galacturonides (3,4-5,3%, fatty oil (8,4-11,1% with predomination of essential fatty acids, proteins and amino acids (2,1-2,5%, flavonoids (0,4-0,9%, tocopherols (3,4-7,7 mg%. A method of complex processing of distillers grains based on application of membrane filtering of liquid phase and liquid extraction by inorganic and organic solvents of solid phase, which allows almost full extraction of the sum of biologically active compounds (BAC from liquid phase (Biobardin BM and solid phase (Biobardin UL. Biobardin BM comprises the following elements: proteins and amino acids (41-69%, reducing sugars (3,5-15,6%, fatty oil (0,2-0,3%, flavonoids (0,2-0,7%, ascorbic acid (17-37 mg%. Biobardin UL includes: oligouronids (16,4-19,5%, proteins and amino acids (11-21%, fatty oil (3,2-4,9% which includes essential acids; flavonoids (0,6-1,5%, tocopherols (6,6-10,2 mg%, carotinoids (0,13-0,21 mg

  13. Biological effects of short-term, high-concentration exposure to methyl isocyanate. II. Blood chemistry and hematologic evaluations.

    OpenAIRE

    Troup, C M; Dodd, D E; Fowler, E H; Frank, F R

    1987-01-01

    Human, rat, and guinea pig packed erythrocytes exposed to 100, 500, or 1000 ppm of methyl isocyanate (MIC) vapor in vitro showed a concentration-related inhibition of cholinesterase (ChE) activity. Rat and guinea pig packed erythrocytes showed an almost complete inhibition of ChE activity at 2000 ppm. In vitro exposures of human and guinea pig blood to 1000 or 2000 ppm of MIC vapor resulted in qualitative alterations in the electrophoretic mobility of hemoglobin (Hb) as measured by citrated a...

  14. Monascus secondary metabolites: production and biological activity.

    Science.gov (United States)

    Patakova, Petra

    2013-02-01

    The genus Monascus, comprising nine species, can reproduce either vegetatively with filaments and conidia or sexually by the formation of ascospores. The most well-known species of genus Monascus, namely, M. purpureus, M. ruber and M. pilosus, are often used for rice fermentation to produce red yeast rice, a special product used either for food coloring or as a food supplement with positive effects on human health. The colored appearance (red, orange or yellow) of Monascus-fermented substrates is produced by a mixture of oligoketide pigments that are synthesized by a combination of polyketide and fatty acid synthases. The major pigments consist of pairs of yellow (ankaflavin and monascin), orange (rubropunctatin and monascorubrin) and red (rubropunctamine and monascorubramine) compounds; however, more than 20 other colored products have recently been isolated from fermented rice or culture media. In addition to pigments, a group of monacolin substances and the mycotoxin citrinin can be produced by Monascus. Various non-specific biological activities (antimicrobial, antitumor, immunomodulative and others) of these pigmented compounds are, at least partly, ascribed to their reaction with amino group-containing compounds, i.e. amino acids, proteins or nucleic acids. Monacolins, in the form of β-hydroxy acids, inhibit hydroxymethylglutaryl-coenzyme A reductase, a key enzyme in cholesterol biosynthesis in animals and humans.

  15. Biological activity of Serratia marcescens cytotoxin

    Directory of Open Access Journals (Sweden)

    G.V. Carbonell

    2003-03-01

    Full Text Available Serratia marcescens cytotoxin was purified to homogeneity by ion-exchange chromatography on a DEAE Sepharose Fast Flow column, followed by gel filtration chromatography on a Sephadex G100 column. The molecular mass of the cytotoxin was estimated to be about 50 kDa. Some biological properties of the cytotoxin were analyzed and compared with well-characterized toxins, such as VT1, VT2 and CNF from Escherichia coli and hemolysin produced by S. marcescens. The sensitivity of the cell lines CHO, HeLa, HEp-2, Vero, BHK-21, MA 104 and J774 to the cytotoxin was determined by the cell viability assay using neutral red. CHO and HEp-2 were highly sensitive, with massive cellular death after 1 h of treatment, followed by BHK-21, HeLa, Vero and J774 cells, while MA 104 was insensitive to the toxin. Cytotoxin induced morphological changes such as cell rounding with cytoplasmic retraction and nuclear compactation which were evident 15 min after the addition of cytotoxin. The cytotoxic assays show that 15 min of treatment with the cytotoxin induced irreversible intoxication of the cells, determined by loss of cell viability. Concentrations of 2 CD50 (0.56 µg/ml of purified cytotoxin did not present any hemolytic activity, showing that the cytotoxin is distinct from S. marcescens hemolysin. Antisera prepared against S. marcescens cytotoxin did not neutralize the cytotoxic activity of VT1, VT2 or CNF toxin, indicating that these toxins do not share antigenic determinants with cytotoxin. Moreover, we did not detect gene sequences for any of these toxins in S. marcescens by PCR assay. These results suggest that S. marcescens cytotoxin is not related to any of these toxins from E. coli.

  16. Biological activity of Serratia marcescens cytotoxin.

    Science.gov (United States)

    Carbonell, G V; Amorim, C R N; Furumura, M T; Darini, A L C; Fonseca, B A L; Yano, T

    2003-03-01

    Serratia marcescens cytotoxin was purified to homogeneity by ion-exchange chromatography on a DEAE Sepharose Fast Flow column, followed by gel filtration chromatography on a Sephadex G100 column. The molecular mass of the cytotoxin was estimated to be about 50 kDa. Some biological properties of the cytotoxin were analyzed and compared with well-characterized toxins, such as VT1, VT2 and CNF from Escherichia coli and hemolysin produced by S. marcescens. The sensitivity of the cell lines CHO, HeLa, HEp-2, Vero, BHK-21, MA 104 and J774 to the cytotoxin was determined by the cell viability assay using neutral red. CHO and HEp-2 were highly sensitive, with massive cellular death after 1 h of treatment, followed by BHK-21, HeLa, Vero and J774 cells, while MA 104 was insensitive to the toxin. Cytotoxin induced morphological changes such as cell rounding with cytoplasmic retraction and nuclear compactation which were evident 15 min after the addition of cytotoxin. The cytotoxic assays show that 15 min of treatment with the cytotoxin induced irreversible intoxication of the cells, determined by loss of cell viability. Concentrations of 2 CD50 (0.56 g/ml) of purified cytotoxin did not present any hemolytic activity, showing that the cytotoxin is distinct from S. marcescens hemolysin. Antisera prepared against S. marcescens cytotoxin did not neutralize the cytotoxic activity of VT1, VT2 or CNF toxin, indicating that these toxins do not share antigenic determinants with cytotoxin. Moreover, we did not detect gene sequences for any of these toxins in S. marcescens by PCR assay. These results suggest that S. marcescens cytotoxin is not related to any of these toxins from E. coli.

  17. Activities of natural methyl farnesoids on pupariation and metamorphosis of Drosophila melanogaster

    Science.gov (United States)

    Methyl farnesoate (MF) and juvenile hormone (JH III), which respectively bind to the receptors USP and MET, and bisepoxy JH III (bisJHIII) were assessed for several activities during Drosophila larval development, and during prepupal development to eclosed adults. Dietary MF and JH III were similar...

  18. Esterification and transesterification of greases to fatty acid methyl esters with highly active diphanylammonium salts

    Science.gov (United States)

    We have conducted an investigation designed to identify alternate catalysts for the production of fatty acid methyl esters (FAME) to be used as biodiesel. Diphenylammonium sulfate (DPAS) and diphenylammonium chloride (DPA-HCl) salts were found to be highly active homogeneous catalysts for the simu...

  19. Esterification and Transesterification of greases to fatty acid methyl esters with highly active diphenylamine salts

    Science.gov (United States)

    Diphenylamine sulfate (DPAS) and diphenylamine hydrochloride (DPACl) salts were found to be highly active catalysts for esterification and transesterification of inexpensive greases to fatty acid methyl esters (FAME). In the presence of catalytic amounts of DPAS or DPACl and excess methanol, the fr...

  20. Unmasking risk loci: DNA methylation illuminates the biology of cancer predisposition: analyzing DNA methylation of transcriptional enhancers reveals missed regulatory links between cancer risk loci and genes.

    Science.gov (United States)

    Aran, Dvir; Hellman, Asaf

    2014-02-01

    Paradoxically, DNA sequence polymorphisms in cancer risk loci rarely correlate with the expression of cancer genes. Therefore, the molecular mechanism underlying an individual's susceptibility to cancer has remained largely unknown. However, recent evaluations of the correlations between DNA methylation and gene expression levels across healthy and cancerous genomes have revealed enrichment of disease-related DNA methylation variations within disease-associated risk loci. Moreover, it appears that transcriptional enhancers embedded in cancer risk loci often contain DNA methylation sites that closely define the expression of prominent cancer genes, despite the lack of significant correlations between gene expression levels and the surrounding disease-associated polymorphic sequences. We suggest that DNA methylation variations may obscure the effect of co-residing risk sequence alleles. Analysis of enhancer methylation data may help to reveal the regulatory circuits underlying predisposition to cancers and other common diseases.

  1. Conjugates of methylated cyclodextrin derivatives and hydroxyethyl starch (HES: Synthesis, cytotoxicity and inclusion of anaesthetic actives

    Directory of Open Access Journals (Sweden)

    Lisa Markenstein

    2014-12-01

    Full Text Available The mono-6-deoxy-6-azides of 2,6-di-O-methyl-β-cyclodextrin (DIMEB and randomly methylated-β-cyclodextrin (RAMEB were conjugated to propargylated hydroxyethyl starch (HES by Cu+-catalysed [2 + 3] cycloaddition. The resulting water soluble polymers showed lower critical solution temperatures (LCST at 52.5 °C (DIMEB-HES and 84.5 °C (RAMEB-HES, respectively. LCST phase separations could be completely avoided by the introduction of a small amount of carboxylate groups at the HES backbone. The methylated CDs conjugated to the HES backbone exhibited significantly lower cytotoxicities than the corresponding monomeric CD derivatives. Since the binding potentials of these CD conjugates were very high, they are promising candidates for new oral dosage forms of anaesthetic actives.

  2. Low intensity ultrasound stimulates biological activity of aerobic activated sludge

    Institute of Scientific and Technical Information of China (English)

    LIU Hong; YAN Yixin; WANG Wenyan; YU Yongyong

    2007-01-01

    This work aims to explore a procedure to improve biological wastewater treatment efficiency using low intensity ultrasound.The aerobic activated sludge from a municipal wastewater treatment plant was used as the experimental material.Oxygen uptake rate(OUR)of the activated sludge (AS)was determined to indicate the changes of AS activity stimulated by ultrasound at 35 kHZ for 0-40 min with ultrasonic intensities of 0-1.2 W/cm2.The highest OUR was observed at the ultrasonic intensity of 0.3 W/cm2 and an irradiation period of 10 min;more than 15% increase was achieved immediately after sonication.More significantly,the AS activity stimulated by ultrasound could last 24 h after sonication,and the AS activity achieved its peak value within 8 h after sonication.or nearly 100% higher than the initial level after sonication.Therefore,to improve the wastewater treatment efficiency of bioreactors,ultrasound with an intensity of 0.3 W/cm2 could be employed to irradiate a part of the AS in the bioreactor for 10 min every 8 h.

  3. Impacts of Activated Carbon Amendment on Hg Methylation, Demethylation and Microbial Activity in Marsh Soils

    Science.gov (United States)

    Gilmour, C. C.; Ghosh, U.; Santillan, E. F. U.; Soren, A.; Bell, J. T.; Butera, D.; McBurney, A. W.; Brown, S.; Henry, E.; Vlassopoulos, D.

    2015-12-01

    In-situ sorbent amendments are a low-impact approach for remediation of contaminants in sediments, particular in habitats like wetlands that provide important ecosystem services. Laboratory microcosm trials (Gilmour et al. 2013) and early field trials show that activated carbon (AC) can effectively increase partitioning of both inorganic Hg and methylmercury to the solid phase. Sediment-water partitioning can serve as a proxy for Hg and MeHg bioavailability in soils. One consideration in using AC in remediation is its potential impact on organisms. For mercury, a critical consideration is the potential impact on net MeHg accumulation and bioavailability. In this study, we specifically evaluated the impact of AC on rates of methylmercury production and degradation, and on overall microbial activity, in 4 different Hg-contaminated salt marsh soils. The study was done over 28 days in anaerobic, sulfate-reducing slurries. A double label of enriched mercury isotopes (Me199Hg and inorganic 201Hg) was used to separately follow de novo Me201Hg production and Me199Hg degradation. AC amendments decreased both methylation and demethylation rate constants relative to un-amended controls, but the impact on demethylation was stronger. The addition of 5% (dry weight) regenerated AC to soil slurries drove demethylation rate constants to nearly zero; i.e. MeHg sorption to AC almost totally blocked its degradation. The net impact was increased solid phase MeHg concentrations in some of the soil slurries with the highest methylation rate constants. However, the net impact of AC amendments was to increase MeHg (and inorganic Hg) partitioning to the soil phase and decrease concentrations in the aqueous phase. AC significantly decreased aqueous phase inorganic Hg and MeHg concentrations after 28 days. Overall, the efficacy of AC in reducing aqueous MeHg was highest in the soils with the highest MeHg concentrations. The AC addition did not significantly impact microbial activity, as

  4. hTERT promoter activity and CpG methylation in HPV-induced carcinogenesis

    Directory of Open Access Journals (Sweden)

    Snijders Peter JF

    2010-06-01

    Full Text Available Abstract Background Activation of telomerase resulting from deregulated hTERT expression is a key event during high-risk human papillomavirus (hrHPV-induced cervical carcinogenesis. In the present study we examined hTERT promoter activity and its relation to DNA methylation as one of the potential mechanisms underlying deregulated hTERT transcription in hrHPV-transformed cells. Methods Using luciferase reporter assays we analyzed hTERT promoter activity in primary keratinocytes, HPV16- and HPV18-immortalized keratinocyte cell lines and cervical cancer cell lines. In the same cells as well as cervical specimens we determined hTERT methylation by bisulfite sequencing analysis of the region spanning -442 to +566 (relative to the ATG and quantitative methylation specific PCR (qMSP analysis of two regions flanking the hTERT core promoter. Results We found that in most telomerase positive cells increased hTERT core promoter activity coincided with increased hTERT mRNA expression. On the other hand basal hTERT promoter activity was also detected in telomerase negative cells with no or strongly reduced hTERT mRNA expression levels. In both telomerase positive and negative cells regulatory sequences flanking both ends of the core promoter markedly repressed exogenous promoter activity. By extensive bisulfite sequencing a strong increase in CpG methylation was detected in hTERT positive cells compared to cells with no or strongly reduced hTERT expression. Subsequent qMSP analysis of a larger set of cervical tissue specimens revealed methylation of both regions analyzed in 100% of cervical carcinomas and 38% of the high-grade precursor lesions, compared to 9% of low grade precursor lesions and 5% of normal controls. Conclusions Methylation of transcriptionally repressive sequences in the hTERT promoter and proximal exonic sequences is correlated to deregulated hTERT transcription in HPV-immortalized cells and cervical cancer cells. The detection of DNA

  5. Synthesis and Biological Activity of 4,5-Dihydro-1,2,4-triazole-5-thione Schiff Base

    Institute of Scientific and Technical Information of China (English)

    SUN, Xiaohong; BAI, Yan; LIU, Yuanfa; CHEN, Bang; JIA, Yingqi; ZENG, Zhenfang

    2009-01-01

    The 4,5-dihydro-1,2,4-triazole Schiff base derivatives were synthesized with 4-amino-4,5-dihydro-3-(phenoxy- methyl)-1H-1,2,4-triazole-5-thione and substituted benzaidehydes. The chemical structures of the compounds have been confirmed by 1H NMR, IR spectra and elemental analysis. Their biological activities were investigated, and the results showed that they exhibited good fungicidal activities.

  6. Geissoschizine methyl ether N-oxide, a new alkaloid with antiacetylcholinesterase activity from Uncaria rhynchophylla.

    Science.gov (United States)

    Jiang, Wei-Wei; Su, Jia; Wu, Xing-De; He, Juan; Peng, Li-Yan; Cheng, Xiao; Zhao, Qin-Shi

    2015-01-01

    Geissoschizine methyl ether N-oxide, a new oxindole alkaloid, along with 14 known alkaloids, was isolated from the aerial part of Uncaria rhynchophylla. Their structures were identified by comprehensive spectral methods, including 2D NMR experiments, and confirmed by comparing with the literature data. In vitro acetylcholinesterase (AChE) inhibitory activity assay showed that the new compound exhibited anti-AChE activity with IC₅₀ value of 23.4 μM.

  7. DNA methylation in an enhancer region of the FADS cluster is associated with FADS activity in human liver.

    Directory of Open Access Journals (Sweden)

    Timothy D Howard

    Full Text Available Levels of omega-6 (n-6 and omega-3 (n-3, long chain polyunsaturated fatty acids (LcPUFAs such as arachidonic acid (AA; 20:4, n-6, eicosapentaenoic acid (EPA; 20:5, n-3 and docosahexaenoic acid (DHA; 22:6, n-3 impact a wide range of biological activities, including immune signaling, inflammation, and brain development and function. Two desaturase steps (Δ6, encoded by FADS2 and Δ5, encoded by FADS1 are rate limiting in the conversion of dietary essential 18 carbon PUFAs (18C-PUFAs such as LA (18:2, n-6 to AA and α-linolenic acid (ALA, 18:3, n-3 to EPA and DHA. GWAS and candidate gene studies have consistently identified genetic variants within FADS1 and FADS2 as determinants of desaturase efficiencies and levels of LcPUFAs in circulating, cellular and breast milk lipids. Importantly, these same variants are documented determinants of important cardiovascular disease risk factors (total, LDL, and HDL cholesterol, triglycerides, CRP and proinflammatory eicosanoids. FADS1 and FADS2 lie head-to-head (5' to 5' in a cluster configuration on chromosome 11 (11q12.2. There is considerable linkage disequilibrium (LD in this region, where multiple SNPs display association with LcPUFA levels. For instance, rs174537, located ∼ 15 kb downstream of FADS1, is associated with both FADS1 desaturase activity and with circulating AA levels (p-value for AA levels = 5.95 × 10(-46 in humans. To determine if DNA methylation variation impacts FADS activities, we performed genome-wide allele-specific methylation (ASM with rs174537 in 144 human liver samples. This approach identified highly significant ASM with CpG sites between FADS1 and FADS2 in a putative enhancer signature region, leading to the hypothesis that the phenotypic associations of rs174537 are likely due to methylation differences. In support of this hypothesis, methylation levels of the most significant probe were strongly associated with FADS1 and, to a lesser degree, FADS2 activities.

  8. Methyl Salicylate Level Increase in Flax after Fusarium oxysporum Infection Is Associated with Phenylpropanoid Pathway Activation

    Science.gov (United States)

    Boba, Aleksandra; Kostyn, Kamil; Kostyn, Anna; Wojtasik, Wioleta; Dziadas, Mariusz; Preisner, Marta; Szopa, Jan; Kulma, Anna

    2017-01-01

    Flax (Linum usitatissimum) is a crop plant valued for its oil and fiber. Unfortunately, large losses in cultivation of this plant are caused by fungal infections, with Fusarium oxysporum being one of its most dangerous pathogens. Among the plant's defense strategies, changes in the expression of genes of the shikimate/phenylpropanoid/benzoate pathway and thus in phenolic contents occur. Among the benzoates, salicylic acid, and its methylated form methyl salicylate play an important role in regulating plants' response to stress conditions. Upon treatment of flax plants with the fungus we found that methyl salicylate content increased (4.8-fold of the control) and the expression profiles of the analyzed genes suggest that it is produced most likely from cinnamic acid, through the β-oxidative route. At the same time activation of some genes involved in lignin and flavonoid biosynthesis was observed. We suggest that increased methyl salicylate biosynthesis during flax response to F. oxysporum infection may be associated with phenylpropanoid pathway activation. PMID:28163709

  9. The ice nucleation activity of biological aerosols

    Science.gov (United States)

    Grothe, H.; Pummer, B.; Bauer, H.; Bernardi, J.

    2012-04-01

    Primary Biological Aerosol Particles (PBAPs), including bacteria, spores and pollen may be important for several atmospheric processes. Particularly, the ice nucleation caused by PBAPs is a topic of growing interest, since their impact on ice cloud formation and thus on radiative forcing, an important parameter in global climate is not yet fully understood. In laboratory model studies we investigated the ice nucleation activity of selected PBAPs. We studied the immersion mode freezing using water-oil emulsion, which we observed by optical microscopy. We particularly focused on pollen. We show that pollen of different species strongly differ in their ice nucleation behavior. The average freezing temperatures in laboratory experiments range from 240 K to 255 K. As the most efficient nuclei (silver birch, Scots pine and common juniper pollen) have a distribution area up to the Northern timberline, their ice nucleation activity might be a cryoprotective mechanism. For comparison the ice nucleation activity of Snomax, fungal spores, and mushrooms will be discussed as well. In the past, pollen have been rejected as important atmospheric IN, as they are not as abundant in the atmosphere as bacteria or mineral dust and are too heavy to reach higher altitudes. However, in our experiments (Pummer et al. 2011) it turned out that water, which had been in contact with pollen and then been separated from the bodies, nucleates as good as the pollen grains themselves. So the ice nuclei have to be easily-suspendable macromolecules (100-300 kDa) located on the pollen. Once extracted, they can be distributed further through the atmosphere than the heavy pollen grains and so augment the impact of pollen on ice cloud formation even in the upper troposphere. It is widely known, that material from the pollen, like allergens and sugars, can indeed leave the pollen body and be distributed independently. The most probable mechanism is the pollen grain bursting by rain, which releases

  10. Synthesis, Characterization and Biological Activities of a New Fluorescent Indicator for the Intracellular Calcium Ions

    Institute of Scientific and Technical Information of China (English)

    HE Huaizhen; LEI Lei; LI Jianli; SHI Zhen

    2009-01-01

    A novel calcium-selective fluorescent indicator Fluo-3M AM was synthesized by introduction of a methyl group into the Ca2+-chelating moiety and adequately characterized by spectral methods (1H NMR, GC-MS, IR and MALDI-TOF MS). Meanwhile, its fluorescence spectra and some biological activities have been also studied. The results indicate that the new fluorescent indicator has relatively high affinity to calcium and a strong fluorescence signal, which should be useful for biomedical researchers to investigate the effects of calcium ions in biosystems.

  11. Multifunctional and biologically active matrices from multicomponent polymeric solutions

    Science.gov (United States)

    Kiick, Kristi L. (Inventor); Yamaguchi, Nori (Inventor); Rabolt, John (Inventor); Casper, Cheryl (Inventor)

    2012-01-01

    A functionalized electrospun matrix for the controlled-release of biologically active agents, such as growth factors, is presented. The functionalized matrix comprises a matrix polymer, a compatibilizing polymer and a biomolecule or other small functioning molecule. In certain aspects the electrospun polymer fibers comprise at least one biologically active molecule functionalized with low molecular weight heparin.

  12. Spectral Characterization and Antimicrobial Activity of Some Schiff Bases Derived from 4-Methyl-2-aminophenol

    Institute of Scientific and Technical Information of China (English)

    Gurbuz, Demet; Cinarli, Adem; Tavman, Aydin; Birteksoz, A. Seher

    2012-01-01

    A series of N-(5-methyl-2-hydroxyphenyl)-(2/3/4/5-substituted)-benzaldimines (I--XlII) were synthesized us- ing appropriate synthetic route. Their structures were characterized by FT-IR, UV-Visible, ESI-MS, 1H- and 13C-NMR spectroscopic techniques and analytical methods. The crystal structure of N-(5-methyl-2-hydroxyphenyl)- 3,4-dimethoxybenzaldimine (XIII) was determined by X-ray diffraction at room temperature. Relationship between the melting points and the structures of the compounds were examined. Antibacterial activities of the compounds were evaluated against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumo- niae, Pseudomonas aeruginosa and Proteus mirabilis. Antifungal activities were reported for Candida albieans. Some of the Schiffbases showed considerable antimicrobial activity against S. aureus and C. albicans.

  13. Evaluation of airborne methyl salicylate for improved conservation biological control of two-spotted spider mite and hop aphid in Oregon hop yards

    Science.gov (United States)

    The use of synthetic herbivore-induced plant volatiles (HIPV) to attract natural enemies has received interest as a tool to enhance conservation biological control (CBC). Methyl salicylate (MeSA) is a HIPV that is attractive to several key predators of two-spotted spider mite, Tetranychus urticae K...

  14. Effects of fulvestrant on biological activity and Wnt expression in rat GH3 cells

    Institute of Scientific and Technical Information of China (English)

    Jiwei Bai; Yan Wang; Chuzhong Li; Yazhuo Zhang

    2012-01-01

    The present study investigated the influence of anti-estrogen treatment (fulvestrant) on pituitary adenoma cell line GH3 biological activity, the estrogen receptor α pathway, the WnT pathway, and mechanisms of decreased Wnt inhibitory factor-1 expression in GH3 cells. Results showed that fulvestrant suppressed GH3 cell proliferation and reduced hormone secretion in a dose-dependent manner. Estrogen receptor α and Wnt4 expression decreased, but Wnt inhibitory factor-1 expression increased in a dose-dependent manner following fulvestrant treatment, and β-catenin expression remained unchanged. Inhibitors of DNA methylation and histone modification upregulated Wnt inhibitory factor-1 expression. Results suggested that fulvestrant suppressed biological activity of GH3 cells via the estrogen receptor α and Wnt pathways. These results suggested that decreased Wnt inhibitory factor-1 expression in GH3 cells played a role in epigenetic mechanisms. Anti-estrogen therapies could provide novel treatments for growth hormone adenomas.

  15. Targeting Platinum Compounds: synthesis and biological activity

    OpenAIRE

    VAN ZUTPHEN, Steven

    2005-01-01

    Inspired by cisplatin, the inorganic drug discovered by Barnett Rosenberg in 1965, the research described in this thesis uses targeting ligands, or ligands varied in a combinatorial fashion, to find platinum complexes with more specific modes of action. These studies have lead to the development of novel (solid-phase) synthetic methods and to the discovery of several compounds with promising biological properties.

  16. Milk inhibits the biological activity of ricin

    Science.gov (United States)

    Ricin is a highly toxic protein produced by the castor plant Ricinus communis. The toxin is relatively easy to isolate and can be used as a biological weapon. There is great interest in identifying effective inhibitors for ricin. In this study, we demonstrated by three independent assays that compon...

  17. Activation of a unique flavin-dependent tRNA-methylating agent.

    Science.gov (United States)

    Hamdane, Djemel; Bruch, Eduardo; Un, Sun; Field, Martin; Fontecave, Marc

    2013-12-10

    TrmFO is a tRNA methyltransferase that uses methylenetetrahydrofolate (CH2THF) and flavin adenine dinucleotide hydroquinone as cofactors. We have recently shown that TrmFO from Bacillus subtilis stabilizes a TrmFO-CH2-FADH adduct and an ill-defined neutral flavin radical. The adduct contains a unique N-CH2-S moiety, with a methylene group bridging N5 of the isoalloxazine ring and the sulfur of an active-site cysteine (Cys53). In the absence of tRNA substrate, this species is remarkably stable but becomes catalytically competent for tRNA methylation following tRNA addition using the methylene group as the source of methyl. Here, we demonstrate that this dormant methylating agent can be activated at low pH, and we propose that this process is triggered upon tRNA addition. The reaction proceeds via protonation of Cys53, cleavage of the C-S bond, and generation of a highly reactive [FADH(N5)═CH2]+ iminium intermediate, which is proposed to be the actual tRNA-methylating agent. This mechanism is fully supported by DFT calculations. The radical present in TrmFO is characterized here by optical and EPR/ENDOR spectroscopy approaches together with DFT calculations and is shown to be the one-electron oxidized product of the TrmFO-CH2-FADH adduct. It is also relatively stable, and its decomposition is facilitated by high pH. These results provide new insights into the structure and reactivity of the unique flavin-dependent methylating agent used by this class of enzymes.

  18. Methylation impact analysis of erythropoietin (EPO) Gene to hypoxia inducible factor-1α (HIF-1α) activity.

    Science.gov (United States)

    Dewi, Firli Rahmah Primula; Fatchiyah, Fatchiyah

    2013-01-01

    Erythropoietin (EPO) is a glycoprotein hormone that play a role as key regulator in the production of red blood cells. The promoter region of EPO is methylated in normoxic (non-hypoxia) condition, but not in hypoxic condition. Methylation of the EPO enhancer region decline the transcription activity of EPO gene. The aim of this study is to investigate how different methylation percentage affected on the regulation and transcriptional activity of EPO gene. The DNA sequence of erythropoietin gene and protein sequence was retrieved from the sequence database of NCBI. DNA structure was constructed using 3D-DART web server and modeling structure of HIF1 predicted using SWISS-MODEL web server. Methylated DNA sequence of EPO gene using performed with YASARA View software and docking of EPO gene and transcription factor HIF1 analyzed by using HADDOCK webserver. Our result showed that binding energy in 46% methylated DNA was higher (-161,45 kcal/mol) than in unmethylated DNA (-194,16 kcal/mol) and 8% methylated DNA (-175,94 kcal/mol). So, we presume that a silencing mechanism of the Epo gene by methylation is correlated with the binding energy, which is required for interaction. A higher methylation percentage correlates with a higher binding energy which can cause an unstable interaction between DNA and transcription factor. In conclution, methylation of promoter and enhancer region of Epo gene leads to silencing.

  19. Biological activity of palladium(II) and platinum(II) complexes of the acetone Schiff bases of S-methyl- and S-benzyldithiocarbazate and the X-ray crystal structure of the [Pd(asme)2] (asme=anionic form of the acetone Schiff base of S-methyldithiocarbazate) complex.

    Science.gov (United States)

    Akbar Ali, Mohammad; Mirza, Aminul Huq; Butcher, Raymond J; Tarafder, M T H; Keat, Tan Boon; Ali, A Manaf

    2002-11-25

    Palladium(II) and platinum(II) complexes of general empirical formula, [M(NS)(2)] (NS=uninegatively charged acetone Schiff bases of S-methyl- and S-benzyldithiocarbazate; M=Pt(II) and Pd(II)) have been prepared and characterized by a variety of physicochemical techniques. Based on conductance, IR and electronic spectral evidence, a square-planar structure is assigned to these complexes. The crystal and molecular structure of the [Pd(asme)(2)] complex (asme=anionic form of the acetone Schiff base of S-methyldithiocarbazate) has been determined by X-ray diffraction. The complex has a distorted cis-square planar structure with the ligands coordinated to the palladium(II) ions as uninegatively charged bidentate NS chelating agents via the azomethine nitrogen and the mercaptide sulfur atoms. The distortion from a regular square-planar geometry is attributed to the restricted bite angles of the ligands. Antimicrobial tests indicate that the Schiff bases exhibit strong activities against the pathogenic bacteria, Bacillus subtilis (mutant defective DNA repair), methicillin-resistant Staphylococcus aureus, B. subtilis (wild type) and Pseudomonas aeruginosa and the fungi, Candida albicans (CA), Candida lypotica (2075), Saccharomyces cerevisiae (20341) and Aspergillus ochraceous (398)-the activities exhibited by these compounds being greater than that of the standard antibacterial and antifungal drugs, streptomycin and nystatin, respectively. The palladium(II) and platinum(II) complexes are inactive against most of these organisms but, the microbe, Pseudomonas aeruginosa shows strong sensitivity to the platinum(II) complexes. Screening of the compounds for their cytotoxicities against T-lymphoblastic leukemia cancer cells has shown that the acetone Schiff base of S-methyldithiocarbazate (Hasme) exhibits a very weak activity, whereas the S-benzyl derivative (Hasbz) is inactive. However, the palladium(II) complexes exhibit strong cytotoxicities against this cancer; their

  20. Effects of methylation status of caspase-8 promoter on antitumor activity of TRAIL to human gastric cancer cells

    Institute of Scientific and Technical Information of China (English)

    ZHANG Ru-gang; FANG Dian-chun; YANG Liu-qin; LUO Yuan-gang

    2004-01-01

    Objective: To study the effects of the methylation status of caspase-8 promoter on the antitumor activity of TRAIL to the human gastric cancer cells. Methods: The methylation of caspase-8 was measured with methylation specific PCR (MSP) and the antitomor capability of TRAIL to human gastric cancer cells was determined with MTT. Results: No methylation of caspase-8 in the human gastric cancer cells was found. The sensitivity of 5 lines of gastric cancer cells to the antitumor activity of TRAIL was different. The administration of the demethylation agent 5-Aza-2'-deoxycytidine ( 5-AzaCdR) increased the sensitivity of gastric cancer cells to TRAIL but did not change the methylation status of caspase-8 promoter in gastric cancer cells. Conclusion: 5-Aza-CdR increases the sensitivity of most of gastric cancer cells to TRAIL but caspase-8 is not involved in the antitumor activity of TRAIL.

  1. Restriction-modification system with methyl-inhibited base excision and abasic-site cleavage activities.

    Science.gov (United States)

    Fukuyo, Masaki; Nakano, Toshiaki; Zhang, Yingbiao; Furuta, Yoshikazu; Ishikawa, Ken; Watanabe-Matsui, Miki; Yano, Hirokazu; Hamakawa, Takeshi; Ide, Hiroshi; Kobayashi, Ichizo

    2015-03-11

    The restriction-modification systems use epigenetic modification to distinguish between self and nonself DNA. A modification enzyme transfers a methyl group to a base in a specific DNA sequence while its cognate restriction enzyme introduces breaks in DNA lacking this methyl group. So far, all the restriction enzymes hydrolyze phosphodiester bonds linking the monomer units of DNA. We recently reported that a restriction enzyme (R.PabI) of the PabI superfamily with half-pipe fold has DNA glycosylase activity that excises an adenine base in the recognition sequence (5'-GTAC). We now found a second activity in this enzyme: at the resulting apurinic/apyrimidinic (AP) (abasic) site (5'-GT#C, # = AP), its AP lyase activity generates an atypical strand break. Although the lyase activity is weak and lacks sequence specificity, its covalent DNA-R.PabI reaction intermediates can be trapped by NaBH4 reduction. The base excision is not coupled with the strand breakage and yet causes restriction because the restriction enzyme action can impair transformation ability of unmethylated DNA even in the absence of strand breaks in vitro. The base excision of R.PabI is inhibited by methylation of the target adenine base. These findings expand our understanding of genetic and epigenetic processes linking those in prokaryotes and eukaryotes.

  2. Adsorption of methyl orange using activated carbon prepared from lignin by ZnCl2 treatment

    Science.gov (United States)

    Mahmoudi, K.; Hamdi, N.; Kriaa, A.; Srasra, E.

    2012-08-01

    Lignocellulosic materials are good and cheap precursors for the production of activated carbon. In this study, activated carbons were prepared from the lignin at different temperatures (200 to 500°C) by ZnCl2. The effects influencing the surface area of the resulting activated carbon are activation temperature, activation time and impregnation ratio. The optimum condition, are found an impregnation ratio of 2, an activation temperature of 450°C, and an activation time of 2 h. The results showed that the surface area and micropores volume of activated carbon at the experimental conditions are achieved to 587 and 0.23 cm3 g-1, respectively. The adsorption behavior of methyl orange dye from aqueous solution onto activated lignin was investigated as a function of equilibrium time, pH and concentration. The Langmuir and Freundlich adsorption models were applied to describe the equilibrium isotherms. A maximum adsorption capacity of 300 mg g-1 of methyl orange by activated carbon was achieved.

  3. Methylation of DACT2 promotes papillary thyroid cancer metastasis by activating Wnt signaling.

    Directory of Open Access Journals (Sweden)

    Zhiyan Zhao

    Full Text Available Thyroid cancer is the most common endocrine malignant disease and the incidence is increasing. DACT2 was found frequently methylated in human lung cancer and hepatocellular carcinoma. To explore the epigenetic change and the role of DACT2 in thyroid cancer, 7 thyroid cancer cell lines, 10 cases of non-cancerous thyroid tissue samples and 99 cases of primary thyroid cancer samples were involved in this study. DACT2 was expressed and unmethylated in K1, SW579, FTC-133, TT, W3 and 8505C cell lines. Loss of expression and complete methylation was found in TPC-1 cells. Restoration of DACT2 expression was induced by 5-aza-2'deoxycytidine treatment. It demonstrates that the expression of DACT2 was regulated by promoter region methylation. In human primary papillary thyroid cancer, 64.6% (64/99 was methylated and methylation of DACT2 was related to lymph node metastasis (p<0.01. Re-expression of DACT2 suppresses cell proliferation, invasion and migration in TPC-1 cells. The activity of TCF/LEF was inhibited by DACT2 in wild-type or mutant β-catenin cells. The activity of TCF/LEF was increased by co-transfecting DACT2 and Dvl2 in wild-type or mutant β-catenin cells. Overexpression of wild-type β-catenin promotes cell migration and invasion in DACT2 stably expressed cells. The expression of β-catenin, c-myc, cyclinD1 and MMP-9 were decreased and the level of phosphorylated β-catenin (p-β-catenin was increased after restoration of DACT2 expression in TPC-1 cells. The expression of β-catenin, c-myc, cyclinD1 and MMP-9 were increased and the level of p-β-catenin was reduced after knockdown of DACT2 in W3 and SW579 cells. These results suggest that DACT2 suppresses human papillary thyroid cancer growth and metastasis by inhibiting Wnt signaling. In conclusion, DACT2 is frequently methylated in papillary thyroid cancer. DACT2 expression was regulated by promoter region methylation. DACT2 suppresses papillary thyroid cancer proliferation and metastasis

  4. Evidence for Methyl-Compound-Activated Life in Coal Bed System 2 km Below Sea Floor

    Science.gov (United States)

    Trembath-reichert, E.; Morono, Y.; Dawson, K.; Wanger, G.; Bowles, M.; Heuer, V.; Hinrichs, K. U.; Inagaki, F.; Orphan, V. J.

    2014-12-01

    IODP Expedition 337 set the record for deepest marine scientific drilling down to 2.4 kmbsf. This cruise also had the unique opportunity to retrieve deep cores from the Shimokita coal bed system in Japan with the aseptic and anaerobic conditions necessary to look for deep life. Onboard scientists prepared nearly 1,700 microbiology samples shared among five different countries to study life in the deep biosphere. Samples spanned over 1 km in sampling depths and include representatives of shale, sandstone, and coal lithologies. Findings from previous IODP and deep mine expeditions suggest the genetic potential for methylotrophy in the deep subsurface, but it has yet to be observed in incubations. A subset of Expedition 337 anoxic incubations were prepared with a range of 13C-methyl substrates (methane, methylamine, and methanol) and maintained near in situ temperatures. To observe 13C methyl compound metabolism over time, we monitored the δ13C of the dissolved inorganic carbon (by-product of methyl compound metabolism) over a period of 1.5 years. Elemental analysis (EA), ion chromatograph (IC), 13C volatile fatty acid (VFA), and mineral-associated microscopy data were also collected to constrain initial and endpoint conditions in these incubations. Our geochemical evidence suggests that the coal horizon incubated with 13C-methane showed the highest activity of all methyl incubations. This provides the first known observation of methane-activated metabolism in the deep biosphere, and suggests there are not only active cells in the deeply buried terrigenous coal bed at Shimokita, but the presence of a microbial community activated by methylotrophic compounds.

  5. Contribution of methylated exudate flavonoids to the anti-inflammatory activity of Grindelia robusta.

    Science.gov (United States)

    Krenn, Liselotte; Wollenweber, Eckhard; Steyrleuthner, Katja; Görick, Cornelia; Melzig, Matthias F

    2009-07-01

    The flavonoid pattern of an acetonic extract of Grindelia robusta Nutt. was investigated in detail. The flavonoids were enriched by CC. In addition to twelve known methylated exudate flavonols four compounds were identified for the first time in G. robusta. Several substances of the flavonoid complex, among them the main compounds quercetin-3-methylether and 6-OH-kaempferol-3,6-dimethylether, were tested for their activity to inhibit neutrophil elastase. Quercetin-3-methylether was shown to be most active with an IC(50) of 19 microM, thus obviously contributing to the anti-inflammatory activity of the drug.

  6. New Synthesis and Antiparasitic Activity of Model 5-Aryl-1-methyl-4-nitroimidazoles

    Directory of Open Access Journals (Sweden)

    Mustafa M. El-Abadelah

    2009-07-01

    Full Text Available A number of 5-aryl-1-methyl-4-nitroimidazoles 5a-f have been synthesized in good yields by the Suzuki coupling reaction between 5-chloro-1-methyl-4-nitroimidazole (3 and arylboronic acids 4a-f, aided by dichlorobis-(triphenylphosphinepalladium(II, K2CO3, and tetrabutylammonium bromide in water at 70-80 °C. Compounds 5a-f were characterized by elemental analysis, NMR and MS spectral data. On the basis of in vitro screening data, 5-(3-chlorophenyl-1-methyl-4-nitro-1H-imidazole (5fexhibited potent lethal activity against Entamoeba histolytica and Giardia intestinalis with IC50 = 1.47 µM/mL, a value lower by a factor of two than that of the standard drug, metronidazole. The boosted activity of 5f was not accompanied by any increased cytotoxicity.The rest of the series also exhibited potent antiparasitic activity with IC50 valuesin the 1.72-4.43 µM/mL range. The cytotoxicity of the derivatives 5c and 5e was increased compared to the precursor compound, metronidazole, although they remain non-cytotoxic at concentrations much higher than the antiparasitic concentration of the two derivatives.

  7. Matricryptins and matrikines: biologically active fragments of the extracellular matrix.

    Science.gov (United States)

    Ricard-Blum, Sylvie; Salza, Romain

    2014-07-01

    Numerous extracellular proteins and glycosaminoglycans (GAGs) undergo limited enzymatic cleavage resulting in the release of fragments exerting biological activities, which are usually different from those of the full-length molecules. In this review, we define matrikines and matricryptins, which are bioactive fragments released from the extracellular matrix proteins, proteoglycans and GAGs and report their major biological activities. These fragments regulate a number of physiopathological processes including angiogenesis, cancer, fibrosis, inflammation, neurodegenerative diseases and wound healing. The challenges to translate these fragments from molecules biologically active in vitro and in experimental models to potential drugs are discussed in the last part of the review.

  8. Ficus carica L. (Moraceae: Phytochemistry, Traditional Uses and Biological Activities

    Directory of Open Access Journals (Sweden)

    Shukranul Mawa

    2013-01-01

    Full Text Available This paper describes the botanical features of Ficus carica L. (Moraceae, its wide variety of chemical constituents, its use in traditional medicine as remedies for many health problems, and its biological activities. The plant has been used traditionally to treat various ailments such as gastric problems, inflammation, and cancer. Phytochemical studies on the leaves and fruits of the plant have shown that they are rich in phenolics, organic acids, and volatile compounds. However, there is little information on the phytochemicals present in the stem and root. Reports on the biological activities of the plant are mainly on its crude extracts which have been proven to possess many biological activities. Some of the most interesting therapeutic effects include anticancer, hepatoprotective, hypoglycemic, hypolipidemic, and antimicrobial activities. Thus, studies related to identification of the bioactive compounds and correlating them to their biological activities are very useful for further research to explore the potential of F. carica as a source of therapeutic agents.

  9. Biological activities of Juglans regia flowers

    Directory of Open Access Journals (Sweden)

    Seyed Fazel Nabavi

    2011-06-01

    Full Text Available Antidepressant, anti-inflammatory, antihypoxic and antioxidant activities of methanol extract of Juglans regia L., Juglandaceae, flower were investigated. Antidepressant activity was examined by forced swimming test and tail suspension test in mice. Antihypoxic activity was investigated in haemic and circulatory models. The effects were pronounced in both models. It produced statistically significant anti-inflammatory activity in carrageenan induced edema at nearly all doses, compared to control groups. IC50 for DPPH radical-scavenging activity was 674±27.6 µg mL-1. Extract showed good Fe2+ chelating ability (IC50 43±1.5 µg mL-1. It exhibited low antioxidant activity in linoleic acid peroxidation test. Its pharmacological effects may be attributed, in part, to the presence of phenols and ISSN 0102-695X flavonoids in the extract.

  10. Acid activated montmorillonite as catalysts in methyl esterification reactions of lauric acid.

    Science.gov (United States)

    Zatta, Leandro; Ramos, Luiz Pereira; Wypych, Fernando

    2012-01-01

    The catalytic activity of acid activated montmorillonite in the esterification of free fatty acids (FFA) is reported. Standard Montmorillonite (MMT) type STx-1 provided by the Clay Mineral Society repository was activated using phosphoric, nitric and sulphuric acids under different conditions and the resulting materials were characterized and evaluated as catalysts in the methyl esterification of lauric acid. Blank reactions carried out in the absence of any added catalyst presented conversions of 32.64, 69.79 and 79.23%, for alcohol:lauric acid molar ratios of 60:1, 12:1 and 6:1, respectively. In the presence of the untreated clay and using molar ratios of 12:1 and 6:1 with 12% of catalyst, conversions of 70.92 and 82.30% were obtained, respectively. For the acid activated clays, conversions up to 93.08% of lauric acid to methyl laurate were obtained, much higher than those observed for the thermal conversion or using untreated montmorillonite. Relative good correlations were observed between the catalytic activity and the development of acid sites and textural properties of the resulting materials. Therefore, a simple acid activation was able to improve the catalytic activity and produce clay catalysts that are environmental friendly, cost effective, noncorrosive and reusable.

  11. Protein complex interactor analysis and differential activity of KDM3 subfamily members towards H3K9 methylation.

    Directory of Open Access Journals (Sweden)

    Michael Brauchle

    Full Text Available Histone modifications play an important role in chromatin organization and gene regulation, and their interpretation is referred to as epigenetic control. The methylation levels of several lysine residues in histone tails are tightly controlled, and JmjC domain-containing proteins are one class of broadly expressed enzymes catalyzing methyl group removal. However, several JmjC proteins remain uncharacterized, gaps persist in understanding substrate recognition, and the integration of JmjC proteins into signaling pathways is just emerging. The KDM3 subfamily is an evolutionarily conserved group of histone demethylase proteins, thought to share lysine substrate specificity. Here we use a systematic approach to compare KDM3 subfamily members. We show that full-length KDM3A and KDM3B are H3K9me1/2 histone demethylases whereas we fail to observe histone demethylase activity for JMJD1C using immunocytochemical and biochemical approaches. Structure-function analyses revealed the importance of a single amino acid in KDM3A implicated in the catalytic activity towards H3K9me1/2 that is not conserved in JMJD1C. Moreover, we use quantitative proteomic analyses to identify subsets of the interactomes of the 3 proteins. Specific interactor candidates were identified for each of the three KDM3 subfamily members. Importantly, we find that SCAI, a known transcriptional repressor, interacts specifically with KDM3B. Taken together, we identify substantial differences in the biology of KDM3 histone demethylases, namely enzymatic activity and protein-protein interactions. Such comparative approaches pave the way to a better understanding of histone demethylase specificity and protein function at a systems level and are instrumental in identifying the more subtle differences between closely related proteins.

  12. Ellagic acid and its methyl-derivatives inhibit a newly found nitratase activity.

    Science.gov (United States)

    Léger, Claude L; Torres-Rasgado, Enrique; Fouret, Gilles; Lauret, Céline; Carbonneau, Marie-Annette

    2010-02-01

    We have recently shown that low density lipoprotein (LDL) was able to denitrate albumin-bound 3-NO(2)-Tyr residues and to concomitantly release NO(3)(-) through a Ca(2+)-dependent process that has been ascribed to a specific protein structure. A lipophilic food component (gamma-tocopherol), which is easily loaded into LDL has been found to totally inhibit denitrating activity. We presently found that ellagic acid (EA) and its methylated derivatives, 4,4'O-methyl- and 3,3'O-methyl-ellagic acids (MeEA1 and MeEA2, respectively), amphipathic phenolic components of certain fruits and beverages, were also able to inhibit this activity, with a total inhibition for EA and a 60% inhibition for MeEA1 and MeEA2. EA exhibited the highest affinity for protein plasma, whereas a higher affinity of MeEA1 and MeEA2 (with MeEA1 > MeEA2) than EA was found for lipoprotein fractions, suggesting that the inhibition-driving property is protein affinity. As a result of this nitratase-inhibition property EA and its natural metabolite MeEA2 may have a beneficial role in special physiopathological conditions.

  13. Synthesis of [3-N-(11) C-methyl]temozolomide via in situ activation of 3-N-hydroxymethyl temozolomide and alkylation with [(11) C]methyl iodide.

    Science.gov (United States)

    Eriksson, Jonas; Van Kooij, Rolph; Schuit, Robert C; Froklage, Femke E; Reijneveld, Jaap C; Hendrikse, N Harry; Windhorst, Albert D

    2015-03-01

    Temozolomide is a chemotherapeutic drug that is mainly used in the treatment of primary glioblastoma multiforme and recurrent high-grade glioma. Here, we report an efficient good manufacturing practice compliant method for the synthesis of [3-N-(11) C-methyl]temozolomide from 3-N-hydroxymethyl temozolomide that cleaves off formaldehyde in situ and becomes activated towards alkylation with [(11) C]methyl iodide. The labelling method was developed for an on-going patient study in which the predictive value of [3-N-(11) C-methyl]temozolomide and positron emission tomography on the outcome of temozolomide treatment is being investigated. The precursor was reacted with [(11) C]methyl iodide in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene in acetonitrile, heated at stepwise increasing temperature. Purification by semipreparative HPLC with pharmaceutical grade eluent and filtration gave approximately 10 mL sterile product solution ready for injection containing 1.55 ± 0.38 GBq (n = 5), the specific activity was 88 ± 25 GBq/µmol and the radiochemical purity was 98.5 ± 1.9%. (13) C-NMR spectroscopy confirmed the labelled position after colabelling with (11) C and (13) C.

  14. Synthesis of 1-isopropyl-3-acyl-5-methyl-benzimidazolone Derivatives and Their Antimicrobial Activity

    Directory of Open Access Journals (Sweden)

    Shaopeng Wei

    2013-03-01

    Full Text Available A series of N-acylated analogues of 1-isopropyl-3-acyl-5-methyl-benzimidazolone were synthesized. Bioassay results indicated that analogues 5-07 and 5-19 exhibited the most potency against Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Analogues 5-02, 5-07, 5-12, 5-15, 5-19, 5-20 and 5-25 could effectively inhibit the spore germination of Botrytis cinerea. The relationship between structure and their antimicrobial activity (SAR has also been discussed according to aliphatic acids and aromatic acids derivatives, respectively. This implied that the N-acylated derivatives of 5-methyl-benzimidazolone might be potential antimicrobial agents.

  15. Biological activities of Croton palanostigma Klotzsch

    Directory of Open Access Journals (Sweden)

    Eduardo Ferreira Mota

    2015-01-01

    Full Text Available Background: Different species of Croton are used in traditional Amazonian medicine. Among the popular uses are treatment of bacterial diseases, poorly healing wounds and fevers. Objective: This study evaluated the antileishmanial, antiplasmodial and antimicrobial activities of the extracts and diterpenes of Croton palanostigma Klotzsch (Euphorbiaceae. Materials and Methods: Leaves and bark were extracted with dichloromethane and methanol. The bark dichloromethane extract (BDE was chromatographed on a column, obtaining cordatin and aparisthman. The extracts and diterpenes were assayed thought agar disk diffusion method and their bactericidal or fungicidal effects were evaluated by minimum bactericidal or fungicidal concentration. The antiplasmodial activity was evaluated after 24 and 72 h of exposition. The antileishmanial activity was performed on promastigotes forms of Leishmania amazonensis. Results: The bark methanol extract (BME and cordatin were not active against any microbial strains tested; BDE and leaves methanol extract (LME were positive for Pseudomonas aeruginosa and aparisthman was positive for Candida albicans. In the determination of the minimum bactericidal concentration, neither of them were active in the highest concentration tested. The extracts and diterpenes were inactive in Plasmodium falciparum, except the LME in 72 h. Any extract was shown to be active in promastigote forms of L. amazonensis. Conclusion: These results indicate that the BDE and LME did not inhibit the bacterial growth, then they probably had bacteriostatic effect. LME presented activity in P. falciparum.

  16. High Resolution Screening of biologically active compounds and metabolites

    NARCIS (Netherlands)

    Kool, J.

    2007-01-01

    High Resolution Screening of biologically active compounds and metabolites Jeroen Kool Biotransformation enzymes play a crucial role in the metabolism of both endogenous compounds and xenobiotics. Usually, the detoxication of these compounds by biotransformation enzymes results in harmless metab

  17. A comparative study of efficacy of misoprostol with methyl ergometrine and carboprost in active management of third stage of labour

    Directory of Open Access Journals (Sweden)

    Pradnya A. Supe

    2016-05-01

    Conclusions: Misoprostol 800ug per rectally is an effective alternative in the active management of third stage of labor as compared to methyl ergometrine and carboprost. [Int J Reprod Contracept Obstet Gynecol 2016; 5(5.000: 1525-1531

  18. Synthesis and Biological Activity of Philanthotoxin Analogs

    Institute of Scientific and Technical Information of China (English)

    Yong An ZHANG; Ke Zhong LIU; Deng Yuan WANG; Yu Zhu WANG; Liang Jian QU; Chang Jin ZHU

    2006-01-01

    The synthesis of four analogs of philanthotoxin is described. The preliminary bioassay showed that these compounds all had good insecticidal activities, and the compound 6a had the best killing effect.

  19. Total synthesis and biological activity of natural product Urukthapelstatin A.

    Science.gov (United States)

    Lin, Chun-Chieh; Tantisantisom, Worawan; McAlpine, Shelli R

    2013-07-19

    Herein we report the first total synthesis of the natural product Urkuthaplestatin A (Ustat A) utilizing a convergent synthetic strategy. The characterization and biological activity match those of the previously published natural product. Interestingly, several intermediates, including the linear and serine cyclized precursors, show a 100-fold decrease in cytotoxicity, with IC50's in the low micromolar range. These data indicate that the rigidity and the consecutive aromatic heterocyclic system are responsible for the biological activity.

  20. Phytochemicals and Their Biological Activities of Plants in Tagetes L.

    Institute of Scientific and Technical Information of China (English)

    XU Li-wei; CHEN Juan; QI Huan-yang; SHI Yan-ping

    2012-01-01

    Tagetes L.,the genus in the family Asteraceae,consists of about 30 species spread in South and Middle America as well as Mexico.More than one hundred secondary metabolites have been obtained in phytochemical investigation on the species,some of which have potent biological activities.The advances in phytochemical studies and biological activities of the plants in Tagetes L.from 1925 to 2011 are summarized in this paper.

  1. Loss of ATRX, associated with DNA methylation pattern of chromosome end, impacted biological behaviors of astrocytic tumors

    OpenAIRE

    CAI, JINQUAN; Chen, Jing; Zhang, Wei; Yang, Pei; Zhang, Chuanbao; Li, Mingyang; Yao, Kun; Wang, Hongjun; Li, Qingbin; Jiang, Chuanlu; Jiang., Tao

    2015-01-01

    Loss of ATRX leads to epigenetic alterations, including abnormal levels of DNA methylation at repetitive elements such as telomeres in murine cells. We conducted an extensive DNA methylation and mRNA expression profile study on a cohort of 82 patients with astrocytic tumors to study whether ATRX expression was associated with DNA methylation level in astrocytic tumors and in which cellular functions it participated. We observed that astrocytic tumors with lower ATRX expression harbored higher...

  2. Cyclical DNA Methylation and Histone Changes Are Induced by LPS to Activate COX-2 in Human Intestinal Epithelial Cells

    Science.gov (United States)

    Brancaccio, Mariarita; Coretti, Lorena; Florio, Ermanno; Pezone, Antonio; Calabrò, Viola; Falco, Geppino; Keller, Simona; Lembo, Francesca; Avvedimento, Vittorio Enrico; Chiariotti, Lorenzo

    2016-01-01

    Bacterial lipopolysaccharide (LPS) induces release of inflammatory mediators both in immune and epithelial cells. We investigated whether changes of epigenetic marks, including selected histone modification and DNA methylation, may drive or accompany the activation of COX-2 gene in HT-29 human intestinal epithelial cells upon exposure to LPS. Here we describe cyclical histone acetylation (H3), methylation (H3K4, H3K9, H3K27) and DNA methylation changes occurring at COX-2 gene promoter overtime after LPS stimulation. Histone K27 methylation changes are carried out by the H3 demethylase JMJD3 and are essential for COX-2 induction by LPS. The changes of the histone code are associated with cyclical methylation signatures at the promoter and gene body of COX-2 gene. PMID:27253528

  3. Biological Activities of a Thai Luminescent Mushroom

    Directory of Open Access Journals (Sweden)

    Jiraporn BURAKORN

    2015-06-01

    Full Text Available Wild fruit bodies of luminescent mushrooms were collected from wood stumps over a period covering August to October 2011 in the Kosumpisai forest, Mahasarakham province, in the Northeast of Thailand. A study of the morphological and genetic characteristics of the luminescent mushroom suggested that it was Neonothopanus nimbi KS. The fruiting bodies and mycelium of Neonothopanus nimbi KS were assayed for their antimicrobial activities, antifungal activity, inhibitory activity against avian influenza H5N1 neuraminidase (NA, and anticancer activity, using organic solvent extracts. The results showed that only the methanol extract of mycelia was effective against Bacillus sphaericus, with the widest inhibition zone of 11.66±2.71 mm, but this was not effective against the other 3 bacteria (Pseudomonas aeruginosa, Serratia marcescens, and Escherichia coli. On the other hand, all of the fruit body extracts were inactive against all four bacteria. The ethylacetate extract of mycelia inhibited the NCI-H187 small lung cancer cell line, KB oral cavity cancer cell line, and the MCF7 breast cancer cell line, including Magnaporthe grisea and Curvularia lunata. The methanol extract of mycelia inhibited the KB oral cavity cell cancer cell line, Magnaporthe grisea, and Curvularia lunata at 96.66, 95.32 and 95.41 %, respectively. The results imply that polar extracts of mycelia are a resource of bioactive compounds, whereas extracts of fruit bodies have less inhibitory activity against cancer, phytopathogenic-fungi and H5N1 neuraminidase.

  4. Transport and biological activities of bile acids.

    Science.gov (United States)

    Zwicker, Brittnee L; Agellon, Luis B

    2013-07-01

    Bile acids have emerged as important biological molecules that support the solubilization of various lipids and lipid-soluble compounds in the gut, and the regulation of gene expression and cellular function. Bile acids are synthesized from cholesterol in the liver and eventually released into the small intestine. The majority of bile acids are recovered in the distal end of the small intestine and then returned to the liver for reuse. The components of the mechanism responsible for the recycling of bile acids within the enterohepatic circulation have been identified whereas the mechanism for intracellular transport is less understood. Recently, the ileal lipid binding protein (ILBP; human gene symbol FABP6) was shown to be needed for the efficient transport of bile acids from the apical side to the basolateral side of enterocytes in the distal intestine. This review presents an overview of the transport of bile acids between the liver and the gut as well as within hepatocytes and enterocytes. A variety of pathologies is associated with the malfunction of the bile acid transport system.

  5. Physical aspects of biological activity and cancer

    Science.gov (United States)

    Pokorný, Jiří

    2012-03-01

    Mitochondria are organelles at the boundary between chemical-genetic and physical processes in living cells. Mitochondria supply energy and provide conditions for physical mechanisms. Protons transferred across the inner mitochondrial membrane diffuse into cytosol and form a zone of a strong static electric field changing water into quasi-elastic medium that loses viscosity damping properties. Mitochondria and microtubules form a unique cooperating system in the cell. Microtubules are electrical polar structures that make possible non-linear transformation of random excitations into coherent oscillations and generation of coherent electrodynamic field. Mitochondria supply energy, may condition non-linear properties and low damping of oscillations. Electrodynamic activity might have essential significance for material transport, organization, intra- and inter-cellular interactions, and information transfer. Physical processes in cancer cell are disturbed due to suppression of oxidative metabolism in mitochodria (Warburg effect). Water ordering level in the cell is decreased, excitation of microtubule electric polar oscilations diminished, damping increased, and non-linear energy transformation shifted towards the linear region. Power and coherence of the generated electrodynamic field are reduced. Electromagnetic activity of healthy and cancer cells may display essential differences. Local invasion and metastastatic growth may strongly depend on disturbed electrodynamic activity. Nanotechnological measurements may disclose yet unknown properties and parameters of electrodynamic oscillations and other physical processes in healthy and cancer cells.

  6. Rhodiola plants: Chemistry and biological activity

    Directory of Open Access Journals (Sweden)

    Hsiu-Mei Chiang

    2015-09-01

    Full Text Available Rhodiola is a genus of medicinal plants that originated in Asia and Europe and are used traditionally as adaptogens, antidepressants, and anti-inflammatory remedies. Rhodiola plants are rich in polyphenols, and salidroside and tyrosol are the primary bioactive marker compounds in the standardized extracts of Rhodiola rosea. This review article summarizes the bioactivities, including adaptogenic, antifatigue, antidepressant, antioxidant, anti-inflammatory, antinoception, and anticancer activities, and the modulation of immune function of Rhodiola plants and its two constituents, as well as their potential to prevent cardiovascular, neuronal, liver, and skin disorders.

  7. Saponins from Swartzia langsdorffii: biological activities

    Directory of Open Access Journals (Sweden)

    Magalhães Aderbal Farias

    2003-01-01

    Full Text Available The presence of saponins and the molluscicidal activity of the roots, leaves, seeds and fruits of Swartzia langsdorffii Raddi (Leguminosae against Biomphalaria glabrata adults and eggs were investigated. The roots, seeds and fruits were macerated in 95% ethanol. These extracts exerted a significant molluscicidal activity against B. glabrata, up to a dilution of 100 mg/l. Four mixtures (A2, B2, C and D of triterpenoid oleanane type saponins were chromatographically isolated from the seed and fruit extracts. Two known saponins (1 and 2 were identified as beta-D-glucopyranosyl-[alpha-L-rhamnopyranosyl-(1->3- beta-D-glucuronopyranosyl-(1->3]-3beta-hydroxyolean-12-ene-28 -oate, and beta-D-glucopyranosyl-(1->3-beta-D-glucuronopyranosyl-(1 ->3]-3beta-hydroxyolean-12-ene-28-oate, respectively. These two saponins were present in all the mixtures, together with other triterpenoid oleane type saponins, which were shown to be less polar, by reversed-phase HPLC. The saponin identifications were based on spectral evidence, including ¹H-¹H two-dimensional correlation spectroscopy, nuclear Overhauser and exchange spectroscopy, heteronuclear multiple quantum coherence, and heteronuclear multiple-bond connectivity experiments. The toxicity of S. langsdorffii saponins to non-target organisms was prescreened by the brine shrimp lethality test.

  8. Spectroscopic and XRD characterisation of zeolite catalysts active for the oxidative methylation of benzene with methane

    Science.gov (United States)

    Adebajo, Moses O.; Long, Mervyn A.; Frost, Ray L.

    2004-03-01

    The benzene methylation with methane over zeolite catalysts was previously shown in our laboratory to require the presence of oxygen. Thus, a two-step mechanism involving the intermediate formation of methanol by partial oxidation of methane followed by the methylation of benzene with methanol in the second step, was postulated. This paper now reports the results of the characterisation of the zeolite catalysts used for the oxidative benzene methylation reaction in order to provide some information about their composition, structure, properties and their behaviour before and after the reaction. The catalysts were characterised by X-ray diffraction (XRD), inductively coupled plasma atomic emission spectroscopy (ICP-AES), X-ray fluorescence (XRF), FT-IR and solid state NMR. XRD results indicate that the crystalline structures of all the ZSM-5 and H-beta catalysts remained unchanged after batch reaction of benzene with methane over the catalysts in agreement with the observation that the catalysts recovered from the reactor could be reused without loss of activity. Elemental analyses and FT-IR data show that as the level of metal ion exchange increases, the Brönsted acid concentration decreases but this metal ion exchange does not totally remove Brönsted acidity. FT-IR results further show that only a small amount of acid sites is actually necessary for a catalyst to be active since used catalysts containing highly reduced Brönsted acidity are found to be reusable without any loss of their activity. 29Si and 27Al magic angle spinning (MAS) NMR together with FT-IR spectra also show that all the active zeolites catalysts contain some extra-framework octahedral aluminium in addition to the normal tetrahedral framework aluminium. The presence of this extra-lattice aluminium does not, however, have any adverse effect on the crystallinity of the catalysts both before and after oxidative benzene methylation reaction. There appears also to be no significant dealumination

  9. Biologically active extracts with kidney affections applications

    Science.gov (United States)

    Pascu (Neagu), Mihaela; Pascu, Daniela-Elena; Cozea, Andreea; Bunaciu, Andrei A.; Miron, Alexandra Raluca; Nechifor, Cristina Aurelia

    2015-12-01

    This paper is aimed to select plant materials rich in bioflavonoid compounds, made from herbs known for their application performances in the prevention and therapy of renal diseases, namely kidney stones and urinary infections (renal lithiasis, nephritis, urethritis, cystitis, etc.). This paper presents a comparative study of the medicinal plant extracts composition belonging to Ericaceae-Cranberry (fruit and leaves) - Vaccinium vitis-idaea L. and Bilberry (fruit) - Vaccinium myrtillus L. Concentrated extracts obtained from medicinal plants used in this work were analyzed from structural, morphological and compositional points of view using different techniques: chromatographic methods (HPLC), scanning electronic microscopy, infrared, and UV spectrophotometry, also by using kinetic model. Liquid chromatography was able to identify the specific compounds of the Ericaceae family, present in all three extracts, arbutosid, as well as specific components of each species, mostly from the class of polyphenols. The identification and quantitative determination of the active ingredients from these extracts can give information related to their therapeutic effects.

  10. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF POLYKETONES

    Institute of Scientific and Technical Information of China (English)

    Ismail A.Alkskas; Altaher M.Alhubge; Faizul Azam

    2013-01-01

    Polyketone resins have been prepared by the Friedel-Crafts polymerization of dithiophenylidenecyclopentanone (Ⅰ),dithiophenylidenecyclohexanone (Ⅱ) and dithiophenylideneacetone (Ⅲ) with adipoyl,sebacoyl and terephthaloyl dichlorides using boron trifluoride as catalyst and carbon disulphide as solvent.Polymers were characterized with IR,1H-NMR,and the results showed the presence of carbonyl of ketonic groups in the main chain.The polyketones have inherent viscosities of 0.40-0.70 dL/g.All the polymers are semicrystalline and most of them are partially soluble in most common organic solvents but freely soluble in aprotic solvents.The temperatures of 50% weight loss are as high as 185℃ to 280℃ in air,indicating that these aromatic polyketones have excellent thermal stability.All the polyketones were tested for their antimicrobial activity against bacteria and fungi.

  11. DNA methylation by CcrM activates the transcription of two genes required for the division of Caulobacter crescentus.

    Science.gov (United States)

    Gonzalez, Diego; Collier, Justine

    2013-04-01

    DNA methylation regulates many processes, including gene expression, by superimposing secondary information on DNA sequences. The conserved CcrM enzyme, which methylates adenines in GANTC sequences, is essential to the viability of several Alphaproteobacteria. In this study, we find that Caulobacter crescentus cells lacking the CcrM enzyme accumulate low levels of the two conserved FtsZ and MipZ proteins, leading to a severe defect in cell division. This defect can be compensated by the expression of the ftsZ gene from an inducible promoter or by spontaneous suppressor mutations that promote FtsZ accumulation. We show that CcrM promotes the transcription of the ftsZ and mipZ genes and that the ftsZ and mipZ promoter regions contain a conserved CGACTC motif that is critical to their activities and to their regulation by CcrM. In addition, our results suggest that the ftsZ promoter has the lowest activity when the CGACTC motif is non-methylated, an intermediate activity when it is hemi-methylated and the highest activity when it is fully methylated. The regulation of ftsZ expression by DNA methylation may explain why CcrM is essential in a subset of Alphaproteobacteria.

  12. Effects of 2'-O-methyl nucleotide substitution on EcoRI endonuclease cleavage activities.

    Directory of Open Access Journals (Sweden)

    Guojie Zhao

    Full Text Available To investigate the effect of sugar pucker conformation on DNA-protein interactions, we used 2'-O-methyl nucleotide (2'-OMeN to modify the EcoRI recognition sequence -TGAATTCT-, and monitored the enzymatic cleavage process using FRET method. The 2'-O-methyl nucleotide has a C3'-endo sugar pucker conformation different from the C2'-endo sugar pucker conformation of native DNA nucleotides. The initial reaction velocities were measured and the kinetic parameters, Km and Vmax were derived using Michaelis-Menten equation. Experimental results showed that 2'-OMeN substitutions for the EcoRI recognition sequence decreased the cleavage efficiency for A2, A3 and T4 substitutions significantly, and 2'-OMeN substitution for T5 residue inhibited the enzymatic activity completely. In contrast, substitutions for G1 and C6 could maintain the original activity. 2'-fluoro nucleic acid (2'-FNA and locked nucleic acid (LNA having similar C3'-endo sugar pucker conformation also demonstrated similar enzymatic results. This position-dependent enzymatic cleavage property might be attributed to the phosphate backbone distortion caused by the switch from C2'-endo to C3'-endo sugar pucker conformation, and was interpreted on the basis of the DNA-EcoRI structure. These 2'-modified nucleotides could behave as a regulatory element to modulate the enzymatic activity in vitro, and this property will have potential applications in genetic engineering and biomedicine.

  13. Photo-activated biological processes as quantum measurements

    CERN Document Server

    Imamoglu, Atac

    2014-01-01

    We outline a framework for describing photo-activated biological reactions as generalized quantum measurements of external fields, for which the biological system takes on the role of a quantum meter. By using general arguments regarding the Hamiltonian that describes the measurement interaction, we identify the cases where it is essential for a complex chemical or biological system to exhibit non-equilibrium quantum coherent dynamics in order to achieve the requisite functionality. We illustrate the analysis by considering measurement of the solar radiation field in photosynthesis and measurement of the earth's magnetic field in avian magnetoreception.

  14. Biological activities of radiation-degraded carrageenan

    Energy Technology Data Exchange (ETDEWEB)

    Relleve, Lorna; Dela Rosa, Alumanda; ABAD, Lucille; Aranilla, Charito; Aliganga, Anne Kathrina [Philippine Nuclear Research Institute, Quezon City (Philippines); Yoshii, Fumio; Kume, Tamikazu; Nagasawa, Naotsugu [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment

    2001-03-01

    Carrageenans were irradiated in solid state to doses 50-1000 kGy in air at ambient temperature. Changes in their molecular weight and functional properties with respect to their FT-IR and UV spectra were evaluated. Irradiation of carrageenans resulted in a rapid decrease of molecular weight indicating main chain scission in their polymeric structures. Formations of some compounds were evident by new absorption peaks in their UV and FT-IR spectra and quantitative analyses of the FT-IR spectra which, in addition, support that there is a breakdown in the carrageenan structure. Irradiated carrageenans were investigated for their plant growth-promoting activity. Carrageenans were added to the nutrient solutions for rice seedlings under non-circulating hydroponics cultivation. Irradiated carrageenan induced weight gain in treated rice seedlings. Maximum weight gain was obtained with KC irradiated at 100 kGy while treatment with IC at 500 kGy. IC exhibited less growth promoting properties than KC. The growth of fungi on the roots disappeared with treatment of IC and KC irradiated at 500 kGy. Growth promotion of some leafy vegetables was also observed with application of degraded KC. The carrageenan molecule has been broken down to smaller molecule (s) or compound (s) that can be absorbed effectively as nourishment factors and anti-microbial agents by plants. (author)

  15. Biological activity of diterpenoids isolated from Anatolian Lamiaceae Plants

    Directory of Open Access Journals (Sweden)

    Gülaçtı Topçu

    2007-05-01

    Full Text Available In this study, antibacterial, antifungal, antimycobacterial, cytotoxic, antitumor, cardiovascular, antifeedant, insecticidal, antileishmanial and some other single activities of diterpenoids and norditerpenoids isolated from Turkish Lamiaceae plants, are reviewed. The diterpenoids were isolated from species of Salvia, Sideritis, and Ballota species growing in Anatolia. Fifty abietanes, ten kaurenes, seven pimaranes, six labdanes with their biological activities were reported. While twenty five diterpenoids showed antibacterial activity, eight of which showed activity against fungi. The most cytotoxic one was found to be taxodione (44 isolated from species of Salvia. Antifeedant, insecticidal and insect repellent activity of kaurenes, antimycobacterial activity and cardioactivity of abietanes and norabietanes together with labdanes were also reported.

  16. 1-Methyl-3-octylimidazolium Chloride—Sorption and Primary Biodegradation Analysis in Activated Sewage Sludge

    Directory of Open Access Journals (Sweden)

    Monika Paszkiewicz

    2009-11-01

    Full Text Available Ionic liquids (ILs are known to be non-volatile and thus to have low potential for atmospheric contamination or intoxication of humans by inhalation. However ILs have the potential to contaminate soil and water as they might be water soluble and can be sorbed onto solids. The investigation of possible natural ways of reducing the concentration of ILs in the environment is of high importane, especially because the requirement for biodegradable chemicals increases, together with pressure for reduction of incineration and landfill waste. It was found that the upper concentration threshold for primary biodegradation of 1-methyl-3-octylimidazolium chloride is 0.2 mM. At higher concentrations the dehydrogenase activity of the cells dropped markedly, indicating that the IL inhibits cell activity. This concentration is in good agreement with the minimal inhibitory concentration of the same compound found for a series of bacteria and fungi by this research group. The sorption of 1-methyl-3-octylimidazolium chloride was found to be significant, and the sorption coefficient was determined to be 98.2 L kg-1.

  17. Characteristics of Nonafluorobutyl Methyl Ether (NFE) Adsorption onto Activated Carbon Fibers and Different-Size-Activated Carbon Particles.

    Science.gov (United States)

    Tanada; Kawasaki; Nakamura; Araki; Tachibana

    2000-08-15

    The characteristics of adsorption of 1,1,1,2,2,3,3,4,4-nonafluorobutyl methyl ether (NFE), a chlorofluorocarbon (CFC) replacement, onto six different activated carbon; preparations (three activated carbon fibers and three different-sized activated carbon particles) were investigated to evaluate the interaction between activated carbon surfaces and NFE. The amount of NFE adsorbed onto the three activated carbon fibers increased with increasing specific surface area and pore volume. The amount of NFE adsorbed onto the three different-sized-activated carbon particles increased with an increase in the particle diameter of the granular activated carbon. The differential heat of the NFE adsorption onto three activated carbon fibers depended on the porosity structure of the activated carbon fibers. The adsorption rate of NFE was also investigated in order to evaluate the efficiency of NFE recovery by the activated carbon surface. The Sameshima equation was used to obtain the isotherms of NFE adsorption onto the activated carbon fibers and different-sized-activated carbon particles. The rate constant k for NFE adsorption onto activated carbon fibers was larger for increased specific surface area and pore volume. The rate of NFE adsorption on activated carbons of three different particle sizes decreased with increasing particle diameter at a low initial pressure. The adsorption isotherms of NFE for the six activated carbons conformed to the Dubinin-Radushkevich equation; the constants BE(0) (the affinity between adsorbate and adsorbent) and W(0) (the adsorption capacity) were calculated. These results indicated that the interaction between the activated carbon and NFE was larger with the smaller specific surface area of the activated carbon fibers and with the smaller particle diameter of the different-sized-activated carbon particles. The degree of packing of NFE in the pores of the activated carbon fibers was greater than that in the pores of the granular activated

  18. N-methyl-D-aspartate receptor encephalitis mediates loss of intrinsic activity measured by functional MRI.

    Science.gov (United States)

    Brier, Matthew R; Day, Gregory S; Snyder, Abraham Z; Tanenbaum, Aaron B; Ances, Beau M

    2016-06-01

    Spontaneous brain activity is required for the development and maintenance of normal brain function. Many disease processes disrupt the organization of intrinsic brain activity, but few pervasively reduce the amplitude of resting state blood oxygen level dependent (BOLD) fMRI fluctuations. We report the case of a female with anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis, longitudinally studied during the course of her illness to determine the contribution of NMDAR signaling to spontaneous brain activity. Resting state BOLD fMRI was measured at the height of her illness and 18 weeks following discharge from hospital. Conventional resting state networks were defined using established methods. Correlation and covariance matrices were calculated by extracting the BOLD time series from regions of interest and calculating either the correlation or covariance quantity. The intrinsic activity was compared between visits, and to expected activity from 45 similarly aged healthy individuals. Near the height of the illness, the patient exhibited profound loss of consciousness, high-amplitude slowing of the electroencephalogram, and a severe reduction in the amplitude of spontaneous BOLD fMRI fluctuations. The patient's neurological status and measures of intrinsic activity improved following treatment. We conclude that NMDAR-mediated signaling plays a critical role in the mechanisms that give rise to organized spontaneous brain activity. Loss of intrinsic activity is associated with profound disruptions of consciousness and cognition.

  19. Biological Activity of Curcuminoids Isolated from Curcuma longa

    Directory of Open Access Journals (Sweden)

    Simay Çıkrıkçı

    2008-04-01

    Full Text Available Curcumin is the most important fraction of turmeric which is responsible for its biological activity. In this study, isolation and biological assessment of turmeric and curcumin have been discussed against standard bacterial and mycobacterial strains such as E.coli , S.aureus, E.feacalis, P.aeuroginosa, M.smegmatis, M.simiae, M.kansasii, M. terrae, M.szulgai and the fungi Candida albicans. The antioxidant activity of curcumin and turmeric were also determined by the CUPRAC method.

  20. Biological Activity of Aminophosphonic Acids and Their Short Peptides

    Science.gov (United States)

    Lejczak, Barbara; Kafarski, Pawel

    The biological activity and natural occurrence of the aminophosphonic acids were described half a century ago. Since then the chemistry and biology of this class of compounds have developed into the separate field of phosphorus chemistry. Today it is well acknowledged that these compounds possess a wide variety of promising, and in some cases commercially useful, physiological activities. Thus, they have found applications ranging from agrochemical (with the herbicides glyphosate and bialaphos being the most prominent examples) to medicinal (with the potent antihypertensive fosinopril and antiosteoporetic bisphosphonates being examples).

  1. Chemical Structure-Biological Activity Models for Pharmacophores’ 3D-Interactions

    Directory of Open Access Journals (Sweden)

    Mihai V. Putz

    2016-07-01

    Full Text Available Within medicinal chemistry nowadays, the so-called pharmaco-dynamics seeks for qualitative (for understanding and quantitative (for predicting mechanisms/models by which given chemical structure or series of congeners actively act on biological sites either by focused interaction/therapy or by diffuse/hazardous influence. To this aim, the present review exposes three of the fertile directions in approaching the biological activity by chemical structural causes: the special computing trace of the algebraic structure-activity relationship (SPECTRAL-SAR offering the full analytical counterpart for multi-variate computational regression, the minimal topological difference (MTD as the revived precursor for comparative molecular field analyses (CoMFA and comparative molecular similarity indices analysis (CoMSIA; all of these methods and algorithms were presented, discussed and exemplified on relevant chemical medicinal systems as proton pump inhibitors belonging to the 4-indolyl,2-guanidinothiazole class of derivatives blocking the acid secretion from parietal cells in the stomach, the 1-[(2-hydroxyethoxy-methyl]-6-(phenylthiothymine congeners’ (HEPT ligands antiviral activity against Human Immunodeficiency Virus of first type (HIV-1 and new pharmacophores in treating severe genetic disorders (like depression and psychosis, respectively, all involving 3D pharmacophore interactions.

  2. Chemical Structure-Biological Activity Models for Pharmacophores’ 3D-Interactions

    Science.gov (United States)

    Putz, Mihai V.; Duda-Seiman, Corina; Duda-Seiman, Daniel; Putz, Ana-Maria; Alexandrescu, Iulia; Mernea, Maria; Avram, Speranta

    2016-01-01

    Within medicinal chemistry nowadays, the so-called pharmaco-dynamics seeks for qualitative (for understanding) and quantitative (for predicting) mechanisms/models by which given chemical structure or series of congeners actively act on biological sites either by focused interaction/therapy or by diffuse/hazardous influence. To this aim, the present review exposes three of the fertile directions in approaching the biological activity by chemical structural causes: the special computing trace of the algebraic structure-activity relationship (SPECTRAL-SAR) offering the full analytical counterpart for multi-variate computational regression, the minimal topological difference (MTD) as the revived precursor for comparative molecular field analyses (CoMFA) and comparative molecular similarity indices analysis (CoMSIA); all of these methods and algorithms were presented, discussed and exemplified on relevant chemical medicinal systems as proton pump inhibitors belonging to the 4-indolyl,2-guanidinothiazole class of derivatives blocking the acid secretion from parietal cells in the stomach, the 1-[(2-hydroxyethoxy)-methyl]-6-(phenylthio)thymine congeners’ (HEPT ligands) antiviral activity against Human Immunodeficiency Virus of first type (HIV-1) and new pharmacophores in treating severe genetic disorders (like depression and psychosis), respectively, all involving 3D pharmacophore interactions. PMID:27399692

  3. Design, structural and spectroscopic elucidation, and the in vitro biological activities of new diorganotin dithiocarbamates.

    Science.gov (United States)

    Ferreira, Isabella P; de Lima, Geraldo M; Paniago, Eucler B; Rocha, Willian R; Takahashi, Jacqueline A; Pinheiro, Carlos B; Ardisson, José D

    2012-12-01

    The reaction of 2,2-dimethoxy-N-methylethyllamine or 2-methyl-1,3-dioxolane with CS(2) in alkaline media produced two novel dithiocarbamate salts. Subsequent reactions with organotin halides yielded six new complexes: [SnMe(2){S(2)CNR(R(1))(2)}(2)] (1), [Sn(n-Bu)(2){S(2)CNR(R(1))(2)}(2)] (2), [SnPh(2){S(2)CNR(R(1))(2)}(2)] (3), [SnMe(2){S(2)CNR(R(2))(2)}(2)] (4), [Sn(n-Bu)(2){S(2)CNR(R(2))(2)}(2)] (5), [SnPh(2){S(2)CNR(R(2))(2)}(2)] (6), where R = methyl, R(1) = CH(2)CH(OMe)(2), and R(2) = 2-methyl-1,3-dioxolane. All compounds were identified in terms of infrared, (1)H and (13)C NMR, and the complexes were also characterized using (119)Sn NMR, (119)Sn Mössbauer and X-ray crystallography. The biological activity of all derivatives has been screened in terms of IC(90) and IC(50) against Aspergillus flavus, Aspergillus niger, Aspergillus parasiticus, Penicillium citrinum, Curvularia senegalensis, Staphylococcus aureus, Listeria monocytogenes, Bacillus cereus, Streptococcus sanguinis, Escherichia coli, Citrobacter freundii, Salmonella typhimurium, and Pseudomonas aeruginosa and the results correlated well with a performed study of structure-activity relationship (SAR). Complexes (3), (5) and (6) displayed the best IC(90) and IC(50) in the presence of the fungi, greater than that of miconazole, used as control drug.

  4. Biological function of activation-induced cytidine deaminase (AID

    Directory of Open Access Journals (Sweden)

    Ritu Kumar

    2014-10-01

    Full Text Available Activation-induced Cytidine Deaminase (AID is an essential regulator of B cell diversification, but its full range of action has until recently been an enigma. Based on homology, it was originally proposed to be an RNA-editing enzyme, but so far, no RNA substrates are known. Rather, it functions by deaminating cytidine, and in this manner, coupled with base-excision repair or mismatch repair machinery, it is a natural mutator. This allows it to play a central role in adaptive immunity, whereby it initiates the processes of class switch recombination and somatic hypermutation to help generate a diverse and high-affinity repertoire of immunoglobulin isotypes. More recently, it has been appreciated that methylated cytidine, already known as a key epigenetic mark on DNA controlling gene expression, can also be a target for AID modification. Coupled with repair machinery, this can facilitate the active removal of methylated DNA. This activity can impact the process of cellular reprogramming, including transition of a somatic cell to pluripotency, which requires major reshuffling of epigenetic memory. Thus, seemingly disparate roles for AID in controlling immune diversity and epigenetic memory have a common mechanistic basis. However, the very activity that is so useful for B cell diversity and cellular reprogramming is dangerous for the integrity of the genome. Thus, AID expression and activity is tightly regulated, and deregulation is associated with diseases including cancer. Here, we review the range of AID functions with a focus on its mechanisms of action and regulation. Major questions remain to be answered concerning how and when AID is targeted to specific loci and how this impacts development and disease.

  5. Biological function of activation-induced cytidine deaminase (AID).

    Science.gov (United States)

    Kumar, Ritu; DiMenna, Lauren J; Chaudhuri, Jayanta; Evans, Todd

    2014-01-01

    Activation-induced Cytidine Deaminase (AID) is an essential regulator of B cell diversification, but its full range of action has until recently been an enigma. Based on homology, it was originally proposed to be an RNA-editing enzyme, but so far, no RNA substrates are known. Rather, it functions by deaminating cytidine, and in this manner, coupled with base-excision repair or mismatch repair machinery, it is a natural mutator. This allows it to play a central role in adaptive immunity, whereby it initiates the processes of class switch recombination and somatic hypermutation to help generate a diverse and high-affinity repertoire of immunoglobulin isotypes. More recently, it has been appreciated that methylated cytidine, already known as a key epigenetic mark on DNA controlling gene expression, can also be a target for AID modification. Coupled with repair machinery, this can facilitate the active removal of methylated DNA. This activity can impact the process of cellular reprogramming, including transition of a somatic cell to pluripotency, which requires major reshuffling of epigenetic memory. Thus, seemingly disparate roles for AID in controlling immune diversity and epigenetic memory have a common mechanistic basis. However, the very activity that is so useful for B cell diversity and cellular reprogramming is dangerous for the integrity of the genome. Thus, AID expression and activity is tightly regulated, and deregulation is associated with diseases including cancer. Here, we review the range of AID functions with a focus on its mechanisms of action and regulation. Major questions remain to be answered concerning how and when AID is targeted to specific loci and how this impacts development and disease.

  6. Recent progress in biological activities of synthesized phenothiazines.

    Science.gov (United States)

    Pluta, Krystian; Morak-Młodawska, Beata; Jeleń, Małgorzata

    2011-08-01

    This review summarizes recent medicinal chemistry investigations in vitro and in vivo in search for new phenothiazines of promising biological activities. New phenothiazine derivatives (over 50 main structures) contain dialkylaminoalkyl, cycloaminoalkyl and aminoalkyl substituents and their acyl and sulfonyl derivatives, and other substituents with varied the monocyclic (pyrazole, thiazole, oxadiazole, thiadiazole, tetrazole) and bicyclic (quinolizine, pyrazolopyrimidine, thiazolopyridine, azabicyclononane and spiro[chromanpyrimidine] heterocycles linked directly or via the alkyl chain with the thiazine nitrogen atom or with the benzene ring. The modifications of the tricyclic ring system with the bicyclic homoaromatic ring (naphthalene) and monocyclic and bicyclic azine rings (pyridine, pyrimidine, pyrazine and quinoline) led to compounds of significant biological activities. Recently obtained phenothiazines exhibit promising antibacterial, antifungal, anticancer, antiviral, anti-inflammatory, antimalarial, antifilarial, trypanocidal, anticonvulsant, analgesic, immunosuppressive and multidrug resistance reversal properties. These activities were the results of the actions of phenothiazines on biological systems via the interaction of the pharmacophoric substituent (in some cases of strict length), via the interaction of the multicyclic ring system (π-π interaction, intercalation in DNA) and via the lipophilic character allowing the penetration through the biological membranes. The activities were examined by using various biological systems such as cell lines, bacteria, viruses, parasites, laboratory mice, rats and rabbits, and monolayer and bilayer membranes. Some mechanisms of the actions are discussed. This review shows current tendency in the phenothiazine synthesis (without synthetic routes) and reveals the phenothiazine core to be very potent pharmacophoric moiety which can be a rich source of new compounds having desirable biological activities.

  7. RELATIONSHIP BETWEEN THE PATTERN OF METHYLATION OF CALCITONIN GENE AND ACTIVITY OF METHYLTRANSFERASE in 8 Tumor Cell Lines

    Institute of Scientific and Technical Information of China (English)

    BAI; Zhi-yong

    2001-01-01

    [1]Baylin SB, Fearon ER, Vogeletein B, et al. Hyper- methylation of 5' the region of the calcitonin gene is a property of human lymphoid and acute myeloid malignancies [J]. Blood 1987; 70:412.[2]Nelkin BD, Przepiorka D, Burke PJ, et al. Abnormal methylation of the calcitonin gene marks progression of chronic myelogenous leukemia [J]. Blood 1991; 77: 2431.[3]Ritter M, Kant EDe, Huhn D, et al. Detection of DNA methylation in the calcitonin gene in human leukemias using differential polymerase chain reaction [J]. Leukemia 1995; 9:915.[4]Wu SL, Xie GL, Bai RK, et al. Semi-quantitative study of calcitonin gene methylation in myelodysplastic syndrome [J]. Chin Med J 1998; 111:690.[5]Admas RL, Rinaldi A, Seivwright CA. Microassay for DNA methyltranferase [J]. J Biochem Biophys Methods 1991; 22:19.[6]Bai ZY, Xu GB, Wu SL. Detection of DNA- methyl- tranferase activity of leukemia cells with radiology microassay [J]. J Beijing Med Univ 2000; 32:76.[7]Issa J, Veritino PM, Wu J, et al. Increased cytosine DNA- Methyltranferase activity during colon cancer pro- gression [J]. J Natl Cancer Inst 1993; 85:1235.[8]Vertino PM, Yen RW, Gao J, et al. De novo methylation of CpG islands sequences in human fibroblasts overexpression DNA (cytosine-5-) methyltranferase [J]. Mol cell Bio 1996; 16:4555.[9]Robertson KD, Uzvolgyi E, Liang G, et al. The human DNA methyltranferase (DNMTs) 1, 3a and 3b: coordinate mRNA expression in normal tissue and overexpression in tumors [J]. Nucleic Acids Res 1999; 27:2291.[10]Okano M, Bell DW, Haber DA, et al. DNA methyl- tranferases Dnmt3a and Dnmt3b are essential for de novo methylation and mammalian development [J]. Cell 1999; 99:247.

  8. Microwave assisted synthesis and biological activity of novel coumarinyltriazolothiadiazoles

    Directory of Open Access Journals (Sweden)

    Kumar P

    2010-01-01

    Full Text Available A series of new 3-(4-methylcoumarinyl-7-oxymethyl-6-substitutedphenyl-5,6-dihydro-s-triazolo (3,4-b(1,3,4-thiadiazoles 2(a-j have been synthesized by reacting 5-(4-methyl coumarinyl-7-oxymethyl-4-amino-3-mercapto(4H-1,2,4-triazole with various aromatic aldehydes by microwave assisted organic synthesis. The structure of the compounds 2 (a-j has been confirmed by IR, 1 H NMR and mass spectral data. All the compounds were screened for antimicrobial and antioxidant activity. Among the compounds tested, compounds 2d (4-dimethyl amino phenyl derivative and 2h (3,4-dimethoxy phenyl derivative showed better antimicrobial and antioxidant activity than rest of the compounds in the series.

  9. Gemini ester quat surfactants and their biological activity.

    Science.gov (United States)

    Łuczyński, Jacek; Frąckowiak, Renata; Włoch, Aleksandra; Kleszczyńska, Halina; Witek, Stanisław

    2013-03-01

    Cationic gemini surfactants are an important class of surface-active compounds that exhibit much higher surface activity than their monomeric counterparts. This type of compound architecture lends itself to the compound being easily adsorbed at interfaces and interacting with the cellular membranes of microorganisms. Conventional cationic surfactants have high chemical stability but poor chemical and biological degradability. One of the main approaches to the design of readily biodegradable and environmentally friendly surfactants involves inserting a bond with limited stability into the surfactant molecule to give a cleavable surfactant. The best-known example of such a compound is the family of ester quats, which are cationic surfactants with a labile ester bond inserted into the molecule. As part of this study, a series of gemini ester quat surfactants were synthesized and assayed for their biological activity. Their hemolytic activity and changes in the fluidity and packing order of the lipid polar heads were used as the measures of their biological activity. A clear correlation between the hemolytic activity of the tested compounds and their alkyl chain length was established. It was found that the compounds with a long hydrocarbon chain showed higher activity. Moreover, the compounds with greater spacing between their alkyl chains were more active. This proves that they incorporate more easily into the lipid bilayer of the erythrocyte membrane and affect its properties to a greater extent. A better understanding of the process of cell lysis by surfactants and of their biological activity may assist in developing surfactants with enhanced selectivity and in widening their range of application.

  10. Evaluation of the Antidepressant Activity, Hepatotoxicity and Blood Brain Barrier Permeability of Methyl Genipin

    Directory of Open Access Journals (Sweden)

    Xin Che

    2016-07-01

    Full Text Available Geniposide (GE is the main bioactive component of Gardeniae Fructus. The hepatotoxicity of geniposide limited clinical application. In order to get a new geniposide derivative that has less hepatotoxicity and still possesses the antidepressant activity, a new C-1 hydroxyl methylation derivative named methyl genipin (MG was synthesized from geniposide. In the present study, we demonstrated that MG did not increase the liver index, alanine aminotransferase (ALT and aspirate aminotransferase (AST. Histopathological examination suggested that no toxic damages were observed in rats treated orally with MG (0.72 mmol/kg. More importantly, a 7-day treatment with MG at 0.13, 0.26, and 0.52 mmol/kg/day could reduce the duration of immobility. It showed that the antidepressant-like effects of MG were similar to GE in the tail suspension test and the forced swim test. Furthermore, we found MG could be detected in the brain homogenate of mice treated orally with MG 0.52 mmol/kg/day for 1 day by HPLC. The area under the curve (AUC of MG in the brain homogenate was enhanced to 21.7 times that of GE. The brain amount and distribution speed of MG were improved significantly after oral administration. This study demonstrated that MG possessed the antidepressant effects and could cross the blood–brain barrier, but had less hepatotoxicity.

  11. Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity.

    Science.gov (United States)

    Cross, R Matthew; Monastyrskyi, Andrii; Mutka, Tina S; Burrows, Jeremy N; Kyle, Dennis E; Manetsch, Roman

    2010-10-14

    Since the 1940s endochin and analogues thereof were known to be causal prophylactic and potent erythrocytic stage agents in avian models. Preliminary screening in a current in vitro assay identified several 4(1H)-quinolones with nanomolar EC(50) against erythrocytic stages of multidrug resistant W2 and TM90-C2B isolates of Plasmodium falciparum. Follow-up structure-activity relationship (SAR) studies on 4(1H)-quinolone analogues identified several key features for biological activity. Nevertheless, structure-property relationship (SPR) studies conducted in parallel revealed that 4(1H)-quinolone analogues are limited by poor solubilities and rapid microsomal degradations. To improve the overall efficacy, multiple 4(1H)-quinolone series with varying substituents on the benzenoid quinolone ring and/or the 3-position were synthesized and tested for in vitro antimalarial activity. Several structurally diverse 6-chloro-2-methyl-7-methoxy-4(1H)-quinolones with EC(50) in the low nanomolar range against the clinically relevant isolates W2 and TM90-C2B were identified with improved physicochemical properties while maintaining little to no cross-resistance with atovaquone.

  12. Methyl-β-cyclodextrin enhanced biodegradation of polycyclic aromatic hydrocarbons and associated microbial activity in contaminated soil

    Institute of Scientific and Technical Information of China (English)

    Mingming Sun; Yongming Luo; Peter Christie; Zhongjun Jia; Zhengao Li; Ying Teng

    2012-01-01

    The contamination of soils by polycyclic aromatic hydrocarbons (PAHs) is a widespread environmental problem and the remediation of PAHs from these areas has been a major concern.The effectiveness of many in situ bioremediation systems may be constrained by low contaminant bipavailability due to limited aqueous solubility or a large magnitude of sorption.The objective of this research was to evaluate the effect of methyl-β-cyclodextrin (MCD) on bioaugmentation by Paracoccus sp.strain HPD-2 of an aged PAH-contaminated soil.When 10% (W/W) MCD amendment was combined with bioaugmentation by the PAH-degrading bacterium Paracoccus sp.strain HPD-2,the percentage degradation of total PAHs was significantly enhanced up to 34.8%.Higher counts of culturable PAH-degrading bacteria and higher soil dehydrogenase and soil polyphenol oxidase activities were observed in 10% (W/W) MCD-assisted bioaugmentation soil.This MCD-assisted bioaugmentation strategy showed significant increases (p < 0.05) in the average well color development (AWCD) obtained by the BIOLOG Eco plate assay,Shannon-Weaver index (H) and Simpson index (λ) compared with the controls,implying that this strategy at least partially restored the microbiological functioning of the PAH-contaminated soil.The results suggest that MCD-aided bioaugmentation by Paracoccus sp.strain HPD-2 may be a promising practical bioremediation strategy for aged PAH-contaminated soils.

  13. TRIAZOLE: A POTENTIAL BIOACTIVE AGENT (SYNTHESIS AND BIOLOGICAL ACTIVITY)

    OpenAIRE

    Pandeya Surendra Nath; Pathak Ashish; Mishra Rupesh

    2011-01-01

    Azoles belong to very important class of Antimicrobial drugs. Triazole is very important Azole which exists in two isomeric forms namely 1, 2, 3-Triazole and 1, 2, 4-Triazole. This Review Article covers the Different approaches to synthesize Triazoles having different substitution and their different biological activity. This Review article can be useful to synthesize new compounds having Triazole nucleolus.

  14. Biologically active substances produced by antarctic cryptoendolithic fungi.

    Science.gov (United States)

    Ocampo-Friedmann, R; Friedmann, E I

    1993-01-01

    Researchers report results of laboratory studies of over 200 microbial strains of fungi, algae, cyanobacteria, and heterotrophic bacteria collected in the Ross Desert region of Antarctica. All of the 35 fungal strains produced substances that inhibited the growth of cyanobacteria and algae. The inhibitory effect of the biologically active substance was evident in crushed cell extract but less in spent broth.

  15. Aspartate and glutamate mimetic structures in biologically active compounds.

    Science.gov (United States)

    Stefanic, Peter; Dolenc, Marija Sollner

    2004-04-01

    Glutamate and aspartate are frequently recognized as key structural elements for the biological activity of natural peptides and synthetic compounds. The acidic side-chain functionality of both the amino acids provides the basis for the ionic interaction and subsequent molecular recognition by specific receptor sites that results in the regulation of physiological or pathophysiological processes in the organism. In the development of new biologically active compounds that possess the ability to modulate these processes, compounds offering the same type of interactions are being designed. Thus, using a peptidomimetic design approach, glutamate and aspartate mimetics are incorporated into the structure of final biologically active compounds. This review covers different bioisosteric replacements of carboxylic acid alone, as well as mimetics of the whole amino acid structure. Amino acid analogs presented include those with different distances between anionic moieties, and analogs with additional functional groups that result in conformational restriction or alternative interaction sites. The article also provides an overview of different cyclic structures, including various cycloalkane, bicyclic and heterocyclic analogs, that lead to conformational restriction. Higher di- and tripeptide mimetics in which carboxylic acid functionality is incorporated into larger molecules are also reviewed. In addition to the mimetic structures presented, emphasis in this article is placed on their steric and electronic properties. These mimetics constitute a useful pool of fragments in the design of new biologically active compounds, particularly in the field of RGD mimetics and excitatory amino acid agonists and antagonists.

  16. Polysaccharies of higher fungi: Biological role, structure and antioxidative activity

    NARCIS (Netherlands)

    Kozarski, M.S.; Klaus, A.; Niksic, M.; Griensven, van L.J.L.D.; Vrvic, M.M.; Jakovljevic, D.M.

    2014-01-01

    The fungal polysaccharides attract a lot of attention due to their multiple challenging bio-logical properties, such as: anti-tumor, anti-viral, anticomplementary, anticoagulant, hypo-lipidemic, immunomodulatory and immune-stimulatory activities, which all together make them suitable for application

  17. Solar Energy Education. Renewable energy activities for biology

    Energy Technology Data Exchange (ETDEWEB)

    1982-01-01

    An instructional aid for teachers is presented that will allow biology students the opportunity to learn about renewable energy sources. Some of the school activities include using leaves as collectors of solar energy, solar energy stored in wood, and a fuel value test for green and dry woods. A study of organic wastes as a source of fuel is included. (BCS)

  18. Occurrence, biological activity and synthesis of drimane sesquiterpenoids

    NARCIS (Netherlands)

    Jansen, B.J.M.; Groot, de Æ.

    2004-01-01

    In this review the names, structures and occurrence of all new drimanes and rearranged drimanes, which have been published between January 1990 and January 2003 have been collected. Subjects that have been treated are biosynthesis, analysis, biological activities, with special attention to cytotoxic

  19. Core shell methyl methacrylate chitosan nanoparticles: In vitro mucoadhesion and complement activation

    Directory of Open Access Journals (Sweden)

    F Atyabi

    2011-10-01

    Full Text Available Background and the purpose of the study: Studies show that chitosan nanoparticles increase mucoadhesivity and penetration of large molecules across mucosal surface. The aim of the present study was to investigate the use of thiolated chitosan in the development of polysaccharide-coated nanoparticles in order to confer specific functionality to the system. Methods: Methyl methacrylate nanoparticles were coated with thiolated chitosan using a radical polymerization method. Thiolation was carried out using glutathione (GSH to improve mucoadhesivity and permeation enhancing properties of chitosan. Mucoadhesion studies were carried out by calculating the amount of mucin adsorbed on nanoparticles in a specific period of time. Complement consumption was assessed in human serum (HS by measurement of the hemolytic capacity of the complement system after contact with nanoparticles.   Results:   The FT-IR and 1HNMR spectra both confirmed the synthesis and showed the conjugation of thiolated chitosan to methyl methacrylate (MMA homopolymer. Nanoparticles were spherical having a mean diameter within the range of about 334-650 nm and their positive zeta potential values indicated the presence of the cationic polysaccharide at the nanoparticle surface. Increasing the amount of thiolated chitosan led to mucoadhesivity and complement activation. However there was not dose dependent correlation between these phenomenons and the absence of thiolated chitosan led to particles with larger size, and without ability to activate complement process. Major conclusion: It can be concluded that nanoparticles could be used for the mucosal delivery of peptides and proteins. Results show that the thiolated chitosan had higher mucoadhesion and complement activation than unmodified chitosan.

  20. Biologically Active Substances of Plants from Sali x L. Genus

    OpenAIRE

    O. O. Frolova; E. V. Kompantseva; T. M. Dementieva

    2016-01-01

    The review systematizes data about chemical composition of bark, leaves, inflorescences, and sprouts of different species of Salix L. The closest attention is payed to investigations of Salix, which has been recently carried out in our country and abroad. For every group of biologically active substances described in Salix there are data about suppressed types of pharmacological activity.

  1. Biologically Active Substances of Plants from Sali x L. Genus

    Directory of Open Access Journals (Sweden)

    O. O. Frolova

    2016-01-01

    Full Text Available The review systematizes data about chemical composition of bark, leaves, inflorescences, and sprouts of different species of Salix L. The closest attention is payed to investigations of Salix, which has been recently carried out in our country and abroad. For every group of biologically active substances described in Salix there are data about suppressed types of pharmacological activity.

  2. Chemical composition and biological activity of the plum seed extract

    OpenAIRE

    Savić, Ivan M.; Nikolić, Vesna D.; Savić-Gajić, Ivana M.; Kundaković, Tatjana D.; Stanojković, Tatjana P.; Najman, Stevo J.; id_orcid 0000-0002-2411-9802

    2016-01-01

    The aim of this paper was to estimate the biological activity of the plum seed extract and to define the chemical composition by using the ESI-MS method. During the investigation of the antioxidant activity, the extract showed a better ability to inhibit DPPH radicals compared with amygdalin standard. The results of the antimicrobial study indicate that the extract has a greater effect on Gram-negative bacteria compared with amygdalin. Gram-positive bacteria and fungi remained resistant in bo...

  3. Secondary Metabolites from Inula britannica L. and Their Biological Activities

    Directory of Open Access Journals (Sweden)

    Yoon-Ha Kim

    2010-03-01

    Full Text Available Inula britannica L., family Asteraceae, is used in traditional Chinese and Kampo Medicines for various diseases. Flowers or the aerial parts are a rich source of secondary metabolites. These consist mainly of terpenoids (sesquiterpene lactones and dimmers, diterpenes and triterpenoids and flavonoids. The isolated compounds have shown diverse biological activities: anticancer, antioxidant, anti-inflammatory, neuroprotective and hepatoprotective activities. This review provides information on isolated bioactive phytochemicals and pharmacological potentials of I. britannica.

  4. Biological function and regulation of histone and non-histone lysine methylation in response to DNA damage

    Institute of Scientific and Technical Information of China (English)

    Yongcan Chen; Wei-Guo Zhu

    2016-01-01

    DNA damage response (DDR) signaling network is initiated to protect cells from various exogenous and endogenous damage resources.Timely and accurate regulation of DDR proteins is required for distinct DNA damage repair pathways.Post-translational modifications of histone and non-histone proteins play a vital role in the DDR factor foci formation and signaling pathway.Phosphorylation,ubiquitylation,SUMOylation,neddylation,poly(ADP-ribosyl)ation,acetylation,and methylation are all involved in the spatial-temporal regulation of DDR,among which phosphorylation and ubiquitylation are well studied.Studies in the past decade also revealed extensive roles of lysine methylation in response to DNA damage.Lysine methylation is finely regulated by plenty of lysine methyltransferases,lysine demethylases,and can be recognized by proteins with chromodomain,plant homeodomain,Tudor domain,malignant brain tumor domain,or prolinetryptophan-tryptophan-proline domain.In this review,we outline the dynamics and regulation of histone lysine methylation at canonical (H3K4,H3K9,H3K27,H3K36,H3K79,and H4K20) and non-canonical sites after DNA damage,and discuss their context-specific functions in DDR protein recruitment or extraction,chromatin environment establishment,and transcriptional regulation.We also present the emerging advances of lysine methylation in non-histone proteins during DDR.

  5. Synthesis, characterization and in vitro antimicrobial activity of some 1-(substitutedbenzylidene-4-(4-(2-(methyl/phenyl-4-oxoquinazolin-3(4H-ylphenylsemicarbazide derivatives

    Directory of Open Access Journals (Sweden)

    Govindaraj Saravanan

    2015-01-01

    Full Text Available A series of 1-(substitutedbenzylidene-4-(4-(2-(methyl/phenyl-4-oxoquinazolin-3(4H-yl phenylsemicarbazide derivatives were synthesized with the aim of developing potential antimicrobials. It was characterized by FT-IR, 1H NMR, Mass spectroscopy and elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique and agar streak dilution method. All title compounds showed activity against the entire strain of microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. Based on the results obtained, compound 5j was found to be very active compared to the rest of the compounds which were subjected to antimicrobial assay.

  6. Synthesis, structure and biological properties of active spirohydantoin derivatives

    Directory of Open Access Journals (Sweden)

    Lazić Anita M.

    2016-01-01

    Full Text Available Spirohidantoins represent an pharmacologically important class of heterocycles since many derivatives have been recognized that display interesting activities against a wide range of biological targets. First synthesis of cycloalkanespiro-5-hydantoins was performed by Bucherer and Lieb 1934 by the reaction of cycloalkanone, potassium cyanide and ammonium-carbonate at reflux in a mixture of ethanol and water. QSAR (Quantitative Structure-Activity Relationship studies showed that a wide range of biological activities of spirohydantoin derivatives strongly depend upon their structure. This paper describes different methods of synthesis of spirohydantoin derivatives, their physico-chemical properties and biological activity. It emphasizes the importance of cycloalkanespiro-5-hydantoins with anticonvulsant, antiproliferative, antipsychotic, antimicrobial and antiinflammatory properties as well as their importance in the treatment of diabetes. Numerous spirohydantoin compounds exhibit physiological activity such as serotonin and fibrinogen antagonist, inhibitors of the glycine binding site of the NMDA receptor also, antagonist of leukocyte cell adhesion, acting as allosteric inhibitors of the protein-protein interactions. Some spirohydantoin derivatives have been identified as antitumor agents. Their activity depends on the substituent presented at position N-3 of the hydantoin ring and increases in order alkene > ester > ether. Besides that, compounds that contain two electron withdrawing groups (e.g. fluorine or chlorine on the third and fourth position of the phenyl ring are better antitumor agents than compounds with a single electron withdrawing group. [Projekat Ministarstva nauke Republike Srbije, br. 172013

  7. Studies on the Scavenger Activities of Salicylaldehyde and Methyl Salicylate Against Hydroxyl Radical

    Institute of Scientific and Technical Information of China (English)

    MA Jian-hua

    2005-01-01

    @@ Introduction Active oxygen species have a carcinogenesis effect, and can cause mutation, cardiovascular diseases, inflammation and aging, etc. Hydroxyl radicals generated either from a radiolysis of water contained in biological tissues or from a redox cycling implicated in a wide range chemical toxicants, have been recognized as the extremely reactive oxidative species which can attack DNA bases and sugar moiety of nucleotides and lead to radiation or chemical injury of DNA and other biological targets[1-5].Therefore, In recent years many pharmacologists and biologists are looking for effective free radical scavengers, especially naturally occurring antioxidants of oxidizing free radicals as drugs.

  8. Altered regulation of DNA ligase IV activity by aberrant promoter DNA methylation and gene amplification in colorectal cancer.

    Science.gov (United States)

    Kuhmann, Christine; Li, Carmen; Kloor, Matthias; Salou, Mariam; Weigel, Christoph; Schmidt, Christopher R; Ng, Linda W C; Tsui, Wendy W Y; Leung, Suet Y; Yuen, Siu T; Becker, Natalia; Weichenhan, Dieter; Plass, Christoph; Schmezer, Peter; Chan, Tsun L; Popanda, Odilia

    2014-04-15

    Colorectal cancer (CRC) presents as a very heterogeneous disease which cannot sufficiently be characterized with the currently known genetic and epigenetic markers. To identify new markers for CRC we scrutinized the methylation status of 231 DNA repair-related genes by methyl-CpG immunoprecipitation followed by global methylation profiling on a CpG island microarray, as altered expression of these genes could drive genomic and chromosomal instability observed in these tumors. We show for the first time hypermethylation of MMP9, DNMT3A and LIG4 in CRC which was confirmed in two CRC patient groups with different ethnicity. DNA ligase IV (LIG4) showed strong differential promoter methylation (up to 60%) which coincided with downregulation of mRNA in 51% of cases. This functional association of LIG4 methylation and gene expression was supported by LIG4 re-expression in 5-aza-2'-deoxycytidine-treated colon cancer cell lines, and reduced ligase IV amounts and end-joining activity in extracts of tumors with hypermethylation. Methylation of LIG4 was not associated with other genetic and epigenetic markers of CRC in our study. As LIG4 is located on chromosome 13 which is frequently amplified in CRC, two loci were tested for gene amplification in a subset of 47 cases. Comparison of amplification, methylation and expression data revealed that, in 30% of samples, the LIG4 gene was amplified and methylated, but expression was not changed. In conclusion, hypermethylation of the LIG4 promoter is a new mechanism to control ligase IV expression. It may represent a new epigenetic marker for CRC independent of known markers.

  9. An increase in pectin methyl esterase activity accompanies dormancy breakage and germination of yellow cedar seeds.

    Science.gov (United States)

    Ren, C; Kermode, A R

    2000-09-01

    Pectin methyl esterase (PME) (EC 3.1.1.11) catalyzes the hydrolysis of methylester groups of cell wall pectins. We investigated the role of this enzyme in dormancy termination and germination of yellow cedar (Chamaecyparis nootkatensis [D. Don] Spach) seeds. PME activity was not detected in dormant seeds of yellow cedar but was induced and gradually increased during moist chilling; high activity coincided with dormancy breakage and germination. PME activity was positively correlated to the degree of dormancy breakage of yellow cedar seeds. The enzyme produced in different seed parts and in seeds at different times during moist chilling, germination, and early post-germinative growth consisted of two isoforms, both basic with isoelectric points of 8.7 and 8.9 and the same molecular mass of 62 kD. The pH optimum for the enzyme was between 7.4 and 8.4. In intact yellow cedar seeds, activities of the two basic isoforms of PME that were induced in embryos and in megagametophytes following dormancy breakage were significantly suppressed by abscisic acid. Gibberellic acid had a stimulatory effect on the activities of these isoforms in embryos and megagametophytes of intact seeds at the germinative stage. We hypothesize that PME plays a role in weakening of the megagametophyte, allowing radicle emergence and the completion of germination.

  10. O-Methylated flavonol isorhamnetin prevents acute inflammation through blocking of NF-κB activation.

    Science.gov (United States)

    Yang, Ji Hye; Kim, Sang Chan; Shin, Bo Yeon; Jin, So Hee; Jo, Mi Jeong; Jegal, Kyung Hwan; Kim, Young Woo; Lee, Jong Rok; Ku, Sae Kwang; Cho, Il Je; Ki, Sung Hwan

    2013-09-01

    Here, we isolated isorhamnetin, a natural 3'-O-methylated flavonoid, from water dropwort (Oenanthe javanica, Umbelliferae) and investigated its ability to protect against acute inflammation in vivo and in vitro. To induce paw swelling, the hind paw of each rat was injected with a carrageenan 1h after vehicle or isorhamnetin treatment. In vitro effect and mechanism studies were performed in lipopolysaccharide (LPS)-activated macrophages. Administration of isorhamnetin markedly inhibited the swelling volume and the thickness of hind paws. Moreover, isorhamnetin significantly reduced inflammatory cell infiltration and pro-inflammatory gene expression in rats. Isorhamnetin pretreatment inhibited inducible nitric oxide synthase (iNOS) expression and NO release in LPS-stimulated cells. Activation of nuclear factor-kappa B (NF-κB) and activating protein-1 (AP-1) is the key step in the iNOS gene induction. Isorhamnetin specifically inhibited NF-κB luciferase activity, but not AP-1. Pretreatment with isorhamnetin suppressed NF-κB nuclear translocation in accordance with decreased phosphorylation and degradation of inhibitory-κB. Consistently, TNF-α, IL-1β and IL-6 expression, representative NF-κB target genes, were almost completely prohibited by isorhamnetin. Furthermore, isorhamnetin inhibited LPS-induced JNK and AKT/IKKα/β phosphorylation. Our results suggest that isorhamnetin inhibited JNK, and AKT/IKKα/β activation, leading to NF-κB inactivation, which might contribute to the inhibition of the acute inflammatory response.

  11. Synthesis, crystal, and biological activity of a novel carbene silver(I) complex with imidazole derivative

    Energy Technology Data Exchange (ETDEWEB)

    Jiu-Fu, Lu, E-mail: jiufulu@163.com; Hong-Guang, Ge; Juan, Shi [Chemical Engineering College, Shaanxi University of Technology (China)

    2015-12-15

    Reaction of 2-(1-methyl-1,2-dihydroimidazol-3-yl)acetonitrile tetrafluoroborate with silver oxide in dichloromethane readily yields [Ag(DIM){sub 2}]BF{sub 4}, where DIM is 2-(1-methyl-1, 2-dihydroimidazol-3-yl)acetonitrile, representing a carbene organic ligand. The title compound was characterized by elemental analysis, IR, MS and single crystal X-ray diffraction. The crystal is of monoclinic system, space group C2/c with a = 14.010(18), b = 8.303(11), c = 14.936(20) Å, β = 93.910(4)°, V = 1639(4) Å{sup 3}, Z = 4, D{sub x} = 1.771 g/cm{sup 3}, F (000) = 864, µ(MoK{sub α}) = 1.278 mm{sup –1}. The final R{sup 1} = 0.0711 and wR{sup 2} = 0.1903 for reflections with I > 2σ(I). In addition, the preliminary biological test showed that the title compound had anti-fungus yeast activity.

  12. Structure-activity relationship of daptomycin analogues with substitution at (2S, 3R) 3-methyl glutamic acid position.

    Science.gov (United States)

    Lin, Du'an; Lam, Hiu Yung; Han, Wenbo; Cotroneo, Nicole; Pandya, Bhaumik A; Li, Xuechen

    2017-02-01

    Daptomycin is a highly effective lipopeptide antibiotic against Gram-positive pathogens. The presence of (2S, 3R) 3-methyl glutamic acid (mGlu) in daptomycin has been found to be important to the antibacterial activity. However the role of (2S, 3R) mGlu is yet to be revealed. Herein, we reported the syntheses of three daptomycin analogues with (2S, 3R) mGlu substituted by (2S, 3R) methyl glutamine (mGln), dimethyl glutamic acid and (2S, 3R) ethyl glutamic acid (eGlu), respectively, and their antibacterial activities. The detailed synthesis of dimethyl glutamic acid was also reported.

  13. Oscillatory Activities in Regulatory Biological Networks and Hopf Bifurcation

    Institute of Scientific and Technical Information of China (English)

    YAN Shi-Wei; WANG Qi; XIE Bai-Song; ZHANG Feng-Shou

    2007-01-01

    Exploiting the nonlinear dynamics in the negative feedback loop, we propose a statistical signal-response model to describe the different oscillatory behaviour in a biological network motif. By choosing the delay as a bifurcation parameter, we discuss the existence of Hopf bifurcation and the stability of the periodic solutions of model equations with the centre manifold theorem and the normal form theory. It is shown that a periodic solution is born in a Hopf bifurcation beyond a critical time delay, and thus the bifurcation phenomenon may be important to elucidate the mechanism of oscillatory activities in regulatory biological networks.

  14. Density functional theory investigations of radical scavenging activity of 3′-Methyl-quercetin

    Directory of Open Access Journals (Sweden)

    Abdullah G. Al-Sehemi

    2016-09-01

    Full Text Available The possible eight rotamers of 3′-Methyl-quercetin have been optimized by using density functional theory (DFT at B3LYP/6-31G∗ level of theory. The molecular structure and molecular properties of the most stable rotamers have been investigated at the same level of theory. We have computed the descriptors; electronegativity (χ, hardness (η, electrophilicity (ω, softness (S and electrophilicity index (ωi by DFT approach. We have shed light on the structure–property relationship. The absorption spectrum has been computed by time dependent density functional theory (TD-DFT at TD-B3LYP/6-31G∗ level of theory. Radical scavenging activity has been explained on the basis of bond dissociation enthalpy (BDE and the adiabatic ionization potential (IP. Two mechanisms have been explained for the radical scavenging processes, i.e., hydrogen atom transfer and one-electron transfer.

  15. Adenosine A1 receptor activation modulates N-methyl-d-aspartate (NMDA) preconditioning phenotype in the brain.

    Science.gov (United States)

    Constantino, Leandra C; Pamplona, Fabrício A; Matheus, Filipe C; Ludka, Fabiana K; Gomez-Soler, Maricel; Ciruela, Francisco; Boeck, Carina R; Prediger, Rui D; Tasca, Carla I

    2015-04-01

    N-methyl-d-aspartate (NMDA) preconditioning is induced by subtoxic doses of NMDA and it promotes a transient state of resistance against subsequent lethal insults. Interestingly, this mechanism of neuroprotection depends on adenosine A1 receptors (A1R), since blockade of A1R precludes this phenomenon. In this study we evaluated the consequences of NMDA preconditioning on the hippocampal A1R biology (i.e. expression, binding properties and functionality). Accordingly, we measured A1R expression in NMDA preconditioned mice (75mg/kg, i.p.; 24h) and showed that neither the total amount of receptor, nor the A1R levels in the synaptic fraction was altered. In addition, the A1R binding affinity to the antagonist [(3)H] DPCPX was slightly increased in total membrane extracts of hippocampus from preconditioned mice. Next, we evaluated the impact of NMDA preconditioning on A1R functioning by measuring the A1R-mediated regulation of glutamate uptake into hippocampal slices and on behavioral responses in the open field and hot plate tests. NMDA preconditioning increased glutamate uptake into hippocampal slices without altering the expression of glutamate transporter GLT-1. Interestingly, NMDA preconditioning also induced antinociception in the hot plate test and both effects were reversed by post-activation of A1R with the agonist CCPA (0.2mg/kg, i.p.). NMDA preconditioning or A1R modulation did not alter locomotor activity in the open field. Overall, the results described herein provide new evidence that post-activation of A1R modulates NMDA preconditioning-mediated responses, pointing to the importance of the cross-talk between glutamatergic and adenosinergic systems to neuroprotection.

  16. Ligands of Peroxisome Proliferator-activated Receptor Inhibit Homocysteineinduced DNA Methylation of Inducible Nitric Oxide Synthase Gene

    Institute of Scientific and Technical Information of China (English)

    Yideng JIANG; Jianzhong ZHANG; Jiantuan XIONG; Jun CAO; Guizhong LI; Shuren WANG

    2007-01-01

    Homocysteine (Hcy) is a risk factor for atherosclerosis. It is generally accepted that inducible nitric oxide synthase (iNOS) is a key enzyme in the regulation of vascular disease. The aim of the present study is to investigate the effects of peroxisome proliferator-activated receptor ligands on iNOS in the presence of Hcy in human monocytes. Foam cells, induced by oxidize low density lipoprotein (ox-LDL) and phorbol myristate acetate (PMA) in the presence of different concentrations of Hcy, clofibrate and pioglitazone in human monocytes for 4 d, were examined by oil red O staining. The activity of iNOS was detected by real-time quantitative reverse transcription-polymerase chain reaction and Western blot analysis. The capability of DNA methylation was measured by assaying endogenous C5 DNA methyltransferase (C5MTase)activity, and the iNOS promoter methylation level was determined by quantitative MethyLight assays. The results indicated that Hcy increased the activity of C5MTase and the level of iNOS gene DNA methylation,resulting in a decrease of iNOS expression. Clofibrate and pioglitazone could antagonize the Hcy effect on iNOS expression through DNA methylation, resulting in attenuation of iNOS transcription. These findings suggested that Hcy decreased the expression of iNOS by elevating iNOS DNA methylation levels, which can repress the transcription of some genes. Peroxisome proliferator-activated receptor α/γ ligands can down-regulate iNOS DNA methylation, and could be useful for preventing Hcy-induced atherosclerosis by repressing iNOS expression.

  17. Synthesis of Lactosylated Piperazinyl Porphyrins and Their Biological Activity

    Institute of Scientific and Technical Information of China (English)

    LI,He-Ping; CAO,Zhong; XIAO,Hua-Wu

    2008-01-01

    The aim of this work is to synthesize of a new family of lactosylated piperazinly porphyrins, in which the galactoside piperazine moieties are linked to the tetra- and mono-phenyl rings of tetraphenylporphyrin (TPP).5,10,15,20-Tetrakis[4-(4-lactobionylpiperazin-1-yl)phenyl]porphyrin (TLPP) and 5-mono[4-(4-lactobionylpiperazin-1-yl)phenyl]-10,15,20-triphenylporphyrin (MLPP) have been synthesized. A detailed 1H NMR study gave their complete structural elucidation. The UV-Visible, mass spectra and elemental analysis are also presented. The biological activity on cancer cells and the pharmacokinetics have also been evaluated, showing a better biological activity, a very high liver to skin ratio and short retention time in tissues. It was suggested that such novel lactosylated piperazinly porphyrins, as potential hepatocyte-selective targeting drugs, exhibit a promising activity in photodynamic therapy (PDT).

  18. Protein stability and enzyme activity at extreme biological temperatures

    Energy Technology Data Exchange (ETDEWEB)

    Feller, Georges, E-mail: gfeller@ulg.ac.b [Laboratory of Biochemistry, Centre for Protein Engineering, Institute of Chemistry B6a, University of Liege, B-4000 Liege (Belgium)

    2010-08-18

    Psychrophilic microorganisms thrive in permanently cold environments, even at subzero temperatures. To maintain metabolic rates compatible with sustained life, they have improved the dynamics of their protein structures, thereby enabling appropriate molecular motions required for biological activity at low temperatures. As a consequence of this structural flexibility, psychrophilic proteins are unstable and heat-labile. In the upper range of biological temperatures, thermophiles and hyperthermophiles grow at temperatures > 100 {sup 0}C and synthesize ultra-stable proteins. However, thermophilic enzymes are nearly inactive at room temperature as a result of their compactness and rigidity. At the molecular level, both types of extremophilic proteins have adapted the same structural factors, but in opposite directions, to address either activity at low temperatures or stability in hot environments. A model based on folding funnels is proposed accounting for the stability-activity relationships in extremophilic proteins. (topical review)

  19. BIOLOGICAL ACTIVITIES OF OXAZINE AND ITS DERIVATIVES: A REVIEW

    Directory of Open Access Journals (Sweden)

    SINDHU T J

    2014-12-01

    Full Text Available Oxazine derivatives are an important class of heterocycles, which has attracted much synthetic interest due to their wide range of biological activities. Oxazine is a heterocyclic compound can be formally derived from benzene, and its reduction products, by suitable substitution of carbon (and hydrogen atoms by nitrogen and oxygen. In the last few years oxazine derivatives have proved to be valuable synthetic intermediates and also possess important biological activities like sedative, analgesic, antipyretic, anticonvulsant, antitubercular, antitumour, antimalarial and antimicrobial. In these days, development of drug resistance is a major problem and to overcome this situation, it is necessary to synthesize new classes of compounds. The aim of the article is to review the generalization of the collected data about the synthesis of oxazine derivatives and their activities. We hope that this work will be a definite interest for researchers concerned with azines in generally and oxazines in particular.

  20. Polysaccharides of higher fungi: Biological role, structure, and antioxidative activity

    Directory of Open Access Journals (Sweden)

    Kozarski Maja S.

    2014-01-01

    Full Text Available Fungal polysaccharides attract a lot of attention due to their multiple challenging biological properties, such as: anti-tumor, anti-viral, anticomplementary, anticoagulant, hypolipidemic and immunomodulatory and immune-stimulatory activities, which all together make them suitable for application in many quite distinctive areas, such as food industry, biomedicine, cosmetology, agriculture, environmental protection and waste water management. This article presents results with respect to biological properties, structure and procedures related to the isolation and activation of polysaccharides of higher fungi. It is considered and presented along with a review of the critical antioxidative activity and possible influence of the structural composition of polysaccharide extracts (isolated from these higher fungi upon their antioxidative properties.

  1. Effect of methyl parathion on the muscle and brain acetylcholinesterase activity of matrinxã (Brycon cephalus

    Directory of Open Access Journals (Sweden)

    Almeida Luciana Cristina de

    2005-01-01

    Full Text Available Farming of the freshwater fish is emerging in Brazil and many species from the wild are promising. The teleost matrinxã (Brycon cephalus holds several characteristics such as fast growth rate, high commercial value and adaptability to artificial raring conditions, which make it a promising species for commerce. The use of pesticides in aquatic environment is frequent in Brazil, and methyl parathion is very common in aquaculture. We have determined the enzymatic activity of acetyl cholinesterase in white muscle and brain of matrinxã exposed to 2ppm of environmental methyl parathion for 24 hours. There was 64% and 69% of acetyl cholinesterase inhibition in muscle and brain respectively. These activities were not recovered after 8 days from exposure to this pesticide. It can be concluded that acetyl cholinesterase from those tissues was inhibited by small amounts of methyl parathion, and the main effect was observed in the brain.

  2. Hydrodynamic collective effects of active proteins in biological membranes

    CERN Document Server

    Koyano, Yuki; Mikhailov, Alexander S

    2016-01-01

    Lipid bilayers forming biological membranes are known to behave as viscous 2D fluids on submicrometer scales; usually they contain a large number of active protein inclusions. Recently, it has been shown [Proc. Nat. Acad. Sci. USA 112, E3639 (2015)] that such active proteins should in- duce non-thermal fluctuating lipid flows leading to diffusion enhancement and chemotaxis-like drift for passive inclusions in biomembranes. Here, a detailed analytical and numerical investigation of such effects is performed. The attention is focused on the situations when proteins are concentrated within lipid rafts. We demonstrate that passive particles tend to become attracted by active rafts and are accumulated inside them.

  3. Synthesis and biological evaluation of 1-(4-[{sup 18}f]fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine for in vivo studies of acetylcholinesterase

    Energy Technology Data Exchange (ETDEWEB)

    Leea, Sang-Yoon; Choe, Yearn Seong E-mail: yschoe@samsung.co.kr; Sugimoto, Hachiro; Kim, Sang Eun; Hwang, Sae Hwan; Lee, Kyung-Han; Choi, Yong; Lee, Jeewoo; Kim, Byung-Tae

    2000-11-01

    We synthesized and evaluated 1-(4-fluorobenzyl)-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine (4-FDP), which is an analog of donepezil. The 4-[{sup 18}F]FDP was prepared by reductive alkylation of debenzylated donepezil with 4-[{sup 18}F]fluorobenzaldehyde in high radiochemical yield (decay-corrected, 40-52%) and with high effective specific activity (30-38 GBq/{mu}mol). Tissue distribution studies in mice demonstrated nonspecific distribution of the 4-[{sup 18}F]FDP in brain regions, suggesting that this radioligand may not be a suitable agent for in vivo studies of acetylcholinesterase (AChE), despite its potent in vitro biological activity.

  4. Dnmt3b Methylates DNA by a Noncooperative Mechanism, and Its Activity Is Unaffected by Manipulations at the Predicted Dimer Interface.

    Science.gov (United States)

    Norvil, Allison B; Petell, Christopher J; Alabdi, Lama; Wu, Lanchen; Rossie, Sandra; Gowher, Humaira

    2016-11-04

    The catalytic domains of the de novo DNA methyltransferases Dnmt3a-C and Dnmt3b-C are highly homologous. However, their unique biochemical properties could potentially contribute to differences in the substrate preferences or biological functions of these enzymes. Dnmt3a-C forms tetramers through interactions at the dimer interface, which also promote multimerization on DNA and cooperativity. Similar to the case for processive enzymes, cooperativity allows Dnmt3a-C to methylate multiple sites on the same DNA molecule; however, it is unclear whether Dnmt3b-C methylates DNA by a cooperative or processive mechanism. The importance of the tetramer structure and cooperative mechanism is emphasized by the observation that the R882H mutation in the dimer interface of DNMT3A is highly prevalent in acute myeloid leukemia and leads to a substantial loss of its activity. Under conditions that distinguish between cooperativity and processivity, we show that in contrast to that of Dnmt3a-C, the activity of Dnmt3b-C is not cooperative and confirm the processivity of Dnmt3b-C and the full length Dnmt3b enzyme. Whereas the R878H mutation (mouse homologue of R882H) led to the loss of cooperativity of Dnmt3a-C, the activity and processivity of the analogous Dnmt3b-C R829H variant were comparable to those of the wild-type enzyme. Additionally, buffer acidification that attenuates the dimer interface interactions of Dnmt3a-C had no effect on Dnmt3b-C activity. Taken together, these results demonstrate an important mechanistic difference between Dnmt3b and Dnmt3a and suggest that interactions at the dimer interface may play a limited role in regulating Dnmt3b-C activity. These new insights have potential implications for the distinct biological roles of Dnmt3a and Dnmt3b.

  5. Regulation and function of DNA methylation in plants and animals

    KAUST Repository

    He, Xinjian

    2011-02-15

    DNA methylation is an important epigenetic mark involved in diverse biological processes. In plants, DNA methylation can be established through the RNA-directed DNA methylation pathway, an RNA interference pathway for transcriptional gene silencing (TGS), which requires 24-nt small interfering RNAs. In mammals, de novo DNA methylation occurs primarily at two developmental stages: during early embryogenesis and during gametogenesis. While it is not clear whether establishment of DNA methylation patterns in mammals involves RNA interference in general, de novo DNA methylation and suppression of transposons in germ cells require 24-32-nt piwi-interacting small RNAs. DNA methylation status is dynamically regulated by DNA methylation and demethylation reactions. In plants, active DNA demethylation relies on the repressor of silencing 1 family of bifunctional DNA glycosylases, which remove the 5-methylcytosine base and then cleave the DNA backbone at the abasic site, initiating a base excision repair (BER) pathway. In animals, multiple mechanisms of active DNA demethylation have been proposed, including a deaminase- and DNA glycosylase-initiated BER pathway. New information concerning the effects of various histone modifications on the establishment and maintenance of DNA methylation has broadened our understanding of the regulation of DNA methylation. The function of DNA methylation in plants and animals is also discussed in this review. © 2011 IBCB, SIBS, CAS All rights reserved.

  6. [Soil biological activities at maize seedling stage under application of slow/controlled release nitrogen fertilizers].

    Science.gov (United States)

    Li, Dongpo; Wu, Zhijie; Chen, Lijun; Liang, Chenghua; Zhang, Lili; Wang, Weicheng; Yang, Defu

    2006-06-01

    With pot experiment and simulating field ecological environment, this paper studied the effects of different slow/ controlled release N fertilizers on the soil nitrate - reductase and urease activities and microbial biomass C and N at maize seedling stage. The results showed that granular urea amended with dicyandiamide (DCD) and N-(n-bultyl) thiophosphoric triamide (NBPT) induced the highest soil nitrate-reductase activity, granular urea brought about the highest soil urease activity and microbial biomass C and N, while starch acetate (SA)-coated granular urea, SA-coated granular urea amended with DCD, methyl methacrylate (MMA) -coated granular urea amended with DCD, and no N fertilization gave a higher soil urease activity. Soil microbial C and N had a similar variation trend after applying various kinds of test slow/controlled release N fertilizers, and were the lowest after applying SA-coated granular urea amended with DCD and NBPT. Coated granular urea amended with inhibitors had a stronger effect on soil biological activities than coated granular urea, and MMA-coating had a better effect than SA-coating.

  7. N-methyl-D-aspartate antagonist activity of alpha- and beta-sulfallorphans.

    Science.gov (United States)

    Shukla, V K; Lemaire, S

    1997-01-01

    Resolved equatorial (alpha) and axial (beta) forms of S-allylmorphinans, alpha-sulfallorphan and beta-sulfallorphan, were tested for their ability to compete with the binding of phencyclidine and sigma receptor ligands to mouse brain membranes and to antagonize N-methyl-D-aspartate (NMDA)-induced convulsions in mice. alpha- and beta-sulfallorphans displayed distinct binding affinities for phencyclidine and sigma sites, inhibiting the binding of [3H]-(5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten++ +-5, 10-imine ([3H]MK-801) with Ki values of 2.32 and 0.13 microM and that of [3H](+)-pentazocine with Ki values of 1.97 and 1.61 microM, respectively. Intracerebroventricular administration of these compounds in mice caused dose-dependent inhibitions of NMDA-induced convulsions, but did not affect convulsions induced by (R,S)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), kainic acid and bicuculline. alpha- and beta-sulfallorphans blocked the convulsive activity of NMDA (1 nmol/mouse; intracerebroventricular) with ED50 values of 0.48 and 0.015 nmol/mouse, as compared with 0.55, 0.039 and 0.013 nmol/mouse for dextrorphan, MK-801 and (+/-)3-(2-carboxypiperazine-4yl)propyl-1-proprionic acid, respectively. The structurally related compound, dextrallorphan, significantly but less potently blocked NMDA-induced convulsions (ED60, 2.68 nmol/mouse). At the protective doses, alpha- and beta-sulfallorphans markedly reduced NMDA- and AMPA-induced mortality without inducing locomotion and falling behavior. These results indicate that alpha- and beta-sulfallorphans are potent and selective NMDA antagonists devoid of motor side effects at protective doses.

  8. Effects of Catechol O-Methyl Transferase Inhibition on Anti-Inflammatory Activity of Luteolin Metabolites.

    Science.gov (United States)

    Ha, Sang Keun; Lee, Jin-Ah; Cho, Eun Jung; Choi, Inwook

    2017-02-01

    Although luteolin is known to have potent anti-inflammatory activities, much less information has been provided on such activities of its hepatic metabolites. Luteolin was subjected to hepatic metabolism in HepG2 cells either without or with catechol O-methyl transferase (COMT) inhibitor. To identify hepatic metabolites of luteolin without (luteolin metabolites, LMs) or with COMT inhibitor (LMs+CI), metabolites were treated by β-glucuronidase and sulfatase, and found that they were composed of glucuronide and sulfate conjugates of diosmetin in LMs or these conjugates of luteolin in LMs+CI. LMs and LMs+CI were examined for their anti-inflammatory activities on LPS stimulated Raw 264.7 cells. Expression of iNOS and production of nitric oxide and pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 were suppressed more effectively by the treatment with LMs+CI than LMs. Our data provide a new insight on possible improvement in functional properties of luteolin on target cells by modifying their metabolic pathway in hepatocytes.

  9. Pectin Methyl Esterase Activity Change in Intermediate Moisture Sun-Dried Figs after Storage

    Directory of Open Access Journals (Sweden)

    Dilek Demirbüker Kavak

    2015-12-01

    Full Text Available Intermediate moisture fruits can be obtained by rehydrating dried fruits. Intermediate moisture fruits are suitable for direct consumption compared to dry fruits and can be directly used in the production of various products such as bakery products, dairy products and candies. Aim of this study is to compare the pectin methyl esterase (PME activity of intermediate moisture figs which causes softening of the texture and to compare their microbial stability after 3 months storage period. For this purpose, dried figs were rehydrated in 30 and 80° C water until they reach 30% moisture content. Rehydrated samples were stored for 3 months at +4°C. Results showed that there was no statistically significant difference between the control samples and the samples rehydrated at 80°C according to the total viable counts. At the end of the storage period, results of residual PME activity in control samples was 24.1 μmol COOH min-1g-1, while it was found 17.4 μmol COOH min-1g-1 in samples rehydrated at 80°C. As a result rehydration conducted at 80°C provided 28% reduction in PME activity compared to the control samples rehydrated at 30°C, although it did not affect the microbial load significantly after storage.

  10. Biological activity of selected plants with adaptogenic effect

    Directory of Open Access Journals (Sweden)

    Eva Ivanišová

    2016-05-01

    Full Text Available The aim of this study was to determine biological activity of plants with adaptogenic effect: Panax ginseng Mayer., Withania somnifera L., Eleuterococcus senticosus Rupr. et Maxim., Astragallus membranaceus Fisch. and Codonopsis pilosulae Franch. The antioxidant activity was detected by DPPH and phosphomolybdenum method, total polyphenol content with Folin – Ciocalteu reagent, flavonoids content by aluminium chloride method. The detection of antimicrobial activity was carried out by disc diffusion method against three species of Gram-negative bacteria: Escherichia coli CCM 3988, Salmonella enterica subsp. enterica CCM 3807, Yersinia enterocolitica CCM 5671 and two Gram-positive bacteria: Bacillus thuringiensis CCM 19, Stapylococcus aureus subsp. aureus CCM 2461. Results showed that plants with adaptogenic effect are rich for biologically active substances. The highest antioxidant activity by DPPH method was determined in the sample of Eleuterococcus senticosus (3.15 mg TEAC – Trolox equivalent antioxidant capacity per g of sample and by phosphomolybdenum method in the sample of Codonopsis pilosulae (188.79 mg TEAC per g of sample. In the sample of Panax ginseng was measured the highest content of total polyphenols (8.10 mg GAE – galic acid equivalent per g of sample and flavonoids (3.41 μg QE – quercetin equivalent per g of sample. All samples also showed strong antimicrobial activity with the best results in Panax ginseng and Withania somnifera in particular for species Yersinia enterocolitica CCM 5671 and Salmonella enterica subsp. enterica CCM 3807. The analyzed species of plant with high value of biological activity can be used more in the future, not only in food, but also in cosmetics and pharmaceutical industries.

  11. Marine Sponge Lectins: Actual Status on Properties and Biological Activities

    Directory of Open Access Journals (Sweden)

    Sandro Mascena Gomes Filho

    2014-12-01

    Full Text Available Marine sponges are primitive metazoans that produce a wide variety of molecules that protect them against predators. In studies that search for bioactive molecules, these marine invertebrates stand out as promising sources of new biologically-active molecules, many of which are still unknown or little studied; thus being an unexplored biotechnological resource of high added value. Among these molecules, lectins are proteins that reversibly bind to carbohydrates without modifying them. In this review, various structural features and biological activities of lectins derived from marine sponges so far described in the scientific literature are discussed. From the results found in the literature, it could be concluded that lectins derived from marine sponges are structurally diverse proteins with great potential for application in the production of biopharmaceuticals, especially as antibacterial and antitumor agents.

  12. MILK KEFIR: COMPOSITION, MICROBIAL CULTURES, BIOLOGICAL ACTIVITIES AND RELATED PRODUCTS

    Directory of Open Access Journals (Sweden)

    Maria Rosa Prado

    2015-10-01

    Full Text Available In recent years, there has been a strong focus on beneficial foods with probiotic microorganisms and functional organic substances. In this context, there is an increasing interest in the commercial use of kefir, since it can be marketed as a natural beverage that has health promoting bacteria. There are numerous commercially available kefir based-products. Kefir may act as a matrix in the effective delivery of probiotic microorganisms in different types of products. Also, the presence of kefir’s exopolysaccharides, known as kefiran, which has biological activity, certainly adds value to products. Kefiran can also be used separately in other food products and as a coating film for various food and pharmaceutical products. This article aims to update the information about kefir and its microbiological composition, biological activity of the kefir’s microflora and the importance of kefiran as a beneficial health substance.

  13. Marine Omega-3 Phospholipids: Metabolism and Biological Activities

    Directory of Open Access Journals (Sweden)

    Nils Hoem

    2012-11-01

    Full Text Available The biological activities of omega-3 fatty acids (n-3 FAs have been under extensive study for several decades. However, not much attention has been paid to differences of dietary forms, such as triglycerides (TGs versus ethyl esters or phospholipids (PLs. New innovative marine raw materials, like krill and fish by-products, present n-3 FAs mainly in the PL form. With their increasing availability, new evidence has emerged on n-3 PL biological activities and differences to n-3 TGs. In this review, we describe the recently discovered nutritional properties of n-3 PLs on different parameters of metabolic syndrome and highlight their different metabolic bioavailability in comparison to other dietary forms of n-3 FAs.

  14. Biological activities of secondary metabolites of the order Zoanthids

    Directory of Open Access Journals (Sweden)

    Zahra Aminikhoei

    2015-11-01

    Full Text Available The phylum Cnidaria is a large, diverse and ecologically important group of marine invertebrates, which produce powerful toxins and venoms. The number of marine natural product from cnidarians isolated from class Anthozoa. Among the Anthozoa, the order of zoanthids are sessile, clonal and mostly brightly colored invertebrate which produce high biodiversity of cytolitic, neurotoxic and cardiotoxic compounds. Zoanthids containing palytoxins are reportedly among the most toxic marine organisms known. In addition, a high concentration of zoanthamine alkaloids extracted from this group.The zoanthamine alkaloids were isolated over 20 years ago, exhibit a broad range of biological activities.The best studied and most well-known biological activity of zoanthamine derivative significantly suppressed bone resorption and enhanced bone formation.

  15. Biological activities and medicinal properties of Gokhru (Pedalium murex L.)

    Institute of Scientific and Technical Information of China (English)

    V Rajashekar; E Upender Rao; Srinivas P

    2012-01-01

    Bada Gokhru (Pedalium murex L.) is perhaps the most useful traditional medicinal plant in India. Each part of the neem tree has some medicinal property and is thus commercially exploitable. During the last five decades, apart from the chemistry of the Pedalium murex compounds, considerable progress has been achieved regarding the biological activity and medicinal applications of this plant. It is now considered as a valuable source of unique natural products for development of medicines against various diseases and also for the development of industrial products. This review gives a bird’s eye view mainly on the biological activities of some of this compounds isolated, pharmacological actions of the extracts, clinical studies and plausible medicinal applications of gokharu along with their safety evaluation.

  16. Visual Analysis of Biological Activity Data with Scaffold Hunter.

    Science.gov (United States)

    Klein, Karsten; Koch, Oliver; Kriege, Nils; Mutzel, Petra; Schäfer, Till

    2013-12-01

    The growing interest in chemogenomics approaches over the last years has led to an increasing amount of data regarding chemical and the corresponding biological activity space. The resulting data, collected in either in-house or public databases, need to be analyzed efficiently to speed-up the increasingly difficult task of drug discovery. Unfortunately, the discovery of new chemical entities or new targets for known drugs ('drug repurposing') is not suitable to a fully automated analysis or a simple drill down process. Visual interactive interfaces that allow to explore chemical space in a systematic manner and facilitate analytical reasoning can help to overcome these problems. Scaffold Hunter is a tool for the visual analysis of chemical compound databases that provides integrated visualization and analysis of biological activity data and fosters the interactive exploration of data imported from a variety of sources. We describe the features and illustrate the use by means of an exemplary analysis workflow.

  17. Fucoidans from brown alga Fucus evanescens: structure and biological activity

    Directory of Open Access Journals (Sweden)

    Roza Menshova

    2016-08-01

    Full Text Available Brown alga Fucus evanescens, widespread in the Far Eastern seas of Russia, is valuable source of sulfated polysaccharides – fucoidans with beneficial biological activities. The most homogenous fraction of fucoidan from F. evanescens was shown to be molecule containing linear main chain of alternating 2-sulfated 1,3- and 1,4-linked α-L-fucose residues. Few sulfate groups were found in position 4 of some 1,3-linked fucose residues. Acetyl groups occupied free C-3 of 1,4-linked residues and/or the C-4 of 1,3-linked fucose residues. Enzymatic hydrolysis, mild acid hydrolysis and autohydrolysis of native fucoidan were used for elucidation of the fine structural characteristics of fucoidan from F. evanescens. The aim of this review to summarize published data on biological activities of fucoidan from F. evanescens: antiviral, anticoagulant, thrombolytic, hepatoprotective, immunomodulatory, anticancer, and their practical application.

  18. Biological activities and medicinal properties of Cajanus cajan (L Millsp.

    Directory of Open Access Journals (Sweden)

    Dilipkumar Pal

    2011-01-01

    Full Text Available Cajanus cajan (L Millsp. (Sanskrit: Adhaki, Hindi: Arhar, English: Pigeon pea, Bengali: Tur (family: Fabaceae is the most important grain legume crop of rain-fed agriculture in semi-arid tropics. It is both a food crop and a cover/forage crop with high levels of proteins and important amino acids like methionine, lysine and tryptophan. During the last few decades extensive studies have been carried out regarding the chemistry of C. cajan and considerable progress has been achieved regarding its biological activities and medicinal applications. This review article gives an overview on the biological activities of the compounds isolated, pharmacological actions and clinical studies of C. cajan extracts apart from its general details.

  19. Synthesis,Characterization and Biological Activities of Novel Acrylamide Compounds

    Institute of Scientific and Technical Information of China (English)

    XU Liang-zhong; XU Zhong-jie; ZHANG Gong-sheng; ZHOU Kai; ZHAI Zhi-wei

    2008-01-01

    With dimethomorph and flumorph as the leading compounds,four novel acrylamide compounds with two types of structure were designed and synthesized by means of the method of"me too chemistry".The target compounds were characterized by 1H NMR,IR,MS,and elemental analysis.The influences of solvent and raw material on the yield were investigated and optimum processing conditions were determined.The results of preliminary biological tests show that all those compounds exhibit certain antifungal activities.

  20. Protein folding activity and the central dogma of molecular biology

    OpenAIRE

    Pallavi, Ghosh; Dipankar, Chatterji

    2003-01-01

    Biological systems, in general, can function effectively when the products of the system are in proper configuration and harmful effects due to misaggregation are avoided. Folding of proteins and their functional consequences have been a subject of active research since several years now. However it is not clear whether during protein synthesis from genetic message, the same set of rules are employed or participation of new efforts take place. In this review we show that at least in the case ...

  1. Chemistry and Biological Activities of Flavonoids: An Overview

    OpenAIRE

    Shashank Kumar; Pandey, Abhay K

    2013-01-01

    There has been increasing interest in the research on flavonoids from plant sources because of their versatile health benefits reported in various epidemiological studies. Since flavonoids are directly associated with human dietary ingredients and health, there is need to evaluate structure and function relationship. The bioavailability, metabolism, and biological activity of flavonoids depend upon the configuration, total number of hydroxyl groups, and substitution of functional groups about...

  2. Biological Activities of Phenolic Compounds Present in Virgin Olive Oil

    OpenAIRE

    2010-01-01

    The Mediterranean diet is associated with a lower incidence of atherosclerosis, cardiovascular disease, neurodegenerative diseases and certain types of cancer. The apparent health benefits have been partially ascribed to the dietary consumption of virgin olive oil by Mediterranean populations. Much research has focused on the biologically active phenolic compounds naturally present in virgin olive oils to aid in explaining reduced mortality and morbidity experienced by people consuming a trad...

  3. Current status of pyrazole and its biological activities.

    Science.gov (United States)

    Naim, Mohd Javed; Alam, Ozair; Nawaz, Farah; Alam, Md Jahangir; Alam, Perwaiz

    2016-01-01

    Pyrazole are potent medicinal scaffolds and exhibit a full spectrum of biological activities. This review throws light on the detailed synthetic approaches which have been applied for the synthesis of pyrazole. This has been followed by an in depth analysis of the pyrazole with respect to their medical significance. This follow-up may help the medicinal chemists to generate new leads possessing pyrazole nucleus with high efficacy.

  4. Biological Activities and Phytochemicals of Swietenia macrophylla King

    Directory of Open Access Journals (Sweden)

    Habsah Abdul Kadir

    2013-08-01

    Full Text Available Swietenia macrophylla King (Meliaceae is an endangered and medicinally important plant indigenous to tropical and subtropical regions of the World. S. macrophylla has been widely used in folk medicine to treat various diseases. The review reveals that limonoids and its derivatives are the major constituents of S. macrophylla. There are several data in the literature indicating a great variety of pharmacological activities of S. macrophylla, which exhibits antimicrobial, anti-inflammatory, antioxidant effects, antimutagenic, anticancer, antitumor and antidiabetic activities. Various other activities like anti-nociceptive, hypolipidemic, antidiarrhoeal, anti-infective, antiviral, antimalarial, acaricidal, antifeedant and heavy metal phytoremediation activity have also been reported. In view of the immense medicinal importance of S. macrophylla, this review aimed at compiling all currently available information on its ethnomedicinal uses, phytochemistry and biological activities of S. macrophylla, showing its importance.

  5. Synthesis, Antifungal Activity and Structure-Activity Relationships of Novel 3-(Difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic Acid Amides

    Directory of Open Access Journals (Sweden)

    Shijie Du

    2015-05-01

    Full Text Available A series of novel 3-(difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid amides were synthesized and their activities were tested against seven phytopathogenic fungi by an in vitro mycelia growth inhibition assay. Most of them displayed moderate to excellent activities. Among them N-(2-(5-bromo-1H-indazol-1-ylphenyl-3-(difluoro-methyl-1-methyl-1H-pyrazole-4-carboxamide (9m exhibited higher antifungal activity against the seven phytopathogenic fungi than boscalid. Topomer CoMFA was employed to develop a three-dimensional quantitative structure-activity relationship model for the compounds. In molecular docking, the carbonyl oxygen atom of 9m could form hydrogen bonds towards the hydroxyl of TYR58 and TRP173 on SDH.

  6. Temperature dependence of methyl-coenzyme M reductase activity and of the formation of the methyl-coenzyme M reductase red2 state induced by coenzyme B.

    Science.gov (United States)

    Goenrich, Meike; Duin, Evert C; Mahlert, Felix; Thauer, Rudolf K

    2005-06-01

    Methyl-coenzyme M reductase (MCR) catalyses the formation of methane from methyl-coenzyme M (CH(3)-S-CoM) and coenzyme B (HS-CoB) in methanogenic archaea. The enzyme has an alpha(2)beta(2)gamma(2) subunit structure forming two structurally interlinked active sites each with a molecule F(430) as a prosthetic group. The nickel porphinoid must be in the Ni(I) oxidation state for the enzyme to be active. The active enzyme exhibits an axial Ni(I)-based electron paramagnetic resonance (EPR) signal and a UV-vis spectrum with an absorption maximum at 385 nm. This state is called the MCR-red1 state. In the presence of coenzyme M (HS-CoM) and coenzyme B the MCR-red1 state is in part converted reversibly into the MCR-red2 state, which shows a rhombic Ni(I)-based EPR signal and a UV-vis spectrum with an absorption maximum at 420 nm. We report here for MCR from Methanothermobacter marburgensis that the MCR-red2 state is also induced by several coenzyme B analogues and that the degree of induction by coenzyme B is temperature-dependent. When the temperature was lowered below 20 degrees C the percentage of MCR in the red2 state decreased and that in the red1 state increased. These changes with temperature were fully reversible. It was found that at most 50% of the enzyme was converted to the MCR-red2 state under all experimental conditions. These findings indicate that in the presence of both coenzyme M and coenzyme B only one of the two active sites of MCR can be in the red2 state (half-of-the-sites reactivity). On the basis of this interpretation a two-stroke engine mechanism for MCR is proposed.

  7. SYNTHESIS OF METHYL TERT-BUTYL ETHER CATALYZED BY ACIDIC ION-EXCHANGE RESINS - INFLUENCE OF THE PROTON ACTIVITY

    NARCIS (Netherlands)

    PANNEMAN, HJ; BEENACKERS, AACM

    1995-01-01

    The catalytic activity of various strong acid ion-exchange resins on the synthesis of methyl tert-butyl ether (MtBE) from methanol and isobutene has been investigated. Relative to Amberlyst 15, Kastel CS 381 and Amberlyst CSP have similar rate constants, whereas Duolite ES 276 and Amberlyst XE 307 h

  8. Expression of biologically active murine interleukin-18 in Lactococcus lactis.

    Science.gov (United States)

    Feizollahzadeh, Sadegh; Khanahmad, Hossein; Rahimmanesh, Ilnaz; Ganjalikhani-Hakemi, Mazdak; Andalib, Alireza; Sanei, Mohammad Hossein; Rezaei, Abbas

    2016-11-01

    The food-grade bacterium Lactococcus lactis is increasingly used for heterologous protein expression in therapeutic and industrial applications. The ability of L. lactis to secrete biologically active cytokines may be used for the generation of therapeutic cytokines. Interleukin (IL)-18 enhances the immune response, especially on mucosal surfaces, emphasizing its therapeutic potential. However, it is produced as an inactive precursor and has to be enzymatically cleaved for maturation. We genetically manipulated L. lactis to secrete murine IL-18. The mature murine IL-18 gene was inserted downstream of a nisin promoter in pNZ8149 plasmid and the construct was used to transform L. lactis NZ3900. The transformants were selected on Elliker agar and confirmed by restriction enzyme digestion and sequencing. The expression and secretion of IL-18 protein was verified by SDS-PAGE, western blotting and ELISA. The biological activity of recombinant IL-18 was determined by its ability to induce interferon (IFN)-γ production in L. lactis co-cultured with murine splenic T cells. The amounts of IL-18 in bacterial lysates and supernatants were 3-4 μg mL(-1) and 0.6-0.7 ng mL(-1), respectively. The successfully generated L. lactis strain that expressed biologically active murine IL-18 can be used to evaluate the possible therapeutic effects of IL-18 on mucosal surfaces.

  9. Isolation of biologically active nanomaterial (inclusion bodies from bacterial cells

    Directory of Open Access Journals (Sweden)

    Peternel Špela

    2010-09-01

    Full Text Available Abstract Background In recent years bacterial inclusion bodies (IBs were recognised as highly pure deposits of active proteins inside bacterial cells. Such active nanoparticles are very interesting for further downstream protein isolation, as well as for many other applications in nanomedicine, cosmetic, chemical and pharmaceutical industry. To prepare large quantities of a high quality product, the whole bioprocess has to be optimised. This includes not only the cultivation of the bacterial culture, but also the isolation step itself, which can be of critical importance for the production process. To determine the most appropriate method for the isolation of biologically active nanoparticles, three methods for bacterial cell disruption were analyzed. Results In this study, enzymatic lysis and two mechanical methods, high-pressure homogenization and sonication, were compared. During enzymatic lysis the enzyme lysozyme was found to attach to the surface of IBs, and it could not be removed by simple washing. As this represents an additional impurity in the engineered nanoparticles, we concluded that enzymatic lysis is not the most suitable method for IBs isolation. During sonication proteins are released (lost from the surface of IBs and thus the surface of IBs appears more porous when compared to the other two methods. We also found that the acoustic output power needed to isolate the IBs from bacterial cells actually damages proteins structures, thereby causing a reduction in biological activity. High-pressure homogenization also caused some damage to IBs, however the protein loss from the IBs was negligible. Furthermore, homogenization had no side-effects on protein biological activity. Conclusions The study shows that among the three methods tested, homogenization is the most appropriate method for the isolation of active nanoparticles from bacterial cells.

  10. EVALUATION OF BIOLOGICALLY ACTIVE MOLECULES ISOLATED FROM OBLIGATE MARINE FUNGI

    Directory of Open Access Journals (Sweden)

    A. KRISHNA SATYA

    2013-01-01

    Full Text Available The marine environment is a tremendous source of natural products. Marine microorganisms have become an important source of pharmacologically active metabolites Fungi are well known for their vast diversity of secondary metabolites that include many life-saving drugs and highly toxic mycotoxins. In general, fungal cultures producing such metabolites are immune to their toxic effects. However, some are known to produce self-toxic compounds that can pose production optimization challenges if the metabolites are needed in large amounts for chemical modification. Objective: The main objective of the present study was the isolation of new and preferably biologically active secondary metabolites from marine microorganisms, especially marine-derived fungi. Method: Marine fungi had isolated from marine soil by serial dilution method from Rose Bengal medium. Single colony was isolated by microscopic and macroscopic observation. Secondary metabolites are produced by marine fungi. Biological evaluation was performed by microbial studies. TLC is performed to identify the number of sub compounds in the crude extract. Further species level identification and structure elucidation of the compound are to be done. Results: The isolated marine fungi Aspergillus sp, showed maximum activity against the Candida rugosa with a zone diameter of 16mm at a concentration of 200μg and for bacterial strains it showed maximum activity against the E.coli with a diameter of 24mm at a concentration of 200μg. From the thin layer chromatography it has nearly 2-3 compounds to be purified. Conclusion: The selected organism which produces the compounds contains the biological activities which include anti-bacterial and anti fungal activities.

  11. Destruction of methyl bromide sorbed to activated carbon by thiosulfate and electrolysis

    Science.gov (United States)

    Methyl bromide is widely used as a fumigant for post-harvest and quarantine uses at port facilities due to the low treatment times required, but it is vented to the atmosphere after its use. Due to the potential contributions of methyl bromide to stratospheric ozone depletion, technologies for the c...

  12. Synthesis, crystal structure and biological activity of novel diester cyclophanes

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Pengfei; Yang, Bingqin; Fang, Xianwen; Cheng, Zhao; Yang, Meipan, E-mail: yangbq@nwu.edu.cn [Department of Chemistry, Key Laboratory of Synthetic and Natural Functional Molecule Chemistry, Northwest University, Shaanxi (China)

    2012-10-15

    A series of novel diester cyclophanes was synthesized by esterification of 1,2-benzenedicarbonyl chloride with eight different diols under high dilution conditions. The structures of the compounds were verified by elemental analysis, {sup 1}H nuclear magnetic resonance (NMR), IR spectroscopy and high resolution mass spectrometry (HRMS). The crystal structures of two compounds were characterized by single crystal X-ray diffractometry (XRD). All the new cyclophanes were evaluated for biological activities and the results showed that some of these compounds have low antibacterial or antifungal activities (author)

  13. Established and emerging biological activity markers of inflammatory bowel disease

    DEFF Research Database (Denmark)

    Nielsen, O H; Vainer, B; Madsen, S M;

    2000-01-01

    Assessment of disease activity in inflammatory bowel disease (IBD), i.e., ulcerative colitis (UC) and Crohn's disease (CD), is done using clinical parameters and various biological disease markers. Ideally, a disease marker must: be able to identify individuals at risk of a given disorder......, be disease specific, mirror the disease activity and, finally, be easily applicable for routine clinical purposes. However, no such disease markers have yet been identified for IBD. In this article, classical disease markers including erythrocyte sedimentation rate, acute phase proteins (especially...

  14. Exogenous methyl jasmonate treatment increases glucosinolate biosynthesis and quinone reductase activity in kale leaf tissue.

    Science.gov (United States)

    Ku, Kang-Mo; Jeffery, Elizabeth H; Juvik, John A

    2014-01-01

    Methyl jasmonate (MeJA) spray treatments were applied to the kale varieties 'Dwarf Blue Curled Vates' and 'Red Winter' in replicated field plantings in 2010 and 2011 to investigate alteration of glucosinolate (GS) composition in harvested leaf tissue. Aqueous solutions of 250 µM MeJA were sprayed to saturation on aerial plant tissues four days prior to harvest at commercial maturity. The MeJA treatment significantly increased gluconasturtiin (56%), glucobrassicin (98%), and neoglucobrassicin (150%) concentrations in the apical leaf tissue of these genotypes over two seasons. Induction of quinone reductase (QR) activity, a biomarker for anti-carcinogenesis, was significantly increased by the extracts from the leaf tissue of these two cultivars. Extracts of apical leaf tissues had greater MeJA mediated increases in phenolics, glucosinolate concentrations, GS hydrolysis products, and QR activity than extracts from basal leaf tissue samples. The concentration of the hydrolysis product of glucoraphanin, sulforphane was significantly increased in apical leaf tissue of the cultivar 'Red Winter' in both 2010 and 2011. There was interaction between exogenous MeJA treatment and environmental conditions to induce endogenous JA. Correlation analysis revealed that indole-3-carbanol (I3C) generated from the hydrolysis of glucobrassicin significantly correlated with QR activity (r = 0.800, Pkale leaf tissues of both cultivars in 2011. Correlation analysis of these results indicated that sulforaphane, NI3C, neoascorbigen, I3C, and diindolylmethane were all significantly correlated with QR activity. Thus, increased QR activity may be due to combined increases in phenolics (quercetin and kaempferol) and GS hydrolysis product concentrations rather than by individual products alone.

  15. Biological effects of short-term, high-concentration exposure to methyl isocyanate. I. Study objectives and inhalation exposure design.

    OpenAIRE

    Dodd, D E; Frank, F R; Fowler, E H; Troup, C M; Milton, R M

    1987-01-01

    Early reports from India indicated that humans were dying within minutes to a few hours from exposure to methyl isocyanate (MIC). Attempts to explain the cause(s) of these rapid mortalities is where Union Carbide Corporation concentrated its post-Bhopal toxicologic investigations. The MIC studies involving rats and guinea pigs focused primarily on the consequences of acute pulmonary damage. All MIC inhalation exposures were acute, of short duration (mainly 15 min), and high in concentration (...

  16. Chemical Composition and Biological Activities of Allium roseum L. var. grandiflorum Briq. Essential Oil.

    Science.gov (United States)

    Touihri, Imen; Boukhris, Maher; Marrakchi, Naziha; Luis, José; Hanchi, Belgacem; Kallech-Ziri, Olfa

    2015-01-01

    Allium roseum L. (Alliaceae) endemic mediterranean specie was represented in the North Africa by 12 different taxa. In the present study, chemical composition, antiproliferative, antioxidant and antimicrobial activities of the essential oil extracted from A. roseum var. grandiflorum Briq. bulbs collected in the North of Tunisia were investigated. Chemical characterization has shown methyl methanethiosulfinate as major sulphurous compounds. A. roseum bulbs essential oil provides interesting antiproliferative activity against two human colonic adenocarcinoma HT29 and CACO2 cell lines in dose-dependent manner with a half-maximal inhibition (IC50) of 4.64 µg/mL and 8.22 µg/mL respectively. The antioxidant activity, as determined by FRAP assay, was 285 µmol equivalent Trolox/g of essential oil. The scavenging effect on DPPH radicals of essential oil was estimated as IC50 values at 156 µg/mL. The inhibition of superoxide anion production in a model of cancer cell lines was significant for both lines HT29 and CACO2 with IC50 of 20.25 µg/mL and 29.12 µg/mL respectively. Allium roseum essential oil exhibited antibacterial and antifungal activities with a high effectiveness against Candida albicans given by an MIC value of 0.019 mg/mL. This biological effect appears to be related mainly to the presence of organosulfur compounds.

  17. Hepatic global DNA and peroxisome proliferator-activated receptor alpha promoter methylation are altered in peripartal dairy cows fed rumen-protected methionine.

    Science.gov (United States)

    Osorio, J S; Jacometo, C B; Zhou, Z; Luchini, D; Cardoso, F C; Loor, J J

    2016-01-01

    The availability of Met in metabolizable protein (MP) of a wide range of diets for dairy cows is low. During late pregnancy and early lactation, in particular, suboptimal Met in MP limits its use for mammary and liver metabolism and also for the synthesis of S-adenosylmethionine, which is essential for many biological processes, including DNA methylation. The latter is an epigenetic modification involved in the regulation of gene expression, hence, tissue function. Thirty-nine Holstein cows were fed throughout the peripartal period (-21 d to 30 d in milk) a basal control (CON) diet (n=14) with no Met supplementation, CON plus MetaSmart (MS; Adisseo NA, Alpharetta, GA; n=12), or CON plus Smartamine M (SM; Adisseo NA; n=13). The total mixed ration dry matter for the close-up and lactation diets was measured weekly, then the Met supplements were adjusted daily and top-dressed over the total mixed ration at a rate of 0.19 (MS) or 0.07% (SM) on a dry matter basis. Liver tissue was collected on -10, 7, and 21 d for global DNA and peroxisome proliferator-activated receptor alpha (PPARα) promoter region-specific methylation. Several PPARα target and putative target genes associated with carnitine synthesis and uptake, fatty acid metabolism, hepatokines, and carbohydrate metabolism were also studied. Data were analyzed using PROC MIXED of SAS (SAS Institute Inc., Cary, NC) with the preplanned contrast CON versus SM + MS. Global hepatic DNA methylation on d 21 postpartum was lower in Met-supplemented cows than CON. However, of 2 primers used encompassing 4 to 12 CpG sites in the promoter region of bovine PPARA, greater methylation occurred in the region encompassing -1,538 to -1,418 from the transcription start site in cows supplemented with Met. Overall expression of PPARA was greater in Met-supplemented cows than CON. Concomitantly, PPARA-target genes, such as ANGPTL4, FGF21, and PCK1, were also upregulated overall by Met supplementation. The upregulation of PPAR

  18. The Chemistry and Biological Activities of Mimosine: A Review.

    Science.gov (United States)

    Nguyen, Binh Cao Quan; Tawata, Shinkichi

    2016-08-01

    Mimosine [β-[N-(3-hydroxy-4-oxypyridyl)]-α-aminopropionic acid] is a non-protein amino acid found in the members of Mimosoideae family. There are a considerable number of reports available on the chemistry, methods for estimation, biosynthesis, regulation, and degradation of this secondary metabolite. On the other hand, over the past years of active research, mimosine has been found to have various biological activities such as anti-cancer, antiinflammation, anti-fibrosis, anti-influenza, anti-virus, herbicidal and insecticidal activities, and others. Mimosine is a leading compound of interest for use in the development of RAC/CDC42-activated kinase 1 (PAK1)-specific inhibitors for the treatment of various diseases/disorders, because PAK1 is not essential for the growth of normal cells. Interestingly, the new roles of mimosine in malignant glioma treatment, regenerative dentistry, and phytoremediation are being emerged. These identified properties indicate an exciting future for this amino acid. The present review is focused on the chemistry and recognized biological activities of mimosine in an attempt to draw a link between these two characteristics. Copyright © 2016 John Wiley & Sons, Ltd.

  19. Biological Activities of Phenolic Compounds of Extra Virgin Olive Oil.

    Science.gov (United States)

    Servili, Maurizio; Sordini, Beatrice; Esposto, Sonia; Urbani, Stefania; Veneziani, Gianluca; Di Maio, Ilona; Selvaggini, Roberto; Taticchi, Agnese

    2013-12-20

    Over the last few decades, multiple biological properties, providing antioxidant, anti-inflammatory, chemopreventive and anti-cancer benefits, as well as the characteristic pungent and bitter taste, have been attributed to Extra Virgin Olive Oil (EVOO) phenols. In particular, growing efforts have been devoted to the study of the antioxidants of EVOO, due to their importance from health, biological and sensory points of view. Hydrophilic and lipophilic phenols represent the main antioxidants of EVOO, and they include a large variety of compounds. Among them, the most concentrated phenols are lignans and secoiridoids, with the latter found exclusively in the Oleaceae family, of which the drupe is the only edible fruit. In recent years, therefore, we have tackled the study of the main properties of phenols, including the relationships between their biological activity and the related chemical structure. This review, in fact, focuses on the phenolic compounds of EVOO, and, in particular, on their biological properties, sensory aspects and antioxidant capacity, with a particular emphasis on the extension of the product shelf-life.

  20. Biological Activities of Phenolic Compounds of Extra Virgin Olive Oil

    Directory of Open Access Journals (Sweden)

    Maurizio Servili

    2013-12-01

    Full Text Available Over the last few decades, multiple biological properties, providing antioxidant, anti-inflammatory, chemopreventive and anti-cancer benefits, as well as the characteristic pungent and bitter taste, have been attributed to Extra Virgin Olive Oil (EVOO phenols. In particular, growing efforts have been devoted to the study of the antioxidants of EVOO, due to their importance from health, biological and sensory points of view. Hydrophilic and lipophilic phenols represent the main antioxidants of EVOO, and they include a large variety of compounds. Among them, the most concentrated phenols are lignans and secoiridoids, with the latter found exclusively in the Oleaceae family, of which the drupe is the only edible fruit. In recent years, therefore, we have tackled the study of the main properties of phenols, including the relationships between their biological activity and the related chemical structure. This review, in fact, focuses on the phenolic compounds of EVOO, and, in particular, on their biological properties, sensory aspects and antioxidant capacity, with a particular emphasis on the extension of the product shelf-life.

  1. DNA methylation profiling of the human major histocompatibility complex: a pilot study for the human epigenome project.

    OpenAIRE

    Rakyan, Vardhman K.; Thomas Hildmann; Novik, Karen L; Jörn Lewin; Jörg Tost; Antony V Cox; T Dan Andrews; Howe, Kevin L.; Thomas Otto; Alexander Olek; Judith Fischer; Gut, Ivo G.; Kurt Berlin; Stephan Beck

    2004-01-01

    The Human Epigenome Project aims to identify, catalogue, and interpret genome-wide DNA methylation phenomena. Occurring naturally on cytosine bases at cytosine–guanine dinucleotides, DNA methylation is intimately involved in diverse biological processes and the aetiology of many diseases. Differentially methylated cytosines give rise to distinct profiles, thought to be specific for gene activity, tissue type, and disease state. The identification of such methylation variable positions will si...

  2. Anti-inflammatory activity of methyl palmitate and ethyl palmitate in different experimental rat models

    Energy Technology Data Exchange (ETDEWEB)

    Saeed, Noha M. [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Egyptian Russian University, Cairo (Egypt); El-Demerdash, Ebtehal [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Cairo (Egypt); Abdel-Rahman, Hanaa M. [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Egyptian Russian University, Cairo (Egypt); Algandaby, Mardi M. [Department of Biology (Botany), Faculty of Science, King Abdulaziz University, Jeddah (Saudi Arabia); Al-Abbasi, Fahad A. [Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah (Saudi Arabia); Abdel-Naim, Ashraf B., E-mail: abnaim@pharma.asu.edu.eg [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Cairo (Egypt)

    2012-10-01

    Methyl palmitate (MP) and ethyl palmitate (EP) are naturally occurring fatty acid esters reported as inflammatory cell inhibitors. In the current study, the potential anti-inflammatory activity of MP and EP was evaluated in different experimental rat models. Results showed that MP and EP caused reduction of carrageenan-induced rat paw edema in addition to diminishing prostaglandin E2 (PGE2) level in the inflammatory exudates. In lipopolysaccharide (LPS)-induced endotoxemia in rats, MP and EP reduced plasma levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). MP and EP decreased NF-κB expression in liver and lung tissues and ameliorated histopathological changes caused by LPS. Topical application of MP and EP reduced ear edema induced by croton oil in rats. In the same animal model, MP and EP reduced neutrophil infiltration, as indicated by decreased myeloperoxidase (MPO) activity. In conclusion, this study demonstrates the effectiveness of MP and EP in combating inflammation in several experimental models. -- Highlights: ► Efficacy of MP and EP in combating inflammation was displayed in several models. ► MP and EP reduced carrageenan-induced rat paw edema and prostaglandin E2 level. ► MP and EP decreased TNF-α and IL-6 levels in experimental endotoxemia. ► MP and EP reduced NF-κB expression and histological changes in rat liver and lung. ► MP and EP reduced croton oil-induced ear edema and neutrophil infiltration.

  3. Effect of Pd surface structure on the activation of methyl acetate

    Energy Technology Data Exchange (ETDEWEB)

    Xu, Lijun [ORNL; Xu, Ye [ORNL

    2011-01-01

    The activation of methyl acetate (CH3COOCH3; MA) has been studied using periodic density functional theory calculations to probe the effect of Pd surface structure on the selectivity in MA activation. The adsorption of MA, dehydrogenated derivatives, enolate (CH2COOCH3; ENL) and methylene acetate (CH3COOCH2; MeA), and several dissociation products (including acetate, acetyl, ketene, methoxy, formaldehyde, CO, C, O, and H); and C-H and C-O (mainly in the RCO-OR position) bond dissociation in MA, ENL, and MeA, are calculated on Pd(111) terrace, step, and kink; and on Pd(100) terrace and step. The adsorption of most species is not strongly affected between (111)- to (100)-type surfaces, but is clearly enhanced by step/kink compared to the corresponding terrace. Going from terrace to step edge and from (111)- to (100)-type surfaces both stabilize the transition states of C-O bond dissociation steps. Going from terrace to step edge also stabilizes the transition states of C-H bond dissociation steps, but going from (111)- to (100)-type surfaces does not clearly do so. We propose that compared to the Pd(111) terrace, the Pd(100) terrace is more selective for C-O bond dissociation that is desirable for alcohol formation, whereas the Pd step edges are more selective for C-H bond dissociation.

  4. Methyl jasmonate affects morphology, number and activity of endoplasmic reticulum bodies in Raphanus sativus root cells.

    Science.gov (United States)

    Gotté, Maxime; Ghosh, Rajgourab; Bernard, Sophie; Nguema-Ona, Eric; Vicré-Gibouin, Maïté; Hara-Nishimura, Ikuko; Driouich, Azeddine

    2015-01-01

    The endoplasmic reticulum (ER) bodies are ER-derived structures that are found in Brassicaceae species and thought to play a role in defense. Here, we have investigated the occurrence, distribution and function of ER bodies in root cells of Raphanus sativus using a combination of microscopic and biochemical methods. We have also assessed the response of ER bodies to methyl jasmonate (MeJA), a phytohormone that mediates plant defense against wounding and pathogens. Our results show that (i) ER bodies do occur in different root cell types from the root cap region to the differentiation zone; (ii) they do accumulate a PYK10-like protein similar to the major marker protein of ER bodies that is involved in defense in Arabidopsis thaliana; and (iii) treatment of root cells with MeJA causes a significant increase in the number of ER bodies and the activity of β-glucosidases. More importantly, MeJA was found to induce the formation of very long ER bodies that results from the fusion of small ones, a phenomenon that has not been reported in any other study so far. These findings demonstrate that MeJA impacts the number and morphology of functional ER bodies and stimulates ER body enzyme activities, probably to participate in defense responses of radish root. They also suggest that these structures may provide a defensive system specific to root cells.

  5. Exogenous methyl jasmonate regulates cytokinin content by modulating cytokinin oxidase activity in wheat seedlings under salinity.

    Science.gov (United States)

    Avalbaev, Azamat; Yuldashev, Ruslan; Fedorova, Kristina; Somov, Kirill; Vysotskaya, Lidiya; Allagulova, Chulpan; Shakirova, Farida

    2016-02-01

    The treatment of 4-days-old wheat seedlings with methyl jasmonate (MeJA) in concentration optimal for their growth (0.1 μM) resulted in a rapid transient almost two-fold increase in the level of cytokinins (CKs). MeJA-induced accumulation of CKs was due to inhibition of both cytokinin oxidase (CKX) (cytokinin oxidase/dehydrogenase, EC 1.5.99.12) gene expression and activity of this enzyme. Pretreatment of wheat seedlings with MeJA decreased the growth-retarding effect of sodium chloride salinity and accelerated growth recovery after withdrawal of NaCl from the incubation medium. We speculate that this protective effect of the hormone might be due to MeJA's ability to prevent the salinity-induced decline in CK concentration that was caused by inhibition of gene expression and activity of CKX in wheat seedlings. The data might indicate an important role for endogenous cytokinins in the implementation of growth-promoting and protective effects of exogenous MeJA application on wheat plants.

  6. Heat-activated persulfate oxidation of methyl- and ethyl-parabens: Effect, kinetics, and mechanism.

    Science.gov (United States)

    Chen, Yiqun; Deng, Pinya; Xie, Pengchao; Shang, Ran; Wang, Zongping; Wang, Songlin

    2017-02-01

    We evaluated the degradation of methylparaben (MeP) and ethylparaben (EtP), two representative parabens, using the heat-activated persulfate system in a laboratory. Both sulfate and hydroxyl radicals contributed to the removal of the two parabens. The degradations of both MeP and EtP were improved by increasing the heating temperature or persulfate dose in accordance with a pseudo-first-order reaction model. The oxidation efficiency of parabens was found to be pH-dependent; decreasing in the order pH 5.0 > 7.0 > 9.0. The presence of chloride, bicarbonate, or humic acid was found to inhibit the degradation of the two parabens to some extent because of competition for the reactive radicals, with humic acid having the most serious effect. Dealkylation of the methyl unit, decarboxylation of the carboxylic group, and subsequent hydrolysis are proposed to be involved in the degradation pathway of MeP. The results suggest that the heat-activated persulfate system might be efficiently applied in the treatment of paraben-containing water samples. This was also supported by the results of applying this system to treat a real water sample containing both MeP and EtP.

  7. Preparation, Characterization and Photocatalytic Activities of TiO2 towards Methyl Red Degradation

    Directory of Open Access Journals (Sweden)

    Aware Dinkar Vishwanath

    2017-02-01

    Full Text Available Highly efficient, photoactive, nanocrystalline TiO2 powder was prepared with the help of modified sol-gel method. The prepared nanomaterials were characterized by modern techniques such as, TG-DTA, XRD, FE-SEM, EDX, TEM, BET surface area and FT-IR analysis for the identification of phase structure, phase composition and morphology. Formation of thermally stable, nanocrystalline, highley photocatalytic active, tetragonal anatase Titania was confirmed by TGA-DTA, XRD and HR-TEM. Similarly, FE-SEM confirms spherical, cauliflower like morphology for all Titania samples prepared with different cationic surfactants. The presence of mesoporous Titania was also confirmed by N2 adsorption-desorption. The effect of addition of various surfactants significantly improves the photocatalytic activity. Prepared nanomaterials were successfully tested under UV-Vis light region for photodegradation of Methyl Red (MR dye material which is act as water pollutant. The C16TAB assisted Titania exhibits enhance photocatalytic efficiency as compared to industrially applied photocatalyst, Titania (Degussa P25 and zinc oxide under similar experimental condition.

  8. Synthesis and Biological Activities of Some New (Nα-Dinicotinoyl- bis-L-Leucyl Linear and Macrocyclic Peptides

    Directory of Open Access Journals (Sweden)

    Suzan Khayyat

    2014-07-01

    Full Text Available A series of linear and macrocyclic peptides 3–12 were synthesized using 3,5-pyridinedicarboxylic acid (1 as starting material and screened for their antimicrobial, anti-inflammatory and anticancer activities. Bis-ester 3 was prepared from 1 and L-leucine methyl ester. Hydrazinolysis and hydrolysis of dipeptide methyl ester 3 with hydrazine hydrate or 1 N sodium hydroxide afforded compounds 4 and 5, respectively. Cyclization of the dipeptide 5 with L-lysine methyl ester afforded cyclic pentapeptide ester 6. Compounds 7–9 were synthesized by reacting hydrazide 4 with phthalic anhydride, 1,8-naphthalene anhydride or acetophenone derivatives. Treatment of acid hydrazide 4 with aromatic aldehydes or tetraacid dianhydrides afforded the corresponding bis-dipeptide hydrazones 10a–e and macrocyclic peptides 11 and 12, respectively. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, biological and pharmacological activities of the synthesized compounds was reported.

  9. Methyl syringate, a low-molecular-weight phenolic ester, as an activator of the chemosensory ion channel TRPA1.

    Science.gov (United States)

    Son, Hee Jin; Kim, Min Jung; Park, Jae-Ho; Ishii, Sho; Misaka, Takumi; Rhyu, Mee-Ra

    2012-12-01

    Transient receptor potential channel ankryn 1 (TRPA1) and transient receptor potential channel vanilloid 1 (TRPV1) are members of the TRP superfamily of structurally related, nonselective cation channels and are often coexpressed in sensory neurons. Extracts of the first leaves of Kalopanax pictus Nakai (Araliaceae) have been shown to activate hTRPA1 and hTRPV1. Therefore, the effects of six commercially available chemicals (methyl syringate, coniferyl alcohol, protocatechuic acid, hederacoside C, α-hederin, and eleutheroside B) found in K. pictus were investigated on cultured cells expressing hTRPA1 and hTRPV1. Of the six compounds, methyl syringate selectively activated hTRPA1 (EC(50) = 507.4 μM), but not hTRPV1. Although methyl syringate had a higher EC(50) compared with allyl isothiocyanate (EC(50) = 7.4 μM) and cinnamaldehyde (EC(50) = 22.2 μM), the present study provides evidence that methyl syringate from K. pictus is a specific and selective activator of hTRPA1.

  10. The cell biology of T-dependent B cell activation

    DEFF Research Database (Denmark)

    Owens, T; Zeine, R

    1989-01-01

    The requirement that CD4+ helper T cells recognize antigen in association with class II Major Histocompatibility Complex (MHC) encoded molecules constrains T cells to activation through intercellular interaction. The cell biology of the interactions between CD4+ T cells and antigen-presenting cells...... includes multipoint intermolecular interactions that probably involve aggregation of both polymorphic and monomorphic T cell surface molecules. Such aggregations have been shown in vitro to markedly enhance and, in some cases, induce T cell activation. The production of T-derived lymphokines that have been...... implicated in B cell activation is dependent on the T cell receptor for antigen and its associated CD3 signalling complex. T-dependent help for B cell activation is therefore similarly MHC-restricted and involves T-B intercellular interaction. Recent reports that describe antigen-independent B cell...

  11. Biologically active traditional medicinal herbs from Balochistan, Pakistan.

    Science.gov (United States)

    Zaidi, Mudassir A; Crow, Sidney A

    2005-01-01

    The biological activities of the following four important medicinal plants of Balochistan, Pakistan were checked; Grewia erythraea Schwein f. (Tiliaceae), Hymenocrater sessilifolius Fisch. and C.A. Mey (Lamiaceae), Vincetoxicum stocksii Ali and Khatoon (Asclepiadaceae) and Zygophyllum fabago L. (Zygophyllaceae). The methanolic extracts were fractionated into hexane, ethyl acetate, chloroform, butanol and water. The antifungal and antibacterial activities of these plants were determined against 12 fungal and 12 bacterial strains by agar well diffusion and disk diffusion assays. The extract of Zygophyllum fabago was found to be highly effective against Candida albicans and Escherichia coli. The extract of Vincetoxicum stocksii was also found to be significantly active against Candida albicans, Bacillus subtilis and Bacillus cereus. Extracts of Hymenocrater sessilifolius and Grewia erythraea showed good activity only against Pseudomonas aeruginosa.

  12. [Influence of biological activated carbon dosage on landfill leachate treatment].

    Science.gov (United States)

    Cui, Yan-Rui; Guo, Yan; Wu, Qing

    2014-08-01

    Effects of biological activated carbon (BAC) dosage on COD removal in landfill leachate treatment were compared. The COD removal efficiency of reactors with 0, 100 and 300 g activated carbon dosage per litre activated sludge was 12.9%, 19.6% and 27.7%, respectively. The results indicated that BAC improved the refractory organic matter removal efficiency and there was a positive correlation between COD removal efficiency and BAC dosage. The output of carbon dioxide after 8h of aeration in reactors was 109, 193 and 306 mg corresponding to the activated carbon dosages mentioned above, which indicated the amount of biodegradation and BAC dosage also had a positive correlation. The combination of adsorption and bioregeneration of BAC resulted in the positive correlation betweem organic matter removal efficiency and BAC dosage, and bioregeneration was the root cause for the microbial decomposition of refractory organics.

  13. Biological activities of triazine derivatives. Combining DFT and QSAR results

    Directory of Open Access Journals (Sweden)

    Majdouline Larif

    2017-02-01

    Full Text Available In order to investigate the relationship between activities and structures, a 3D-QSAR study is applied to a set of 43 molecules based on triazines. This study was conducted using the principal component analysis (PCA method, the multiple linear regression method (MLR and the artificial neural network (ANN. The predicted values of activities are in good agreement with the experimental results. The artificial neural network (ANN techniques, considering the relevant descriptors obtained from the MLR, showed a correlation coefficient of 0.9 with an 8-3-1 ANN model which is a good result. As a result of quantitative structure–activity relationships, we found that the model proposed in this study is constituted of major descriptors used to describe these molecules. The obtained results suggested that the proposed combination of several calculated parameters could be useful to predict the biological activity of triazine derivatives.

  14. Biological activities of water-soluble fullerene derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Nakamura, S; Mashino, T [Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shiba-koen, Minato-ku, Tokyo 105-8512 (Japan)], E-mail: mashino-td@pha.keio.ac.jp

    2009-04-01

    Three types of water-soluble fullerene derivatives were synthesized and their biological activities were investigated. C{sub 60}-dimalonic acid, an anionic fullerene derivative, showed antioxidant activity such as quenching of superoxide and relief from growth inhibition of E. coli by paraquat. C{sub 60}-bis(7V,7V-dimethylpyrrolidinium iodide), a cationic fullerene derivative, has antibacterial activity and antiproliferative effect on cancer cell lines. The mechanism is suggested to be respiratory chain inhibition by reactive oxygen species produced by the cationic fullerene derivative. Proline-type fullerene derivatives showed strong inhibition activities on HIV-reverse transcriptase. The IC{sub 50} values were remarkably lower than nevirapine, a clinically used anti-HIV drug. Fullerene derivatives have a big potential for a new type of lead compound to be used as medicine.

  15. Synthesis, Spatial Structure and Analgesic Activity of Sodium 3-Benzylaminocarbonyl-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazin-4-olate Solvates

    Directory of Open Access Journals (Sweden)

    Igor V. Ukrainets

    2016-10-01

    Full Text Available In order to obtain and then test pharmocologically any possible conformers of the new feasible analgesic N-benzyl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide, its 4-O-sodium salt was synthesized using two methods. X-ray diffraction study made possible to determine that, depending on the chosen synthesis conditions, the above-mentioned compound forms either monosolvate with methanol or monohydrate, where organic anion exists in the form of three different conformers. Pharmacological testing of the two known pseudo-enantiomeric forms of the original N-benzylamide and of the two solvates of its sodium salt was performed simultaneously under the same conditions and in equimolar doses. Comparison of the results obtained while studying the peculiarities of the synthesized compounds spatial structure and biological properties revealed an important structure-action relationship. In particular, it was shown that the intensity of analgesic effect of different conformational isomers of N-benzyl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide may change considerably: while low active conformers are comparable with piroxicam, highly active conformers are more than twice as effective as meloxicam.

  16. Synthesis, Spatial Structure and Analgesic Activity of Sodium 3-Benzylaminocarbonyl-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazin-4-olate Solvates

    Science.gov (United States)

    Ukrainets, Igor V.; Petrushova, Lidiya A.; Shishkina, Svitlana V.; Grinevich, Lina A.; Sim, Galina

    2016-01-01

    In order to obtain and then test pharmocologically any possible conformers of the new feasible analgesic N-benzyl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide, its 4-O-sodium salt was synthesized using two methods. X-ray diffraction study made possible to determine that, depending on the chosen synthesis conditions, the above-mentioned compound forms either monosolvate with methanol or monohydrate, where organic anion exists in the form of three different conformers. Pharmacological testing of the two known pseudo-enantiomeric forms of the original N-benzylamide and of the two solvates of its sodium salt was performed simultaneously under the same conditions and in equimolar doses. Comparison of the results obtained while studying the peculiarities of the synthesized compounds spatial structure and biological properties revealed an important structure-action relationship. In particular, it was shown that the intensity of analgesic effect of different conformational isomers of N-benzyl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide may change considerably: while low active conformers are comparable with piroxicam, highly active conformers are more than twice as effective as meloxicam. PMID:27775559

  17. Enhanced Photocatalytic Activity for Degradation of Methyl Orange over Silica-Titania

    Directory of Open Access Journals (Sweden)

    Yaping Guo

    2011-01-01

    Full Text Available Silica-modified titania (SMT powders with different atomic ratios of silica to titanium (Rx were successfully synthesized by a simple ultrasonic irradiation technique. The prepared samples were characterized by X-ray diffraction (XRD, FT-IR spectroscopy, transmission electron microscopy (TEM, X-ray photoelectron spectroscopy (XPS, and ultraviolet visible spectroscopy. The specific surface area was measured according to BET theory. Results indicate that the addition of silica to titania can suppress the crystalline size growth and the transformation of anatase phase to rutile phase of titania, enlarge specific surface area of the titania particles, and result in a blue shift of absorption edge compared to pure titania. The photocatalytic activity of the SMT samples was evaluated by decolorizing methyl orange aqueous solutions under UV-visible light irradiation. It was found in our study that this activity was affected by silica content, calcination temperature, H2SO4, and oxidants such as KIO4, (NH42S2O8 and H2O2. The results reveal that the photocatalytic activity of 0.1-SMT catalyst is the best among all samples calcined at 550°C for 1 h and it is 1.56 times higher than that of Degussa P-25 titania, which is a widely used commercial TiO2 made by Germany Degussa company and has been most widely used in industry as photocatalyst, antiultraviolet product, and thermal stabilizer. The optimal calcination temperature for preparation was 550°C. The photocatalytic activity of SMT samples is significantly enhanced by H2SO4 solution treatment and oxidants.

  18. Mangiferin: A review of sources and interventions for biological activities.

    Science.gov (United States)

    Jyotshna; Khare, Puja; Shanker, Karuna

    2016-09-10

    Xanthones are naturally synthesized in various biological systems such as plants, lichens, and fungi and are stored as by-products. In addition to taxonomic significance they are also important in the treatment/management of a number of human disorders. Mangiferin and its derived lead molecule have never qualified for use in a clinical trial despite a number of pharmacological studies that have proven its effectiveness as an antioxidant, analgesic, antidiabetic, antiproliferative, chemopreventive, radioprotective, cardiotonic, immunomodulatory, and diuretic. For centuries in the traditional practice of medicine in India and China the use of plants containing mangiferin has been a major component for disease management and health benefits. While it resembles biflavones, the C-glucosyl xanthone (mangiferin) has great nutritional and medicinal significance due to its unique structural characteristics. The C-glycoside link of mangiferin, mimicked to nucleophilic phloroglucinol substitution, facilitates its bioavailability and also is responsible for its antioxidant properties. Researchers have also utilized its xanthonic framework for both pharmacophoric backbone and for its use as a substitution group for synthesis and prospects. To date more than 500 derivatives using about 80 reactions have been generated. These reactions include: lipid peroxidation, phosphorylation, glycosylation, methylation, fermentation, deglycosylation, hydrolysis, polymerization, sulfation, acylation, etherification, peroxidation among others. Multiple studies on efficacy and safety have increased the global demand of mangiferin-based food supplements. This review highlights the distribution of mangiferin in plants, its isolation, and assay methods applicable to different sample matrices. In addition we include updates on various strategies and derived products intended for designated pharmacological actions. © 2016 BioFactors, 42(5):504-514, 2016.

  19. Biological significance of DNA adducts investigated by simultaneous analysis of different endpoints of genotoxicity in L5178Y mouse lymphoma cells treated with methyl methanesulfonate.

    Science.gov (United States)

    Brink, Andreas; Schulz, Berta; Stopper, Helga; Lutz, Werner K

    2007-12-01

    The biological significance of DNA adducts is under continuous discussion because analytical developments allow determination of adducts at ever lower levels. Central questions refer to the biological consequences of adducts and to the relationship between background DNA damage and exposure-related increments. These questions were addressed by measuring the two DNA adducts 7-methylguanine (7-mG) and O(6)-methyl-2'-deoxyguanosine (O(6)-mdGuo) by LC-MS/MS in parallel to two biological endpoints of genotoxicity (comet assay and in vitro micronucleus test), using large batches of L5178Y mouse lymphoma cells treated with methyl methanesulfonate (MMS). The background level of 7-mG was 1440 adducts per 10(9) nucleotides while O(6)-mdGuo was almost 50-fold lower (32 adducts per 10(9) nucleotides). In the comet assay and the micronucleus test, background was in the usual range seen with smaller batches of cells (2.1% Tail DNA and 12 micronuclei-containing cells per 1000 binucleated cells, respectively). For the comparison of the four endpoints for dose-related increments above background in the low-response region we assumed linearity at low dose and used the concept of the "doubling dose", i.e., we estimated the concentration of MMS necessary to double the background measures. Doubling doses of 4.3 and 8.7microM MMS were deduced for 7-mG and O(6)-mdGuo, respectively. For doubling the background measures in the comet assay and the micronucleus test, 5 to 15-fold higher concentrations of MMS were necessary (45 and 66microM, respectively). This means that the contribution of an increase in DNA methylation to biological endpoints of genotoxicity is overestimated. For xenobiotics that generate adducts without background, the difference is even more pronounced because the dose-response curve starts at zero and the limit of detection of an increase is not affected by background variation. Consequences for the question of thresholds in dose-response relationships and for the

  20. Synthesis, structural characterization and biological activity of a trinuclear zinc(II) complex: DNA interaction study and antimicrobial activity

    Indian Academy of Sciences (India)

    Bhaskar Biswas; Niranjan Kole; Moumita Patra; Shampa Dutta; Mousumi Ganguly

    2013-11-01

    A trinuclear zinc(II) complex [Zn3L2(-O2CCH3)2(H2O)2]·H2O·2CH3OH (1) was synthesized from an in situ reaction between zinc acetate and a Schiff base ligand (H2L = 2-((2-hydroxyphenylimino) methyl)-6-methoxyphenol). The ligand was prepared by (1:1) condensation of ortho-vanillin and ortho-aminophenol. The ligand and zinc(II) complex were characterized by elemental analysis, Fourier Transform Infrared (FTIR), 1H-Nuclear Magnetic Resonance (NMR), UV-Vis spectroscopy, Powder X-ray Diffraction (PXRD) and thermogravimetric analysis. 1 crystallizes in P-1 space group with = 11.9241(3) Å, = 12.19746 Å, = 20.47784 Å with unit cell volume is 2674.440 (Å)3. Binding property of the complex with calf thymus DNA (CT-DNA) has been investigated using absorption and emission studies. Thermal melting and viscosity experiments were further performed to determine the mode of binding of 1 with CT-DNA. Spectroscopic and viscosity investigations revealed an intercalative binding mode of 1 with CT-DNA. The ligand and its zinc complex were screened for their biological activity against bacterial species and fungi. Activity data show that the metal complex has more antibacterial and antifungal activity than the parent Schiff base ligand and against those bacterial or fungi species.

  1. Mutant p53: multiple mechanisms define biologic activity in cancer

    Directory of Open Access Journals (Sweden)

    Michael Paul Kim

    2015-11-01

    Full Text Available The functional importance of p53 as a tumor suppressor gene is evident through its pervasiveness in cancer biology. The p53 gene is the most commonly altered gene in human cancer; however, not all genetic alterations are biologically equivalent. The majority of p53 alterations involve missense mutations that result in the production of mutant p53 proteins. Such mutant p53 proteins lack normal p53 function and may acquire novel functions, often with deleterious effects. Here, we review characterized mechanisms of mutant p53 gain of function in multiple model systems. In addition, we review mutant p53 addiction as emerging evidence suggests that tumors may depend on sustained mutant p53 activity for continued growth. We also discuss the role of p53 in stromal elements and their contribution to tumor initiation and progression. Lastly, current genetic mouse models of mutant p53 are reviewed and their limitations discussed.

  2. Bone-inducing Activity of Biological Piezoelectric Ceramic

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    To simulate the piezoelectric effect of nature bone, two kinds of biological piezoelectric composite ceramics consisted of hydroxyapatite ( HA ) and lithium sodium potassium riobate (LNK) ceramic of which the ratio of HA/ LNK was 1: 10 and 5:5( wt/ wt ) were prepared. Their piezoelectric property and growth of apatite crystal in the ceramics surface were investigated. With the increase of LNK amount, piezoelectric activity increased correspondingly. By immersing the poled piezoelectric ceramics in simulated body fluid (SBF) at 36.5 ℃ for 7,14, and 21 days, apatite crystal was formed on negatively charged surfaces. After 21 days immersion in SBF,the thickest apatite crystal on the negatively charged surfaces increased to 3.337μm. The novel biological piezoelectric ceramics show an excellent piezoelectric property and superior potential bioactivity.

  3. Radiometric microbiologic assay for the biologically active forms of niacin

    Energy Technology Data Exchange (ETDEWEB)

    Kertcher, J.A.; Guilarte, T.R.; Chen, M.F.; Rider, A.A.; McIntyre, P.A.

    1979-05-01

    A radiometric microbiologic assay has been developed for the determination of niacin in biologic fluids. Lactobacillus plantarum produced /sup 14/CO/sub 2/ from L-(U-/sup 14/C) malic acid in quantities proportional to the amount of niacin present. The assay is specific for the biologically active forms of niacin in humans. Thirty normal hemolysates were analyzed and the values ranged from 13.0 to 17.8 ..mu..g niacin/ml RBC (mean = 15.27 +- 1.33 s.d.). Good recovery and reproducibility studies were obtained with this assay. On thirty blood samples, correlation was excellent between the radiometric and the conventional turbidimetric assays.

  4. Glutarimides: Biological activity, general synthetic methods and physicochemical properties

    Directory of Open Access Journals (Sweden)

    Popović-Đorđević Jelena B.

    2015-01-01

    Full Text Available Glutarimides, 2,6-dioxopiperidines are compounds that rarely occur in natural sources, but so far isolated ones exert widespread pharmacological activities, which makes them valuable as potential pharmacotherapeutics. Glutarimides act as androgen receptor antagonists, anti-inflammatory, anxiolytics, antibacterials, and tumor suppressing agents. Some synthetic glutarimide derivatives are already in use as immunosuppressive and sedative (e.g., thalidomide or anxiolytics (buspirone drugs. The wide applicability of this class of compounds, justify the interest of scientists to explore new pathways for its syntheses. General methods for synthesis of six-membered imide ring, are presented in this paper. These methods include: a reaction of dicarboxylic acids with ammonia or primary amine, b reactions of cyclization: amido-acids, diamides, dinitriles, nitrilo-acids, amido-nitriles, amido-esters, amidoacyl-chlorides or diacyl-chlorides, c adition of carbon-monoxide on a,b-unsaturated amides, d oxidation reactions, e Michael adition of active methylen compounds on methacrylamide or conjugated amides. Some of the described methods are used for closing glutarimide ring in syntheses of farmacological active compounds sesbanimide and aldose reductase inhibitors (ARI. Analyses of the geometry, as well as, the spectroscopic analyses (NMR and FT-IR of some glutarimides are presented because of their broad spectrum of pharmacological activity. To elucidate structures of glutarimides, geometrical parameters of newly synthesized tert-pentyl-1-benzyl-4-methyl-glutarimide-3-carboxylate (PBMG are analyzed and compared with the experimental data from X-ray analysis for glutarimide. Moreover, molecular electrostatic potential (MEP surface which is plotted over the optimized geometry to elucidate the reactivity of PBMG molecule is analyzed. The electronic properties of glutarimide derivatives are explained on the example of thalidomide. The Frontier Molecular Orbital

  5. Fibrillarin methylates H2A in RNA polymerase I trans-active promoters in Brassica oleracea

    Directory of Open Access Journals (Sweden)

    lloyd eLoza-Muller

    2015-11-01

    Full Text Available Fibrillarin is a well conserved methyltransferase involved in several if not all of the more than 100 methylations sites in rRNA which are essential for proper ribosome function. It is mainly localized in the nucleoli and Cajal bodies inside the cell nucleus where it exerts most of its functions. In plants, fibrillarin binds directly the guide RNA together with Nop56, Nop58 and 15.5ka proteins to form a snoRNP complex that selects the sites to be methylated in pre-processing of ribosomal RNA. Recently, the yeast counterpart NOP1 was found to methylate histone H2A in the nucleolar regions. Here we show that plant fibrillarin can also methylate histone H2A. In Brassica floral meristem cells the methylated histone H2A is mainly localized in the nucleolus but unlike yeast or human cells it also localize in the periphery of the nucleus. In specialized transport cells the pattern is altered and it exhibits a more diffuse staining in the nucleus for methylated histone H2A as well as for fibrillarin. Here we also show that plant fibrillarin is capable of interacting with H2A and carry out its methylation in the rDNA promoter.

  6. Fibrillarin methylates H2A in RNA polymerase I trans-active promoters in Brassica oleracea

    Science.gov (United States)

    Loza-Muller, Lloyd; Rodríguez-Corona, Ulises; Sobol, Margarita; Rodríguez-Zapata, Luis C.; Hozak, Pavel; Castano, Enrique

    2015-01-01

    Fibrillarin is a well conserved methyltransferase involved in several if not all of the more than 100 methylations sites in rRNA which are essential for proper ribosome function. It is mainly localized in the nucleoli and Cajal bodies inside the cell nucleus where it exerts most of its functions. In plants, fibrillarin binds directly the guide RNA together with Nop56, Nop58, and 15.5ka proteins to form a snoRNP complex that selects the sites to be methylated in pre-processing of ribosomal RNA. Recently, the yeast counterpart NOP1 was found to methylate histone H2A in the nucleolar regions. Here we show that plant fibrillarin can also methylate histone H2A. In Brassica floral meristem cells the methylated histone H2A is mainly localized in the nucleolus but unlike yeast or human cells it also localize in the periphery of the nucleus. In specialized transport cells the pattern is altered and it exhibits a more diffuse staining in the nucleus for methylated histone H2A as well as for fibrillarin. Here we also show that plant fibrillarin is capable of interacting with H2A and carry out its methylation in the rDNA promoter. PMID:26594224

  7. Synthesis, Crystal Structure and Antibacterial Activities of 3-[3-Methyl-(2-thienyl)methyl-enehydrazinocarbonyl]-(1H)-1,2,4-triazole

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    The title compound, C9HgN5OS, was synthesized by the reaction of 3-(1H)-1,2,4-triazole hydrazine with 3-methyl-2-thiophenecarboxaldehyde in ethanol. The single crystal structure has been determined by X-ray diffraction analysis. The crystal belongs to monoclinic system,space group P21/n with a = 9.5550(10), b = 11.9847(12), c = 10.1074(11) A, β= 112.995(2)°, V=1065.47(19) A3, Z = 4, μ = 0.290 mm-1, Mr= 235.27, Dc = 1.467 g/cm3 and F(000) = 488. The structure was solved by direct methods and refined to R = 0.0449. The crystal structure involves certain antibacterial activity.

  8. Preparation and characterization of new biologically active polyurethane foams.

    Science.gov (United States)

    Savelyev, Yuri; Veselov, Vitali; Markovskaya, Ludmila; Savelyeva, Olga; Akhranovich, Elena; Galatenko, Natalya; Robota, Ludmila; Travinskaya, Tamara

    2014-12-01

    Biologically active polyurethane foams are the fast-developed alternative to many applications of biomedical materials. Due to the polyurethane structure features and foam technology it is possible to incorporate into their structure the biologically active compounds of target purpose via structural-chemical modification of macromolecule. A series of new biologically active polyurethane foams (PUFs) was synthesized with polyethers (MM 2500-5000), polyesters MM (500-2200), 2,4(2,6) toluene diisocyanate, water as a foaming agent, catalysts, foam stabilizers and functional compounds. Different functional compounds: 1,4-di-N-oxy-2,3-bis-(oxymethyl)-quinoxaline (DOMQ), partial sodium salt of poly(acrylic acid) and 2,6-dimethyl-N,N-diethyl aminoacetatanilide hydrochloride were incorporated into the polymer structure/composition due to the chemical and/or physical bonding. Structural peculiarities of PUFs were studied by FTIR spectroscopy and X-ray scattering. Self-adhesion properties of PUFs were estimated by measuring of tensile strength at break of adhesive junction. The optical microscopy method was performed for the PUF morphology studies. Toxicological estimation of the PUFs was carried out in vitro and in vivo. The antibacterial action towards the Gram-positive and Gram-negative bacteria (Escherichia coli ATC 25922, E. coli ATC 2150, Klebsiella pneumoniae 6447, Staphylococcus aureus 180, Pseudomonas aeruginosa 8180, Proteus mirabilis F 403, P. mirabilis 6054, and Proteus vulgaris 8718) was studied by the disc method on the solid nutrient. Physic-chemical properties of the PUFs (density, tensile strength and elongation at break, water absorption and vapor permeability) showed that all studied PUFs are within the operational requirements for such materials and represent fine-cellular foams. Spectral studies confirmed the incorporation of DOMQ into the PUF's macrochain. PUFs are characterized by microheterogeneous structure. They are antibacterially active, non

  9. Inhibition and recovery of maternal and fetal cholinesterase enzyme activity following a single cutaneous dose of methyl parathion and diazinon, alone and in combination, in pregnant rats.

    Science.gov (United States)

    Abu-Qare, A W; Abou-Donia, M B

    2001-01-01

    Pregnant Sprague-Dawley rats (14-18 days of gestation) were treated with a single cutaneous subclinical dose(s) of 10 mg kg(-1) (15% of LD(50)) of methyl parathion (O,O-dimethyl O-4-nitrophenyl phosphorothioate) and 65 mg kg(-1) (15% of LD(50)) of diazinon (O,O)-diethyl O-2-isopropyl-6-methylpyrimidinyl phosphorothioate, and their combination. Animals were sacrificed at 1, 2, 4, 12, 24, 48, 72, and 96 h after dosing. Inhibition of maternal and fetal cholinesterase enzyme activity has been determined. Methyl parathion significantly inhibited maternal and fetal brain acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BuChE) activity within 24 h after dosing. Diazinon and a mixture of methyl parathion and diazinon caused lesser inhibition compared with methyl parathion alone. Recovery of maternal and fetal brain AChE activity was in the order of diazinon > combination of diazinon and methyl parathion > methyl parathion 96 h after dosing. Although fetal plasma BuChE activity recovered to 100% of control within 96 h of application, maternal BuChE activity remained inhibited to 55% and 32% of control 96 h after application of methyl parathion and a mixture of methyl parathion and diazinon, respectively. Following a single dermal dose of methyl parathion, the activity of maternal liver BuChE was 63% of control 2 h after dosing, whereas inhibition of placental AChE or BuChE activity occurred 12 and 1 h following a single dose of methyl parathion, corresponding to activities of 63% and 54% of control, respectively. Diazinon, alone or in combination with methyl parathion, did not inhibit significantly the maternal liver BuChE or placental AChE and BuChE activity. The results suggest that dermal application of a single dose of methyl parathion and diazinon, alone or in combination, has an easy access into maternal and fetal tissues, resulting in inhibition of cholinesterase enzymes. The lower inhibitory effect of the combination of methyl parathion and diazinon

  10. Study of the spectroscopic characteristics of methyl (ligand) cobaloximes and their antibacterial activity

    Indian Academy of Sciences (India)

    N Navaneetha; P A Nagarjun; S Satyanarayana

    2007-01-01

    Spectroscopic characterization (IR, NMR and electronic spectra) of methyl (ligand) cobaloxime was done, where ligand = pyrazole, dimethyl pyrazole, alanine and alanine methyl ester. The frequency changes in the IR spectra and shifts in the NMR were explained on the basis of basicity of the ligand, steric hindrance, HSAB principle and - back-bonding from metal to ligand. Alanine and alanine methyl ester form more stable complexes than pyrazole and dimethyl pyrazole. Based on their IR and 1H NMR spectra it is inferred that pyrazole and dimethylpyrazole bind to Co (III) via N-2 ring nitrogen, i.e. monodentate coordination.

  11. Soil biological activity at European scale - two calculation concepts

    Science.gov (United States)

    Krüger, Janine; Rühlmann, Jörg

    2014-05-01

    The CATCH-C project aims to identify and improve the farm-compatibility of Soil Management Practices including to promote productivity, climate change mitigation and soil quality. The focus of this work concentrates on turnover conditions for soil organic matter (SOM). SOM is fundamental for the maintenance of quality and functions of soils while SOM storage is attributed a great importance in terms of climate change mitigation. The turnover conditions depend on soil biological activity characterized by climate and soil properties. To assess the turnover conditions two model concepts are applied: (I) Biological active time (BAT) regression approach derived from CANDY model (Franko & Oelschlägel 1995) expresses the variation of air temperature, precipitation and soil texture as a timescale and an indicator of biological activity for soil organic matter (SOM) turnover. (II) Re_clim parameter within the Introductory Carbon Balance Model (Andrén & Kätterer 1997) states the soil temperature and soil water to estimate soil biological activity. The modelling includes two strategies to cover the European scale and conditions. BAT was calculated on a 20x20 km grid basis. The European data sets of precipitation and air temperature (time period 1901-2000, monthly resolution), (Mitchell et al. 2004) were used to derive long-term averages. As we focus on agricultural areas we included CORINE data (2006) to extract arable land. The resulting BATs under co-consideration of the main soil textures (clay, silt, sand and loam) were investigated per environmental zone (ENZs, Metzger et al. 2005) that represents similar conditions for precipitation, temperature and relief to identify BAT ranges and hence turnover conditions for each ENZ. Re_clim was quantified by climatic time series of more than 250 weather stations across Europe presented by Klein Tank et al. (2002). Daily temperature, precipitation and potential evapotranspiration (maximal thermal extent) were used to calculate

  12. Fracture-induced mechanophore activation and solvent healing in poly(methyl methacrylate)

    Science.gov (United States)

    Celestine, Asha-Dee N.

    Damage detection is a highly desirable functionality in engineering materials. The potential of using mechanophores, stress-sensitive molecules, as material stress sensors has been established through tensile, compressive and shear tests. Spiropyran (SP) has been the chosen mechanophore and this molecule undergoes a ring opening reaction (activation) upon the application of mechanical stress. This activation is accompanied by a change in color and fluorescence as the colorless SP is converted to the highly colored merocyanine (MC) form. One requirement for SP activation in bulk polymers is large scale plastic deformation. In order to induce this plastic deformation during fracture testing of SP-linked brittle polymers such as poly(methyl methacrylate) (PMMA), rubber nanoparticles can be incorporated into the matrix material. These nanoparticles facilitate the increased shear yielding necessary for SP activation during mechanical testing. Cross-linked SP-PMMA, containing 7.3 wt% rubber nanoparticles is synthesized via a free radical polymerization. Specimens of this material are fabricated for Single Edge Notch Tension (SENT) testing. The rubber toughened SP-PMMA specimens are first prestretched to approximately 35% axial strain to align the spiropyran molecules in the direction of applied force and thus increase the likelihood of fracture-induced activation. After prestretching the specimens are pre-notched and irradiated with 532 nm wavelength light to revert the colored merocyanine to the colorless spiropyran form. Specimens are then fracture tested to failure using the SENT test. The evolution of mechanophore activation is monitored via in situ fluorescence imaging and inspection of the specimens after testing. Activation of the SP is observed ahead of the crack tip and along the propagated crack. Also, the degree of activation is found to increase with crack growth and the size of the activation zone is linearly correlated to the size of the plastic zone ahead

  13. Biological activity of trisporoids and trisporoid analogues in Mucor mucedo (-).

    Science.gov (United States)

    Schachtschabel, Doreen; Schimek, Christine; Wöstemeyer, Johannes; Boland, Wilhelm

    2005-06-01

    In the course of their sexual interactions, zygomycete fungi communicate via an elaborate series of carotene-derived compounds, namely trisporic acid and its biosynthetic progenitors. A novel building-block strategy allowed the systematic generation of structurally modified trisporoids along with putative early biosynthetic precursors for physiological tests. The impact of discrete structural elements was documented by the ability of individual compounds to induce sexually committed hyphae in Mucor mucedo. The activity screening contributed to establish general structure-function relationships for trisporoid action. Most crucial for activity were the dimension of the longer side chain, the polarity of functional groups at C(4) and C(13), and the number of conjugated double bonds in the side chain. The presence of an oxygen substituent at the cyclohexene ring is not essential for function. The overall biological activity apparently results from the combination of the various structural elements.

  14. Hydrodynamic collective effects of active proteins in biological membranes

    Science.gov (United States)

    Koyano, Yuki; Kitahata, Hiroyuki; Mikhailov, Alexander S.

    2016-08-01

    Lipid bilayers forming biological membranes are known to behave as viscous two-dimensional fluids on submicrometer scales; usually they contain a large number of active protein inclusions. Recently, it was shown [A. S. Mikhailov and R. Kapral, Proc. Natl. Acad. Sci. USA 112, E3639 (2015), 10.1073/pnas.1506825112] that such active proteins should induce nonthermal fluctuating lipid flows leading to diffusion enhancement and chemotaxislike drift for passive inclusions in biomembranes. Here, a detailed analytical and numerical investigation of such effects is performed. The attention is focused on the situations when proteins are concentrated within lipid rafts. We demonstrate that passive particles tend to become attracted by active rafts and are accumulated inside them.

  15. Chemical Analysis and Biological Activity of Jordanian Chamomile Extracts

    Directory of Open Access Journals (Sweden)

    Nawal Hassan Al Bahtiti

    2012-02-01

    Full Text Available The Jordanian chamomile (Matricaria chamomilla has been researched more thoroughly to evaluate its useful properties. It is investigated and found that Jordanian chamomile is rich in phenolic compounds, with beneficial biological activities. By applying the most promising HPLC method, the content of total phenolics in methanolic extract was determined according to the Folin-Clocalteu procedure, and was found (GAE>20 mg/g. The flavonoid types were found as flavones and flavonolos.The minimum inhibitory concentration values for methanolic extracts of Jordanian chamomile were determined for different kinds of bacteria. The extracts have activity against Staphylococcus aurous, candida albicans, Esherichia Coli, Betula pubescens and Pinus sylvestris. The activity has been observed to be due to the tannins and a pigenin present in the extract. To utilize these significant sources of natural compounds, further characterization of phenolic composition is needed.

  16. Established and emerging biological activity markers of inflammatory bowel disease

    DEFF Research Database (Denmark)

    Nielsen, O H; Vainer, B; Madsen, S M;

    2000-01-01

    Assessment of disease activity in inflammatory bowel disease (IBD), i.e., ulcerative colitis (UC) and Crohn's disease (CD), is done using clinical parameters and various biological disease markers. Ideally, a disease marker must: be able to identify individuals at risk of a given disorder...... molecules. It is concluded that none of the pertinent laboratory surrogate markers of disease activity in IBD are specific or sensitive enough to replace basic clinical observation such as the number of daily bowel movements, general well-being, and other parameters in parallel. Further studies are highly...... warranted to identify and assess the clinical importance and applicability of new laboratory markers for the diagnosis or the disease activity of IBD....

  17. Involvement of mitogen-activated protein kinase pathways in N-methyl-D-aspartate-induced excitotoxicity

    Institute of Scientific and Technical Information of China (English)

    Xiaorong Yang; Ping Sun; Huaping Qin; Rui Wang; Ye Wang; Ruihong Shi; Xin Zhao; Ce Zhang

    2011-01-01

    Previous studies have shown that mitogen-activated protein kinase (MAPK) signaling pathways are involved in N-methyl-D-aspartate (NMDA)-mediated excitotoxicity. However, a systematic observation or analysis of the role of these various MAPK pathways in excitotoxicity processes does not exist. The present study further evaluated the role and contribution of three MAPK pathways extracellular signal-regulated kinase, c-Jun N-terminal kinase, and p38 MAPK in an NMDA-mediated excitotoxicity model using MAPK-specific inhibitor. Results demonstrated that c-Jun N-terminal kinase inhibitor SP600125 and/or p38 MAPK inhibitor SB203580 inhibited NMDA-induced reduction in cell viability, as well as reduced NMDA-induced lactate dehydrogenase leakage and reactive oxygen species production. However, PD98059, an inhibitor of extracellular signal-regulated kinase, did not influence this model. Results demonstrated an involvement of c-Jun N-terminal kinase and p38 MAPK, but not extracellular signal-regulated kinase, in NMDA-mediated excitotoxicity in cortical neurons.

  18. Pereskia aculeata Muller (Cactaceae Leaves: Chemical Composition and Biological Activities

    Directory of Open Access Journals (Sweden)

    Lucèia Fàtima Souza

    2016-09-01

    Full Text Available The aims of this work were to study the chemical composition of the essential oil from the leaves of Pereskia aculeata and to evaluate some biological activities of three leaf extracts. The phenolic content, antioxidant activity, and in vitro antimicrobial and antifungal activities were determined. The methanol extract showed antioxidant activity (EC50 7.09 mg/mL and high polyphenols content (15.04 ± 0.31 mg gallic acid equivalents (GAE/g. The petroleum ether extract exhibited potent antibacterial activity against Escherichia coli, whereas the chloroform extract showed inhibitory activity against Bacillus cereus and Staphylococcus aureus. The petroleum ether and methanol extracts were more effective in inhibiting the growth of Aspergillus versicolor. The possible cytotoxicity of extracts on neuroblastoma SH-SY5Y cancer cell line and the influence on adenylate cyclase (ADCY expression was also studied. P. aculeata chloroform extract showed antiproliferative activity with an IC50 value of 262.83 µg/mL. Treatments of SH-SY5Y neuroblastoma cells with 100 µg/mL of methanol extract significantly reduced ADCY1 expression.

  19. Pereskia aculeata Muller (Cactaceae) Leaves: Chemical Composition and Biological Activities.

    Science.gov (United States)

    Souza, Lucèia Fàtima; Caputo, Lucia; Inchausti De Barros, Ingrid Bergman; Fratianni, Florinda; Nazzaro, Filomena; De Feo, Vincenzo

    2016-09-03

    The aims of this work were to study the chemical composition of the essential oil from the leaves of Pereskia aculeata and to evaluate some biological activities of three leaf extracts. The phenolic content, antioxidant activity, and in vitro antimicrobial and antifungal activities were determined. The methanol extract showed antioxidant activity (EC50 7.09 mg/mL) and high polyphenols content (15.04 ± 0.31 mg gallic acid equivalents (GAE)/g). The petroleum ether extract exhibited potent antibacterial activity against Escherichia coli, whereas the chloroform extract showed inhibitory activity against Bacillus cereus and Staphylococcus aureus. The petroleum ether and methanol extracts were more effective in inhibiting the growth of Aspergillus versicolor. The possible cytotoxicity of extracts on neuroblastoma SH-SY5Y cancer cell line and the influence on adenylate cyclase (ADCY) expression was also studied. P. aculeata chloroform extract showed antiproliferative activity with an IC50 value of 262.83 µg/mL. Treatments of SH-SY5Y neuroblastoma cells with 100 µg/mL of methanol extract significantly reduced ADCY1 expression.

  20. Biological Activities and Cytotoxicity of Diterpenes from Copaifera spp. Oleoresins

    Directory of Open Access Journals (Sweden)

    Fabiano de S. Vargas

    2015-04-01

    Full Text Available Copaifera spp. are Amazonian species widely studied and whose oleoresins are used by local people for various medicinal purposes. However, a detailed study of the activity of the main phytochemical components of these oleoresins remains to be done. Here, we studied the cytotoxicity and in vitro anti-inflammatory effects of six diterpene acids: copalic, 3-hydroxy-copalic, 3-acetoxy-copalic, hardwickiic, kolavic-15-metyl ester, and kaurenoic, isolated from the oleoresins of Copaifera spp. The diterpenes did not show cytotoxicity in normal cell lines, nor did they show significant changes in viability of tumoral line cells. The 3-hydroxy-copalic was able to inhibit the enzyme tyrosinase (64% ± 1.5% at 250 µM. The kolavic-15-metyl ester at 200 µM showed high inhibitory effect on lipoxygenase (89.5% ± 1.2%. Among the diterpenes tested, only kaurenoic and copalic acids showed significant hemolytic activities with 61.7% and 38.4% at 100 µM, respectively. In addition, it was observed that only the copalic acid (98.5% ± 1.3% and hardwickiic acid (92.7% ± 4.9% at 100 mM inhibited nitric oxide production in macrophages activated by lipopolysaccharide. In this assay, the diterpenes did not inhibit tumor necrosis factor-α production. The acids inhibited the production of IL-6, 3-acetoxy-copalic (23.8% ± 8.2%, kaurenoic (11.2% ± 5.7%, kolavic-15-methyl ester (17.3% ± 4.2%, and copalic (4.2% ± 1.8%, respectively, at 25 µM. The kaurenoic, 3-acetoxy-copalic and copalic acids increased IL-10 production. This study may provide a basis for future studies on the therapeutic role of diterpenic acids in treating acute injuries such as inflammation or skin disorders.

  1. Biological activities and cytotoxicity of diterpenes from Copaifera spp. Oleoresins.

    Science.gov (United States)

    de S Vargas, Fabiano; D O de Almeida, Patrícia; Aranha, Elenn Suzany P; de A Boleti, Ana Paula; Newton, Peter; de Vasconcellos, Marne C; Junior, Valdir F Veiga; Lima, Emerson S

    2015-04-09

    Copaifera spp. are Amazonian species widely studied and whose oleoresins are used by local people for various medicinal purposes. However, a detailed study of the activity of the main phytochemical components of these oleoresins remains to be done. Here, we studied the cytotoxicity and in vitro anti-inflammatory effects of six diterpene acids: copalic, 3-hydroxy-copalic, 3-acetoxy-copalic, hardwickiic, kolavic-15-metyl ester, and kaurenoic, isolated from the oleoresins of Copaifera spp. The diterpenes did not show cytotoxicity in normal cell lines, nor did they show significant changes in viability of tumoral line cells. The 3-hydroxy-copalic was able to inhibit the enzyme tyrosinase (64% ± 1.5%) at 250 µM. The kolavic-15-metyl ester at 200 µM showed high inhibitory effect on lipoxygenase (89.5% ± 1.2%). Among the diterpenes tested, only kaurenoic and copalic acids showed significant hemolytic activities with 61.7% and 38.4% at 100 µM, respectively. In addition, it was observed that only the copalic acid (98.5% ± 1.3%) and hardwickiic acid (92.7% ± 4.9%) at 100 mM inhibited nitric oxide production in macrophages activated by lipopolysaccharide. In this assay, the diterpenes did not inhibit tumor necrosis factor-α production. The acids inhibited the production of IL-6, 3-acetoxy-copalic (23.8% ± 8.2%), kaurenoic (11.2% ± 5.7%), kolavic-15-methyl ester (17.3% ± 4.2%), and copalic (4.2% ± 1.8%), respectively, at 25 µM. The kaurenoic, 3-acetoxy-copalic and copalic acids increased IL-10 production. This study may provide a basis for future studies on the therapeutic role of diterpenic acids in treating acute injuries such as inflammation or skin disorders.

  2. Structure-activity relationship studies of N-methylated and N-hydroxylated spider polyamine toxins as inhibitors of ionotropic glutamate receptors

    DEFF Research Database (Denmark)

    Nørager, Niels G; Poulsen, Mette H; Jensen, Anna G;

    2014-01-01

    Polyamine toxins from spiders and wasps are potent open-channel blockers of ionotropic glutamate (iGlu) receptors. It is well-established that secondary amino groups in the polyamine moiety of these toxins are key to both selectivity and potency at iGlu receptors, still some native spider polyamine...... toxins comprise both N-methyl and N-hydroxy functionalities. Here, we investigate the effect of both N-methylation and N-hydroxylation of spider polyamine toxins by the synthesis and biological evaluation of the naturally occurring N-methylated argiopinines and pseudoargiopinines I and II, N...

  3. Comparison of anti amoebic activity of stereoisomeric diamino and monoamino pregnene alkaloids and their N-methylated analogs

    Indian Academy of Sciences (India)

    Raj M Vaid; K K Bhutani

    2013-01-01

    The steroidal alkaloid 3, 20-diamino-pregn-5-ene (kurchamine) obtained from the stem bark of Holarrhena antidysenterica is reported to have appreciable amoebicidal activity. Its three stereoisomers namely 3, 20-diamino-pregn-5-ene, 3,20-diamino-pregn-5-ene and 3, 20-diamino-pregn-5-ene and their intermediate stereoisomeric monoamino pregnene alkaloids namely 3-amino-pregn-5-ene-20-one, 3-aminopregn-5-ene-20-one, 20-amino-pregn-5-ene-3-ol, 20-amino-pregn-5-ene-3-ol were synthesized. The natural stereoisomer and synthesized diamino and monoamino stereoisomers were N-methylated and all the compounds were evaluated for amoebicidal activity comparison. The natural stereoisomer 3,20-diamino-pregn-5-ene (kurchamine) was found to be superior than other stereoisomers and N-methylation was found to have insignificant effect on amoebicidal activity of stereoisomers.

  4. Activating and inhibiting connections in biological network dynamics

    Directory of Open Access Journals (Sweden)

    Knight Rob

    2008-12-01

    Full Text Available Abstract Background Many studies of biochemical networks have analyzed network topology. Such work has suggested that specific types of network wiring may increase network robustness and therefore confer a selective advantage. However, knowledge of network topology does not allow one to predict network dynamical behavior – for example, whether deleting a protein from a signaling network would maintain the network's dynamical behavior, or induce oscillations or chaos. Results Here we report that the balance between activating and inhibiting connections is important in determining whether network dynamics reach steady state or oscillate. We use a simple dynamical model of a network of interacting genes or proteins. Using the model, we study random networks, networks selected for robust dynamics, and examples of biological network topologies. The fraction of activating connections influences whether the network dynamics reach steady state or oscillate. Conclusion The activating fraction may predispose a network to oscillate or reach steady state, and neutral evolution or selection of this parameter may affect the behavior of biological networks. This principle may unify the dynamics of a wide range of cellular networks. Reviewers Reviewed by Sergei Maslov, Eugene Koonin, and Yu (Brandon Xia (nominated by Mark Gerstein. For the full reviews, please go to the Reviewers' comments section.

  5. Synthesis and biological activities of turkesterone 11?-acyl derivatives

    Directory of Open Access Journals (Sweden)

    Laurence Dinan

    2003-02-01

    Full Text Available Turkesterone is a phytoecdysteroid possessing an 11alpha-hydroxyl group. It is an analogue of the insect steroid hormone 20-hydroxyecdysone. Previous ecdysteroid QSAR and molecular modelling studies predicted that the cavity of the ligand-binding domain of the ecdysteroid receptor would possess space in the vicinity of C-11/C-12 of the ecdysteroid. We report the regioselective synthesis of a series of turkesterone 11alpha-acyl derivatives in order to explore this possibility. The structures of the analogues have been unambiguously determined by spectroscopic means (NMR and low-resolution mass spectrometry. Purity was verified by HPLC. Biological activities have been determined in Drosophila melanogaster BII cell-based bioassay for ecdysteroid agonists and in an in vitro radioligand-displacement assay using bacterially expressed D. melanogaster EcR/USP receptor proteins. The 11alpha-acyl derivatives do retain a significant amount of biological activity relative to the parent ecdysteroid. Further, although activity initially drops with the extension of the acyl chain length (C2 to C4, it then increases (C6 to C10, before decreasing again (C14 and C20. The implications of these findings for the interaction of ecdysteroids with the ecdysteroid receptor and potential applications in the generation of affinity-labelled and fluorescently-tagged ecdysteroids are discussed.

  6. Isolation of biologically-active exosomes from human plasma.

    Science.gov (United States)

    Muller, Laurent; Hong, Chang-Sook; Stolz, Donna B; Watkins, Simon C; Whiteside, Theresa L

    2014-09-01

    Effects of exosomes present in human plasma on immune cells have not been examined in detail. Immunological studies with plasma-derived exosomes require their isolation by procedures involving ultracentrifugation. These procedures were largely developed using supernatants of cultured cells. To test biologic activities of plasma-derived exosomes, methods are necessary that ensure adequate recovery of exosome fractions free of contaminating larger vesicles, cell fragments and protein/nucleic acid aggregates. Here, an optimized method for exosome isolation from human plasma/serum specimens of normal controls (NC) or cancer patients and its advantages and pitfalls are described. To remove undesirable plasma-contaminating components, ultrafiltration of differentially-centrifuged plasma/serum followed by size-exclusion chromatography prior to ultracentrifugation facilitated the removal of contaminants. Plasma or serum was equally acceptable as a source of exosomes based on the recovered protein levels (in μg protein/mL plasma) and TEM image quality. Centrifugation on sucrose density gradients led to large exosome losses. Fresh plasma was the best source of morphologically-intact exosomes, while the use of frozen/thawed plasma decreased exosome purity but not their biologic activity. Treatments of frozen plasma with DNAse, RNAse or hyaluronidase did not improve exosome purity and are not recommended. Cancer patients' plasma consistently yielded more isolated exosomes than did NCs' plasma. Cancer patients' exosomes also mediated higher immune suppression as evidenced by decreased CD69 expression on responder CD4+ T effector cells. Thus, the described procedure yields biologically-active, morphologically-intact exosomes that have reasonably good purity without large protein losses and can be used for immunological, biomarker and other studies.

  7. THE ROLE OF VALENCE AND METHYLATION STATE ON THE ACTIVITY OF ARSENIC DURING MITOSIS

    Science.gov (United States)

    Trivalent methylated arsenicals are much more potent DNA damaging agents, clastogens, and large deletion mutagens than are their inorganic and pentavalent counterparts. Previously we had noticed that many of the arsenicals induced "c-type" anaphases characteristic of spindle pois...

  8. Labdanolic acid methyl ester (LAME) exerts anti-inflammatory effects through inhibition of TAK-1 activation

    Energy Technology Data Exchange (ETDEWEB)

    Cuadrado, Irene [Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense, Plaza Ramón y Cajal s/n, 28040 Madrid (Spain); Cidre, Florencia; Herranz, Sandra [Unidad de Inflamación y Cáncer. Área de Biología Celular y Desarrollo. Centro Nacional de Microbiología, Instituto de Salud Carlos III, Madrid (Spain); Estevez-Braun, Ana [Instituto Universitario de Bio-Orgánica “Antonio González”. Universidad de La Laguna. Avda. Astrofísico Fco. Sánchez 2. 38206. La Laguna, Tenerife (Spain); Instituto Canario de Investigaciones del Cáncer (ICIC) (Spain); Heras, Beatriz de las, E-mail: lasheras@farm.ucm.es [Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense, Plaza Ramón y Cajal s/n, 28040 Madrid (Spain); Hortelano, Sonsoles, E-mail: shortelano@isciii.es [Unidad de Inflamación y Cáncer. Área de Biología Celular y Desarrollo. Centro Nacional de Microbiología, Instituto de Salud Carlos III, Madrid (Spain)

    2012-01-01

    Labdane derivatives obtained from the diterpenoid labdanediol suppressed NO and PGE{sub 2} production in LPS-stimulated RAW 264.7 macrophages. However, mechanisms involved in these inhibitory effects are not elucidated. In this study, we investigated the signaling pathways involved in the anti-inflammatory effects of labdanolic acid methyl ester (LAME) in peritoneal macrophages and examined its therapeutic effect in a mouse endotoxic shock model. LAME reduced the production of NO and PGE{sub 2} in LPS-activated macrophages. This effect involved the inhibition of NOS-2 and COX-2 gene expression, acting at the transcription level. Examination of the effects of the diterpene on NF-κB signaling showed that LAME inhibits the phosphorylation of IκBα and IκBβ, preventing their degradation and the nuclear translocation of the NF-κB p65 subunit. Moreover, inhibition of MAPK signaling was also observed. A further experiment revealed that LAME inhibited the phosphorylation of transforming growth factor-β (TGF-β)-activated kinase 1 (TAK1), an upstream signaling molecule required for IKK and mitogen-activated protein kinases (MAPKs) activation. Inflammatory cytokines such as IL-6, TNF-α and IP-10 were downregulated in the presence of this compound after stimulation with LPS. Additionally, LAME also improved survival in a mouse model of endotoxemia and reduced the circulatory levels of cytokines (IL-6, TNF-α). In conclusion, these results indicate that labdane diterpene LAME significantly attenuates the pro-inflammatory response induced by LPS both in vivo and in vitro. Highlights: ► LAME reduced the production of NO and PGE{sub 2} in LPS-activated macrophages. ► IL-6, TNF-α and IP-10 were also inhibited by LAME. ► Inhibition of TAK-1 activation is the mechanism involved in this process. ► LAME improved survival in a mouse model of endotoxemia. ► LAME reduced the circulatory levels of cytokines (IL-6, TNF-α).

  9. Polysaccharides from Arctium lappa L.: Chemical structure and biological activity.

    Science.gov (United States)

    Carlotto, Juliane; de Souza, Lauro M; Baggio, Cristiane H; Werner, Maria Fernanda de P; Maria-Ferreira, Daniele; Sassaki, Guilherme L; Iacomini, Marcello; Cipriani, Thales R

    2016-10-01

    The plant Arctium lappa L. is popularly used to relieve symptoms of inflammatory disorders. A crude polysaccharide fraction (SAA) resulting of aqueous extraction of A. lappa leaves showed a dose dependent anti-edematogenic activity on carrageenan-induced paw edema, which persisted for up to 48h. Sequential fractionation by ultrafiltration at 50kDa and 30kDa cut-off membranes yielded three fractions, namely RF50, RF30, and EF30. All these maintained the anti-edematogenic effect, but RF30 showed a more potent action, inhibiting 57% of the paw edema at a dose of 4.9mg/kg. The polysaccharide RF30 contained galacturonic acid, galactose, arabinose, rhamnose, glucose, and mannose in a 7:4:2:1:2:1 ratio and had a Mw of 91,000g/mol. Methylation analysis and NMR spectroscopy indicated that RF30 is mainly constituted by a type I rhamnogalacturonan branched by side chains of types I and II arabinogalactans, and arabinan.

  10. Effects of the herbicides clomazone, quinclorac, and metsulfuron methyl on acetylcholinesterase activity in the silver catfish (Rhamdia quelen) (Heptapteridae).

    Science.gov (United States)

    dos Santos Miron, Denise; Crestani, Márcia; Rosa Shettinger, Maria; Maria Morsch, Vera; Baldisserotto, Bernardo; Angel Tierno, Miguel; Moraes, Gilberto; Vieira, Vania Lucia Pimentel

    2005-07-01

    Fingerlings of the silver catfish (Rhamdia quelen) were exposed to three herbicides widely used in rice culture in south Brazil: clomazone, quinclorac, and metsulfuron methyl. LC50 was determined and acetylcholinesterase (AChE) activity was evaluated in brain and muscle tissue of fish exposed to different herbicide concentrations after 96h (short term). The LC50 value (nominal concentration) was 7.32 mg/L for clomazone and 395 mg/L for quinclorac, but was not obtained for metsulfuron-methyl since all fingerlings survived the highest concentration of 1200 mg/L. Brain and muscle AChE activity in unexposed fish were 17.9 and 9.08 micromol/min/g protein, respectively. Clomazone significantly inhibited AChE activity in both tissues, achieving maximal inhibition of about 83% in brain and 89% in muscle tissue. In contrast, quinclorac and metsulfuron methyl caused increases in enzyme activity in the brain (98 and 179%, respectively) and inhibitions in muscle tissue (88 and 56%, respectively). This study demonstrated short-term effects of exposure to environmentally relevant concentrations of rice field herbicides on AChE activity in brain and muscle tissue of silver catfish.

  11. Functionalization of hydroxyl terminated polybutadiene with biologically active fluorescent molecule

    Indian Academy of Sciences (India)

    R Murali Sankar; Subhadeep Saha; K Seeni Meera; Tushar Jana

    2009-10-01

    A biologically active molecule, 2-chloro-4,6-bis(dimethylamino)-1,3,5-triazine (CBDT), has been covalently attached at the terminal carbon atoms of the hydroxyl terminated polybutadiene (HTPB) backbone. The modification of HTPB backbone by CBDT molecule does not affect the unique physico-chemical properties such as fluidity, hydroxyl value and microstructure of the parent HTPB. The formation of hydrogen bonding between the terminal hydroxyl groups and the nitrogen atoms of triazine moiety is the driving force for the terminal attachment chemistry. The functionalized HTPB (HTPB–CBDT) shows a strong fluorescence emission at 385 nm.

  12. A Conceptual Framework for Organizing Active Learning Experiences in Biology Instruction

    Science.gov (United States)

    Gardner, Joel; Belland, Brian R.

    2012-08-01

    Introductory biology courses form a cornerstone of undergraduate instruction. However, the predominantly used lecture approach fails to produce higher-order biology learning. Research shows that active learning strategies can increase student learning, yet few biology instructors use all identified active learning strategies. In this paper, we present a framework to design biology instruction that incorporates all active learning strategies. We review active learning research in undergraduate biology courses, present a framework for organizing active learning strategies, and provide clear implications and future research for designing instruction in introductory undergraduate biology courses.

  13. Elucidating GPR Response to Biological Activity: Field and Laboratory Experiments

    Science.gov (United States)

    Tsoflias, G. P.; Schillig, P. C.; McGlashan, M. A.; Roberts, J. A.; Devlin, J. F.

    2010-12-01

    Recent studies of the geophysical signatures of biological processes in earth environments have resulted in the emergent field of “biogeophysics”. The ability to monitor remotely and to quantify active biological processes in the subsurface can have transformative implications to a wide range of investigations, including the bioremediation of contaminated sites. Previous studies have demonstrated that ground-penetrating radar (GPR) can be used to detect the products of microbial activity in the subsurface, such as changes in bulk electrical conductivity, mineral dissolution and precipitation, and the formation of biogenic gas. We present field and laboratory experiments that offer insights to the response of GPR signals to microbial activity. In the field, time-lapse borehole radar tomography was used to monitor biodegradation of a hydrocarbon plume over a period of two years. A dense grid of fourteen borehole pairs monitoring the bioactive region showed radar wave velocity changes of +/-4% and signal attenuation changes of +/-25%. These GPR observations correlated spatially and temporally to independent measurements of groundwater velocity and geochemical variations that occurred in response to microbial activity. The greatest relative changes in radar wave velocity of propagation and attenuation were observed in the region of enhanced bacterial stimulation where biomass growth was the greatest. Radar wave velocity and attenuation decreased during periods of enhanced biostimulation. Two laboratory experiments were conducted to further assess radar response to biomass growth. The first experiment monitored GPR wave transmission through a water-saturated quartz-sand reactor during the course of enhanced biostimulation. Radar wave velocity initially decreased as a result of bacterial activity and subsequently increased rapidly as biogenic gas formed in the pore space. Radar signal attenuation increased during the course of the experiment as a result of an

  14. Treatment of 2-phenylamino-3-methyl-6-di-n-butylaminofluoran production effluent by combination of biological treatments and Fenton's oxidation

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    High strength refractory organic stream is produced during the production of 2-phenylamino-3-methyl-6-di-n-butylaminofluoran(One Dye Black 2, abbr. ODB 2), a novel heat-sensitive material with a promising market. In this study, a combination of acidificationprecipitation, primary biological treatment, Fenton's oxidation and another biological treatment was successfully used for the removal of COD from 18000-25000 mg/L to below 200 mg/L from the ODB 2 production wastewater in a pilot experiment. A COD removal of 70%-80% was achieved by acidification-precipitation under a pH of 2.5-3.0. The first step biodegradation permitted an average COD removal of 70% under an hydraulic residence time (HRT) of 30 h. By batch tests, the optimum conditions of Fenton's oxidation were acquired as: Fe2+ dose 6.0 mmol/L; H2O2 dose 3000 mg/L; and reaction time 6 h. The second step biological treatment could ensure an effluent COD below 200 mg/L under an HRT of 10 h following the Fenton's treatment.

  15. Palladium(II) complexes as biologically potent metallo-drugs: Synthesis, spectral characterization, DNA interaction studies and antibacterial activity

    Science.gov (United States)

    Prasad, Kollur Shiva; Kumar, Linganna Shiva; Chandan, Shivamallu; Naveen Kumar, R. M.; Revanasiddappa, Hosakere D.

    2013-04-01

    Four novel mononuclear Pd(II) complexes have been synthesized with the biologically active Schiff base ligands (L1-L4) derived from 3-amino-2-methyl-4(3H)-quinazolinone. The structure of the complexes has been proposed by elemental analysis, molar conductance, IR, 1H NMR, mass, UV-Vis spectrometric and thermal studies. The investigation of interaction of the complexes with calf thymus DNA (CT-DNA) has been performed with absorption and fluorescence spectroscopic studies. The nuclease activity was done using pUC19 supercoiled DNA by gel-electrophoresis. All the ligands and their Pd(II) complexes have also been screened for their antibacterial activity by discolor diffusion technique.

  16. Synthesis, Characterization and Biological Activities of N-Acyl-3-(3-pyridyl)-5-aryl-pyrazoles

    Institute of Scientific and Technical Information of China (English)

    KANG Yan-fang; WANG Dun-jia; XU Ben-po; WEI Xian-hong; ZHENG Jing

    2013-01-01

    Ten novel N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles were synthesized by Claisen condensation of the aryl methyl ketones with ethyl nicotinate,the cyclization with hydrazine hydrate and the N-acylation with acyl chloride in turn.The structures of all the compounds synthesized were confirmed by means of Fourier transform infrared(FTIR),1H NMR,mass spectroscopy and elemental analysis.The biological activities of the title compounds were examined by disc diffusion method against Escherichia coli,Staphylococcus aureus,Pyricularia oryzae and Rhizoctnia solani.All the N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles exhibited a certain degree of antibacterial and antifungal activities.Comparatively,compounds 3c and 3d exhibited much significant antibacterial and antifungal activities than the other pyrazole derivatives.

  17. Effect of dietary high- and low-methylated citrus pectin on the activity of the ileal microflora and morphology of the small intestinal wall of broiler chicks

    NARCIS (Netherlands)

    Langhout, D.J.; Schutte, J.B.; Leeuwen, P. van; Wiebenga, J.; Tamminga, S.

    1999-01-01

    1. A study was conducted with broiler chicks to evaluate the effects of dietary high-methylated citrus pectin (HMC) or low-methylated citrus pectin (LMC) on the performance, nutrient digestibility, morphology of the small intestinal wall and ileal microbial activity. 2. Both pectin products were tes

  18. Prenatal polycyclic aromatic hydrocarbon, adiposity, peroxisome proliferator-activated receptor (PPAR γ methylation in offspring, grand-offspring mice.

    Directory of Open Access Journals (Sweden)

    Zhonghai Yan

    Full Text Available RATIONALE: Greater levels of prenatal exposure to polycyclic aromatic hydrocarbon (PAH have been associated with childhood obesity in epidemiological studies. However, the underlying mechanisms are unclear. OBJECTIVES: We hypothesized that prenatal PAH over-exposure during gestation would lead to weight gain and increased fat mass in offspring and grand-offspring mice. Further, we hypothesized that altered adipose gene expression and DNA methylation in genes important to adipocyte differentiation would be affected. MATERIALS AND METHODS: Pregnant dams were exposed to a nebulized PAH mixture versus negative control aerosol 5 days a week, for 3 weeks. Body weight was recorded from postnatal day (PND 21 through PND60. Body composition, adipose cell size, gene expression of peroxisome proliferator-activated receptor (PPAR γ, CCAAT/enhancer-binding proteins (C/EBP α, cyclooxygenase (Cox-2, fatty acid synthase (FAS and adiponectin, and DNA methylation of PPAR γ, were assayed in both the offspring and grand-offspring adipose tissue. FINDINGS: Offspring of dams exposed to greater PAH during gestation had increased weight, fat mass, as well as higher gene expression of PPAR γ, C/EBP α, Cox2, FAS and adiponectin and lower DNA methylation of PPAR γ. Similar differences in phenotype and DNA methylation extended through the grand-offspring mice. CONCLUSIONS: Greater prenatal PAH exposure was associated with increased weight, fat mass, adipose gene expression and epigenetic changes in progeny.

  19. Enhanced biological activity of carotenoids stabilized by phenyl groups.

    Science.gov (United States)

    You, Ji Suk; Jeon, Sunhwa; Byun, Youn Jung; Koo, Sangho; Choi, Shin Sik

    2015-06-15

    Carotenoids are lipid soluble food ingredients with multifunction including antioxidant and anticancer activities. However, carotenoids are destructively oxidized upon reaction with radicals resulting in toxic effects on biological systems. Two synthetic carotenoids (BAS and BTS) containing the aromatic phenyl groups with a para-substituent (OMe and Me, respectively) at C-13 and C-13' position were prepared in order to overcome a structural instability of carotenoid. Both BAS and BTS exerted stronger radical scavenging activity than β-carotene in DPPH and ABTS assays. In particular, BTS significantly reduced in vivo ROS (reactive oxygen species) levels and improved body growth and reproduction of Caenorhabditiselegans. BTS has a great potential for the advanced and modified carotenoid material with stability leading to enhanced bioavailability.

  20. Synthesis, characterization and biological activity of Rhein-cyclodextrin conjugate

    Science.gov (United States)

    Liu, Manshuo; Lv, Pin; Liao, Rongqiang; Zhao, Yulin; Yang, Bo

    2017-01-01

    Cyclodextrin conjugate complexation is a useful method to enhance the solubility and absorption of poorly soluble drugs. A series of new Rhein-β-cyclodextrin conjugates (Rh-CD conjugates) have been synthesized and examined. Rhein is covalently linked with the β-CD by amido linkage in a 1:1 molar ratio. The conjugates were characterized by 1H NMR, 13C NMR, HRMS, powder X-ray diffraction (powder XRD) as well as thermogravimetric analysis (TGA). The results reveal that incorporation of β-CD could improve the aqueous solubility of Rhein and the cytotoxicity against hepatocellular carcinoma (HepG2) cell line as well as antibacterial activity against three organisms. The improved biological activity and the satisfactory water solubility of the conjugates will be potentially useful for developing novel drug-cyclodextrin conjugates, such as herbal medicine.

  1. Posttranslational modulation on the biological activities of molecular chaperones

    Institute of Scientific and Technical Information of China (English)

    2009-01-01

    Molecular chaperones are a family of proteins that were first noticed to exist about 45 years ago from their increased transcription under heat shock conditions.As a result,the regulation of their encoding genes has been subject to extensive studies.Recent studies revealed that the biological activities of molecular chaperones can also be effectively modulated at the protein level.The ways of modulation so far elucidated include allosteric effect,covalent modification,protein-protein interaction,and con-formational alteration induced by such macro-environmental conditions as temperature and pH.These latter aspects were reviewed here.Emphasized here is the importance of such immediate structural alterations that lead to an immediate activity increase,providing the immediate protection needed for the cells to survive the stress conditions.

  2. Posttranslational modulation on the biological activities of molecular chaperones

    Institute of Scientific and Technical Information of China (English)

    CHANG ZengYi

    2009-01-01

    Molecular chaperones are a family of proteins that were first noticed to exist about 45 years ago from their increased transcription under heat shock conditions. As a result, the regulation of their encoding genes has been subject to extensive studies. Recent studies revealed that the biological activities of molecular chaperones can also be effectively modulated at the protein level. The ways of modulation so far elucidated include allosteric effect, covalent modification, protein-protein interaction, and con-formational alteration induced by such macro-environmental conditions as temperature and pH. These latter aspects were reviewed here. Emphasized here is the importance of such immediate structural alterations that lead to an immediate activity increase, providing the immediate protection needed for the cells to survive the stress conditions.

  3. Distribution and biological activity of obestatin in the rat.

    Science.gov (United States)

    Dun, Siok L; Brailoiu, G Cristina; Brailoiu, Eugen; Yang, Jun; Chang, Jaw Kang; Dun, Nae J

    2006-11-01

    Obestatin, a 23 amino acid peptide recently isolated from the rat stomach, is encoded by the same gene that encodes ghrelin. With the use of an antiserum directed against the mouse/rat obestatin, obestatin immunoreactivity (irOBS) was detected in cells of the gastric mucosa, myenteric plexus, and in Leydig cells of the testis in Sprague-Dawley rats. Double labeling the myenteric plexus with obestatin antiserum and choline acetyltransferase (ChAT) antiserum revealed that nearly all irOBS neurons were ChAT positive and vice versa. For comparative purposes, myenteric ganglion cells, cells in the gastric mucosa, and Leydig cells of the testis were shown to be immunoreactive to preproghrelin. The biological activity of obestatin on rat central neurons was assessed by the calcium microfluorimetric Fura-2 method. Obestatin (100 nM) administered to dissociated and cultured rat cerebral cortical neurons elevated cytosolic calcium concentrations [Ca2+]i in a population of cortical neurons. The result provides the first immunohistochemical evidence that obestatin is expressed in cells of the gastric mucosa and myenteric ganglion cells, and also in Leydig cells of the testis; the peptide is biologically active on central neurons.

  4. Fruit cuticular waxes as a source of biologically active triterpenoids.

    Science.gov (United States)

    Szakiel, Anna; Pączkowski, Cezary; Pensec, Flora; Bertsch, Christophe

    2012-06-01

    The health benefits associated with a diet rich in fruit and vegetables include reduction of the risk of chronic diseases such as cardiovascular disease, diabetes and cancer, that are becoming prevalent in the aging human population. Triterpenoids, polycyclic compounds derived from the linear hydrocarbon squalene, are widely distributed in edible and medicinal plants and are an integral part of the human diet. As an important group of phytochemicals that exert numerous biological effects and display various pharmacological activities, triterpenoids are being evaluated for use in new functional foods, drugs, cosmetics and healthcare products. Screening plant material in the search for triterpenoid-rich plant tissues has identified fruit peel and especially fruit cuticular waxes as promising and highly available sources. The chemical composition, abundance and biological activities of triterpenoids occurring in cuticular waxes of some economically important fruits, like apple, grape berry, olive, tomato and others, are described in this review. The need for environmentally valuable and potentially profitable technologies for the recovery, recycling and upgrading of residues from fruit processing is also discussed.

  5. Inhalable DNase I microparticles engineered with biologically active excipients.

    Science.gov (United States)

    Osman, Rihab; Al Jamal, Khuloud T; Kan, Pei-Lee; Awad, Gehanne; Mortada, Nahed; El-Shamy, Abd-Elhameed; Alpar, Oya

    2013-12-01

    Highly viscous mucus poses a big challenge for the delivery of particulates carrying therapeutics to patients with cystic fibrosis. In this study, surface modifying DNase I loaded particles using different excipients to achieve better lung deposition, higher enzyme stability or better biological activity had been exploited. For the purpose, controlled release microparticles (MP) were prepared by co-spray drying DNase I with the polymer poly-lactic-co-glycolic acid (PLGA) and the biocompatible lipid surfactant 1,2-dipalmitoyl-Sn-phosphatidyl choline (DPPC) using various hydrophilic excipients. The effect of the included modifiers on the particle morphology, size, zeta potential as well as enzyme encapsulation efficiency, biological activity and release had been evaluated. Powder aerosolisation performance and particle phagocytosis by murine macrophages were also investigated. The results showed that more than 80% of enzyme activity was recovered after MP preparation and that selected surface modifiers greatly increased the enzyme encapsulation efficiency. The particle morphology was greatly modified altering in turn the powders inhalation indices where dextran, ovalbumin and chitosan hydrochloride increased considerably the respirable fraction compared to the normal hydrophilic carriers lactose and PVP. Despite of the improved aerosolisation caused by chitosan hydrochloride, yet retardation of chitosan coated particles in artificial mucus samples discouraged its application. On the other hand, dextran and polyanions enhanced DNase I effect in reducing cystic fibrosis mucus viscosity. DPPC proved good ability to reduce particles phagocytic uptake even in the presence of the selected adjuvants. The prepared MP systems were biocompatible with lung epithelial cells. To conclude, controlled release DNase I loaded PLGA-MP with high inhalation indices and enhanced mucolytic activity on CF sputum could be obtained by surface modifying the particles with PGA or dextran.

  6. Comparison of biological activities of Glycyrrhiza glabra and G. uralensis

    Directory of Open Access Journals (Sweden)

    Park Chun-Geon

    2014-01-01

    Full Text Available The biological activities of Glycyrrhiza (GLs extracts (GL-1, Glycyrrhiza glabra from Eumseong, Korea; GL-2, G. uralensis from Eumseong, Korea; GL-3, G. uralensis from Yeongcheon, Korea; GL-4, G. uralensis from Neimenggu, China: GL-5, G. uralensis purchased from Korea Medicine Herbal Association, Korea were investigated. G. uralensis (GLs-2, -3, -4, and -5 extracts exhibited higher free radical scavenging activity against DPPH and OH radicals than G. glabra (GL-1. In addition, all GLs had antibacterial activity against E. coli, S. aureus, and H. pylori. GL-3 inhibited the growth of E. coli and S. aureus, while GL-1 had antibacterial activity against H. pylori. All GL extracts tested inhibited the lipopolysaccharide- and interferon-γ-induced inflammatory activity of RAW 264.7 cells. G. glabra and G. uralensis reduced NO generation. GL-3 also inhibited the growth of AGS human gastric adenocarcinoma cells. GLs-3 and -4 showed the inhibition of rat lens aldose reductase. GL-4 had a higher total content of glycyrrhizin (1, glycyrrhetinic acid (2, glabridin (3, and isoliquiritigenin (4. G. uralensis (GLs-2, -3, -4, and -5 is thus more effective than G. glabra (GL-1.

  7. (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: II. In vivo characterization.

    Science.gov (United States)

    Decker, M W; Brioni, J D; Sullivan, J P; Buckley, M J; Radek, R J; Raszkiewicz, J L; Kang, C H; Kim, D J; Giardina, W J; Wasicak, J T

    1994-07-01

    (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). Compared to (-)-nicotine, ABT 418 has reduced potency to interact with the subunit isoforms of nAChR found in sympathetic ganglia, and it does not compete for alpha-bungarotoxin binding sites in brain or at the neuromuscular junction. ABT 418 [minimum effective dose (MED), 0.062 mumol/kg i.p.) was 10-fold more potent in improving retention of avoidance learning in normal mice than (-)-nicotine, whereas the (R)-enantiomer of ABT 418, A-81754, was inactive. The memory-enhancing effect of ABT 418 was prevented by the nAChR channel blocker, mecamylamine. In the elevated plus-maze model of anxiety, ABT 418 (MED, 0.19 mumol/kg i.p.) increased open-arm exploration in mice, as previously shown for (-)-nicotine (MED, 0.62 mumol/kg i.p.). A-81754, did not have anxiolytic-like effects in this test. Unlike the classical anxiolytic, diazepam, ABT 418 did not impair rotorod performance in the dose range where beneficial effects occurred. In rats, ABT 418 (MED, 0.002 mumol/kg i.v.) was remarkably potent in enhancing basal forebrain-elicited increases in cortical cerebral blood flow, whereas resting cerebral blood flow was unaffected. Free running cortical electroencephalography in rats was unaffected by ABT 418 at a dose of 1.9 mumol/kg i.p., whereas the same dose of (-)-nicotine caused cortical activation (decreased power in the 1-13 Hz range and increased power in the 25-50 Hz range). Whereas ABT 418 was approximately 3- to 10-fold more potent than (-)-nicotine in memory enhancement and anxiolytic test paradigms, the compound had less emetic liability in dogs as compared to (-)-nicotine, and was less potent than (-)-nicotine in eliciting hypothermia, seizures, death and reduction of locomotor activity in mice. The measured

  8. Behaviour of Some Activated Nitriles Toward Barbituric Acid, Thiobarbituric Acid and 3-Methyl-1-Phenylpyrazol-5-one

    Directory of Open Access Journals (Sweden)

    M. M. Habashy

    2000-05-01

    Full Text Available The effect of some active methylene containing heterocyclic compounds, namely barbituric acid, thiobarbituric acid and 3-methyl-1-phenylpyrazol-5-one on a-cyano-3,4,5-trimethoxycinnamonitrile and ethyl a-cyano-3,4,5-trimethoxycinnamate (1a,b was investigated. The structure of the new products was substantiated by their IR,1H-NMR and mass spectra.

  9. Sensitization of rat facial cutaneous mechanoreceptors by activation of peripheral N-methyl-d-aspartate receptors.

    Science.gov (United States)

    Gazerani, Parisa; Dong, Xudong; Wang, Mianwei; Kumar, Ujendra; Cairns, Brian E

    2010-03-10

    The effect of subcutaneous injection of glutamate on the mechanical sensitivity of rat facial cutaneous mechanoreceptors was examined. Individual facial mechanoreceptors were recorded in the trigeminal ganglion of anesthetized Sprague-Dawley rats. An electronic von Frey hair was used to measure the mechanical threshold (MT) of the afferent fibers at baseline and following subcutaneous injection of glutamate (0, 0.01, 0.1, 1M; 10microl) or glutamate (0, 0.1M) plus the competitive N-methyl-d-aspartate (NMDA) receptor antagonist 2-amino-5-phosphonovalerate (APV; 0.01M). Subcutaneous injections were randomized and the investigator was unaware of their content. Changes in MT were assessed with a repeated measure ANOVA with time, sex and treatment as factors. Immunohistochemistry was used to confirm NMDA receptor expression by cutaneous nerve fibers. A total of 100 (50 per sex) facial mechanoreceptors were recorded from 61 (32 females, 29 males) rats in two separate experiments. Subcutaneous injections of higher concentrations of glutamate (1, 0.1M) induced a significant mechanical sensitization of skin afferent fibers (compared to 0 and 0.01M). Females (EC(50)=16.2mM) were more sensitive to glutamate than males (EC(50)=73.0mM). Facial cutaneous nerve fibers in both sexes expressed NMDA receptors. APV blocked the mechanical sensitization of the afferent fibers treated by glutamate 0.1M in both sexes with a lower effect in females at a 10-20minute post-injection. Subcutaneous injection of glutamate mechanically sensitizes rat facial cutaneous mechanoreceptors through activation of peripheral NMDA receptors. Peripheral NMDA receptor antagonists may be considered for craniofacial pain.

  10. Inhibition of aromatase activity by methyl sulfonyl PCB metabolites in primary culture of human mammary fibroblasts

    Energy Technology Data Exchange (ETDEWEB)

    Berg, M. van den; Heneweer, M.; Geest, M. de; Sanderson, T. [Inst. for Risk Assessment Sciences and Utrecht Univ. (Netherlands); Jong, P. de [St. Antonius Hospital, Nieuwegein (Netherlands); Bergman, A. [Stockholm Univ., Stockholm (Sweden)

    2004-09-15

    Methyl sulfonyl PCB metabolites (MeSO2-PCBs) are persistent contaminants and are ubiquitously present in humans and the environment. Lipophilicity of MeSO2- PCB metabolites is similar to the parent compounds and they have been detected in human milk, adipose, liver and lung tissue. 4- MeSO2-PCB-149 is the most abundant PCB metabolite in human adipose tissue and milk at a level of 1.5 ng/g lipids. Human blood concentration of 4-MeSO2-PCB-149 is approximately 0.03 nM. 3- MeSO2-PCB-101 is the predominant PCB metabolite in muscle and blubber in wildlife, such as otter, mink and grey seal. In the environment, they have been linked to chronic and reproductive toxicity in exposed mink. Additionaly, some MeSO{sub 2}-PCBs have been shown to be glucocorticoid receptor (GR) antagonists. Since approximately 60% of all breast tumors are estrogen responsive, exposure to compounds that are able to alter estrogen synthesis through interference with the aromatase enzyme, can lead to changes in estrogen levels and possibly to accelerated or inhibit breast tumor growth. Therefore, it is important to identify exogenous compounds that can alter aromatase activity in addition to those compounds which have direct interaction with the estrogen receptor (ER). Aromatase (CYP19) comprises the ubiquitous flavoprotein, NADPH-cytochrome P450 reductase, and a unique cytochrome P450 that is exclusively expressed in estrogen producing cells. Previous studies have revealed that expression of the aromatase gene is regulated in a species- and tissue specific manner. In healthy breast tissue, the predominantly active aromatase promoter region I.4 is regulated by glucocorticoids and class I cytokines. Therefore, it is important to investigate possible aromatase inhibiting properties of MeSO{sub 2}-PCBs (as anti glucocorticoids?) in relevant human tissues. We used primary human mammary fibroblasts because of their role in breast cancer development. We compared the results in primary fibroblasts with

  11. Potato tuber pectin structure is influenced by pectin methyl esterase activity and impacts on cooked potato texture.

    Science.gov (United States)

    Ross, Heather A; Wright, Kathryn M; McDougall, Gordon J; Roberts, Alison G; Chapman, Sean N; Morris, Wayne L; Hancock, Robert D; Stewart, Derek; Tucker, Gregory A; James, Euan K; Taylor, Mark A

    2011-01-01

    Although cooked potato tuber texture is an important trait that influences consumer preference, a detailed understanding of tuber textural properties at the molecular level is lacking. Previous work has identified tuber pectin methyl esterase activity (PME) as a potential factor impacting on textural properties. In this study, tuber PME isoform and gene expression profiles have been determined in potato germplasm with differing textural properties as assessed using an amended wedge fracture method and a sloughing assay, revealing major differences between the potato types. Differences in pectin structure between potato types with different textural properties were revealed using monoclonal antibodies specific for different pectic epitopes. Chemical analysis of tuber pectin clearly demonstrated that, in tubers containing a higher level of total PME activity, there was a reduced degree of methylation of cell wall pectin and consistently higher peak force and work done values during the fracture of cooked tuber samples, demonstrating the link between PME activity, the degree of methylation of cell wall pectin, and cooked tuber textural properties.

  12. [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indoles: Synthesis, SAR and biological evaluation as a novel class of 5-HT6 Receptor Antagonists

    Indian Academy of Sciences (India)

    Ramakrishna V S Nirogi; Rajesh Kumar Badange; Kiran Kumar Kandukuri; Mukkanti Khagga

    2015-03-01

    In continuation to our efforts to develop better treatment options for cognitive decline, we have been focussing on 5-HT6 receptor (5-HT6R) antagonists, which are known to be involved in improving cognitive function in numerous animal models. In this paper, we report a novel series of [3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indole derivatives as potent and selective 5-HT6R antagonists. The lead compound from this series shows potent in vitro binding affinity, functional antagonistic activity at 5-HT6R, good pharmacokinetic profile, excellent selectivity and no Cytochrome P450 liabilities.

  13. Heavy-ion radiation induces both activation of multiple endogenous transposable elements and alterations in DNA methylation in rice

    Science.gov (United States)

    Zhang, Meng; Sun, Yeqing; Li, Xishan; Xiaolin, Cui; Li, Xiang

    2012-07-01

    Space radiation represents a complex environmental condition in which several interacting factors such as electron, neutron, proton, heavy-ion are involved, which may provoke stress responses and jeopardize genome integrity. Given the inherent property of epigenetic modifications to respond to intrinsic aswell as external perturbations, it is conceivable that epigenetic markers like DNA methylation and transposition may undergo alterations in response to space radiation. Cytosine DNA methylation plays important roles in maintaining genome stability and controlling gene expression. A predominant means for Transposable elements (TEs) to cause genetic instability is via their transpositional activation. To find the detailed molecular characterization of the nature of genomic changes induced by space radiation, the seeds of rice were exposed to 0.02, 0.2, 1, 2 and 20 Gy dose of ^{12}C heavy-ion radiation, respectively. We found that extensive alteration in both DNA methylation and gene expression occurred in rice plants after different dose of heavy-ion radiation. Here we shown that heavy-ion radiation has induced transposition of mPing and Tos17 in rice, which belong to distinct classes including the miniature inverted terminal repeat TEs (MITEs) and long-terminal repeat (LTR) retrotransposons, respectively. mPing and Tos17 mobility were found to correlate with cytosine methylation alteration detected by MSAP and genetic variation detected by AFLP. The result showed that at least in some cases transposition of TEs was associated with cytosine demethylation within the elements. Our results implicate that the heavy-ion radiation represents a potent mutagenic agent that can cause genomic instabilities by eliciting transposition of endogenous TEs in rice. Keywords: Heavy-ion radiation, DNA methylation, Transposable elements, mPing, Tos17

  14. Phytochemical profile and biological activity of Juglans regia.

    Science.gov (United States)

    Panth, Nisha; Paudel, Keshav Raj; Karki, Rajendra

    2016-09-01

    Juglans regia Linn. (Juglandaceae), popularly known as English or Persian walnut, is a valuable medicinal plant with a potency to cure various diseases in traditional medicine. Since ancient time, different local ethnic groups have used various part of J. regia for a wide array of ailments including helminthiasis, diarrhea, sinusitis, stomach ache, arthritis, asthma, eczema, scrofula, skin disorders, diabetes mellitus, anorexia, thyroid dysfunction, cancer and infectious diseases. Biological activities of J. regia have been reported in several peer review journals and scientific attention is increasing. The present review attempts to provide comprehensive information on plant description, ethnobotanical use, toxicity, phytochemical profile, pharmacology, clinical studies and current research prospective of the J. regia. Currently, there is an immense interest on isolation/identification of active constituents from walnut and screening those active compounds for pharmacological activities. In addition, researchers are performing clinical trials as well as screening various solvent extracts or fractions of J. regia in several animal diseases models to identify promising therapeutic benefits. In the present work, we review the latest information based on published scientific investigations of J. regia.

  15. Synthesis and biological activity of hydroxycinnamoyl containing antiviral drugs

    Directory of Open Access Journals (Sweden)

    Chochkova Maya G.

    2014-01-01

    Full Text Available Seven N-hydroxycinnamoyl amides were synthesized by EDC/HOBt coupling of the corresponding substituted cinnamic acids (p-coumaric-, ferulic-, sinapic- and caffeic acids with influenza antivirals (amantadine, rimantadine and oseltamivir. DPPH (1,1-diphenyl-2-picrylhydrazyl scavenging abilities and the inhibitory effect on mushroom tyrosinase activity (using L-tyrosine as the substrate were investigated in vitro. Amongst the synthesized compounds, N-[(E-3-(3’,4’-dihydroxyphenyl-2-propenoyl]oseltamivir (1 and N-[(E-3-(3’,4’-dihydroxyphenyl-2-propenoyl]rimantadine (4, containing catechol moiety, exhibited the most potent DPPH radical-scavenging activity. Amide (1 displayed also tyrosinase inhibitory effect toward L-tyrosine as the substrate (~50%. Due to its biological activities revealed so far compound (1 can be considered as a promising candidate for a cosmetic ingredient. The synthesized compounds were also investigated for their in vitro inhibitory activity against the replication of influenza virus A (H3N2.

  16. Biological Activities of Oleanolic Acid Derivatives from Calendula officinalis Seeds.

    Science.gov (United States)

    Zaki, Ahmed; Ashour, Ahmed; Mira, Amira; Kishikawa, Asuka; Nakagawa, Toshinori; Zhu, Qinchang; Shimizu, Kuniyoshi

    2016-05-01

    Phytochemical examination of butanol fraction of Calendula officinalis seeds led to the isolation of two compounds identified as 28-O-β-D-glucopyranosyl-oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS1) and oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS2). Biological evaluation was carried out for these two compounds such as melanin biosynthesis inhibitory, hyaluronic acid production activities, anti obesity using lipase inhibition and adipocyte differentiation as well as evaluation of the protective effect against hydrogen peroxide induced neurotoxicity in neuro-2A cells. The results showed that, compound CS2 has a melanin biosynthesis stimulatory activity; however, compound CS1 has a potent stimulatory effect for the production of hyaluronic acid on normal human dermal fibroblast from adult (NHDF-Ad). Both compounds did not show any inhibitory effect on both lipase and adipocyte differentiation. Compound CS2 could protect neuro-2A cells and increased cell viability against H2 O2 . These activities (melanin biosynthesis stimulatory and protective effect against H2 O2 of CS2 and hyaluronic acid productive activities of these triterpene derivatives) have been reported for the first time. Copyright © 2016 John Wiley & Sons, Ltd.

  17. Soil degradation effect on biological activity in Mediterranean calcareous soils

    Science.gov (United States)

    Roca-Pérez, L.; Alcover-Sáez, S.; Mormeneo, S.; Boluda, R.

    2009-04-01

    Soil degradation processes include erosion, organic matter decline, compaction, salinization, landslides, contamination, sealing and biodiversity decline. In the Mediterranean region the climatological and lithological conditions, together with relief on the landscape and anthropological activity are responsible for increasing desertification process. It is therefore considered to be extreme importance to be able to measure soil degradation quantitatively. We studied soil characteristics, microbiological and biochemical parameters in different calcareous soil sequences from Valencia Community (Easter Spain), in an attempt to assess the suitability of the parameters measured to reflect the state of soil degradation and the possibility of using the parameters to assess microbiological decline and soil quality. For this purpose, forest, scrubland and agricultural soil in three soil sequences were sampled in different areas. Several sensors of the soil biochemistry and microbiology related with total organic carbon, microbial biomass carbon, soil respiration, microorganism number and enzyme activities were determined. The results show that, except microorganism number, these parameters are good indicators of a soil biological activity and soil quality. The best enzymatic activities to use like indicators were phosphatases, esterases, amino-peptidases. Thus, the enzymes test can be used as indicators of soil degradation when this degradation is related with organic matter losses. There was a statistically significant difference in cumulative O2 uptake and extracellular enzymes among the soils with different degree of degradation. We would like to thank Spanish government-MICINN for funding and support (MICINN, project CGL2006-09776).

  18. Chemistry and biological activities of flavonoids: an overview.

    Science.gov (United States)

    Kumar, Shashank; Pandey, Abhay K

    2013-01-01

    There has been increasing interest in the research on flavonoids from plant sources because of their versatile health benefits reported in various epidemiological studies. Since flavonoids are directly associated with human dietary ingredients and health, there is need to evaluate structure and function relationship. The bioavailability, metabolism, and biological activity of flavonoids depend upon the configuration, total number of hydroxyl groups, and substitution of functional groups about their nuclear structure. Fruits and vegetables are the main dietary sources of flavonoids for humans, along with tea and wine. Most recent researches have focused on the health aspects of flavonoids for humans. Many flavonoids are shown to have antioxidative activity, free radical scavenging capacity, coronary heart disease prevention, hepatoprotective, anti-inflammatory, and anticancer activities, while some flavonoids exhibit potential antiviral activities. In plant systems, flavonoids help in combating oxidative stress and act as growth regulators. For pharmaceutical purposes cost-effective bulk production of different types of flavonoids has been made possible with the help of microbial biotechnology. This review highlights the structural features of flavonoids, their beneficial roles in human health, and significance in plants as well as their microbial production.

  19. Chemistry and Biological Activities of Flavonoids: An Overview

    Directory of Open Access Journals (Sweden)

    Shashank Kumar

    2013-01-01

    Full Text Available There has been increasing interest in the research on flavonoids from plant sources because of their versatile health benefits reported in various epidemiological studies. Since flavonoids are directly associated with human dietary ingredients and health, there is need to evaluate structure and function relationship. The bioavailability, metabolism, and biological activity of flavonoids depend upon the configuration, total number of hydroxyl groups, and substitution of functional groups about their nuclear structure. Fruits and vegetables are the main dietary sources of flavonoids for humans, along with tea and wine. Most recent researches have focused on the health aspects of flavonoids for humans. Many flavonoids are shown to have antioxidative activity, free radical scavenging capacity, coronary heart disease prevention, hepatoprotective, anti-inflammatory, and anticancer activities, while some flavonoids exhibit potential antiviral activities. In plant systems, flavonoids help in combating oxidative stress and act as growth regulators. For pharmaceutical purposes cost-effective bulk production of different types of flavonoids has been made possible with the help of microbial biotechnology. This review highlights the structural features of flavonoids, their beneficial roles in human health, and significance in plants as well as their microbial production.

  20. Biological Activities of the Essential Oil from Erigeron floribundus

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    Riccardo Petrelli

    2016-08-01

    Full Text Available Erigeron floribundus (Asteraceae is an herbaceous plant widely used in Cameroonian traditional medicine to treat various diseases of microbial and non-microbial origin. In the present study, we evaluated the in vitro biological activities displayed by the essential oil obtained from the aerial parts of E. floribundus, namely the antioxidant, antimicrobial and antiproliferative activities. Moreover, we investigated the inhibitory effects of E. floribundus essential oil on nicotinate mononucleotide adenylyltransferase (NadD, a promising new target for developing novel antibiotics, and Trypanosoma brucei, the protozoan parasite responsible for Human African trypanosomiasis. The essential oil composition was dominated by spathulenol (12.2%, caryophyllene oxide (12.4% and limonene (8.8%. The E. floribundus oil showed a good activity against Staphylococcus aureus (inhibition zone diameter, IZD of 14 mm, minimum inhibitory concentration, MIC of 512 µg/mL. Interestingly, it inhibited the NadD enzyme from S. aureus (IC50 of 98 µg/mL, with no effects on mammalian orthologue enzymes. In addition, T. brucei proliferation was inhibited with IC50 values of 33.5 µg/mL with the essential oil and 5.6 µg/mL with the active component limonene. The essential oil exhibited strong cytotoxicity on HCT 116 colon carcinoma cells with an IC50 value of 14.89 µg/mL, and remarkable ferric reducing antioxidant power (tocopherol-equivalent antioxidant capacity, TEAC = 411.9 μmol·TE/g.

  1. Catalytically and biologically active silver nanoparticles synthesized using essential oil

    Science.gov (United States)

    Vilas, Vidya; Philip, Daizy; Mathew, Joseph

    2014-11-01

    There are numerous reports on phytosynthesis of silver nanoparticles and various phytochemicals are involved in the reduction and stabilization. Pure explicit phytosynthetic protocol for catalytically and biologically active silver nanoparticles is of importance as it is an environmentally benign green method. This paper reports the use of essential oil of Myristica fragrans enriched in terpenes and phenyl propenes in the reduction and stabilization. FTIR spectra of the essential oil and the synthesized biogenic silver nanoparticles are in accordance with the GC-MS spectral analysis reports. Nanosilver is initially characterized by an intense SPR band around 420 nm, followed by XRD and TEM analysis revealing the formation of 12-26 nm sized, highly pure, crystalline silver nanoparticles. Excellent catalytic and bioactive potential of the silver nanoparticles is due to the surface modification. The chemocatalytic potential of nanosilver is exhibited by the rapid reduction of the organic pollutant, para nitro phenol and by the degradation of the thiazine dye, methylene blue. Significant antibacterial activity of the silver colloid against Gram positive, Staphylococcus aureus (inhibition zone - 12 mm) and Gram negative, Escherichia coli (inhibition zone - 14 mm) is demonstrated by Agar-well diffusion method. Strong antioxidant activity of the biogenic silver nanoparticles is depicted through NO scavenging, hydrogen peroxide scavenging, reducing power, DPPH and total antioxidant activity assays.

  2. Biological Activities of the Essential Oil from Erigeron floribundus.

    Science.gov (United States)

    Petrelli, Riccardo; Orsomando, Giuseppe; Sorci, Leonardo; Maggi, Filippo; Ranjbarian, Farahnaz; Biapa Nya, Prosper C; Petrelli, Dezemona; Vitali, Luca A; Lupidi, Giulio; Quassinti, Luana; Bramucci, Massimo; Hofer, Anders; Cappellacci, Loredana

    2016-08-13

    Erigeron floribundus (Asteraceae) is an herbaceous plant widely used in Cameroonian traditional medicine to treat various diseases of microbial and non-microbial origin. In the present study, we evaluated the in vitro biological activities displayed by the essential oil obtained from the aerial parts of E. floribundus, namely the antioxidant, antimicrobial and antiproliferative activities. Moreover, we investigated the inhibitory effects of E. floribundus essential oil on nicotinate mononucleotide adenylyltransferase (NadD), a promising new target for developing novel antibiotics, and Trypanosoma brucei, the protozoan parasite responsible for Human African trypanosomiasis. The essential oil composition was dominated by spathulenol (12.2%), caryophyllene oxide (12.4%) and limonene (8.8%). The E. floribundus oil showed a good activity against Staphylococcus aureus (inhibition zone diameter, IZD of 14 mm, minimum inhibitory concentration, MIC of 512 µg/mL). Interestingly, it inhibited the NadD enzyme from S. aureus (IC50 of 98 µg/mL), with no effects on mammalian orthologue enzymes. In addition, T. brucei proliferation was inhibited with IC50 values of 33.5 µg/mL with the essential oil and 5.6 µg/mL with the active component limonene. The essential oil exhibited strong cytotoxicity on HCT 116 colon carcinoma cells with an IC50 value of 14.89 µg/mL, and remarkable ferric reducing antioxidant power (tocopherol-equivalent antioxidant capacity, TEAC = 411.9 μmol·TE/g).

  3. Phytochemical profi le and biological activity of Juglans regia

    Institute of Scientific and Technical Information of China (English)

    Nisha Panth; Keshav Raj Paudel; Rajendra Karki

    2016-01-01

    Juglans regia Linn. (Juglandaceae), popularly known as English or Persian walnut, is a valuable medicinal plant with a potency to cure various diseases in traditional medicine. Since ancient time, different local ethnic groups have used various part ofJ. regia for a wide array of ailments including helminthiasis, diarrhea, sinusitis, stomach ache, arthritis, asthma, eczema, scrofula, skin disorders, diabetes melitus, anorexia, thyroid dysfunction, cancer and infectious diseases. Biological activities of J. regia have been reported in several peer review journals and scientifi c attention is increasing. The present review attempts to provide comprehensive information on plant description, ethnobotanical use, toxicity, phytochemical profi le, pharmacology, clinical studies and current research prospective of theJ. regia. Currently, there is an immense interest on isolation/identifi cation of active constituents from walnut and screening those active compounds for pharmacological activities. In addition, researchers are performing clinical trials as wel as screening various solvent extracts or fractions ofJ. regiain several animal diseases models to identify promising therapeutic benefi ts. In the present work, we review the latest information based on published scientifi c investigations ofJ. regia.

  4. Design, synthesis and in vitro antibacterial activities of methyl-4-((substituted phenyl) [6H-indolo (2,3-b)quinoxalin-6-yl]methyl-amino)benzoate derivatives

    Institute of Scientific and Technical Information of China (English)

    Yellajyosula Lakshmi Narasimha Murthy; Nagalakshmi Karthikeyan; Govindh Boddeti; Bhagavathula S. Diwakar; E. Rajendra Singh

    2011-01-01

    A series of new methyl-4-((substituted phenyl) [6H-indolo (2,3-b)quinoxalin-6yllmethylamino)benzoate derivatives have been synthesized and assayed for their antibacterial activity on 9 different bacterial strains. Among the screened compounds 2e-2g exhibited potent inhibitory activity compared to standard drug employed, worth further investigation.

  5. Structure, function and carcinogenicity of metabolites of methylated and non-methylated polycyclic aromatic hydrocarbons: a comprehensive review.

    Science.gov (United States)

    Flesher, James W; Lehner, Andreas F

    2016-01-01

    The Unified Theory of PAH Carcinogenicity accommodates the activities of methylated and non-methylated polycyclic aromatic hydrocarbons (PAHs) and states that substitution of methyl groups on meso-methyl substituted PAHs with hydroxy, acetoxy, chloride, bromide or sulfuric acid ester groups imparts potent cancer producing properties. It incorporates specific predictions from past researchers on the mechanism of carcinogenesis by methyl-substituted hydrocarbons, including (1) requirement for metabolism to an ArCH2X type structure where X is a good leaving group and (2) biological substitution of a meso-methyl group at the most reactive center in non-methylated hydrocarbons. The Theory incorporates strong inferences of Fieser: (1) The mechanism of carcinogenesis involves a specific metabolic substitution of a hydrocarbon at its most reactive center and (2) Metabolic elimination of a carcinogen is a detoxifying process competitive with that of carcinogenesis and occurring by a different mechanism. According to this outlook, chemical or biochemical substitution of a methyl group at the reactive meso-position of non-methylated hydrocarbons is the first step in the mechanism of carcinogenesis for most, if not all, PAHs and the most potent metabolites of PAHs are to be found among the meso methyl-substituted hydrocarbons. Some PAHs and their known or potential metabolites and closely related compounds have been tested in rats for production of sarcomas at the site of subcutaneous injection and the results strongly support the specific predictions of the Unified Theory.

  6. Novel biological activity of ameloblastin in enamel matrix derivative

    Directory of Open Access Journals (Sweden)

    Sachiko KURAMITSU-FUJIMOTO

    2015-02-01

    Full Text Available Objective Enamel matrix derivative (EMD is used clinically to promote periodontal tissue regeneration. However, the effects of EMD on gingival epithelial cells during regeneration of periodontal tissues are unclear. In this in vitro study, we purified ameloblastin from EMD and investigated its biological effects on epithelial cells. Material and Methods Bioactive fractions were purified from EMD by reversed-phase high-performance liquid chromatography using hydrophobic support with a C18 column. The mouse gingival epithelial cell line GE-1 and human oral squamous cell carcinoma line SCC-25 were treated with purified EMD fraction, and cell survival was assessed with a WST-1 assay. To identify the proteins in bioactive fractions of EMD, we used proteome analysis with two-dimensional gel electrophoresis followed by identification with liquid chromatography-tandem mass spectrometry (LC-MS/MS analysis. Results Purified fractions from EMD suppressed proliferation of GE-1 and SCC-25. LC-MS/MS revealed that ameloblastin in EMD is the component responsible for inhibiting epithelial cell proliferation. The inhibitory effect of ameloblastin on the proliferation of GE-1 and SCC-25 was confirmed using recombinant protein. Conclusion The inhibitory effects of EMD on epithelial cell proliferation are caused by the biological activities of ameloblastin, which suggests that ameloblastin is involved in regulating epithelial downgrowth in periodontal tissues.

  7. Cassia senna inhibits mutagenic activities of benzo[a]-pyrene, aflatoxin B1, shamma and methyl methanesulfonate.

    Science.gov (United States)

    al-Dakan, A A; al-Tuffail, M; Hannan, M A

    1995-10-01

    Ethanol extract of Senokot tablets (Cassia senna concentrate used as vegetable laxative), was found to be non-mutagenic while it inhibited the mutagenicity of benzo[a]pyrene, shamma, aflatoxin B1 and methyl methanesulfonate in the Ames histidine reversion assay using the Salmonella typhimurium tester strain TA98. While the Senokot extract completely inhibited the mutagenicity of promutagens (i.e. metabolic activation dependent) like benzo[a]pyrene and shamma, it reduced the mutagenic activity of the direct acting mutagen methyl methanesulfonate by only 58%. The mutagen aflatoxin B1 showed a 25-fold increase in the number of histidine revertants per plate at low concentrations (1.0-4.0 micrograms/plate) in the presence of metabolic activation system while at high concentrations (10.0-30.0 micrograms/plate) it proved to be weakly mutagenic (with a 5-fold increase in the number of histidine revertants/plate) without metabolic activation. The Senokot extract completely inhibited the mutagenic effect of low concentrations of aflatoxin B1 in the presence of metabolic activation but not that resulting from higher concentrations without metabolic activation. The results obtained with benzo[a]pyrene, shamma and aflatoxin B1 indicated that the antimutagenic effects of Senokot extract could be largely due to an interaction with the metabolic process involved in the activation of procarcinogens. However, the results obtained with methyl methanesulfonate suggested that factors in Senokot may also interact with direct mutagens to produce some antimutagenic effects. An ethanol extract of crude senna leaves found to be weakly mutagenic also inhibited (though less than Senokot) the mutagenic effect of benzo[a]pyrene suggesting that the antimutagenic principle is present in the complex plant material itself.

  8. Relationships between the stereochemistry and biological activity of fungal phytotoxins.

    Science.gov (United States)

    Evidente, Antonio; Andolfi, Anna; Cimmino, Alessio

    2011-10-01

    Toxins produced by phytopathogenic fungi assume great importance because of their involvement in several plant diseases. Although such pathogens are known to have seriously damaged crops, forest, and environmental resources, they represent a very important tool to develop new environmentally friendly herbicides and fungicides. This review deals with the relationships between the biological activity of some phytotoxins produced by pathogenic fungi for major forest plants and for damaging weeds and their stereochemistry. In particular, the methods used to determine their relative and/or absolute configuration will be illustrated. These include the application of Mosher's and Murata's methods, X-ray diffractometric analysis, circular dichroism, and the use of computational methods to determine the theoretical optical rotatory power as well as the CD spectrum. The importance of determining the absolute configuration to achieve the total synthesis of some phytotoxins, interesting for their potential practical application, is also discussed.

  9. Efficient expression and purification of biologically active human cystatin proteins.

    Science.gov (United States)

    Chauhan, Sakshi; Tomar, Raghuvir S

    2016-02-01

    Cystatins are reversible cysteine protease inhibitor proteins. They are known to play important roles in controlling cathepsins, neurodegenerative disease, and in immune system regulation. Production of recombinant cystatin proteins is important for biochemical and function characterization. In this study, we cloned and expressed human stefin A, stefin B and cystatin C in Escherichia coli. Human stefin A, stefin B and cystatin C were purified from soluble fraction. For cystatin C, we used various chaperone plasmids to make cystatin C soluble, as it is reported to localize in inclusion bodies. Trigger factor, GroES-GroEL, DnaK-DnaJ-GrpE chaperones lead to the presence of cystatin C in the soluble fraction. Immobilized metal affinity chromatography, glutathione sepharose and anion exchange chromatography techniques were employed for efficient purification of these proteins. Their biological activities were tested by inhibition assays against cathepsin L and H3 protease.

  10. Advances in the Chemical Analysis and Biological Activities of Chuanxiong

    Directory of Open Access Journals (Sweden)

    Jin-Ao Duan

    2012-09-01

    Full Text Available Chuanxiong Rhizoma (Chuan-Xiong, CX, the dried rhizome of Ligusticum chuanxiong Hort. (Umbelliferae, is one of the most popular plant medicines in the World. Modern research indicates that organic acids, phthalides, alkaloids, polysaccharides, ceramides and cerebrosides are main components responsible for the bioactivities and properties of CX. Because of its complex constituents, multidisciplinary techniques are needed to validate the analytical methods that support CX’s use worldwide. In the past two decades, rapid development of technology has advanced many aspects of CX research. The aim of this review is to illustrate the recent advances in the chemical analysis and biological activities of CX, and to highlight new applications and challenges. Emphasis is placed on recent trends and emerging techniques.

  11. Production and biological activities of yellow pigments from Monascus fungi.

    Science.gov (United States)

    Chen, Gong; Wu, Zhenqiang

    2016-08-01

    Monascus yellow pigments (MYPs), are azaphilone compounds and one of the three main components of total Monascus pigments (MPs). Thirty-five hydrophilic or hydrophobic MYPs have been identified, with the majority being hydrophobic. Apart from screening special Monascus strains, some advanced approaches, such as extractive and high-cell-density fermentations, have been applied for developing or producing new MYPs, especially extracellular hydrophilic MYPs. The outstanding performance of MYPs in terms of resistance to photodegradation, as well as tolerance for temperature and pH, give natural MYPs reasonable prospects, compared with the orange and red MPs, for practical use in the present and future. Meanwhile, MYPs have shown promising potential for applications in the food and pharmaceutical industries based on their described bioactivities. This review briefly summarizes the reports to date on chemical structures, biological activities, biosynthetic pathways, production technologies, and physicochemical performances of MYPs. The existing problems for MYPs are discussed and research prospects proposed.

  12. Infrared Spectra and Hydrogen Bonds of Biologically Active Benzaldehydes

    Science.gov (United States)

    Tolstorozhev, G. B.; Skornyakov, I. V.; Belkov, M. V.; Shimko, A. N.; Shadyro, O. I.; Brinkevich, S. D.; Samovich, S. N.

    2013-09-01

    IR-Fourier spectra of solutions and crystals of biologically active benzaldehyde derivatives were studied. Specific features of the formation of intra- and intermolecular hydrogen bonds were analyzed. Spectral signatures that characterized participation of the hydroxyl OH group and also the OCH3 and C=O groups in the formation of intramolecular hydrogen bonds of the three different types O-H···O-H, O-H···O-CH3, and O-H···O=C were revealed. Intramolecular hydrogen bonds of the types O-H···O-H and O-H···O-CH3 were absent for benzaldehyde derivatives in the crystal phase. Only hydroxyl and carbonyl groups participated in intermolecular interactions. This resulted in the formation of linear intermolecular dimers. Seven various configurations of the linear dimers were identified in solutions and crystals.

  13. Biological effects of short-term, high-concentration exposure to methyl isocyanate. I. Study objectives and inhalation exposure design

    Energy Technology Data Exchange (ETDEWEB)

    Dodd, D.E.; Frank, F.R.; Fowler, E.H.; Troup, C.M.; Milton, R.M.

    1987-06-01

    Early reports from India indicated that humans were dying within minutes to a few hours from exposure to methyl isocyanate (MIC). Attempts to explain the cause(s) of these rapid mortalities is where Union Carbide Corporation concentrated its post-Bhopal toxicologic investigations. The MIC studies involving rats and guinea pigs focused primarily on the consequences of acute pulmonary damage. All MIC inhalation exposures were acute, of short duration (mainly 15 min), and high in concentration. MIC vapors were statically generated in a double chamber exposure design. Precautionary measures taken during exposures are discussed. Guinea pigs were more susceptible than rats to MIC exposure-related early mortality. A greater than one order of magnitude difference was observed between an MIC concentration that caused no early mortality in rats (3506 ppm) and an MIC concentration that caused partial (6%) early mortality in guinea pigs (225 ppm) for exposures of 10 to 15 min duration. For both species, the most noteworthy clinical signs during exposure were lacrimation, blepharospasm, and mouth breathing. Fifteen minute LC/sub 50/ tests with 14-day postexposure follow-up were conducted, and the LC/sub 50/ (95% confidence limit) values were 171 (114-256) ppm for rats and 112 (61-204) ppm for guinea pigs. Target exposure concentrations for the toxicologic investigations of MIC-induced early mortality were established. A short summary of pertinent results of Union Carbide Corporation's post-Bhopal toxicologic investigations is presented.

  14. ATRX tolerates activity-dependent histone H3 methyl/phos switching to maintain repetitive element silencing in neurons.

    Science.gov (United States)

    Noh, Kyung-Min; Maze, Ian; Zhao, Dan; Xiang, Bin; Wenderski, Wendy; Lewis, Peter W; Shen, Li; Li, Haitao; Allis, C David

    2015-06-02

    ATRX (the alpha thalassemia/mental retardation syndrome X-linked protein) is a member of the switch2/sucrose nonfermentable2 (SWI2/SNF2) family of chromatin-remodeling proteins and primarily functions at heterochromatic loci via its recognition of "repressive" histone modifications [e.g., histone H3 lysine 9 tri-methylation (H3K9me3)]. Despite significant roles for ATRX during normal neural development, as well as its relationship to human disease, ATRX function in the central nervous system is not well understood. Here, we describe ATRX's ability to recognize an activity-dependent combinatorial histone modification, histone H3 lysine 9 tri-methylation/serine 10 phosphorylation (H3K9me3S10ph), in postmitotic neurons. In neurons, this "methyl/phos" switch occurs exclusively after periods of stimulation and is highly enriched at heterochromatic repeats associated with centromeres. Using a multifaceted approach, we reveal that H3K9me3S10ph-bound Atrx represses noncoding transcription of centromeric minor satellite sequences during instances of heightened activity. Our results indicate an essential interaction between ATRX and a previously uncharacterized histone modification in the central nervous system and suggest a potential role for abnormal repetitive element transcription in pathological states manifested by ATRX dysfunction.

  15. Optimization of hypocrellin B derivative amphiphilicity and biological activity

    Institute of Scientific and Technical Information of China (English)

    LIU Xin; XIE Jie; ZHANG LuYong; CHEN HongXia; GU Ying; ZHAO JingQuan

    2009-01-01

    To satisfy the dual requirements of the fluent transportation in blood and the affinity to the target tissues of vascular diseases, hypocrellin derivatives with optimized amphiphilicity are expected. In this work, 3-amino-1-propanesulfonic acid and 4-amino-1-butanesulfonic acid substituted hypocrellin B,named compounds 1 and 2, were designed, synthesized in high yields and characterized. Besides greatly strengthened red absorption, the maximum solubility of compound 2 in phosphate buffered saline (PBS) is 4.2 mg/mL which is just enough to prepare an aqueous solution for intravenous injection in clinically acceptable concentration, while the partition coefficient between n-octanol and PBS,5.6, benefits the cell-uptake and biological activity as well. Furthermore, EPR measurements reveal that the photosensitization activities of the two compounds to generate semiquinone anion radicals, superoxide anion radicals and singlet oxygen are a little bit higher than those of taurine substituted hypocrellin B (THB), but the photodynamic activities to human lung cancer A549 cells are several times that of THB, mainly due to increases in lipophilicity and cell-uptake.

  16. Immobilization biological activated carbon used in advanced drinking water treatment

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    Bacteria separated from a mature filter bed of groundwater treatment plants were incubated in a culture media containing iron and manganese. A consortium of 5 strains of bacteria removing iron and manganese were obtained by repeated enrichment culturing. It was shown from the experiments of effect factors that ironmanganese removal bacteria in the culture media containing both Fe and Mn grew better than in that containing only Fe, however, they were unable to grow in the culture media containing only Mn. When comparing the bacteria biomass in the case ofρ (DO) =2.8 mg/L andρ (DO) =9.0 mg/L, no significant difference was found.The engineering bacteria removing the organic and the bacteria removing iron and manganese were simultaneously inoculated into activated carbon reactor to treat the effluent of distribution network. The experimental results showed that by using IBAC ( Immobilization Biological Activated Carbon) treatment, the removal efficiency of iron, manganese and permanganate index was more than 98% , 96% and 55% , respectively. After the influent with turbidity of 1.5 NTU, color of 25 degree and offensive odor was treated, the turbidity and color of effluence were less than 0.5 NTU and 15 degree, respectively, and it was odorless. It is determined that the cooperation function of engineering bacteria and activated carbon achieved advanced drinking water treatment.

  17. Evaluation of the biological activity of sunflower hull extracts

    Energy Technology Data Exchange (ETDEWEB)

    Taha, F. S.; Wagdy, S. M.; Hassanein, M. M. M.; Hamed, S. F.

    2012-11-01

    This work was planned with the aim of adding value to sunflower seed hulls, a waste product of the oil industry by preparing a sunflower hull phenolic extract rich in chlorogenic acid (CGA). In order to fulfill this goal, the optimization for the extraction of a phenolic extract from the hulls was investigated. The parameters studied were: type of solvent, solvent to water ratio and hull to solvent ratio. In addition, the solvent mixtures were also studied. The resulting phenolic extracts were evaluated for their biological activities. This included phenolic content determination, evaluation of the antioxidant and antimicrobial activities. Chlorogenic acid was determined in two chosen hull extracts using the UV spectrophotometric method and HPLC analysis. The anti carcinogenic activity of the two chosen extracts was tested on seven different cell line carcinomas. The results revealed that all the phenolic extracts of sunflower hull studied contain between 190-312.5 mg phenolics/ 100 g hulls. The highest phenolic extraction was achieved with 80% methanol (1:30, hull to solvent, w/v ratio) and methanol to ethanol to water (7:7:6 v/v/v) mixture with values of 312.5 and 306.5 mg phenolics/100 g hulls, respectively. The free radical scavenging activity and antioxidant activity of all the samples ranged from 33.6-72.6%. The highest antioxidant activity and free radical scavenging activity were achieved by the same extracts that possessed the highest phenolic content, namely methanol to ethanol to water extract and 80% methanol with values 71.8 and 72.6%, 68.2 and 70.9% respectively, compared to 77.9 and 76.9% respectively for TBHQ. All the phenolic extracts possessed antimicrobial activity but to different levels against different pathogenic bacteria. The two chosen extracts also possessed anti carcinogenic activity, which differed among varying cell line carcinomas. The HPLC analysis indicated that chlorogenic acid was the main phenolic acid in the extract. Thus it can

  18. Phytochemical Analysis and Biological Activities of Cola nitida Bark.

    Science.gov (United States)

    Dah-Nouvlessounon, Durand; Adoukonou-Sagbadja, Hubert; Diarrassouba, Nafan; Sina, Haziz; Adjanohoun, Adolphe; Inoussa, Mariam; Akakpo, Donald; Gbenou, Joachim D; Kotchoni, Simeon O; Dicko, Mamoudou H; Baba-Moussa, Lamine

    2015-01-01

    Kola nut is chewed in many West African cultures and is used ceremonially. The aim of this study is to investigate some biological effects of Cola nitida's bark after phytochemical screening. The bark was collected, dried, and then powdered for the phytochemical screening and extractions. Ethanol and ethyl acetate extracts of C. nitida were used in this study. The antibacterial activity was tested on ten reference strains and 28 meat isolated Staphylococcus strains by disc diffusion method. The antifungal activity of three fungal strains was determined on the Potato-Dextrose Agar medium mixed with the appropriate extract. The antioxidant activity was determined by DPPH and ABTS methods. Our data revealed the presence of various potent phytochemicals. For the reference and meat isolated strains, the inhibitory diameter zone was from 17.5 ± 0.7 mm (C. albicans) to 9.5 ± 0.7 mm (P. vulgaris). The MIC ranged from 0.312 mg/mL to 5.000 mg/mL and the MBC from 0.625 mg/mL to >20 mg/mL. The highest antifungal activity was observed with F. verticillioides and the lowest one with P. citrinum. The two extracts have an excellent reducing free radical activity. The killing effect of A. salina larvae was perceptible at 1.04 mg/mL. The purified extracts of Cola nitida's bark can be used to hold meat products and also like phytomedicine.

  19. Phytochemical Analysis and Biological Activities of Cola nitida Bark

    Directory of Open Access Journals (Sweden)

    Durand Dah-Nouvlessounon

    2015-01-01

    Full Text Available Kola nut is chewed in many West African cultures and is used ceremonially. The aim of this study is to investigate some biological effects of Cola nitida’s bark after phytochemical screening. The bark was collected, dried, and then powdered for the phytochemical screening and extractions. Ethanol and ethyl acetate extracts of C. nitida were used in this study. The antibacterial activity was tested on ten reference strains and 28 meat isolated Staphylococcus strains by disc diffusion method. The antifungal activity of three fungal strains was determined on the Potato-Dextrose Agar medium mixed with the appropriate extract. The antioxidant activity was determined by DPPH and ABTS methods. Our data revealed the presence of various potent phytochemicals. For the reference and meat isolated strains, the inhibitory diameter zone was from 17.5±0.7 mm (C. albicans to 9.5±0.7 mm (P. vulgaris. The MIC ranged from 0.312 mg/mL to 5.000 mg/mL and the MBC from 0.625 mg/mL to >20 mg/mL. The highest antifungal activity was observed with F. verticillioides and the lowest one with P. citrinum. The two extracts have an excellent reducing free radical activity. The killing effect of A. salina larvae was perceptible at 1.04 mg/mL. The purified extracts of Cola nitida’s bark can be used to hold meat products and also like phytomedicine.

  20. Synthesis and biological evaluation of Novel N-(3-(6-methyl-[1,2,4]triazolo [4,3-b]pyridazin-3-yl aryl carboxamide and aryl sulfonamide derivatives

    Directory of Open Access Journals (Sweden)

    K. Thirumurugan

    2016-08-01

    Full Text Available A novel derivatives of N-(3-6-methyl-[1,2,4]triazolo[4,3-b]pyridazine-3-ylphenylbenzamide and sulphonamide were prepared from 3-(6-Methyl-[1,2,4]triazolo[4,3-b]pyridazine-3-ylphenyl aniline and these derivatives were subjected to preliminary antimicrobial activities against microorganism. All these compounds exhibit good to moderate activity.

  1. Methyl bromide release from activated carbon and the soil/water/carbon interface

    Science.gov (United States)

    Methyl Bromide (MB) is a major source of stratospheric bromine radical, a known depletor of ozone. The use of ozone-depleting chemicals, including MB, is regulated by the Montreal Protocol. Critical uses of MB are permitted, such as when postharvest fumigation is mandated by an importing country. Fo...

  2. Asymmetric synthesis and biological activities of natural product (+)-balasubramide and its derivatives.

    Science.gov (United States)

    Li, Jun; Li, Jianzu; Xu, Yuan; Wang, Yunjie; Zhang, Luyong; Ding, Li; Xuan, Yining; Pang, Tao; Lin, Hansen

    2016-01-01

    The natural product (+)-balasubramide (3j) and its derivatives (3a-3i) were synthesized using a two-step asymmetric synthesis, and the biological activities of 3a-3j were determined in vitro. Methyl (2S,3R)-(+)-3-phenyloxirane-2-carboxylate (1h), the asymmetric synthesis of which was described in a previous paper, was selected as the starting material. Compounds 3a-3j were evaluated for their neuroprotective, antioxidative, and anti-neuroinflammatory effects. (+)-Balasubramide and its derivatives with different electronegative groups in the 6-phenyl ring produced little neuroprotection and antioxidation, but induced potent anti-neuroinflammatory effects in BV-2 microglial cells (with the exception of 3g). Compound 3c, with a trifluoromethyl group in its 6-phenyl ring, was a particularly potent anti-neuroinflammatory agent. These results demonstrated that the electronegativity of the 6-phenyl ring of (+)-balasubramide is an important determinant of its inhibitory effect on neuroinflammation. More electronegative substituents result in more potent anti-neuroinflammatory effects. Moreover, cytotoxicity assays indicated no significant effects of the tested compounds.

  3. INFLUENCE OF BIOLOGICALLY ACTIVE AGENTS ON A STRUCTURAL STATE AND THE ENZYMATIC ACTIVITY OF BLACK ORDINARY CARBONATED SOIL

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    Lychman V. A.

    2014-04-01

    Full Text Available The results of a long-term research of the influence of various biologically active agents (a humic preparation Lignogumat and microbiological Baikal EM fertilizer on a structural state and the enzymatic activity of ordinary carbonated black soil are presented. It has been established that biologically active substances contribute to increased enzymatic activity, humus and improve the soil structure

  4. Phenolic Compounds Characterization and Biological Activities of Citrus aurantium Bloom

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    Armin Oskoueian

    2012-01-01

    Full Text Available Citrus plants are known to possess beneficial biological activities for human health. In addition, ethnopharmacological application of plants is a good tool to explore their bioactivities and active compounds. This research was carried out to evaluate the phenolic and flavonoid analysis, antioxidant properties, anti inflammatory and anti cancer activity of Citrus aurantium bloom. The total phenolics and flavonoids results revealed that methanolic extract contained high total phenolics and flavonoids compared to ethanolic and boiling water extracts. The obtained total phenolics value for methanolic Citrus aurantium bloom extract was 4.55 ± 0.05 mg gallic acid equivalent (GAE/g dry weight (DW, and for total flavonoids it was 3.83 ± 0.05 mg rutin equivalent/g DW. In addition, the RP-HPLC analyses of phenolics and flavonoids indicated the presence of gallic acid, pyrogallol, syringic acid, caffeic acid, rutin, quercetin and naringin as bioactive compounds. The antioxidant activity of Citrus aurantium bloom were examined by the 1,1-diphenyl-2-picryl-hydrazyl (DPPH assay and the ferric reducing/antioxidant potential (FRAP. The free radical scavenging and ferric reducing power activities were higher for the methanolic extract of Citrus aurantium bloom at a concentration of 300 μg/mL, with values of 55.3% and 51.7%, respectively, as compared to the corresponding boiling water and ethanolic extracts, but the activities were lower than those of antioxidant standards such as BHT and α-tocopherol. Furthermore, the anti-inflammatory result of methanolic extract showed appreciable reduction in nitric oxide production of stimulated RAW 264.7 cells at the presence of plant extract. Apart from that, the anticancer activity of the methanolic extract was investigated in vitro against human cancer cell lines (MCF-7; MDA-MB-231, human colon adenocarcinoma (HT-29 and Chang cell as a normal human hepatocyte. The obtained result demonstrated the moderate to

  5. A Conceptual Framework for Organizing Active Learning Experiences in Biology Instruction

    Science.gov (United States)

    Gardner, Joel; Belland, Brian R.

    2012-01-01

    Introductory biology courses form a cornerstone of undergraduate instruction. However, the predominantly used lecture approach fails to produce higher-order biology learning. Research shows that active learning strategies can increase student learning, yet few biology instructors use all identified active learning strategies. In this paper, we…

  6. Synthesis, Characterization and Biological Activities of Organotin (IV Methylcyclohexyldithiocarbamate Compounds

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    Normah Awang

    2011-01-01

    Full Text Available Problem statement: The growing interest in the chemistry of sulphur donor ligands are due to their encouraging anticancer, antibacterial and antifungal activities as well as their widespread industrial application. Dithiocarbamates belong to this class and much attention has been paid to them. Approach: Novel organotin compounds with the molecular formula RmSn[S2CN(CH3(C6H11]4-m (where m = 2, R = CH3, C2H5; m = 3, R = C6H5 have been synthesized using in situ method. These compounds were characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy. Results: Elemental analysis revealed that all compounds were of good purity. Infrared spectra of the compounds showed that the thioureide ν(C-N band was in the region 1450-1500 cm−1. The unsplitting band of ν(C-S in the region 974-979 cm−1 indicated the bidentate nature of the chelated dithiocarbamato legends. The 13C NMR chemical shift of the carbon atom in the N-CS2 group appeared in the range of 196.29-199.82 ppm. Single crystal analysis from one of these compounds showed that the chelating mode of the dithiocarbamate groups was isobidentate. These compounds have been screened for antibacterial activity against four bacteria; Staphylococcus aureus, Salmonella typhimurium, Pseudomonas aeruginosa and Bacillus subtilis. Only one of these compounds shows promising results against S. aureus and S. typhi. Cytotoxicity screening on human leukemic promyelocyte HL-60 cells found that two of these compounds were very active with CD50 values of 0.87 and 0.18 µg mL−1. Conclusion: The studied compounds were found to have the potential in biological activity especially in cytotoxicity where this possibly can be used for clinical trials after further research.

  7. [Composition and content of biologically active substances in rose hips].

    Science.gov (United States)

    Dubtsova, G N; Negmatulloeva, R N; Bessonov, V V; Baĭkov, V G; Sheviakova, L V; Makhova, N N; Perederiaev, O I; Bogachuk, M N; Baĭgarin, E K

    2012-01-01

    The paper studies the chemical composition of the powders obtained from the pulp with the skins and seeds of fruits of wild rose hips. Research results have shown that the main fraction of the powder is dietary fiber, powder of seeds of insoluble fiber in 1,6 and 2,3 higher than in the powder of the fruit with a thin skin and pulp, respectively. The greatest amount of carbohydrates and protein found in powders and pulp of the fruit with a thin skin, and lipids predominate in the powder from the seeds. Found that the lipid powder rosehip richest in oleic, linoleic and linolenic acids, the share of oleic acid has 6,4-19,2%, linoleic and linolenic 19,7-45,8 and 23,3-33,9% of the amount of fatty acids. Lipids powders of hips and seeds of rose have higher levels of essential linoleic acid and powder from the pulp with the skins - linolenic acid. In the study established the presence of sterols 7 fractions, the predominant of which is the beta-sitosterol. In the powder from the pulp with the skins found the greatest amount of ascorbic acid, carotenoids, and the powder of seeds - vitamin E. Carotenoids in powders are beta-carotene and lycopene. The high content of ascorbic acid, vitamin E and carotenoids in powder from wild rose hips makes them a good source of antioxidants. Therefore, we studied the possibility of using vegetable powders obtained from hips of wild rose, to enrich biologically active substances such as vitamins C, E and carotenoids, food supply, particularly of health care use. Rosehip powder from the pulp with the skins had the highest antioxidant activity, antioxidant activity of hips powders was 74% of the activity of powder from the pulp with the skins, the lowest antioxidant activity was observed in the powder from the wild rose seeds. That's way, based on the analysis of the chemical composition of rose hip powder found high levels they ascorbic acid, carotenoids, flavonoids,found their high antioxidant activity. It allows to recommend powders

  8. Increased intragenic IGF2 methylation is associated with repression of insulator activity and elevated expression in serous ovarian carcinoma

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    Zhiqing eHuang

    2013-05-01

    Full Text Available Overexpression of insulin-like growth factor-II (IGF2 is a prominent characteristic of many epithelial ovarian malignancies. IGF2 imprinting and transcription are regulated in part through DNA methylation, which in turn regulates binding of the insulator protein, CTCF, within the IGF2/H19 imprint center. We have shown that IGF2 overexpression in ovarian cancer is associated with hypermethylation of CTCF binding sites within the IGF2/H19 imprint center. The aim of this study was to investigate the methylation and binding capacity of a novel putative CTCF binding motif located intragenic to IGF2 and determine how this relates to IGF2 expression. In 35 primary serous epithelial ovarian cancer specimens, methylation of two CpGs, including one within the core binding motif and another adjacent to this motif, was higher in the 18 cancers with elevated IGF2 expression versus 10 with low expression (avg. 68.2% vs. 38.5%; p<0.0001. We also found that the CpG site within the CTCF binding motif is hypermethylated in male gametes (>92%; avg. 93.2%; N=16. We confirmed binding of CTCF to this region in ovarian cancer cells, as well as the paralog of CTCF, BORIS, which is frequently overexpressed in cancers. The unmethylated CTCF binding motif has insulator activity in cells that express CTCF or BORIS, but not in cells that express both CTCF and BORIS. These intragenic CpG dinucleotides comprise a novel paternal germline imprint mark and are located in a binding motif for the insulator protein CTCF. Methylation of the CpG dinucleotides is positively correlated with IGF2 transcription, supporting that increased methylation represses insulator function. These combined results suggest that methylation and CTCF binding at this region play important roles in regulating the level of IGF2 transcription. Our data have revealed a novel epigenetic regulatory element within the IGF2/H19 imprinted domain that is highly relevant to aberrant IGF2 expression in ovarian

  9. Oat Phytochrome Is Biologically Active in Transgenic Tomatoes.

    Science.gov (United States)

    Boylan, M. T.; Quail, P. H.

    1989-08-01

    To determine the functional homology between phytochromes from evolutionarily divergent species, we used the cauliflower mosaic virus 35S promoter to express a monocot (oat) phytochrome cDNA in a dicot plant (tomato). Immunoblot analysis shows that more than 50% of the transgenic tomato plants synthesize the full-length oat phytochrome polypeptide. Moreover, leaves of light-grown transgenic plants contain appreciably less oat phytochrome than leaves from dark-adapted plants, and etiolated R1 transgenic seedlings have higher levels of spectrally active phytochrome than wild-type tomato seedlings in direct proportion to the level of immunochemically detectable oat polypeptide present. These data suggest that the heterologous oat polypeptide carries a functional chromophore, allowing reversible photoconversion between the two forms of the molecule, and that the far-red absorbing form (Pfr) is recognized and selectively degraded by the Pfr-specific degradative machinery in the dicot cell. The overexpression of oat phytochrome has pleiotropic, phenotypic consequences at all major phases of the life cycle. Adult transgenic tomato plants expressing high levels of the oat protein tend to be dwarfed, with dark green foliage and fruits. R1 transgenic seedlings have short hypocotyls with elevated anthocyanin contents. We conclude that a monocot phytochrome can be synthesized and correctly processed to a biologically active form in a dicot cell, and that the transduction pathway components that interact with the photoreceptor are evolutionarily conserved.

  10. Biological Activities of Phosphocitrate: A Potential Meniscal Protective Agent

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    Yubo Sun

    2013-01-01

    Full Text Available Phosphocitrate (PC inhibited meniscal calcification and the development of calcium crystal-associated osteoarthritis (OA in Hartley guinea pigs. However, the mechanisms remain elusive. This study sought to examine the biological activities of PC in the absence of calcium crystals and test the hypothesis that PC is potentially a meniscal protective agent. We found that PC downregulated the expression of many genes classified in cell proliferation, ossification, prostaglandin metabolic process, and wound healing, including bloom syndrome RecQ helicase-like, cell division cycle 7 homolog, cell division cycle 25 homolog C, ankylosis progressive homolog, prostaglandin-endoperoxide synthases-1/cyclooxygenase-1, and plasminogen activator urokinase receptor. In contrast, PC stimulated the expression of many genes classified in fibroblast growth factor receptor signaling pathway, collagen fibril organization, and extracellular structure organization, including fibroblast growth factor 7, collagen type I, alpha 1, and collagen type XI, alpha 1. Consistent with its effect on the expression of genes classified in cell proliferation, collagen fibril organization, and ossification, PC inhibited the proliferation of OA meniscal cells and meniscal cell-mediated calcification while stimulating the production of collagens. These findings indicate that PC is potentially a meniscal-protective agent and a disease-modifying drug for arthritis associated with severe meniscal degeneration.

  11. Estimates of iodine in biological materials by epithermal neutron activation analysis

    Energy Technology Data Exchange (ETDEWEB)

    Sato, T. (Tokyo Metropolitan Inst. for Neurosciences, Fuchu (Japan)); Kato, T. (Tohoku Univ., Sendai (Japan). Coll. of General Education)

    1982-01-01

    Iodine abundances in NBS biological SRMs and various organs of rats were evaluated by epithermal neutron activation analysis with a boron carbide filter. The detectability of iodine in different biological materials by this method is discussed.

  12. Caspase-3 activation in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice.

    Science.gov (United States)

    Turmel, H; Hartmann, A; Parain, K; Douhou, A; Srinivasan, A; Agid, Y; Hirsch, E C

    2001-03-01

    In 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) models of Parkinson's disease (PD), dopaminergic (DA) neurons have been shown to die by apoptosis. Moreover, recent postmortem and in vitro results have indicated that apoptotic cell death induced by 1-methyl-4-phenylpyridinium (MPP(+)) may be mediated by caspase-3. To establish whether caspase-3 activation may indeed play a role in an in vivo model of PD, we studied caspase-3 activation in C57Bl/6 mice subchronically intoxicated with MPTP. We show that caspase-3 activation peaks early, at days 1 and 2 after the end of MPTP intoxication. In contrast, pycnotic neurons persist until day 7 postintoxication, indicating that caspase-3 activation is an early and transient phenomenon in apoptotic death of DA neurons. We further demonstrate that loss of tyrosine hydroxylase (TH) immunoreactivity in this model is indeed due to cell loss rather than to loss of TH protein expression. We conclude that mice subchronically intoxicated with MPTP represent a valid PD model to study and manipulate caspase activation in vivo.

  13. Probing the active center of benzaldehyde lyase with substitutions and the pseudosubstrate analogue benzoylphosphonic acid methyl ester.

    Science.gov (United States)

    Brandt, Gabriel S; Nemeria, Natalia; Chakraborty, Sumit; McLeish, Michael J; Yep, Alejandra; Kenyon, George L; Petsko, Gregory A; Jordan, Frank; Ringe, Dagmar

    2008-07-22

    Benzaldehyde lyase (BAL) catalyzes the reversible cleavage of ( R)-benzoin to benzaldehyde utilizing thiamin diphosphate and Mg (2+) as cofactors. The enzyme is important for the chemoenzymatic synthesis of a wide range of compounds via its carboligation reaction mechanism. In addition to its principal functions, BAL can slowly decarboxylate aromatic amino acids such as benzoylformic acid. It is also intriguing mechanistically due to the paucity of acid-base residues at the active center that can participate in proton transfer steps thought to be necessary for these types of reactions. Here methyl benzoylphosphonate, an excellent electrostatic analogue of benzoylformic acid, is used to probe the mechanism of benzaldehyde lyase. The structure of benzaldehyde lyase in its covalent complex with methyl benzoylphosphonate was determined to 2.49 A (Protein Data Bank entry 3D7K ) and represents the first structure of this enzyme with a compound bound in the active site. No large structural reorganization was detected compared to the complex of the enzyme with thiamin diphosphate. The configuration of the predecarboxylation thiamin-bound intermediate was clarified by the structure. Both spectroscopic and X-ray structural studies are consistent with inhibition resulting from the binding of MBP to the thiamin diphosphate in the active centers. We also delineated the role of His29 (the sole potential acid-base catalyst in the active site other than the highly conserved Glu50) and Trp163 in cofactor activation and catalysis by benzaldehyde lyase.

  14. Effect of a biological activated carbon filter on particle counts

    Institute of Scientific and Technical Information of China (English)

    Su-hua WU; Bing-zhi DONG; Tie-jun QIAO; Jin-song ZHANG

    2008-01-01

    Due to the importance of biological safety in drinking water quality and the disadvantages which exist in traditional methods of detecting typical microorganisms such as Cryptosporidium and Giardia,it is necessary to develop an alternative.Particle counts is a qualitative measurement of the amount of dissolved solids in water.The removal rate of particle counts was previously used as an indicator of the effectiveness of a biological activated carbon(BAC)filter in removing Cryptosporidium and Giardia.The particle counts in a BAC filter effluent over one operational period and the effects of BAC filter construction and operational parameters were investigated with a 10 m3/h pilot plant.The results indicated that the maximum particle count in backwash remnant water was as high as 1296 count/ml and it needed about 1.5 h to reduce from the maximum to less than 50 count/ml.During the standard filtration period,particle counts stay constant at less than 50 count/ml for 5 d except when influ-enced by sand filter backwash remnant water.The removal rates of particle counts in the BAC filter are related to characteristics of the carbon.For example,a columned carbon and a sand bed removed 33.3% and 8.5% of particles,respectively,while the particle counts in effluent from a cracked BAC filter was higher than that of the influent.There is no significant difference among particle removal rates with different filtration rates.High post-ozone dosage(>2 mg/L)plays an important role in particle count removal;when the dosage was 3 mg/L,the removal rates by carbon layers and sand beds decreased by 17.5% and increased by 9.5%,respectively,compared with a 2 mg/L dosage.

  15. Activation of methanogenesis in arid biological soil crusts despite the presence of oxygen.

    Directory of Open Access Journals (Sweden)

    Roey Angel

    Full Text Available Methanogenesis is traditionally thought to occur only in highly reduced, anoxic environments. Wetland and rice field soils are well known sources for atmospheric methane, while aerated soils are considered sinks. Although methanogens have been detected in low numbers in some aerated, and even in desert soils, it remains unclear whether they are active under natural oxic conditions, such as in biological soil crusts (BSCs of arid regions. To answer this question we carried out a factorial experiment using microcosms under simulated natural conditions. The BSC on top of an arid soil was incubated under moist conditions in all possible combinations of flooding and drainage, light and dark, air and nitrogen headspace. In the light, oxygen was produced by photosynthesis. Methane production was detected in all microcosms, but rates were much lower when oxygen was present. In addition, the δ(13C of the methane differed between the oxic/oxygenic and anoxic microcosms. While under anoxic conditions methane was mainly produced from acetate, it was almost entirely produced from H(2/CO(2 under oxic/oxygenic conditions. Only two genera of methanogens were identified in the BSC-Methanosarcina and Methanocella; their abundance and activity in transcribing the mcrA gene (coding for methyl-CoM reductase was higher under anoxic than oxic/oxygenic conditions, respectively. Both methanogens also actively transcribed the oxygen detoxifying gene catalase. Since methanotrophs were not detectable in the BSC, all the methane produced was released into the atmosphere. Our findings point to a formerly unknown participation of desert soils in the global methane cycle.

  16. Studies on the metabolism and biological activity of the epimers of sulindac.

    Science.gov (United States)

    Brunell, David; Sagher, Daphna; Kesaraju, Shailaja; Brot, Nathan; Weissbach, Herbert

    2011-06-01

    Sulindac is a nonsteroidal, anti-inflammatory drug (NSAID) that has also been studied for its anticancer activity. Recent studies suggest that sulindac and its metabolites act by sensitizing cancer cells to oxidizing agents and drugs that affect mitochondrial function, resulting in the production of reactive oxygen species and death by apoptosis. In contrast, normal cells are not killed under these conditions and, in some instances, are protected against oxidative stress. Sulindac has a methyl sulfoxide moiety with a chiral center and was used in all of the previous studies as a mixture of the R- and S-epimers. Because epimers of a compound can have very different chemical and biological properties, we have separated the R- and S-epimers of sulindac, studied their individual metabolism, and performed preliminary experiments on their effect on normal and lung cancer cells exposed to oxidative stress. Previous results had indicated that the reduction of (S)-sulindac to sulindac sulfide, the active NSAID, was catalyzed by methionine sulfoxide reductase (Msr) A. In the present study, we purified an enzyme that reduces (R)-sulindac and resembles MsrB in its substrate specificity. The oxidation of both epimers to sulindac sulfone is catalyzed primarily by the microsomal cytochrome P450 (P450) system, and the individual enzymes responsible have been identified. (S)-Sulindac increases the activity of the P450 system better than (R)-sulindac, but both epimers increase primarily the enzymes that oxidize (R)-sulindac. Both epimers can protect normal lung cells against oxidative damage and enhance the killing of lung cancer cells exposed to oxidative stress.

  17. Actinobacteria from arid and desert habitats: diversity and biological activity

    Directory of Open Access Journals (Sweden)

    Joachim eWink

    2016-01-01

    Full Text Available Abstract The lack of new antibiotics in the pharmaceutical pipeline guides more and more researchers to leave the classical isolation procedures and to look in special niches and ecosystems. Bioprospecting of extremophilic Actinobacteria through mining untapped strains and avoiding resiolation of known biomolecules is among the most promising strategies for this purpose. With this approach, members of acidtolerant, alkalitolerant, psychrotolerant, thermotolerant, halotolerant and xerotolerant Actinobacteria have been obtained from respective habitats. Among these, little survey exists on the diversity of Actinobacteria in arid areas, which are often adapted to relatively high temperatures, salt concentrations, and radiation. Therefore, arid and desert habitats are special ecosystems which can be recruited for the isolation of uncommon Actinobacteria with new metabolic capability.At the time of this writing, members of Streptomyces, Micromonospora, Saccharothrix, Streptosporangium, Cellulomonas, Amycolatopsis, Geodermatophilus, Lechevalieria, Nocardia and Actinomadura are reported from arid habitats. However, metagenomic data present dominant members of the communities in desiccating condition of areas with limited water availability that are not yet isolated. Furthermore, significant diverse types of polyketide synthase (PKS and nonribosomal peptide synthetase (NRPS genes are detected in xerophilic and xerotolerant Actinobacteria and some bioactive compounds are reported from them. Rather than pharmaceutically active metabolites, molecules with protection activity against drying such as Ectoin and Hydroxyectoin with potential application in industry and agriculture have also been identified from xerophilic Actinobacteria. In addition, numerous biologically active small molecules are expected to be discovered from arid adapted Actinobacteria in the future. In the current survey, the diversity and biotechnological potential of Actinobacteria

  18. [Studies on acetylspiramycin. II. Biological activities of spiramycin components].

    Science.gov (United States)

    Kondo, A; Sato, K; Shuto, K; Yamashita, K; Ichikawa, S; Takahashi, K; Kita, K; Nishiie, Y; Sano, H; Yamaguchi, K

    1990-09-01

    Acetylspiramycin (ASPM) was fractionated using high performance liquid chromatography (HPLC). The peak fractions were named F1 to F7 successively in order of increasing retention times (Rt), i.e., increasing hydrophobicity, and studied for 1) antibacterial activities (MIC), 2) antibacterial potency against Bacillus subtilis ATCC 6633, 3) therapeutic effect on mice infected with Streptococcus pneumoniae III, Staphylococcus aureus Smith, 4) acute toxicity by i.p. administration to mice (LD50) and 5) cytotoxicities to fibroblasts derived from Chinese-hamster lung (CHL), cow pulmonary artery endothelial cells (CPAE) and rat hepatic cells. The results obtained are summarized below. 1. Components F1 and 4'-acetylspiramycin F2 had significantly different biological activities from those of other components: F1 showed the lowest antibacterial potency of 492 micrograms (potency)/mg, F2 showed the highest antibacterial potency of 2,040 micrograms (potency)/mg and correspondingly the lowest LD50 value of 692 mg/kg (the highest toxicity). The therapeutic effect of F2 on infections in mice was found to be the second smallest and was superior only to that of F1. The LD50 value of F1 was 1,200 mg/kg and similar to that of ASPM. 2. Antibacterial potencies of F3, F4, F5 and F6 were 1,165, 1,266, 1,374 and 1,530 micrograms (potency)/mg, respectively; fraction with the higher antibacterial activities corresponded to the longer retention times, i.e., the greater hydrophobicities. The most hydrophobic component, F7, 3-propionyl-3",4"-diacetylspiramycin, however, showed a low antibacterial potency of 1,085 micrograms (potency)/mg, next to the lowest one, F1, a fact which was in contradiction to with the sequential relation between hydrophobicities and potencies from F3 to F6.(ABSTRACT TRUNCATED AT 250 WORDS)

  19. Biological treatment of TMAH (tetra-methyl ammonium hydroxide) in a full-scale TFT-LCD wastewater treatment plant.

    Science.gov (United States)

    Hu, Tai-Ho; Whang, Liang-Ming; Liu, Pao-Wen Grace; Hung, Yu-Ching; Chen, Hung-Wei; Lin, Li-Bin; Chen, Chia-Fu; Chen, Sheng-Kun; Hsu, Shu Fu; Shen, Wason; Fu, Ryan; Hsu, Romel

    2012-06-01

    This study evaluated biological treatment of TMAH in a full-scale methanogenic up-flow anaerobic sludge blanket (UASB) followed by an aerobic bioreactor. In general, the UASB was able to perform a satisfactory TMAH degradation efficiency, but the effluent COD of the aerobic bioreactor seemed to increase with an increased TMAH in the influent wastewater. The batch test results confirmed that the UASB sludge under methanogenic conditions would be favored over the aerobic ones for TMAH treatment due to its superb ability of handling high strength of TMAH-containing wastewaters. Based on batch experiments, inhibitory chemicals present in TFT-LCD wastewater like surfactants and sulfate should be avoided to secure a stable methanogenic TMAH degradation. Finally, molecular monitoring of Methanomethylovorans hollandica and Methanosarcina mazei in the full-scale plant, the dominant methanogens in the UASB responsible for TMAH degradation, may be beneficial for a stable TMAH treatment performance.

  20. CMTM5 exhibits tumor suppressor activity through promoter methylation in oral squamous cell carcinoma

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Heyu [Central Laboratory, Peking University School of Stomatology, Beijing (China); Nan, Xu [Center for Human Disease Genomics, Department of Immunology, Key Laboratory of Medical Immunology, Ministry of Health, School of Basic Medical Sciences, Peking University, Beijing (China); Li, Xuefen [Central Laboratory, Peking University School of Stomatology, Beijing (China); Chen, Yan; Zhang, Jianyun [Department of Oral Pathology, Peking University School of Stomatology, Beijing (China); Sun, Lisha [Central Laboratory, Peking University School of Stomatology, Beijing (China); Han, Wenlin [Center for Human Disease Genomics, Department of Immunology, Key Laboratory of Medical Immunology, Ministry of Health, School of Basic Medical Sciences, Peking University, Beijing (China); Li, Tiejun, E-mail: litiejun22@vip.sina.com [Department of Oral Pathology, Peking University School of Stomatology, Beijing (China)

    2014-05-02

    Highlights: • Down-regulation of CMTM5 expression in OSCC tissues was found. • The promoter methylation status of CMTM5 was measured. • CMTM5-v1 inhibited cell proliferation and migration and induced apoptosis. • CMTM5 might act as a putative tumor suppressor gene in OSCC. - Abstract: Oral squamous cell carcinoma (OSCC) is one of the most common types of malignancies in the head and neck region. CKLF-like MARVEL transmembrane domain-containing member 5 (CMTM5) has been recently implicated as a tumor suppressor gene in several cancer types. Herein, we examined the expression and function of CMTM5 in oral squamous cell carcinoma. CMTM5 was down-regulated in oral squamous cell lines and tumor samples from patients with promoter methylation. Treatment with the demethylating agent 5-aza-2′-deoxycytidine restored CMTM5 expression. In the OSCC cell lines CAL27 and GNM, the ectopic expression of CMTM5-v1 strongly inhibited cell proliferation and migration and induced apoptosis. In addition, CMTM5-v1 inhibited tumor formation in vivo. Therefore, CMTM5 might act as a putative tumor suppressor gene through promoter methylation in oral squamous cell carcinoma.

  1. N-methyl-D-aspartate (NMDA) and the regulation of mitogen-activated protein kinase (MAPK) signaling pathways: a revolving neurochemical axis for therapeutic intervention?

    Science.gov (United States)

    Haddad, John J

    2005-11-01

    Excitatory synaptic transmission in the central nervous system (CNS) is mediated by the release of glutamate from presynaptic terminals onto postsynaptic channels gated by N-methyl-D-aspartate (NMDA) and non-NMDA (AMPA and KA) receptors. Extracellular signals control diverse neuronal functions and are responsible for mediating activity-dependent changes in synaptic strength and neuronal survival. Influx of extracellular calcium ([Ca(2+)](e)) through the NMDA receptor (NMDAR) is required for neuronal activity to change the strength of many synapses. At the molecular level, the NMDAR interacts with signaling modules, which, like the mitogen-activated protein kinase (MAPK) superfamily, transduce excitatory signals across neurons. Recent burgeoning evidence points to the fact that MAPKs play a crucial role in regulating the neurochemistry of NMDARs, their physiologic and biochemical/biophysical properties, and their potential role in pathophysiology. It is the purpose of this review to discuss: (i) the MAPKs and their role in a plethora of cellular functions; (ii) the role of MAPKs in regulating the biochemistry and physiology of NMDA receptors; (iii) the kinetics of MAPK-NMDA interactions and their biologic and neurochemical properties; (iv) how cellular signaling pathways, related cofactors and intracellular conditions affect NMDA-MAPK interactions and (v) the role of NMDA-MAPK pathways in pathophysiology and the evolution of disease conditions. Given the versatility of the NMDA-MAPK interactions, the NMDA-MAPK axis will likely form a neurochemical target for therapeutic interventions.

  2. Cytochrome P450 2B (CYP2B)-mediated activation of methyl-parathion in rat brain extracts.

    Science.gov (United States)

    Albores, A; Ortega-Mantilla, G; Sierra-Santoyo, A; Cebrián, M E; Muñoz-Sánchez, J L; Calderón-Salinas, J V; Manno, M

    2001-10-15

    The role of cytochrome P450 (CYP) and the CYP isoform involved in the activation of the widely used pesticide methyl-parathion (MePA) were investigated in rat brain extracts by measuring the effect of different CYP inhibitors on acetylcholinesterase (AChE) inhibition by MePA. Brain extracts provide a useful tool to study the activation mechanisms of organophosphorus compounds (OP) since they contain both the activating enzyme(s) and the molecular target for OP toxicity. As expected, in incubations of rat brain extract supplemented with NADPH, AChE activity was non-competitively inhibited by the presence of MePA, indicating that MePA was activated to its reactive metabolite methyl-paraoxon (MePO). Indeed, Vmax(app) decreased from 13.4 to 8.7 micromol thionitrobenzoic acid (TNB)/min per mg protein. MePA activation by rat brain extracts, as measured by the AChE inhibition produced by the presence of the pesticide in the incubation, was fully prevented by previously bubbling the incubation mix with CO, by the presence of monoclonal anti-rat CYP2B1/2B2 antibodies and by the addition of phenobarbital (PB), a CYP2B substrate. Interestingly, MePA showed a greater affinity for CYP2B than PB. CYP1A1 antibodies showed no effect on MePA activation. The presence of cytochrome P450 2B (CYP2B) in the rat brain extracts was confirmed by immunoblotting. These results demonstrate indisputably the responsibility of CYP2B in MePA activation in the rat brain in vitro, suggesting that metabolic activation of OP compounds in situ might be crucial for their organ specific toxicity to the central nervous system also in vivo.

  3. Single-Turnover Kinetics of Methyl Transfer to tRNA by Methyltransferases

    Science.gov (United States)

    Hou, Ya-Ming

    2016-01-01

    Summary Methyl transfer from S-adenosyl methionine (abbreviated as AdoMet) to biologically active molecules such as mRNAs and tRNAs is one of the most fundamental and widespread reactions in nature, occurring in all three domains of life. The measurement of kinetic constants of AdoMet-dependent methyl transfer is therefore important for understanding the reaction mechanism in the context of biology. When kinetic constants of methyl transfer are measured in steady state over multiple rounds of turnover, the meaning of these constants is difficult to define and is often limited by non-chemical steps of the reaction, such as product release after each turnover. Here the measurement of kinetic constants of methyl transfer by tRNA methyltransferases in rapid equilibrium binding condition for one methyl transfer is described. The advantage of such a measurement is that the meaning of kinetic constants can be directly assigned to the steps associated with the chemistry of methyl transfer, including the substrate binding affinity to the methyl transferase, the pre-chemistry re-arrangement of the active site, and the chemical step of methyl transfer. An additional advantage is that kinetic constants measured for one methyl transfer can be correlated with structural information of the methyl transferase to gain direct insight into its reaction mechanism. PMID:26965259

  4. Indium-mediated Facile Synthesis of (6-Chloropyridine-3-yl)methyl Heterocyclic Thioether Derivatives in Aqueous Media

    Institute of Scientific and Technical Information of China (English)

    Bao An SONG; Gang LIU; De Yu HU; Hua ZHANG

    2004-01-01

    A series of substituted (6-chloropyridine-3-yl)methyl heterocyclic thioether derivatives were prepared by indium mediating in water. The preliminary biological tests showed that compound 3d exhibited good antiviral activity.

  5. Isolation of methyl syringate as a specific aflatoxin production inhibitor from the essential oil of Betula alba and aflatoxin production inhibitory activities of its related compounds.

    Science.gov (United States)

    Jermnak, Usuma; Yoshinari, Tomoya; Sugiyama, Yasumasa; Tsuyuki, Rie; Nagasawa, Hiromichi; Sakuda, Shohei

    2012-02-15

    Methyl syringate was isolated from the essential oil of Betula alba as an aflatoxin production inhibitor. It inhibited aflatoxin production of Aspergillus parasiticus and Aspergillus flavus with IC(50) values of 0.9 and 0.8 mM, respectively, without significantly inhibiting fungal growth. Methyl syringate reduced mRNA levels of genes (aflR, pksA, and omtB) [corrected] encoding proteins required for aflatoxin biosynthesis. Methyl gallate, methyl 3,4,5-trimethoxybenzoate, and methyl 3-O-methylgallate inhibited both aflatoxin production and fungal growth of A. parasiticus and A. flavus. However, their acids and syringic acid did not inhibit aflatoxin production and growth of A. parasiticus significantly, although gallic acid inhibited aflatoxin production of A. flavus with selectivity. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity of methyl syringate was much weaker than that of gallic acid. These results showed that methyl syringate has a unique inhibitory activity toward aflatoxin production with a different mode of action from that of gallic acid.

  6. Biological aerosol detection with combined passive-active infrared measurements

    Science.gov (United States)

    Ifarraguerri, Agustin I.; Vanderbeek, Richard G.; Ben-David, Avishai

    2004-12-01

    A data collection experiment was performed in November of 2003 to measure aerosol signatures using multiple sensors, all operating in the long-wave infrared. The purpose of this data collection experiment was to determine whether combining passive hyperspectral and LIDAR measurements can substantially improve biological aerosol detection performance. Controlled releases of dry aerosols, including road dust, egg albumin and two strains of Bacillus Subtilis var. Niger (BG) spores were performed using the ECBC/ARTEMIS open-path aerosol test chamber located in the Edgewood Area of Aberdeen Proving Grounds, MD. The chamber provides a ~ 20' path without optical windows. Ground truth devices included 3 aerodynamic particle sizers, an optical particle size spectrometer, 6 nephelometers and a high-volume particle sampler. Two sensors were used to make measurements during the test: the AIRIS long-wave infrared imaging spectrometer and the FAL CO2 LIDAR. The AIRIS and FAL data sets were analyzed for detection performance relative to the ground truth. In this paper we present experimental results from the individual sensors as well as results from passive-active sensor fusion. The sensor performance is presented in the form of receiver operating characteristic curves.

  7. Intramolecular Hydrogen Bond in Biologically Active o-Carbonyl Hydroquinones

    Directory of Open Access Journals (Sweden)

    Maximiliano Martínez-Cifuentes

    2014-07-01

    Full Text Available Intramolecular hydrogen bonds (IHBs play a central role in the molecular structure, chemical reactivity and interactions of biologically active molecules. Here, we study the IHBs of seven related o-carbonyl hydroquinones and one structurally-related aromatic lactone, some of which have shown anticancer and antioxidant activity. Experimental NMR data were correlated with theoretical calculations at the DFT and ab initio levels. Natural bond orbital (NBO and molecular electrostatic potential (MEP calculations were used to study the electronic characteristics of these IHB. As expected, our results show that NBO calculations are better than MEP to describe the strength of the IHBs. NBO energies (∆Eij(2 show that the main contributions to energy stabilization correspond to LPàσ* interactions for IHBs, O1…O2-H2 and the delocalization LPàπ* for O2-C2 = Cα(β. For the O1…O2-H2 interaction, the values of ∆Eij(2 can be attributed to the difference in the overlap ability between orbitals i and j (Fij, instead of the energy difference between them. The large energy for the LP O2àπ* C2 = Cα(β interaction in the compounds 9-Hydroxy-5-oxo-4,8, 8-trimethyl-l,9(8H-anthracenecarbolactone (VIII and 9,10-dihydroxy-4,4-dimethylanthracen-1(4H-one (VII (55.49 and 60.70 kcal/mol, respectively when compared with the remaining molecules (all less than 50 kcal/mol, suggests that the IHBs in VIII and VII are strongly resonance assisted.

  8. Polyphenols from Bee Pollen: Structure, Absorption, Metabolism and Biological Activity

    Directory of Open Access Journals (Sweden)

    Anna Rzepecka-Stojko

    2015-12-01

    Full Text Available Bee pollen constitutes a natural source of antioxidants such as phenolic acids and flavonoids, which are responsible for its biological activity. Research has indicated the correlation between dietary polyphenols and cardioprotective, hepatoprotective, anti-inflammatory, antibacterial, anticancerogenic, immunostimulating, antianaemic effects, as well as their beneficial influence on osseous tissue. The beneficial effects of bee pollen on health result from the presence of phenolic acids and flavonoids which possess anti-inflammatory properties, phytosterol and linolenic acid which play an anticancerogenic role, and polysaccharides which stimulate immunological activity. Polyphenols are absorbed in the alimentary tract, metabolised by CYP450 enzymes, and excreted with urine and faeces. Flavonoids and phenolic acids are characterised by high antioxidative potential, which is closely related to their chemical structure. The high antioxidant potential of phenolic acids is due to the presence and location of hydroxyl groups, a carboxyl group in the immediate vicinity of ortho-diphenolic substituents, and the ethylene group between the phenyl ring and the carboxyl group. As regards flavonoids, essential structural elements are hydroxyl groups at the C5 and C7 positions in the A ring, and at the C3′ and C4′ positions in the B ring, and a hydroxyl group at the C3 position in the C ring. Furthermore, both, the double bond between C2 and C3, and a ketone group at the C4 position in the C ring enhance the antioxidative potential of these compounds. Polyphenols have an ideal chemical structure for scavenging free radicals and for creating chelates with metal ions, which makes them effective antioxidants in vivo.

  9. Polyphenols from Bee Pollen: Structure, Absorption, Metabolism and Biological Activity.

    Science.gov (United States)

    Rzepecka-Stojko, Anna; Stojko, Jerzy; Kurek-Górecka, Anna; Górecki, Michał; Kabała-Dzik, Agata; Kubina, Robert; Moździerz, Aleksandra; Buszman, Ewa

    2015-12-04

    Bee pollen constitutes a natural source of antioxidants such as phenolic acids and flavonoids, which are responsible for its biological activity. Research has indicated the correlation between dietary polyphenols and cardioprotective, hepatoprotective, anti-inflammatory, antibacterial, anticancerogenic, immunostimulating, antianaemic effects, as well as their beneficial influence on osseous tissue. The beneficial effects of bee pollen on health result from the presence of phenolic acids and flavonoids which possess anti-inflammatory properties, phytosterol and linolenic acid which play an anticancerogenic role, and polysaccharides which stimulate immunological activity. Polyphenols are absorbed in the alimentary tract, metabolised by CYP450 enzymes, and excreted with urine and faeces. Flavonoids and phenolic acids are characterised by high antioxidative potential, which is closely related to their chemical structure. The high antioxidant potential of phenolic acids is due to the presence and location of hydroxyl groups, a carboxyl group in the immediate vicinity of ortho-diphenolic substituents, and the ethylene group between the phenyl ring and the carboxyl group. As regards flavonoids, essential structural elements are hydroxyl groups at the C5 and C7 positions in the A ring, and at the C3' and C4' positions in the B ring, and a hydroxyl group at the C3 position in the C ring. Furthermore, both, the double bond between C2 and C3, and a ketone group at the C4 position in the C ring enhance the antioxidative potential of these compounds. Polyphenols have an ideal chemical structure for scavenging free radicals and for creating chelates with metal ions, which makes them effective antioxidants in vivo.

  10. Lycopene Enhances Antioxidant Enzyme Activities and Immunity Function in N-Methyl-N′-nitro-N-nitrosoguanidine–Induced Gastric Cancer Rats

    OpenAIRE

    Xian-Guo Wu; Cong Luo

    2011-01-01

    To investigate anticancer effect of lycopene, we examined the effects of lycopene on the oxidative injury and immunity activities of N-methyl-N′-nitro-N-nitrosoguanidine (MNNG)-induced gastric cancer rats. The animals were divided into five groups. Group I served as the normal control and was given corn oil orally for 20 weeks. Group II were induced with MNNG 200 mg/kg body weight by oral gavage at days 0 and 14, and saturated NaCl (1 mL per rats) was given once every three days for four week...

  11. An RNA Polymerase II-coupled function for histone H3K36 methylation in checkpoint activation and DSB repair

    OpenAIRE

    Jha, Deepak Kumar; Brian D Strahl

    2014-01-01

    Histone modifications are major determinants of DNA double-strand break (DSB) response and repair. Here we elucidate a DSB repair function for transcription-coupled Set2 methylation at H3 lysine 36 (H3K36me). Cells devoid of Set2/H3K36me are hypersensitive to DNA-damaging agents and site-specific DSBs, fail to properly activate the DNA-damage checkpoint, and show genetic interactions with DSB-sensing and repair machinery. Set2/H3K36me3 is enriched at DSBs, and loss of Set2 results in altered ...

  12. A nickel hydride complex in the active site of methyl-coenzyme m reductase: implications for the catalytic cycle.

    Science.gov (United States)

    Harmer, Jeffrey; Finazzo, Cinzia; Piskorski, Rafal; Ebner, Sieglinde; Duin, Evert C; Goenrich, Meike; Thauer, Rudolf K; Reiher, Markus; Schweiger, Arthur; Hinderberger, Dariush; Jaun, Bernhard

    2008-08-20

    Methanogenic archaea utilize a specific pathway in their metabolism, converting C1 substrates (i.e., CO2) or acetate to methane and thereby providing energy for the cell. Methyl-coenzyme M reductase (MCR) catalyzes the key step in the process, namely methyl-coenzyme M (CH3-S-CoM) plus coenzyme B (HS-CoB) to methane and CoM-S-S-CoB. The active site of MCR contains the nickel porphinoid F430. We report here on the coordinated ligands of the two paramagnetic MCR red2 states, induced when HS-CoM (a reversible competitive inhibitor) and the second substrate HS-CoB or its analogue CH3-S-CoB are added to the enzyme in the active MCR red1 state (Ni(I)F430). Continuous wave and pulse EPR spectroscopy are used to show that the MCR red2a state exhibits a very large proton hyperfine interaction with principal values A((1)H) = [-43,-42,-5] MHz and thus represents formally a Ni(III)F430 hydride complex formed by oxidative addition to Ni(I). In view of the known ability of nickel hydrides to activate methane, and the growing body of evidence for the involvement of MCR in "reverse" methanogenesis (anaerobic oxidation of methane), we believe that the nickel hydride complex reported here could play a key role in helping to understand both the mechanism of "reverse" and "forward" methanogenesis.

  13. Trypanocidal activity of 8-methyl-5'-{[(Z)-4-aminobut-2-enyl]-(methylamino)}adenosine (Genz-644131), an adenosylmethionine decarboxylase inhibitor.

    Science.gov (United States)

    Bacchi, Cyrus J; Barker, Robert H; Rodriguez, Aixa; Hirth, Bradford; Rattendi, Donna; Yarlett, Nigel; Hendrick, Clifford L; Sybertz, Edmund

    2009-08-01

    Genzyme 644131, 8-methyl-5'-{[(Z)-4-aminobut-2-enyl](methylamino)}adenosine, is an analog of the enzyme activated S-adenosylmethionine decarboxylase (AdoMetDC) inhibitor and the trypanocidal agent MDL-7381, 5-{[(Z)-4-aminobut-2-enyl](methylamino)}adenosine. The analog differs from the parent in having an 8-methyl group on the purine ring that bestows favorable pharmacokinetic, biochemical, and trypanocidal activities. The compound was curative in acute Trypanosoma brucei brucei and drug-resistant Trypanosoma brucei rhodesiense model infections, with single-dose activity in the 1- to 5-mg/kg/day daily dose range for 4 days against T. brucei brucei and 25- to 50-mg/kg twice-daily dosing against T. brucei rhodesiense infections. The compound was not curative in the TREU 667 central nervous system model infection but cleared blood parasitemia and extended time to recrudescence in several groups. This study shows that AdoMetDC remains an attractive chemotherapeutic target in African trypanosomes and that chemical changes in AdoMetDC inhibitors can produce more favorable drug characteristics than the lead compound.

  14. Methylation associated inactivation of RASSF1A and its synergistic effect with activated K-Ras in nasopharyngeal carcinoma

    Directory of Open Access Journals (Sweden)

    Yu Jing

    2009-12-01

    Full Text Available Abstract Background Epigenetic silencing of tumor suppressor genes associated with promoter methylation is considered to be a hallmark of oncogenesis. RASSF1A is a candidate tumor suppressor gene which was found to be inactivated in many human cancers. Although we have had a prelimilary cognition about the function of RASSF1A, the exact mechanisms about how RASSF1A functions in human cancers were largely unknown. Moreover, the effect of mutated K-Ras gene on the function of RASSF1A is lacking. The aim of this study was to investigate the expression profile and methylation status of RASSF1A gene, and to explore its concrete mechanisms as a tumor suppressor gene in Nasopharyngeal Carcinoma. Methods We examined the expression profile and methylation status of RASSF1A in two NPC cell lines, 38 primary nasopharyngeal carcinoma and 14 normal nasopharyngeal epithelia using RT-PCR and methylated specific PCR(MSP respectively. 5-aza-dC was then added to confirm the correlation between hypermethylation status and inactivation of RASSF1A. The NPC cell line CNE-2 was transfected with exogenous pcDNA3.1(+/RASSF1A plasmid in the presence or absence of mutated K-Ras by liposome-mediated gene transfer method. Flow cytometry was used to examine the effect of RASSF1A on cell cycle modulation and apoptosis. Meanwhile, trypan blue dye exclusion assays was used to detect the effect of RASSF1A transfection alone and the co-transfection of RASSF1A and K-Ras on cell proliferation. Results Promoter methylation of RASSF1A could be detected in 71.05% (27/38 of NPC samples, but not in normal nasopharyngeal epithelia. RASSF1A expression in NPC primary tumors was lower than that in normal nasopharyngeal epithelial (p p p p Conclusion Expression of RASSF1A is down-regulated in NPC due to the hypermethylation of promoter. Exogenous expression of RASSF1A is able to induce growth inhibition effect and apoptosis in tumor cell lines, and this effect could be enhanced by activated

  15. DNA methylation in porcine preimplantation embryos developed in-vivo or produced by in-vitro fertilization, parthenogenetic activation and somatic cell nuclear transfer

    DEFF Research Database (Denmark)

    Deshmukh, Rahul Shahaji; Østrup, Olga; Østrup, Esben;

    2011-01-01

    DNA demethylation and remethylation are crucial for reprogramming of the differentiated parental/somatic genome in the recipient ooplasm upon somatic cell nuclear transfer. Here, we analyzed the DNA methylation dynamics during porcine preimplantation development. Porcine in vivo developed (IV......), in vitro fertilized (IVF), somatic cell nuclear transfer (SCNT) and parthenogenetically activated (PA) embryos were evaluated for DNA methylation quantification at different developmental stages. Fertilized (IV and IVF) one-cell stages lacked a substantial active demethylation of the paternal genome....... Embryos produced under in vitro conditions had higher levels of DNA methylation than IV. A lineage-specific DNA methylation (hypermethylation of the inner cell mass and hypomethylation of the trophectoderm) was observed in porcine IV late blastocysts, but was absent in PA- and SCNT-derived blastocysts...

  16. DNA methylation in porcine preimplantation embryos developed in vivo and produced by in vitro fertilization, parthenogenetic activation and somatic cell nuclear transfer

    DEFF Research Database (Denmark)

    Deshmukh, Rahul Shahaji; Østrup, Olga; Østrup, Esben;

    2011-01-01

    DNA demethylation and remethylation are crucial for reprogramming of the differentiated parental/somatic genome in the recipient ooplasm upon somatic cell nuclear transfer. Here, we analyzed the DNA methylation dynamics during porcine preimplantation development. Porcine in vivo developed (IV......), in vitro fertilized (IVF), somatic cell nuclear transfer (SCNT) and parthenogenetically activated (PA) embryos were evaluated for DNA methylation quantification at different developmental stages. Fertilized (IV and IVF) one-cell stages lacked a substantial active demethylation of the paternal genome....... Embryos produced under in vitro conditions had higher levels of DNA methylation than IV. A lineage-specific DNA methylation (hypermethylation of the inner cell mass and hypomethylation of the trophectoderm) was observed in porcine IV late blastocysts, but was absent in PA- and SCNT-derived blastocysts...

  17. DNA methylation in porcine preimplantation embryos developed in vivo or produced by in vitro fertilization, parthenogenetic activation and somatic cell nuclear transfer

    DEFF Research Database (Denmark)

    Deshmukh, Rahul Shahaji; Østrup, Olga; Østrup, Esben;

    2011-01-01

    DNA demethylation and remethylation are crucial for reprogramming of the differentiated parental/somatic genome in the recipient ooplasm upon somatic cell nuclear transfer. Here, we analyzed the DNA methylation dynamics during porcine preimplantation development. Porcine in vivo developed (IV......), in vitro fertilized (IVF), somatic cell nuclear transfer (SCNT) and parthenogenetically activated (PA) embryos were evaluated for DNA methylation quantification at different developmental stages. Fertilized (IV and IVF) one-cell stages lacked a substantial active demethylation of the paternal genome....... Embryos produced under in vitro conditions had higher levels of DNA methylation than IV. A lineage-specific DNA methylation (hypermethylation of the inner cell mass and hypomethylation of the trophectoderm) was observed in porcine IV late blastocysts, but was absent in PA- and SCNT-derived blastocysts...

  18. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF SOME NOVEL ARYL AND HETROARYL CHALCONE ANALOGUES

    Directory of Open Access Journals (Sweden)

    Tribhuvan Singh

    2012-07-01

    Full Text Available A new series of Heterocyclic chalcones showed diversified biological activities. In view of potential biological activities of Heterocyclic chalcones derivative were prepared by claisen-Schmidt condensation technique. The compound were screened for anti-inflammatory and antibacterial activity.

  19. Altered expression of BRG1 and histone demethylases, and aberrant H3K4 methylation in less developmentally competent embryos at the time of embryonic genome activation.

    Science.gov (United States)

    Glanzner, Werner G; Wachter, Audrey; Coutinho, Ana Rita S; Albornoz, Marcelo S; Duggavathi, Raj; GonÇAlves, Paulo B D; Bordignon, Vilceu

    2017-01-01

    Epigenetics is a fundamental regulator underlying many biological functions, such as development and cell differentiation. Epigenetic modifications affect key chromatin regulation, including transcription and DNA repair, which are critical for normal embryo development. In this study, we profiled the expression of epigenetic modifiers and patterns of epigenetic changes in porcine embryos around the period of embryonic genome activation (EGA). We observed that Brahma-related gene 1 (BRG1) and Lysine demethylase 1A (KDM1A), which can alter the methylation status of lysine 4 in histone 3 (H3K4), localize to the nucleus at Day 3-4 of development. We then compared the abundance of epigenetic modifiers between early- and late-cleaving embryos, which were classified based on the time to the first cell cleavage, to investigate if their nuclear localization contributes to developmental competence. The mRNA abundance of BRG1, KDM1A, as well as other lysine demethylases (KDM1B, KDM5A, KDM5B, and KDM5C), were significantly higher in late- compared to early-cleaving embryos near the EGA period, although these difference disappeared at the blastocyst stage. The abundance of H3K4 mono- (H3K4me) and di-methylation (H3K4me2) during the EGA period was reduced in late-cleaving and less developmentally competent embryos. By contrast, BRG1, KDM1A, and H3K4me2 abundance was greater in embryos with more than eight cells at Day 3-4 of development compared to those with fewer than four cells. These findings suggest that altered epigenetic modifications of H3K4 around the EGA period may affect the developmental capacity of porcine embryos to reach the blastocyst stage. Mol. Reprod. Dev. 84: 19-29, 2017. © 2016 Wiley Periodicals, Inc.

  20. Synthesis and biological activity of new 1,8-diaza-2,9,10-anthracenetrione derivatives.

    Science.gov (United States)

    Gesto, C; de la Cuesta, E; Avendaño, C; Emling, F

    1992-08-01

    Diels-Alder heterocycloaddition reactions of 2,5,8-quinolinetriones and 1-azadienes afford 1,8-diaza-2,9,10-anthracenetriones, which are simple analogues of the antitumoral antibiotic diazaquinomicin A. Cytotoxicity in this series and antitumor activity of the lead compound, 6-methyl-1,8-diaza-2,9,10-anthracenetrione, are reported.

  1. Investigating the Use of Inquiry & Web-Based Activities with Inclusive Biology Learners

    Science.gov (United States)

    Bodzin, Alec M.; Waller, Patricia L.; Edwards, Lana; Darlene Kale, Santoro

    2007-01-01

    A Web-integrated biology program is used to explore how to best assist inclusive high school students to learn biology with inquiry-based activities. Classroom adaptations and instructional strategies teachers may use to assist in promoting biology learning with inclusive learners are discussed.

  2. Ubiquitin vinyl methyl ester binding orients the misaligned active site of the ubiquitin hydrolase UCHL1 into productive conformation

    Energy Technology Data Exchange (ETDEWEB)

    Boudreaux, David A.; Maiti, Tushar K.; Davies, Christopher W.; Das, Chittaranjan (Purdue)

    2010-07-06

    Ubiquitin carboxy-terminal hydrolase L1 (UCHL1) is a Parkinson disease-associated, putative cysteine protease found abundantly and selectively expressed in neurons. The crystal structure of apo UCHL1 showed that the active-site residues are not aligned in a canonical form, with the nucleophilic cysteine being 7.7 {angstrom} from the general base histidine, an arrangement consistent with an inactive form of the enzyme. Here we report the crystal structures of the wild type and two Parkinson disease-associated variants of the enzyme, S18Y and I93M, bound to a ubiquitin-based suicide substrate, ubiquitin vinyl methyl ester. These structures reveal that ubiquitin vinyl methyl ester binds primarily at two sites on the enzyme, with its carboxy terminus at the active site and with its amino-terminal {beta}-hairpin at the distal site - a surface-exposed hydrophobic crevice 17 {angstrom} away from the active site. Binding at the distal site initiates a cascade of side-chain movements in the enzyme that starts at a highly conserved, surface-exposed phenylalanine and is relayed to the active site resulting in the reorientation and proximal placement of the general base within 4 {angstrom} of the catalytic cysteine, an arrangement found in productive cysteine proteases. Mutation of the distal-site, surface-exposed phenylalanine to alanine reduces ubiquitin binding and severely impairs the catalytic activity of the enzyme. These results suggest that the activity of UCHL1 may be regulated by its own substrate.

  3. Electrodermal screening of biologically active points for upper gastrointestinal bleeding.

    Science.gov (United States)

    Tseng, Ying-Jung; Hu, Wen-Long; Hung, I-Ling; Hsieh, Chia-Jung; Hung, Yu-Chiang

    2014-01-01

    The purpose of this case-control study was to investigate the relationship between the electrical resistance of the skin at biologically active points (BAPs) on the main meridians and upper gastrointestinal bleeding (UGIB). Electrical resistance to direct current at 20 BAPs on the fingers and toes of 100 patients with (38 men, 12 women; mean age [range], 58.20 ± 19.62 [18-83] years) and without (27 men, 23 women; 49.54 ± 12.12 [22-74] years) UGIB was measured through electrodermal screening (EDS), based on the theory of electroacupuncture according to Voll (EAV). Data were compared through analysis of variance (ANOVA), receiver operating characteristic (ROC) curve analysis, and logistic regression. The initial readings were lower in the UGIB group, indicating blood and energy deficiency due to UGIB. Significant differences in indicator drop values were observed at nine BAPs (p < 0.05) on the bilateral small intestine, bilateral stomach, bilateral circulation, bilateral fibroid degeneration, and right lymph meridians. The area under the ROC curve values of the BAPs on the bilateral small intestine and stomach meridians were larger than 0.5, suggesting the diagnostic accuracy of EDS for UGIB on the basis of the indicator drop of these BAPs. Logistic regression revealed that when the indicator drop of the BAP on the left stomach meridian increased by one score, the risk of UGIB increased by about 1.545-3.523 times. In conclusion, the change in the electrical resistance of the skin measured by EDS at the BAPs on the bilateral small intestine and stomach meridians provides specific information on UGIB.

  4. Erasing the methyl mark: histone demethylases at the center of cellular differentiation and disease

    DEFF Research Database (Denmark)

    Cloos, Paul A C; Christensen, Jesper; Agger, Karl;

    2008-01-01

    The enzymes catalyzing lysine and arginine methylation of histones are essential for maintaining transcriptional programs and determining cell fate and identity. Until recently, histone methylation was regarded irreversible. However, within the last few years, several families of histone...... demethylases erasing methyl marks associated with gene repression or activation have been identified, underscoring the plasticity and dynamic nature of histone methylation. Recent discoveries have revealed that histone demethylases take part in large multiprotein complexes synergizing with histone deacetylases......, histone methyltransferases, and nuclear receptors to control developmental and transcriptional programs. Here we review the emerging biochemical and biological functions of the histone demethylases and discuss their potential involvement in human diseases, including cancer....

  5. Biologic

    CERN Document Server

    Kauffman, L H

    2002-01-01

    In this paper we explore the boundary between biology and the study of formal systems (logic). In the end, we arrive at a summary formalism, a chapter in "boundary mathematics" where there are not only containers but also extainers ><, entities open to interaction and distinguishing the space that they are not. The boundary algebra of containers and extainers is to biologic what boolean algebra is to classical logic. We show how this formalism encompasses significant parts of the logic of DNA replication, the Dirac formalism for quantum mechanics, formalisms for protein folding and the basic structure of the Temperley Lieb algebra at the foundations of topological invariants of knots and links.

  6. Epigenetic regulation: methylation of histone and non-histone proteins

    Institute of Scientific and Technical Information of China (English)

    2009-01-01

    Histone methylation is believed to play important roles in epigenetic memory in various biological processes. However, questions like whether the methylation marks themselves are faithfully transmit- ted into daughter cells and through what mechanisms are currently under active investigation. Previ- ously, methylation was considered to be irreversible, but the recent discovery of histone lysine de- methylases revealed a dynamic nature of histone methylation regulation on four of the main sites of methylation on histone H3 and H4 tails (H3K4, H3K9, H3K27 and H3K36). Even so, it is still unclear whether demethylases specific for the remaining two sites, H3K79 and H4K20, exist. Furthermore, be- sides histone proteins, the lysine methylation and demethylation also occur on non-histone proteins, which are probably subjected to similar regulation as histones. This review discusses recent pro- gresses in protein lysine methylation regulation focusing on the above topics, while referring readers to a number of recent reviews for the biochemistry and biology of these enzymes.

  7. Epigenetic regulation: methylation of histone and non-histone proteins

    Institute of Scientific and Technical Information of China (English)

    LAN Fei; SHI Yang

    2009-01-01

    Histone methylation is believed to play important roles In epigenetic memory in various biological processes. However, questions like whether the methylation marks themselves are faithfully transmit-ted into daughter cells and through what mechanisms are currently under active investigation. Previ-ously, methylation was considered to be irreversible, but the recent discovery of histone lysine de-methylases revealed a dynamic nature of histone methylation regulation on four of the main sites of methylation on histone H3 and H4 tails (H3K4, H3K9, H3K27 and H3K36). Even so, it is stlll unclear whether demethylases specific for the remaining two sites, H3K79 and H4K20, exist. Furthermore, be-sides hlstone proteins, the lysine methylation and demethylation also occur on non-histone proteins,which are probably subjected to similar regulation as histones. This review discusses recent pro-gresses In protein lysine methylation regulation focusing on the above topics, while referring readers to a number of recent reviews for the biochemistry and biology of these enzymes.

  8. Evaluation of the biological activity of sunflower hull extracts

    Directory of Open Access Journals (Sweden)

    Taha, F. S.

    2012-06-01

    Full Text Available This work was planned with the aim of adding value to sunflower seed hulls, a waste product of the oil industry by preparing a sunflower hull phenolic extract rich in chlorogenic acid (CGA. In order to fulfill this goal, the optimization for the extraction of a phenolic extract from the hulls was investigated. The parameters studied were: type of solvent, solvent to water ratio and hull to solvent ratio. In addition, the solvent mixtures were also studied. The resulting phenolic extracts were evaluated for their biological activities. This included phenolic content determination, evaluation of the antioxidant and antimicrobial activities. Chlorogenic acid was determined in two chosen hull extracts using the UV spectrophotometric method and HPLC analysis. The anticarcinogenic activity of the two chosen extracts was tested on seven different cell line carcinomas. The results revealed that all the phenolic extracts of sunflower hull studied contain between 190-312.5 mg phenolics/ 100 g hulls. The highest phenolic extraction was achieved with 80% methanol (1:30, hull to solvent, w/v ratio and methanol to ethanol to water (7:7:6 v/v/v mixture with values of 312.5 and 306.5 mg phenolics/100 g hulls, respectively. The free radical scavenging activity and antioxidant activity of all the samples ranged from 33.6-72.6%. The highest antioxidant activity and free radical scavenging activity were achieved by the same extracts that possessed the highest phenolic content, namely methanol to ethanol to water extract and 80% methanol with values 71.8 and 72.6%, 68.2 and 70.9% respectively, compared to 77.9 and 76.9% respectively for TBHQ. All the phenolic extracts possessed antimicrobial activity but to different levels against different pathogenic bacteria. The two chosen extracts also possessed anticarcinogenic activity, which differed among varying cell line carcinomas. The HPLC analysis indicated that chlorogenic acid was the main phenolic acid in the

  9. Systems Biology Graphical Notation: Activity Flow language Level 1 Version 1.2.

    Science.gov (United States)

    Mi, Huaiyu; Schreiber, Falk; Moodie, Stuart; Czauderna, Tobias; Demir, Emek; Haw, Robin; Luna, Augustin; Le Novère, Nicolas; Sorokin, Anatoly; Villéger, Alice

    2015-09-04

    The Systems Biological Graphical Notation (SBGN) is an international community effort for standardized graphical representations of biological pathways and networks. The goal of SBGN is to provide unambiguous pathway and network maps for readers with different scientific backgrounds as well as to support efficient and accurate exchange of biological knowledge between different research communities, industry, and other players in systems biology. Three SBGN languages, Process Description (PD), Entity Relationship (ER) and Activity Flow (AF), allow for the representation of different aspects of biological and biochemical systems at different levels of detail. The SBGN Activity Flow language represents the influences of activities among various entities within a network. Unlike SBGN PD and ER that focus on the entities and their relationships with others, SBGN AF puts the emphasis on the functions (or activities) performed by the entities, and their effects to the functions of the same or other entities. The nodes (elements) describe the biological activities of the entities, such as protein kinase activity, binding activity or receptor activity, which can be easily mapped to Gene Ontology molecular function terms. The edges (connections) provide descriptions of relationships (or influences) between the activities, e.g., positive influence and negative influence. Among all three languages of SBGN, AF is the closest to signaling pathways in biological literature and textbooks, but its well-defined semantics offer a superior precision in expressing biological knowledge.

  10. H3 lysine 4 is acetylated at active gene promoters and is regulated by H3 lysine 4 methylation.

    Directory of Open Access Journals (Sweden)

    Benoit Guillemette

    2011-03-01

    Full Text Available Methylation of histone H3 lysine 4 (H3K4me is an evolutionarily conserved modification whose role in the regulation of gene expression has been extensively studied. In contrast, the function of H3K4 acetylation (H3K4ac has received little attention because of a lack of tools to separate its function from that of H3K4me. Here we show that, in addition to being methylated, H3K4 is also acetylated in budding yeast. Genetic studies reveal that the histone acetyltransferases (HATs Gcn5 and Rtt109 contribute to H3K4 acetylation in vivo. Whilst removal of H3K4ac from euchromatin mainly requires the histone deacetylase (HDAC Hst1, Sir2 is needed for H3K4 deacetylation in heterochomatin. Using genome-wide chromatin immunoprecipitation (ChIP, we show that H3K4ac is enriched at promoters of actively transcribed genes and located just upstream of H3K4 tri-methylation (H3K4me3, a pattern that has been conserved in human cells. We find that the Set1-containing complex (COMPASS, which promotes H3K4me2 and -me3, also serves to limit the abundance of H3K4ac at gene promoters. In addition, we identify a group of genes that have high levels of H3K4ac in their promoters and are inadequately expressed in H3-K4R, but not in set1Δ mutant strains, suggesting that H3K4ac plays a positive role in transcription. Our results reveal a novel regulatory feature of promoter-proximal chromatin, involving mutually exclusive histone modifications of the same histone residue (H3K4ac and H3K4me.

  11. Synthesis of TiO2 nano-particles and their photocatalytic activity for formaldehyde and methyl orange degradation

    Institute of Scientific and Technical Information of China (English)

    XIAO Xinyan; LIAO Dongliang; ZHANG Huiping; CHEN Huanqin

    2007-01-01

    TiO2 nano-particles were synthesized by sol-gel technique and characterized by X-ray diffractometer (XRD)and transmission electron microscope (TEM).Their photocatalytic activities for formaldehyde (FA) and methyl orange (MO) degradation were tested using degradation rate (η) as an evaluation index.Based on the orthogonal test results,the optimal condition for TiO2 preparation was obtained.Results showed that particle sizes were in the range of 10-40 nm,and that prepared TiO2 had better photocatalytic activity than P25.A simplified model was developed to evaluate the apparent quantum efficiency (Φapp) of this photocatalytic reaction system.

  12. [DNA methylation and epigenetics].

    Science.gov (United States)

    Vaniushin, B F

    2006-09-01

    In eukaryotic cells, nuclear DNA is subject to enzymatic methylation with the formation of 5-methylcytosine residues, mostly within the CG and CNG sequences. In plants and animals this DNA methylation is species-, tissue-, and organelle-specific. It changes (decreases) with age and is regulated by hormones. On the other hand, genome methylation can control hormonal signal. Replicative and post-replicative DNA methylation types are distinguished. They are mediated by multiple DNA methyltransferases with different site-specificity. Replication is accompanied by the appearance of hemimethylated DNA sites. Pronounced asymmetry of the DNA strand methylation disappears to the end of the cell cycle. A model of methylation-regulated DNA replication is proposed. DNA methylation controls all genetic processes in the cell (replication, transcription, DNA repair, recombination, and gene transposition). It is the mechanism of cell differentiation, gene discrimination and silencing. In animals, suppression of DNA methylation stops development (embryogenesis), switches on apoptosis, and is usually lethal. Disruption of DNA methylation pattern results in the malignant cell transformation and serves as one of the early diagnostic features of carcinogenesis. In malignant cell the pattern of DNA methylation, as well as the set of DNA methyltransferase activities, differs from that in normal cell. In plants inhibition of DNA methylation is accompanied by the induction of seed storage and florescence genes. In eukaryotes one and the same gene can be simultaneously methylated both at cytosine and adenine residues. It can be thus suggested, that the plant cell contains at least two different, and probably, interdependent systems of DNA methylation. The first eukaryotic adenine DNA methyltransferase was isolated from plants. This enzyme methylates DNA with the formation of N6-methyladenine residues in the sequence TGATCA (TGATCA-->TGm6ATCA). Plants possess AdoMet-dependent endonucleases

  13. Body size, physical activity and risk of colorectal cancer with or without the CpG island methylator phenotype (CIMP.

    Directory of Open Access Journals (Sweden)

    Laura A E Hughes

    Full Text Available BACKGROUND: We investigated how body size and physical activity influence the risk of the CpG island methylator phenotype (CIMP in colorectal cancer (CRC. METHODS: In the Netherlands Cohort Study (n = 120,852, risk factors were self-reported at baseline in 1986. After 7.3 years of follow-up, 603 cases and 4,631 sub-cohort members were available. CIMP status according to the Weisenberger markers was determined using methylation specific PCR on DNA from paraffin embedded tumor tissue. Hazard rate ratios (HR and 95% confidence intervals for CIMP (27.7% and non-CIMP (72.3% tumors were calculated according to BMI, BMI at age 20, BMI change, trouser/skirt size, height, and physical activity. RESULTS: BMI modeled per 5 kg/m(2 increase was associated with both CIMP and non-CIMP tumors, however, HRs were attenuated when additionally adjusted for trouser/skirt size. Trouser/skirt size, per 2 size increase, was associated with both tumor subtypes, even after adjustment for BMI (CIMP HR: 1.20, 95%CI: 1.01-1.43; non-CIMP HR: 1.14, 95%CI: 1.04-1.28. Height per 5 cm was associated with both tumor sub-types, but HRs were attenuated when adjusted for body weight. BMI at age 20 was positively associated with increased risk of CIMP tumors and the association was significantly less pronounced for non-CIMP tumors (P-heterogeneity = 0.01. Physical activity was inversely associated with both subtypes, but a dose-response association was observed only for non-CIMP tumors (P-trend = 0.02. CONCLUSIONS: Body size, especially central adiposity, may increase the risk of both CIMP and non-CIMP tumors. Body fat at young age may differentially influence risk. Physical activity appears to decrease the risk of CRC regardless of these molecular subtypes.

  14. Bioactivity of marine organisms. Part 3. Screening of marine algae of Indian coast for biological activity

    Digital Repository Service at National Institute of Oceanography (India)

    Kamat, S.Y.; Wahidullah, S.; Naik, C.G.; DeSouza, L.; Jayasree, V.; Ambiye, V.; Bhakuni, D.S.; Goel, A.K.; Garg, H.S.; Srimal, R.C.

    Ethanolic extracts from Indian marine algae have been tested for anti-viral, anti-bacterial, anti-fungal, anti-fertility, hypoglycaemic and a wide range of pharmacological activities. Of 34 species investigated 17 appeared biologically active. Six...

  15. Biological Activity of Peanut (Arachis hypogaea) Phytoalexins and Selected Natural and Synthetic Stilbenoids

    Science.gov (United States)

    2011-02-11

    for their effects on economically important plant pathogenic fungi of the genera Colletotrichum, Botrytis, Fusarium, and Phomopsis. We further...hypogaea, peanuts, groundnuts, stilbenoids, resveratrol, phytoalexins, biological activity, antifungal, antitumor, anticancer , cytotoxic, antioxidant...prenylated flavonoids have been identified as constituents in plants, and display biological activities, such as anticancer , antiandrogen, anti-Leishmania, and

  16. Design, Synthesis and Biological Activities of Novel Benzoyl Hydrazines Containing Pyrazole

    Institute of Scientific and Technical Information of China (English)

    闫涛; 于淑晶; 刘鹏飞; 刘卓; 王宝雷; 熊丽霞; 李正名

    2012-01-01

    In search of environmentally benign compounds with high biological activity, low toxicity and low resistance, 8 novel benzoyl hydrazines containing pyrazole were designed and synthesized. All compounds were characterized by I H NMR spectra and HRMS. The preliminary results of biological activity assessment indicated that most of title compounds exhibited certain insecticidal activities against M),thimna separata Walker at 200 mg L-1 but excellent fungicidal activities against six fungus at 50 mg L-1, which were better than the control.

  17. Design, synthesis and hypoglycemic activity of 3-methyl-1-phe nyl-4-{ 4-[ ( 5-m et hyl-2-phenyloxazol-4-yl) methoxy ] benzylene (benzyl) }-2-pyrazol-5-one

    Institute of Scientific and Technical Information of China (English)

    Xing LIU; Yalou WANG; Guanzhong WU; Jiangchuan LI; Xiaoyan WU

    2008-01-01

    Based on the SAR (structure activity relation-ship) of TZDs (thiazolidinediones), 3-methyl-1-phenyl-2-pyrazoline-5-one was selected as a substitute for TZD. Compounds of 3-methyl- 1-phenyl-4- {4-[(5-methyl-2-phe-nyloxazol-4-yl)methoxy]benzylene(benzyl) }-2-pyrazol-5-one were designed and synthesized to find some more hypoglycemic active agents and further investigate the SAR of this class of compounds. Butanedione monoxime reacted with (substituted) benzaldehyde via cyclization and chlorination to give 4-(chloromethyl)-5-methyl-2-phenyloxazole derivatives, which condensed with 4-hydroxybenzaldehyde or vanillin, and was followed by the Knoevenagel reaction with 3-methyl-1-phenyl-2-pyrazol-5-one to give compounds Ⅰa-Ⅰh. Compounds Ⅰa-Ⅰh were hydrogenated with Pd-C to giveⅡa-Ⅱh, and their hypoglycemic activity was evaluated with a glucose oxidase kit and insulin load test on normal mice. Sixteen new target compounds were synthesized. All the com-pounds were characterized by 1H NMR, IR, MS and elemental analysis. The preliminary pharmacological tests show that the compounds have good hypoglycemic activity and can enhance the action of insulin, especially Ib, Id and If.

  18. Using Active Learning to Teach Concepts and Methods in Quantitative Biology.

    Science.gov (United States)

    Waldrop, Lindsay D; Adolph, Stephen C; Diniz Behn, Cecilia G; Braley, Emily; Drew, Joshua A; Full, Robert J; Gross, Louis J; Jungck, John A; Kohler, Brynja; Prairie, Jennifer C; Shtylla, Blerta; Miller, Laura A

    2015-11-01

    This article provides a summary of the ideas discussed at the 2015 Annual Meeting of the Society for Integrative and Comparative Biology society-wide symposium on Leading Students and Faculty to Quantitative Biology through Active Learning. It also includes a brief review of the recent advancements in incorporating active learning approaches into quantitative biology classrooms. We begin with an overview of recent literature that shows that active learning can improve students' outcomes in Science, Technology, Engineering and Math Education disciplines. We then discuss how this approach can be particularly useful when teaching topics in quantitative biology. Next, we describe some of the recent initiatives to develop hands-on activities in quantitative biology at both the graduate and the undergraduate levels. Throughout the article we provide resources for educators who wish to integrate active learning and technology into their classrooms.

  19. First principles and DFT supported investigations on vibrational spectra and electronic structure of 2-((phenylamino)methyl)isoindoline-1,3-dione - An antioxidant active Mannich base

    Science.gov (United States)

    Boobalan, Maria susai; Amaladasan, M.; Ramalingam, S.; Tamilvendan, D.; Venkatesa Prabhu, G.; Bououdina, M.

    2015-02-01

    The 2-((phenylamino)methyl)isoindoline-1,3-dione (PID) is a synthesized Mannich base which has significant antioxidant activity and biological importance. Quantum mechanical calculations on energy, geometry and vibrational wavenumber of PID were computed using ab initio HF and density functional theory (DFT/B3LYP) methods with 6-31+G/6-311++G(d,p) basis sets. Optimized geometrical parameters obtained by HF and DFT calculations were indicatively agreement with experimental crystal geometry. The experimental FT-Raman and FT-IR spectra of PID has been recorded and analyzed by comparing with simulated spectra. The 1H and 13C NMR spectra of title molecule records the chemical shift resulted from shielding and deshielding effects. Natural bond orbital (NBO) analysis has been carried out to calculate various intramolecular interactions that are accountable for the stabilization of this Mannich base. The predicted HOMO-LUMO gap offers interesting information on intramolecular charge transfer and reactivity of the molecular system. Molecular electrostatic potential (MEP) imprint visualize the reactive sites in PID, which is also supported by Mulliken, ESP, Hirshfeld and NBO charges. Thermodynamic properties of PID at various temperatures have been calculated at B3LYP/6-311++G(d,p) in gas phase and the correlations between standard entropies (S), internal energy (E or U) and standard heat capacity (C) with different temperatures.

  20. Evaluation of airborne methyl salicylate for improved conservation biological control of two-spotted spider mite and hop aphid in Oregon hop yards.

    Science.gov (United States)

    Woods, J L; James, D G; Lee, J C; Gent, D H

    2011-12-01

    The use of synthetic herbivore-induced plant volatiles (HIPV) to attract natural enemies has received interest as a tool to enhance conservation biological control (CBC). Methyl salicylate (MeSA) is a HIPV that is attractive to several key predators of two-spotted spider mite, Tetranychus urticae Koch (Acari: Tetranychidae), and hop aphid, Phorodon humuli (Schrank) (Homoptera: Aphididae). A 2-year study was conducted to evaluate the recommended commercial use of MeSA in hop yards in Oregon. Slow-release MeSA dispensers were stapled to supporting poles in 0.5 ha plots and these plots were compared to a paired non-treated plot on each of three farms in 2008 and 2009. Across both years, there was a trend for reduced (range 40-91%) mean seasonal numbers of T. urticae in five of the six MeSA-baited plots. Stethorus spp., key spider mite predators, tended to be more numerous in MeSA-baited plots compared to control plots on a given farm. Mean seasonal densities of hop aphid and other natural enemies (e.g., Orius spp. and Anystis spp.) were similar between MeSA-treated and control plots. Variability among farms in suppression of two-spotted spider mites and attraction of Stethorus spp. suggests that the use of MeSA to enhance CBC of spider mites in commercial hop yards may be influenced by site-specific factors related to the agroecology of individual farms or seasonal effects that require further investigation. The current study also suggests that CBC of hop aphid with MeSA in this environment may be unsatisfactory.

  1. ACTIVE AND PARTICIPATORY METHODS IN BIOLOGY: PROBLEM-SOLVING

    Directory of Open Access Journals (Sweden)

    Adela NEMEŞ

    2010-01-01

    Full Text Available We face with considerable challenge of developing students’ problem solving skills in our difficult environment. Good problem solving skills empower managers in their professional and personal lives. Problem solving skills are valued by academics and employers. The informations in Biology are often presented in abstract forms without contextualisation. Creative problem-solving process involves a few steps, which together provide a structured procedure for identifying challenges, generating ideas and implementing innovative solutions: identifying the problem, searching for possible solutions, selecting the most optimal solution and implementing a possible solution. Each aspect of personality has a different orientation to problem solving, different criteria for judging the effectiveness of the process and different associated strengths. Using real-world data in sample problems will also help facilitate the transfer process, since students can more easily identify with the context of a given situation. The paper describes the use of the Problem-Solving in Biology and the method of its administration. It also presents the results of a study undertaken to evaluate the value in teaching Biology. Problem-solving is seen as an essential skill that is developed in biology education.

  2. ICBP90, a novel methyl K9 H3 binding protein linking protein ubiquitination with heterochromatin formation.

    Science.gov (United States)

    Karagianni, Panagiota; Amazit, Larbi; Qin, Jun; Wong, Jiemin

    2008-01-01

    Methylation of histone H3 on lysine 9 is critical for diverse biological processes including transcriptional repression, heterochromatin formation, and X inactivation. The biological effects of histone methylation are thought to be mediated by effector proteins that recognize and bind to specific patterns of methylation. Using an unbiased in vitro biochemical approach, we have identified ICBP90, a transcription and cell cycle regulator, as a novel methyl K9 H3-specific binding protein. ICBP90 and its murine homologue Np95 are enriched in pericentric heterochromatin of interphase nuclei, and this localization is dependent on H3K9 methylation. Specific binding of ICBP90 to methyl K9 H3 depends on two functional domains, a PHD (plant homeodomain) finger that defines the binding specificity and an SRA (SET- and RING-associated) domain that promotes binding activity. Furthermore, we present evidence that ICBP90 is required for proper heterochromatin formation in mammalian cells.

  3. Phlorotannins from Ecklonia cava (Phaeophyceae): biological activities and potential health benefits.

    Science.gov (United States)

    Wijesekara, Isuru; Yoon, Na Young; Kim, Se-Kwon

    2010-01-01

    The importance of bioactive derivatives as functional ingredients has been well recognized due to their valuable health beneficial effects. Therefore, isolation and characterization of novel functional ingredients with biological activities from seaweeds have gained much attention. Ecklonia cava Kjellman is an edible seaweed, which has been recognized as a rich source of bioactive derivatives mainly, phlorotannins. These phlorotannins exhibit various beneficial biological activities such as antioxidant, anticancer, antidiabetic, anti-human immunodeficiency virus, antihypertensive, matrix metalloproteinase enzyme inhibition, hyaluronidase enzyme inhibition, radioprotective, and antiallergic activities. This review focuses on biological activities of phlorotannins with potential health beneficial applications in functional foods, pharmaceuticals, and cosmeceuticals.

  4. On the mechanism of biological methane formation: structural evidence for conformational changes in methyl-coenzyme M reductase upon substrate binding.

    Science.gov (United States)

    Grabarse, W; Mahlert, F; Duin, E C; Goubeaud, M; Shima, S; Thauer, R K; Lamzin, V; Ermler, U

    2001-05-25

    Methyl-coenzyme M reductase (MCR) catalyzes the final reaction of the energy conserving pathway of methanogenic archaea in which methylcoenzyme M and coenzyme B are converted to methane and the heterodisulfide CoM-S-S-CoB. It operates under strictly anaerobic conditions and contains the nickel porphinoid F430 which is present in the nickel (I) oxidation state in the active enzyme. The known crystal structures of the inactive nickel (II) enzyme in complex with coenzyme M and coenzyme B (MCR-ox1-silent) and in complex with the heterodisulfide CoM-S-S-CoB (MCR-silent) were now refined at 1.16 A and 1.8 A resolution, respectively. The atomic resolution structure of MCR-ox1-silent describes the exact geometry of the cofactor F430, of the active site residues and of the modified amino acid residues. Moreover, the observation of 18 Mg2+ and 9 Na+ ions at the protein surface of the 300 kDa enzyme specifies typical constituents of binding sites for either ion. The MCR-silent and MCR-ox1-silent structures differed in the occupancy of bound water molecules near the active site indicating that a water chain is involved in the replenishment of the active site with water molecules. The structure of the novel enzyme state MCR-red1-silent at 1.8 A resolution revealed an active site only partially occupied by coenzyme M and coenzyme B. Increased flexibility and distinct alternate conformations were observed near the active site and the substrate channel. The electron density of the MCR-red1-silent state aerobically co-crystallized with coenzyme M displayed a fully occupied coenzyme M-binding site with no alternate conformations. Therefore, the structure was very similar to the MCR-ox1-silent state. As a consequence, the binding of coenzyme M induced specific conformational changes that postulate a molecular mechanism by which the enzyme ensures that methylcoenzyme M enters the substrate channel prior to coenzyme B as required by the active-site geometry. The three different

  5. Metabolite Profile Resulting from the Activation/Inactivation of 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine and 2-Methyltetrahydro-β-carboline by Oxidative Enzymes

    Directory of Open Access Journals (Sweden)

    Tomás Herraiz

    2013-01-01

    Full Text Available Metabolic enzymes are involved in the activation/deactivation of the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyiridine (MPTP neurotoxin and its naturally occurring analogs 2-methyltetrahydro-β-carbolines. The metabolic profile and biotransformation of these protoxins by three enzymes, monoamine oxidase (MAO, cytochrome P450, and heme peroxidases (myeloperoxidase and lactoperoxidase, were investigated and compared. The metabolite profile differed among the enzymes investigated. MAO and heme peroxidases activated these substances to toxic pyridinium and β-carbolinium species. MAO catalyzed the oxidation of MPTP to 1-methyl-4-phenyl-2,3-dihydropyridinium cation (MPDP+, whereas heme peroxidases catalyzed the oxidation of MPDP+ to 1-methyl-4-phenylpyridinium (MPP+ and of 2-methyltetrahydro-β-carboline to 2-methyl-3,4-dihydro-β-carbolinium cation (2-Me-3,4-DHβC+. These substances were inactivated by cytochrome P450 2D6 through N-demethylation and aromatic hydroxylation (MPTP and aromatic hydroxylation (2-methyltetrahydro-β-carboline. In conclusion, the toxicological effects of these protoxins might result from a balance between the rate of their activation to toxic products (i.e., N-methylpyridinium-MPP+ and MPDP+- and N-methyl-β-carbolinium—βC+— by MAO and heme peroxidases and the rate of inactivation (i.e., N-demethylation, aromatic hydroxylation by cytochrome P450 2D6.

  6. Physicochemical and porosity characteristics of thermally regenerated activated carbon polluted with biological activated carbon process.

    Science.gov (United States)

    Dong, Lihua; Liu, Wenjun; Jiang, Renfu; Wang, Zhansheng

    2014-11-01

    The characteristics of thermally regenerated activated carbon (AC) polluted with biological activated carbon (BAC) process were investigated. The results showed that the true micropore and sub-micropore volume, pH value, bulk density, and hardness of regenerated AC decreased compared to the virgin AC, but the total pore volume increased. XPS analysis displayed that the ash contents of Al, Si, and Ca in the regenerated AC respectively increased by 3.83%, 2.62% and 1.8%. FTIR spectrum showed that the surface functional groups of virgin and regenerated AC did not change significantly. Pore size distributions indicated that the AC regeneration process resulted in the decrease of micropore and macropore (D>10 μm) volume and the increase of mesopore and macropore (0.1 μmbiological waste (spent AC) from BAC process.

  7. Mango ginger (Curcuma amada Roxb.) – A promising spice for phytochemicals and biological activities

    Indian Academy of Sciences (India)

    R S Policegoudra; S M Aradhya; L Singh

    2011-09-01

    Mango ginger (Curcuma amada Roxb.) is a unique spice having morphological resemblance with ginger but imparts a raw mango flavour. The main use of mango ginger rhizome is in the manufacture of pickles and culinary preparations. Ayurveda and Unani medicinal systems have given much importance to mango ginger as an appetizer, alexteric, antipyretic, aphrodisiac, diuretic, emollient, expectorant and laxative and to cure biliousness, itching, skin diseases, bronchitis, asthma, hiccough and inflammation due to injuries. The biological activities of mango ginger include antioxidant activity, antibacterial activity, antifungal activity, anti-inflammatory activity, platelet aggregation inhibitory activity, cytotoxicity, antiallergic activity, hypotriglyceridemic activity, brine-shrimp lethal activity, enterokinase inhibitory activity, CNS depressant and analgesic activity. The major chemical components include starch, phenolic acids, volatile oils, curcuminoids and terpenoids like difurocumenonol, amadannulen and amadaldehyde. This article brings to light the major active components present in C. amada along with their biological activities that may be important from the pharmacological point of view.

  8. Computation of Accurate Activation Barriers for Methyl-Transfer Reactions of Sulfonium and Ammonium Salts in Aqueous Solution.

    Science.gov (United States)

    Gunaydin, Hakan; Acevedo, Orlando; Jorgensen, William L; Houk, K N

    2007-05-01

    The energetics of methyl-transfer reactions from dimethylammonium, tetramethylammonium, and trimethylsulfonium to dimethylamine were computed with density functional theory, MP2, CBS-QB3, and quantum mechanics/molecular mechanics (QM/MM) Monte Carlo methods. At the CBS-QB3 level, the gas-phase activation enthalpies are computed to be 9.9, 15.3, and 7.9 kcal/mol, respectively. MP2/6-31+G(d,p) activation enthalpies are in best agreement with the CBS-QB3 results. The effects of aqueous solvation on these reactions were studied with polarizable continuum model, generalized Born/surface area (GB/SA), and QM/MM Monte Carlo simulations utilizing free-energy perturbation theory in which the PDDG/PM3 semiempirical Hamiltonian for the QM and explicit TIP4P water molecules in the MM region were used. In the aqueous phase, all of these reactions proceed more slowly when compared to the gas phase, since the charged reactants are stabilized more than the transition structure geometries with delocalized positive charges. In order to obtain the aqueous-phase activation free energies, the gas-phase activation free energies were corrected with the solvation free energies obtained from single-point conductor-like polarizable continuum model and GB/SA calculations for the stationary points along the reaction coordinate.

  9. Multiple signaling pathways involved in stimulation of osteoblast differentiation by N-methyl-D-aspartate receptors activation in vitro

    Institute of Scientific and Technical Information of China (English)

    Jie-li LI; Lin ZHAO; Bin CUI; Lian-fu DENG; Guang NING; Jian-min LIU

    2011-01-01

    Aim: Glutamate receptors are expressed in osteoblastic cells. The present study was undertaken to investigate the mechanisms underlying the stimulation of osteoblast differentiation by N-methyl-D-aspartate (NMDA) receptor activation in vitro.Methods: Primary culture of osteoblasts was prepared from SD rats. Microarray was used to detect the changes of gene expression.The effect of NMDA receptor agonist or antagonist on individual gene was examined using RT-PCR. The activity of alkaloid phosphotase (ALP) was assessed using a commercial ALP staining kit.Results: Microarray analyses revealed that 10 genes were up-regulated by NMDA (0.5 mmol/L) and down-regulated by MK801 (100μmol/L), while 13 genes down-regulated by NMDA (0.5 mmol/L) and up-regulated by MK801 (100 μmol/L). Pretreatment of osteoblasts with the specific PKC inhibitor Calphostin C (0.05 μmol/L), the PKA inhibitor H-89 (20 nmol/L), or the PI3K inhibitor wortmannin (100 nmol/L) blocked the ALP activity increase caused by NMDA (0.5 mmol/L). Furthermore, NMDA (0.5 mmol/L) rapidly increased PI3K phosphorylation, which could be blocked by pretreatment of wortmannin (100 nmol/L).Conclusion: The results suggest that activation of NMDA receptors stimulates osteoblasts differentiation through PKA, PKC, and PI3K signaling pathways, which is a new role for glutamate in regulating bone remodeling.

  10. Relationship between changes of N-methyl-D-aspartate receptor activity and brain edema after brain injury in rats

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Objective: To investigate the relationship between the changes of N-methyl-D-aspartate (NMDA) receptor activity and brain edema after injury in rats.   Methods: The brain injury models were made by using a free-falling body. The treatment model was induced by means of injecting AP5 into lateral ventricle before brain injury; water contents in brain cortex were measured with dry-wet method; and NMDA receptor activity was detected with a radio ligand binding assay.   Results: The water contents began to increase at 30 minutes and reached the peak at 6 hours after brain injury. The maximal binding (Bmax) of NMDA receptor increased significantly at 15 minutes and reached the peak at 30 minutes, then decreased gradually and had the lowest value 6 hours after brain injury. Followed the treatment with AP5, NMDA receptor activity in the injured brain showed a normal value; and the water contents were lower than that of AP5-free injury group 24 hours after brain injury.   Conclusions: It suggests that excessive activation of NMDA receptor may be one of the most important factors to induce the secondary cerebral impairments, and AP5 may protect the brain from edema after brain injury.

  11. Synthesis of new α aminophosphonate system bearing Indazole moiety and their biological activity.

    Science.gov (United States)

    Ali, Nasir ali Shafakat; Zakir, Shaikh; Patel, Muqtadir; Farooqui, Mazahar

    2012-04-01

    We are reporting herein for the first time the synthesis of α-aminophosphonates containing Indazole moiety in two steps. In the first step, imines of substituted N-benzylidene-1-methyl-1H-indazole-3-carbohydrazide are synthesized and in the next step it has converted to α-aminophosphonates using chlorotrimethylsilane (TMSCl) and triethyl phosphite. Some of the synthesized derivatives are evaluated for antibacterial activity against different bacterial strains.

  12. Arylesterase activity is associated with antioxidant intake and paraoxonase-1 (PON1) gene methylation in metabolic syndrome patients following an energy restricted diet.

    Science.gov (United States)

    de la Iglesia, Rocio; Mansego, Maria L; Sánchez-Muniz, Francisco J; Zulet, M Angeles; Martinez, J Alfredo

    2014-01-01

    The arylesterase (ARE) activity linked to the paraoxonase-1 (PON1) gene is known to protect lipoproteins from oxidation and provide defense against metabolic syndrome (MetS) and cardiovascular diseases. The epigenetic regulation of enzymatic activities is gaining importance nowadays. This research aimed to assess the potential relationships between the ARE activity with the methylation levels of the PON1 gene transcriptional regulatory region, anthropometrics, biochemical markers and antioxidant dietary components. Forty-seven subjects (47 ± 10 y.o; BMI 36.2 ± 3.8 kg/m(2); 46.8 % female) with MetS features, who followed a six-month energy-restricted dietary weight-loss intervention, were included in this study (www.clinicaltrials.gov; NCT01087086). Anthropometric, biochemical, enzymatic and dietary data were assessed using validated procedures. PON1 transcriptional regulatory region methylation was analyzed by a microarray technical approach. Volunteers reduced ARE activity in parallel with body weight (p = 0.005), BMI (p = 0.006), total fat mass (p = 0.020), diastolic blood pressure (p = 0.018), mean blood pressure (p = 0.022) and triglycerides (p = 0.014). Methylation levels of some CpG sites of the PON1 gene correlated negatively with ARE activity (p < 0.05). Interestingly, dietary vitamin C (p = 0.001), tocopherols (p = 0.009) and lycopene (p = 0.038) were positively associated with ARE activity and showed an inverse correlation (p = 0.004, p = 0.029 and p = 0.021, respectively) with the methylation of some selected CpG sites of the PON1 gene. In conclusion, ARE activity decreased in parallel with MetS-related markers associated to the energy restriction, while dietary antioxidants might enhance the ARE activity by lowering the PON1 gene methylation in patients with MetS features.

  13. N-acetyltransferase-dependent activation of 2-hydroxyamino-1-methyl-6-phenylimidazo[4,5-b]pyridine: formation of 2-amino-1-methyl-6-(5-hydroxy)phenylimidazo [4,5-b]pyridine, a possible biomarker for the reactive dose of 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine

    DEFF Research Database (Denmark)

    Frandsen, Henrik Lauritz; Alexander, J.

    2000-01-01

    2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) is a mutagenic and carcinogenic heterocyclic amine formed during ordinary cooking. PhIP is metabolically activated to the ultimate mutagenic metabolite by CYP P450-mediated N-hydroxylation followed by phase II esterification, Incubation of N...

  14. Biological Opinion Compliance Report and Permit Activity Report

    Science.gov (United States)

    1999-03-01

    T.W. Custer. 1986. Hatching Success of Caspian Terns Nesting on the Lower Laguna Madre , Texas , USA. Colonial Birds. 9(1). Pp 86-89. Persons working with...U.S. Fish and Wildlife Service on November 14,’ 1 990. Initial District implementation of that Biological Opinion began in 1 992, following the...known as the "Red Book." The Red Book was reviewed by the U.S. Fish and Wildlife Service and approved for implementation by the Missouri River Division

  15. Evaluation of in vivo biological activity profile of isoorientin.

    Science.gov (United States)

    Küpeli, Esra; Aslan, Mustafa; Gürbüz, Ilhan; Yesilada, Erdem

    2004-01-01

    Anti-nociceptive, anti-inflammatory and gastroprotective activities of the known C-glycosyl flavonoid, isoorientin, were studied in rats and mice. For the anti-nociceptive activity assessment the p-benzoquinone-induced writing test, for the anti-inflammatory activity the carrageenan-induced hind paw edema model in mice, and for the gastroprotective activity the EtOH-induced ulcerogenesis model in rats were used. Isoorientin was shown to possess significant anti-nociceptive and anti-inflammatory activities at 15 mg/kg and 30 mg/kg doses, without inducing any apparent acute toxicity as well as gastric damage. However, the compound did not possess any significant gastroprotective activity against EtOH-induced ulcerogenesis.

  16. Synthesis and biological activity of benzamide DNA minor groove binders.

    Science.gov (United States)

    Khan, Gul Shahzada; Pilkington, Lisa I; Barker, David

    2016-02-01

    A range of di- and triaryl benzamides were synthesised to investigate the effect of the presence and nature of a polar sidechain, bonding and substitution patterns and functionalisation of benzylic substituents. These compounds were tested for their antiproliferative activity as well as their DNA binding activity. The most active compounds in all assays were unsymmetrical triaryl benzamides with a bulky or alkylating benzylic substituent and a polar amino sidechain.

  17. Biological activity of fucoidan from leafy bladderwort (Utricularia aurea Lour.)

    OpenAIRE

    Chotigeat, W.; Phongdara, A.; Choosawad, D.

    2005-01-01

    Fucoidan extracted from aquatic plant Utricularia aurea was 1.3% of dry weight and comprised glucuronic acid 62.5% and fucose 4.98% of the crude extract and 28.74% of the fucose was sulfate. The fucoidan was investigated for antibacterial activity. The minimal inhibitory concentration (MIC) of crude fucoidan against Vibrio harveyi and Escherichia coli was 20 and 10 mg/ml. Moreover, the fucoidan had anticoagulant activity. The crude fucoidan had activated partial thromboplastin time (APTT) at ...

  18. Studies on Synthesis and Biological Activities of Novel Triazole Compounds Containing 1,3-Dioxolane

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Nine title compounds were synthesized. Their strucures were identified by means of IR, EA, 1H NMR and MS. The results from the primary biological test show that all the compounds have some activitiies of fungicide and plant growth regulator. When R group is 2,4-Cl2C6H3, compound 2 or compound 4 shows better biological activities.

  19. Synthesis and antiulcer activity of 2-[5-substituted-1--benzo(d) imidazol-2-yl sulfinyl]methyl-3-substituted quinazoline-4-(3) ones

    Indian Academy of Sciences (India)

    Avinash Patil; Swastika Ganguly; Sanjay Surana

    2010-05-01

    2-[5-substituted-1--benzo(d)imidazol-2-yl sulfinyl]methyl-3-substituted quinazoline-4-(3)-one derivatives were synthesized and tested for antiulcer activity against pylorus ligation-induced, aspirin induced and ethanol induced ulcer in rat model. All the synthesized compounds were characterized by using IR, MS and 1H NMR spectral and elemental analysis. The compounds were scramed for their antiulcer activity: compounds 5k and 5n showed higher activity than omeprazole used as standard.

  20. Preparation, characterization of Y3+-doped TiO2 nanoparticles and their photocatalytic activities for methyl orange degradation

    Institute of Scientific and Technical Information of China (English)

    NIU Xinshu; LI Sujuan; CHU Huihui; ZHOU Jianguo

    2011-01-01

    A series of pure and Y3+-doped TiO2 nanoparticles with high photocatalytic activities were prepared by a sol-gel method using tetra-n-butyl titanate as precursor. The as-prepared catalysts were characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM) and diffuse reflectance spectroscopy (DRS). The results indicated that yttrium doping could effectively reduce the crystalline size, inhibit the anatase-to-tutile phase transformation and surppress the recombination of the photogenerated electron-hole pairs. The DRS results showed that the optical absorption edge shifted to red direction owing to yttrium ion doping. The photocatalytic activities of samples were evaluated by the photodegradation of methyl orange (MO) aqueous solution under 300 W high pressure mercury lamp irradiation. Photodegradation results revealed that Y3+ doping could greatly improve the photocatalytic activity of TiO2. In this experiment, the optimal dosage was 1 .5 mol.% when samples were calcined at 773 K for 2 h, which caused a MO photodegradation rate of 99.8% under UV irradiation for 70 min.

  1. Growth inhibitory, apoptotic and anti-inflammatory activities displayed by a novel modified triterpenoid, cyano enone of methyl boswellates

    Indian Academy of Sciences (India)

    Palaniyandi Ravanan; Sanjay K Singh; G S R Subba Rao; Paturu Kondaiah

    2011-06-01

    Triterpenoids are pentacyclic secondary metabolites present in many terrestrial plants. Natural triterpenoids have been reported to exhibit anti-inflammatory and anti-carcinogenic activities. Here, we show that modifications of ring A of boswellic acid (2 cyano, 3 enone) resulted in a highly active growth inhibitory, anti-inflammatory, prodifferentiative and anti-tumour triterpenoid compound called cyano enone of methyl boswellates (CEMB). This compound showed cytotoxic activity on a number of cancer cell lines with IC50 ranging from 0.2 to 0.6 M. CEMB inhibits DNA synthesis and induces apoptosis in A549 cell line at 0.25 M and 1 M concentrations, respectively. CEMB induces adipogenic differentiation in 3T3-L1 cells at a concentration of 0.1 M. Finally, administration of CEMB intra-tumourally significantly inhibited the growth of C6 glioma tumour xenograft in immuno-compromised mice. Collectively, these results suggest that CEMB is a very potent anti-tumour compound.

  2. Pretreatment of Parsley (Petroselinum crispum L.) Suspension Cultures with Methyl Jasmonate Enhances Elicitation of Activated Oxygen Species.

    Science.gov (United States)

    Kauss, H.; Jeblick, W.; Ziegler, J.; Krabler, W.

    1994-05-01

    Suspension-cultured cells of parsley (Petroselinum crispum L.) were used to demonstrate an influence of jasmonic acid methyl ester (JAME) on the elicitation of activated oxygen species. Preincubation of the cell cultures for 1 d with JAME greatly enhanced the subsequent induction by an elicitor preparation from cell walls of Phytophtora megasperma f. sp. glycinea (Pmg elicitor) and by the polycation chitosan. Shorter preincubation times with JAME were less efficient, and the effect was saturated at about 5 [mu]M JAME. Treatment of the crude Pmg elicitor with trypsin abolished induction of activated oxygen species, an effect similar to that seen with elicitation of coumarin secretion. These results suggest that JAME conditioned the parsley suspension cells in a time-dependent manner to become more responsive to elicitation, reminiscent of developmental effects caused by JAME in whole plants. It is interesting that pretreatment of the parsley cultures with 2,6-dichloroisonicotinic and 5-chlorosalicylic acid only slightly enhanced the elicitation of activated oxygen species, whereas these substances greatly enhanced the elicitation of coumarin secretion. Therefore, these presumed inducers of systemic acquired resistance exhibit a specificity different from JAME.

  3. Regulation of Active DNA Demethylation by a Methyl-CpG-Binding Domain Protein in Arabidopsis thaliana.

    Directory of Open Access Journals (Sweden)

    Qi Li

    2015-05-01

    Full Text Available Active DNA demethylation plays crucial roles in the regulation of gene expression in both plants and animals. In Arabidopsis thaliana, active DNA demethylation is initiated by the ROS1 subfamily of 5-methylcytosine-specific DNA glycosylases via a base excision repair mechanism. Recently, IDM1 and IDM2 were shown to be required for the recruitment of ROS1 to some of its target loci. However, the mechanism(s by which IDM1 is targeted to specific genomic loci remains to be determined. Affinity purification of IDM1- and IDM2- associating proteins demonstrated that IDM1 and IDM2 copurify together with two novel components, methyl-CpG-binding domain protein 7 (MBD7 and IDM2-like protein 1 (IDL1. IDL1 encodes an α-crystallin domain protein that shows high sequence similarity with IDM2. MBD7 interacts with IDM2 and IDL1 in vitro and in vivo and they form a protein complex associating with IDM1 in vivo. MBD7 directly binds to the target loci and is required for the H3K18 and H3K23 acetylation in planta. MBD7 dysfunction causes DNA hypermethylation and silencing of reporter genes and a subset of endogenous genes. Our results suggest that a histone acetyltransferase complex functions in active DNA demethylation and in suppression of gene silencing at some loci in Arabidopsis.

  4. Electronic transport in methylated fragments of DNA

    Energy Technology Data Exchange (ETDEWEB)

    Almeida, M. L. de; Oliveira, J. I. N.; Lima Neto, J. X.; Gomes, C. E. M.; Fulco, U. L., E-mail: umbertofulco@gmail.com; Albuquerque, E. L. [Departamento de Biofísica e Farmacologia, Universidade Federal do Rio Grande do Norte, 59072-970 Natal-RN (Brazil); Freire, V. N. [Departamento de Física, Universidade Federal do Ceará, 60455-760 Fortaleza, CE (Brazil); Caetano, E. W. S. [Instituto Federal de Educação, Ciência e Tecnologia do Ceará, 60040-531 Fortaleza, CE (Brazil); Moura, F. A. B. F. de; Lyra, M. L. [Instituto de Física, Universidade Federal de Alagoas, 57072-900 Maceió-AL (Brazil)

    2015-11-16

    We investigate the electronic transport properties of methylated deoxyribonucleic-acid (DNA) strands, a biological system in which methyl groups are added to DNA (a major epigenetic modification in gene expression), sandwiched between two metallic platinum electrodes. Our theoretical simulations apply an effective Hamiltonian based on a tight-binding model to obtain current-voltage curves related to the non-methylated/methylated DNA strands. The results suggest potential applications in the development of novel biosensors for molecular diagnostics.

  5. BIOLOGICAL VALUE OF PUNY FRUITS RELATED TO THEIR ANTIRADICAL ACTIVITY

    Directory of Open Access Journals (Sweden)

    M. BALOGHOVÁ

    2013-12-01

    Full Text Available All analysed species of puny fruits (red currant (Ribes rubrum L variant Jonkheervan Tets, white currant (Ribes vulgare L. variant Blanka, black currant (Ribesnigrum L. variant Eva, blueberry (Vaccinium myrtilis variant Berkeley, elderberry(Sambucus nigra L. variant Sambo, hawthorn (Crataegus oxyacantha, mulberry(Morus nigra L. genotypes M152 and M047 are natural sources of anthocyanpigments and vitamin C with a high antiradical activity. Due to the fact that thehighest antiradical activity is not accompanied by the highest content of anthocyansand vitamin C in puny fruits, we suppose that the antiradical activity of plantmaterials is also connected with the presence of other compounds with antioxidantand antiradical activity. From our results follows that all studied puny fruits with ahigh antiradical activity increase the antioxidant value of human nutrition and alsoits prophylactic and medicinal effect.

  6. Phytochemical prospection and biological activity of Duroia macrophylla (Rubiaceae

    Directory of Open Access Journals (Sweden)

    Daiane Martins

    2014-12-01

    Full Text Available Context: Duroia macrophylla (Rubiaceae is endemic from the Amazon Rainforest. Aims: To perform phytochemical profile of Duroia macrophylla extracts and to evaluate them as antioxidant, insecticidal and cytotoxic. Methods: Dichloromethane and methanol extracts of leaves and branches (collected three times were subjected to phytochemical screening by comparative thin layer chromatography and NMR analyses. The extracts were assayed to antioxidant (DPPH and Fe-phenanthroline, at 10 μg/mL, insecticidal on Sitophilus zeamais (by ingestion of stored grains and contact, both at 10 mg/mL and toxic activities on Artemia salina (1000 μg/mL. Results: There were found evidences of terpenes, phenolic substances (phenols and flavonoids and alkaloids, with differences between the vegetal part, collection period and solvent used. Antioxidant evaluations showed three of twelve were active and two were considered moderately active, with a relationship dependently of concentration. All methanol extracts showed the presence of phenolic substances (phenols and flavonoids but one showed only phenols. For insecticidal activity, there were three most active extracts, two of which showed only presence of terpenes and the other, besides terpenes, phenolic substances (phenols and flavonoids. For Artemia salina toxicity assay, the five most active were all from the 2nd and 3rd collections. Conclusions: The active extracts of D. macrophylla in each test were different. Three methanol extracts showed antioxidant activity; three extracts showed insecticidal activity and the presence of terpenic substances and five extracts presented cytotoxic activity, but it was not possible to correlate it with any specific secondary metabolite.

  7. Tests of biological activity of metabolites from Penicillium expansum (Link Thom various isolates

    Directory of Open Access Journals (Sweden)

    Halina Borecka

    2013-12-01

    Full Text Available Aqrobacterium tumefaciens and cucumber, mustard and linseeds were compared as test organisms for evaluation of the biological activity of patulin. It was found that the reaction of cucumber seeds and linseed to the patulin concentrations was more pronounced than that of mustard and Aqrobacterium tumefaciens. The activity of metabolites produced by Penicillium expansum was investigated with the use of cucumber seeds. As measure of activity served the percentage of radicule growth inhibition was compared with the growth in control seeds. The biological activity of the metabolites was specific for the isolates, those from apples being more active. Thirty two isolates from pears and 34 from apples were examined.

  8. Activated carbons from end-products of tree nut and tree fruit production as sorbents for removing methyl bromide in ventilation effluent from postharvest chamber fumigation

    Science.gov (United States)

    End-products of tree nuts and tree fruits grown in California, USA were evaluated for the ability to remove methyl bromide from the ventilation effluent of postharvest chamber fumigations. Activated carbon sorbents from walnut and almond shells as well as peach and prune pits were prepared using dif...

  9. Antioxidant activity of gallic acid and methyl gallate in triacylglycerols of Kilka fish oil and its oil-in-water emulsion.

    Science.gov (United States)

    Asnaashari, Maryam; Farhoosh, Reza; Sharif, Ali

    2014-09-15

    The anti-DPPH radical effect as well as anti-peroxide activity of gallic acid, methyl gallate, and α-tocopherol in a bulk Kilka fish oil and its oil-in-water emulsion stabilized by soy protein isolate at 55°C were investigated. Gallic acid with the lowest hydrophobicity (log P=-0.28) was found to be the most active antiradical agent (IC50=29.5 μM), followed by methyl gallate (IC50=38.0 μM, log P=-0.23) and α-tocopherol (IC50=105.3 μM, log P=0.70). The anti-peroxide activity in the bulk oil system decreased in the order of methyl gallate>gallic acid>α-tocopherol. In the emulsion system, methyl gallate still behaved better than gallic acid, but the highest activity belonged to α-tocopherol. Based on the calculation of a number of kinetic parameters, the antioxidants, in general, showed better performances in the bulk oil system than in the emulsion system.

  10. Antimycobacterial Activities of Novel 5-(1H-1,2,3-TriazolylMethyl Oxazolidinones

    Directory of Open Access Journals (Sweden)

    Oludotun Adebayo Phillips

    2012-01-01

    Full Text Available The antibacterial activities of a series of triazolyl oxazolidinones against Mycobacterium tuberculosis strain in vitro and in vivo in a mice model are presented. Most active compounds were noncytotoxic against VERO cells with acceptable selectivity indexes (SI as measures of compound tolerability. Structure activity relationships (SARs revealed that analogs with alkylcarbonyl (IC90: < 0.2 to 0.422 μg/mL and arylcarbonyl (IC90: < 0.2 to 2.103 μg/mL groups at the piperazine 4N-position-displayed potent antimycobacterium activities, comparable to the methanesulfonyl (IC90: < 0.2 μg/mL analog, linezolid (IC90: < 0.2 μg/mL, and isoniazid (IC90: < 0.034 μg/mL. The furanylcarbonyl derivative also displayed potent activity, while the arylsulfonyl analogs were inactive. Of the triazolyl oxazolidinones, the morpholino (PH-27 derivative with medium bioavailability in plasma was most active in vivo, but relatively less efficacious than isoniazid.

  11. Synthesis and Antiplatelet Activity of Antithrombotic Thiourea Compounds: Biological and Structure-Activity Relationship Studies

    Directory of Open Access Journals (Sweden)

    André Luiz Lourenço

    2015-04-01

    Full Text Available The incidence of hematological disorders has increased steadily in Western countries despite the advances in drug development. The high expression of the multi-resistance protein 4 in patients with transitory aspirin resistance, points to the importance of finding new molecules, including those that are not affected by these proteins. In this work, we describe the synthesis and biological evaluation of a series of N,N'-disubstituted thioureas derivatives using in vitro and in silico approaches. New designed compounds inhibit the arachidonic acid pathway in human platelets. The most active thioureas (compounds 3d, 3i, 3m and 3p displayed IC50 values ranging from 29 to 84 µM with direct influence over in vitro PGE2 and TXA2 formation. In silico evaluation of these compounds suggests that direct blockage of the tyrosyl-radical at the COX-1 active site is achieved by strong hydrophobic contacts as well as electrostatic interactions. A low toxicity profile of this series was observed through hemolytic, genotoxic and mutagenic assays. The most active thioureas were able to reduce both PGE2 and TXB2 production in human platelets, suggesting a direct inhibition of COX-1. These results reinforce their promising profile as lead antiplatelet agents for further in vivo experimental investigations.

  12. Capturing Biological Activity in Natural Product Fragments by Chemical Synthesis.

    Science.gov (United States)

    Crane, Erika A; Gademann, Karl

    2016-03-14

    Natural products have had an immense influence on science and have directly led to the introduction of many drugs. Organic chemistry, and its unique ability to tailor natural products through synthesis, provides an extraordinary approach to unlock the full potential of natural products. In this Review, an approach based on natural product derived fragments is presented that can successfully address some of the current challenges in drug discovery. These fragments often display significantly reduced molecular weights, reduced structural complexity, a reduced number of synthetic steps, while retaining or even improving key biological parameters such as potency or selectivity. Examples from various stages of the drug development process up to the clinic are presented. In addition, this process can be leveraged by recent developments such as genome mining, antibody-drug conjugates, and computational approaches. All these concepts have the potential to identify the next generation of drug candidates inspired by natural products.

  13. Chemical Constituents of Descurainia sophia L. and its Biological Activity

    Directory of Open Access Journals (Sweden)

    Nawal H. Mohamed

    2009-01-01

    Full Text Available Seven coumarin compounds were isolated for the first time from the aerial parts of DescurainiaSophia L. identified as scopoletine, scopoline, isoscopoline, xanthtoxol, xanthtoxin, psoralene and bergaptane.Three flavonoids namely kaempferol, quercetine and isorhamnetine and three terpenoid compounds -sitosterol-amyrine and cholesterol were also isolated and identified by physical and chemical methods; melting point, Rfvalues, UV and 1H NMR spectroscopy. Qualitative and quantitative analyses of free and protein amino acidsusing amino acid analyzer were performed. The plant contains 15 amino acids as free and protein amino acidswith different range of concentrations. Fatty acid analysis using GLC, revealed the presence of 10 fatty acids,the highest percentage was palmitic acid (27.45 % and the lowest was lauric acid (0.13%. Biological screeningof alcoholic extract showed that the plant is highly safe and has analgesic, antipyretic and anti-inflammatoryeffects.

  14. Chemical Constituents and Biological Activities of Artemisia herba-alba

    Directory of Open Access Journals (Sweden)

    Abou El-Hamd H. Mohamed

    2010-01-01

    Full Text Available Artemisia, one of the larger genera in the family Asteraceae and the largest genus in the tribe Anthemideae, comprises from 200 to more than 500 taxa at the specific or subspecific level. Many Artemisia species have a high economic value in several fields, as food plants and as antihelminthic and antimalaria in medicine. Artemisia herba-alba was known for its therapeutic and medicinal properties, it was used in both traditional and modern medicine. Several papers have been published on the chemical composition of specimens of A. herba-alba. The aim of this work is to review all available scientific literature published on A. herba-alba. The focus will be on the chemical constitutions which have been identified from this species, in addition to all of the reported biological activites of this species have been included as well as the pharmacology and toxicology

  15. Isolation, biological activity, synthesis, and medicinal chemistry of the pederin/mycalamide family of natural products.

    Science.gov (United States)

    Mosey, R Adam; Floreancig, Paul E

    2012-09-01

    This review highlights the broad range of science that has arisen from the isolation of pederin, the mycalamides, theopederins, and onnamides, and psymberin. Specific topics include structure determination, biological activity, synthesis, and analog preparation and analysis.

  16. Environmental Contaminants Monitoring in Selected Wetlands of Wyoming: Biologically Active Elements Study

    Data.gov (United States)

    US Fish and Wildlife Service, Department of the Interior — Sediment, water and biota were collected from selected wetlands in Wyoming for the Biologically Active Elements (BAE) Study in 1988, 1989 and 1990 to identify...

  17. Bioactive Components and Functional Properties of Biologically Activated Cereal Grains: A Bibliographic Review.

    Science.gov (United States)

    Singh, Arashdeep; Sharma, Savita

    2015-10-14

    Whole grains provide energy, nutrients, fibres and bioactive compounds that may synergistically contribute to their protective effects. A wide range of these compounds is affected by germination. While some compounds, such as β-glucans are degraded, others, like antioxidants and total phenolics are increased by means of biological activation of grains. The water and oil absorption capacity as well as emulsion and foaming capacity of biologically activated grains are also improved. Application of biological activation of grains is of emerging interest, which may significantly enhance the nutritional, functional and bioactive content of grains, as well as improve palatability of grain foods in a natural way. Therefore, biological activation of cereals can be a way to produce food grains enriched with health promoting compounds and enhanced functional attributes.

  18. Therapeutic Uses and Pharmacological Properties of Garlic, Shallot, and Their Biologically Active Compounds

    Directory of Open Access Journals (Sweden)

    Peyman Mikaili

    2013-10-01

    Garlic and shallots are safe and rich sources of biologically active compounds with low toxicity. Further studies are needed to confirm the safety and quality of the plants to be used by clinicians as therapeutic agents.

  19. Biological activity of fucoidan from leafy bladderwort (Utricularia aurea Lour.

    Directory of Open Access Journals (Sweden)

    Chotigeat, W.

    2005-12-01

    Full Text Available Fucoidan extracted from aquatic plant Utricularia aurea was 1.3% of dry weight and comprised glucuronic acid 62.5% and fucose 4.98% of the crude extract and 28.74% of the fucose was sulfate. The fucoidan was investigated for antibacterial activity. The minimal inhibitory concentration (MIC of crude fucoidan against Vibrio harveyi and Escherichia coli was 20 and 10 mg/ml. Moreover, the fucoidan had anticoagulant activity. The crude fucoidan had activated partial thromboplastin time (APTT at 4.47 IU/mg.

  20. Developmentally programmed 3' CpG island methylation confers tissue- and cell-type-specific transcriptional activation

    Science.gov (United States)

    During development, a small but significant number of CpG islands (CGIs) becomes methylated. The timing of developmentally programmed CGI methylation and associated mechanisms of transcriptional regulation during cellular differentiation, however, remain poorly characterized. Here we used genome-wid...

  1. Chemical constituents from Cornus officinalis and their biological activity 1

    Directory of Open Access Journals (Sweden)

    Zhan-Ying Ma

    2012-01-01

    Full Text Available Objective: To study the chemical constituents from Cornus officinalis Sieb., Et Zucc, and their peroxisome proliferator-activated receptors (PPARs agonist activity. Materials and Methods: The leaves of C. officinalis were extracted three times with 90% EtOH at room temperature. The ethanol extracts were combined and concentrated under reduced pressure to yield residue, which was isolated and purified by silica gel and reverse-phase C 18 column chromatography. The structures were elucidated on the basis of spectroscopic evidence and their physiochemical characteristics. Cell-based luciferase reporter gene assays were used to evaluate PPARα/γ agonistic activities. Results: Five compounds were isolated and elucidated as 10-hydroxyhastatoside (1, β-dihydrocornin (2, isoquercitrin (3, loganin (4 and oleanolic acid (5. Conclusion: Compounds 1 and 2 were obtained from C. officinalis for the first time. Compound 3 exhibited moderate agonistic activities for PPARα, with EC 50 values of 29.5 μM.

  2. Synthesis and biological activity of novel tiliroside derivants.

    Science.gov (United States)

    Qin, Nan; Li, Chun-Bao; Jin, Mei-Na; Shi, Li-Huan; Duan, Hong-Quan; Niu, Wen-Yan

    2011-10-01

    A series of new tiliroside derivatives were synthesized and characterized by analytical (1)H NMR, (13)C NMR and mass spectrometry. All of the compounds were evaluated for anti-diabetic properties in vitro using HepG2 cells. Compounds 3c, 3d, and 3i-l caused significant enhancements in glucose consumption by insulin-resistant HepG2 cells compared with control cells and cells that were exposed to metformin (an anti-diabetic drug). Moreover, compound 3l significantly activated adenosine 5'-monophosphate-activated protein kinase activity and reduced acetyl-CoA carboxylase activity. Thus, the tiliroside derivative 3l offers potential to be developed as a new approach for treating type II diabetes.

  3. CHARACTERIZATION ADN BIOLOGICAL ACTIVITY OF SECONDARY METABOLITES FROM ARMILLARIA TABESCENS

    Science.gov (United States)

    Ethyl acetate extracts from liquid cultures of Armillaria tabescens showed good antimicrobial activity against Candida albicans, Cryptococcus neoformans, Escherichia coli and Mycobacterium intracellulare. Chemical analyses of extract constituents led to the isolation and identification of two new co...

  4. Baltic cyanobacteria- A source of biologically active compounds

    Digital Repository Service at National Institute of Oceanography (India)

    Mazur-Marzec, H.; Błaszczyk, A; Felczykowska, A; Hohlfeld, N; Kobos, J.; Toruńska-Sitarz, A; PrabhaDevi; Montalva`o, S.; DeSouza, L.; Tammela, P.; Mikosik, A; Bloch, S.; Nejman-Faleńczyk, B.; Węgrzyn, G.

    and chemotypes were tested in a wide variety of assays. The cyanobacteria showed strain-specific differences in the induced effects. The extracts from Nodularia spumigena CCNP1401 were active in the highest number of tests, including protease and phosphatase...

  5. SYNTHESIS AND BIOLOGICAL ACTIVITY OF AMIDE DERIVATIVES OF GINKGOLIDE A

    Institute of Scientific and Technical Information of China (English)

    LI-HONG HU; ZHONG-LIANG CHEN; YU-YUAN XIE

    2001-01-01

    Amide derivatives of ginkgolide A were prepared and evaluated for their in vitro ability to inhibit the PAF-induced aggregation of rabbit platelets. They showed less activities than their parent compound ginkgolide A.

  6. Synthesis and Biological Activities of Camphor Hydrazone and Imine Derivatives

    Science.gov (United States)

    da Silva, Emerson T.; da Silva Araújo, Adriele; Moraes, Adriana M.; de Souza, Leidiane A.; Silva Lourenço, Maria Cristina; de Souza, Marcus V. N.; Wardell, James L.; Wardell, Solange M. S. V.

    2015-01-01

    Both sonochemical and classical methodologies have been employed to convert camphor, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-one, C9H16C=O, into a number of derivatives including hydrazones, C9H16C=N-NHAr 3, imines, C9H16C=N-R 7, and the key intermediate nitroimine, C9H16C=N-NO2 6. Reactions of nitroamine 6 with nucleophiles by classical methods provided the desired compounds in a range of yields. In evaluations of activity against Mycobacterium tuberculosis, compound 7j exhibited the best activity (minimal inhibitory concentration (MIC) = 3.12 µg/mL), comparable to that of the antitubercular drug ethambutol. The other derivatives displayed modest antimycobacterial activities at 25–50 µg/mL. In in vitro tests against cancer cell lines, none of the synthesized camphor compounds exhibited cytotoxic activities.

  7. Synthesis and biological activity of nifuroxazide and analogs. II.

    Science.gov (United States)

    Tavares, L C; Chisté, J J; Santos, M G; Penna, T C

    1999-09-01

    Nifuroxazyde and six analogs were synthesized by varying the substitute from the para-position of the benzenic ring and the heteroatom of the heterocyclic ring. The MIC of seven resultant compounds was determined by serial dilutions, testing the ATCC 25923 strain of Staphylococcus aureus. A significant increase in the anti-microbial activity of thyophenic analogs, as compared with furanic and pyrrholic analogs, was observed. In addition, unlike the cyano and hydroxyl groups, the acetyl group promoted anti-microbial activity.

  8. Chromatography methods in investigation of lipophilicity of the biological active substances

    OpenAIRE

    Odović Jadranka V.; Trbojević-Stanković Jasna B.

    2009-01-01

    This paper presents the review of the methods used in research of the biological active substances hydrophobicity, a very important property. The biological activity of some substances depends on their pharmacokinetics and pharmacodynamics. These processes depend on the molecule's capability to interact with two different media: aqueous (cells interior) and non-aqueous (cells membrane), or on the molecule lipophilicity. Today, great attention is given to investigation and systematic determina...

  9. Terpenes from the soft corals of the genus Sarcophyton: chemistry and biological activities.

    Science.gov (United States)

    Liang, Lin-Fu; Guo, Yue-Wei

    2013-12-01

    This review covers structural diversity and biological activities of terpenes from soft corals of the genus of Sarcophyton, reported from 1995 to July, 2011. During this period, besides undefined species, 16 species of the genus Sarcophyton, from different geographical areas, had been chemically examined. Two hundred and five terpenes had been isolated from this genus, including eleven sesquiterpenes, 165 diterpenes, 29 biscembranoids, some of which had novel skeletons. They exhibited various biological features, such as antifeedant, anti-inflammatory, antiviral, and antifouling activities.

  10. Intracellular and membrane-damaging activities of methyl gallate isolated from Terminalia chebula against multidrug-resistant Shigella spp.

    Science.gov (United States)

    Acharyya, Saurabh; Sarkar, Prodipta; Saha, Dhira R; Patra, Amarendra; Ramamurthy, T; Bag, Prasanta K

    2015-08-01

    Shigella spp. (Shigella dysenteriae, Shigella flexneri, Shigella boydii and Shigella sonnei) cause bacillary dysentery (shigellosis), which is characterized by bloody mucous diarrhoea. Although a variety of antibiotics have been effective for treatment of shigellosis, options are becoming limited due to globally emerging drug resistance. In the present study, in vitro antibacterial activity of methyl gallate (MG) isolated from Terminalia chebula was determined by performing MIC, minimal bactericidal concentration (MBC) and time-kill kinetic studies. Bacterial membrane-damaging activity of MG was determined by membrane perturbation and transmission electron microscopy (TEM). Cellular drug accumulation, cell infection and assessment of intracellular activities of MG and reference antibiotics were performed using HeLa cell cultures. The bactericidal activity of MG against multidrug-resistant (MDR) Shigella spp. in comparison with other commonly used drugs including fluoroquinolone was demonstrated here. TEM findings in the present study revealed that MG caused the total disintegration of inner and outer membranes, and leakage of the cytoplasmic contents of S. dysenteriae. The level of accumulation of MG and tetracycline in HeLa cells incubated for 24  h was relatively higher than that of ciprofloxacin and nalidixic acid (ratio of intracellular concentration/extracellular concentration of antibiotic for MG and tetracycline>ciprofloxacin and nalidixic acid). The viable number of intracellular S. dysenteriae was decreased in a time-dependent manner in the presence of MG (4 × MBC) and reduced to zero within 20  h. The significant intracellular activities of MG suggested that it could potentially be used as an effective antibacterial agent for the treatment of severe infections caused by MDR Shigella spp.

  11. Using Active Learning in a Studio Classroom to Teach Molecular Biology

    Science.gov (United States)

    Nogaj, Luiza A.

    2013-01-01

    This article describes the conversion of a lecture-based molecular biology course into an active learning environment in a studio classroom. Specific assignments and activities are provided as examples. The goal of these activities is to involve students in collaborative learning, teach them how to participate in the learning process, and give…

  12. Research and Teaching: Instructor Use of Group Active Learning in an Introductory Biology Sequence

    Science.gov (United States)

    Auerbach, Anna Jo; Schussler, Elisabeth E.

    2016-01-01

    Active learning (or learner-centered) pedagogies have been shown to enhance student learning in introductory biology courses. Student collaboration has also been shown to enhance student learning and may be a critical part of effective active learning practices. This study focused on documenting the use of individual active learning and group…

  13. Biological Activities of Aerial Parts Extracts of Euphorbia characias

    Directory of Open Access Journals (Sweden)

    Maria Barbara Pisano

    2016-01-01

    Full Text Available The aim of the present study was to evaluate antioxidant, antimicrobial, anti-HIV, and cholinesterase inhibitory activities of aqueous and alcoholic extracts from leaves, stems, and flowers of Euphorbia characias. The extracts showed a high antioxidant activity and were a good source of total polyphenols and flavonoids. Ethanolic extracts from leaves and flowers displayed the highest inhibitory activity against acetylcholinesterase and butyrylcholinesterase, showing potential properties against Alzheimer’s disease. Antimicrobial assay showed that leaves and flowers extracts were active against all Gram-positive bacteria tested. The ethanolic leaves extract appeared to have the strongest antibacterial activity against Bacillus cereus with MIC value of 312.5 μg/mL followed by Listeria monocytogenes and Staphylococcus aureus that also exhibited good sensitivity with MIC values of 1250 μg/mL. Moreover, all the extracts possessed anti-HIV activity. The ethanolic flower extract was the most potent inhibitor of HIV-1 RT DNA polymerase RNA-dependent and Ribonuclease H with IC50 values of 0.26 and 0.33 μg/mL, respectively. The LC-DAD metabolic profile showed that ethanolic leaves extract contains high levels of quercetin derivatives. This study suggests that Euphorbia characias extracts represent a good source of natural bioactive compounds which could be useful for pharmaceutical application as well as in food system for the prevention of the growth of food-borne bacteria and to extend the shelf-life of processed foods.

  14. Preparation of TiO2 Nanoparticle Loaded MCM-41 and Study of Its Photo-Catalytic Activity Towards Decolorization of Methyl Orange.

    Science.gov (United States)

    Naik, Bhanudas; Hazra, Subhenjit; Dayananda, Desagani; Prasad, V S; Ghosh, Narendra Nath

    2015-09-01

    Here we report the synthesis of TiO2 nanoparticle loaded mesoporous MCM-41 photocatalysts for degradation of methyl orange dye in aqueous medium under sunlight exposure. TiO2 loaded MCM-41 was synthesized by impregnation method. Anatase form of TiO2 nanoparticles were formed in the porous matrix of the silicate MCM-41. The synthesized materials were characterized using powder X-ray diffraction method, surface area and porosimetry analysis; diffuse reflectance analysis, particle size analysis and transmission electron microscopy. The photocatalytic property of the synthesized materials were investigated towards the degradation of methyl orange under sunlight exposure and monitored by UV-visible spectrophotometer. Synthesized catalysts showed high photocatalytic activity for the degradation of methyl orange.

  15. Synthesis Characterization and Antimicrobial Activity of Metal Chelates of 1, 7-Di (2-hydroxyphenyl 1, 7 di (N-methyl aza-1, 3, 5 heptarine-3-ol hydrochloride

    Directory of Open Access Journals (Sweden)

    Nalin P. Patani

    2010-01-01

    Full Text Available The Schiff base complexes derived from 2-furancarboxaldehyde and N-methyl-2-amino phenol have been prepared and characterized using several physical techniques, like elemental analysis, thermogravimetric analysis, magnetic moment measurements, infrared and resonance spectra. N-Methyl-2-amino phenol was condensed stoichiometrically with 2-furancarboxaldehyde in presence of methanol. The resulting 1,7-di(2-hydroxyphenyl 1,7 di(N-methyl aza-1,3,5 heptarine-3-ol hydrochloride was characterized by elemental analysis and spectral studies. The transition metal complexes of Cu2+, Zn2+, Ni2+, Co2+ and Mn2+ of the synthesized complexes were prepared. Metal ligand (M:L ratio, IR, reflectance spectral studies, magnetic properties and antimicrobial activity of the synthesized complexes and its metal complexes were carried out.

  16. Metal Complexation Studies of 1-(4-Carboxy-3-hydroxy-N-methyl phenyl- amino methyl 2-methyl perimidine

    Directory of Open Access Journals (Sweden)

    Umang N. Patel

    2009-01-01

    Full Text Available Aminomethylation of 2-methyl perimidine was carried out by treating 2-methyl perimidine with formaldehyde and 4-aminosalicylic acid. The resultant compound was designed as 1-(4-caroxy-3-hydroxy-N-methyl phenylamino methyl2-methyl perimidine. The transition metal complexes of Cu2+, Co2+, Ni2+, Mn2+ and Zn2+ have been prepared and characterized by elemental analysis, spectral studies, magnetic moment determination, molar conductivity measurement and antimicrobial activity.

  17. Biologic therapy improves psoriasis by decreasing the activity of monocytes and neutrophils.

    Science.gov (United States)

    Yamanaka, Keiichi; Umezawa, Yoshinori; Yamagiwa, Akisa; Saeki, Hidehisa; Kondo, Makoto; Gabazza, Esteban C; Nakagawa, Hidemi; Mizutani, Hitoshi

    2014-08-01

    Therapy with monoclonal antibodies to tumor necrosis factor (TNF)-α and the interleukin (IL)-12/23 p40 subunit has significantly improved the clinical outcome of patients with psoriasis. These antibodies inhibit the effects of the target cytokines and thus the major concern during their use is the induction of excessive immunosuppression. Recent studies evaluating the long-term efficacy and safety of biologic therapy in psoriasis have shown no significant appearance of serious adverse effects including infections and malignancies. However, the immunological consequence and the mechanism by which the blockade of a single cytokine by biologics can successfully control the activity of psoriasis remain unclear. In the current study, we investigated the effect of biologic therapy on cytokine production of various lymphocytes and on the activity of monocytes and neutrophils in psoriatic patients. Neutrophils, monocytes and T cells were purified from heparinized peripheral venous blood by Ficoll density gradient centrifugation, and γ-interferon, TNF-α and IL-17 production from lymphocytes was measured by flow cytometer. The activation maker of neutrophils and the activated subsets of monocytes were also analyzed. Biologic therapy induced no significant changes in the cytokine production by lymphocytes from the skin and gut-homing T cells. However, neutrophil activity and the ratio of activated monocyte population increased in severely psoriatic patients were normalized in psoriatic patients receiving biologic therapy. The present study showed that biologic therapy ameliorates clinical symptoms and controls the immune response in patients with psoriasis.

  18. Size-Dependent Photodynamic Activity of Gold Nanoparticles Conjugate of Water Soluble Purpurin-18-N-Methyl-D-Glucamine

    Directory of Open Access Journals (Sweden)

    Byambajav Lkhagvadulam

    2013-01-01

    Full Text Available Gold nanoparticles (GNPs conjugates of water soluble ionic photosensitizer (PS, purpurin-18-N-methyl-D-glucamine (Pu-18-NMGA, were synthesized using various molar ratios between HAuCl4 and Pu-18-NMGA without adding any particular reducing agents and surfactants. The PS-GNPs conjugates showed long wavelength absorption of range 702–762 nm, and their different shapes and diameters depend on the molar ratios used in the synthesis. In vitro anticancer efficacy of the PS-GNPs conjugates was investigated by MTT assay against A549 cells, resulting in higher photodynamic activity than that of the free Pu-18-NMGA. Among the PS-GNPs conjugates, the GNPs conjugate from the molar ratio of 1 : 2 (Au(III: Pu-18-NMGA exhibits the highest photodynamic activity corresponding to bigger size (~60 nm of the GNPs conjugate which could efficiently transport the PS into the cells than that of smaller size of the GNPs conjugate.

  19. Long-term imipramine treatment increases N-methyl-d-aspartate receptor activity and expression via epigenetic mechanisms.

    Science.gov (United States)

    Nghia, Nguyen An; Hirasawa, Takae; Kasai, Hirotake; Obata, Chie; Moriishi, Kohji; Mochizuki, Kazuki; Koizumi, Schuichi; Kubota, Takeo

    2015-04-05

    Imipramine, a major antidepressant, is known to inhibit reuptake of serotonin and norepinephrine, which contributes to recovery from major depressive disorder. It has recently been reported that acute imipramine treatment inhibits N-methyl-d-aspartate (NMDA) receptor activity. However, the mechanisms underlying long-term effects of imipramine have not been identified. We tested these distinct effects in mouse cortical neurons and found that acute (30s) imipramine treatment decreased Ca(2+) influx through NMDA receptors, whereas long-term treatment (48h) increased Ca(2+) influx via the same receptors. Furthermore, long-term treatment increased NMDA receptor 2B (NR2B) subunit expression via epigenetic changes, including increased acetylation of histones H3K9 and H3K27 in the NR2B promoter and decreased activity of histone deacetylase 3 (HDAC3) and HDAC4. These results suggest that the long-term effects of imipramine on NMDA receptors are quite different from its acute effects. Furthermore, increased NR2B expression via epigenetic alterations might be a part of the mechanism responsible for this long-term effect.

  20. Current parallel chemistry principles and practice: application to the discovery of biologically active molecules.

    Science.gov (United States)

    Edwards, Paul J

    2009-11-01

    This article describes the use of parallel chemistry techniques for drug discovery, based on publications from January 2006 to December 2008. Chemical libraries that yielded active compounds across a range of biological targets are presented, together with synthetic details when appropriate. Background information for the biological targets involved and any SAR that could be discerned within members of a library series also is discussed. New technological developments, as applied to library design and synthesis and, more generally, in the discovery of biologically active entities, are highlighted. In addition, the likely future directions for parallel chemistry in its ability to impact upon drug discovery are also presented.

  1. Smart interactive electronic system for monitoring the electromagnetic activities of biological systems

    Science.gov (United States)

    Popa, Sorin G.; Shahinpoor, Mohsen

    2001-08-01

    A novel electronic device capable of sensing and monitoring the myoelectric, polarization wave and electromagnetic activities of the biological systems and in particular the human body is presented. It is known that all the physical and chemical processes within biological systems are associated with polarization, depolarization waves from the brain, neural signals and myoelectric processes that manifest themselves in ionic and dipole motion. The technology developed in our laboratory is based on certain charge motion sensitive electronics. The electronic system developed is capable of sensing the electromagnetic activities of biological systems. The information obtained is then processed by specialized software in order to interpret it from physical and chemical point of view.

  2. The chemistry and biological activity of heterocycle-fused quinolinone derivatives: A review.

    Science.gov (United States)

    Shiro, Tomoya; Fukaya, Takayuki; Tobe, Masanori

    2015-06-05

    Among all heterocycles, the heterocycle-fused quinolinone scaffold is one of the privileged structures in drug discovery as heterocycle-fused quinolinone derivatives exhibit various biological activities allowing them to act as anti-inflammatory, anticancer, antidiabetic, and antipsychotic agents. This wide spectrum of biological activity has attracted a great deal of attention in the field of medicinal chemistry. In this review, we provide a comprehensive description of the biological and pharmacological properties of various heterocycle-fused quinolinone scaffolds and discuss the synthetic methods of some of their derivatives.

  3. Spectroscopic study of molecular structure, antioxidant activity and biological effects of metal hydroxyflavonol complexes

    Science.gov (United States)

    Samsonowicz, Mariola; Regulska, Ewa

    2017-02-01

    Flavonols with varied hydroxyl substitution can act as strong antioxidants. Thanks to their ability to chelate metals as well as to donate hydrogen atoms they have capacity to scavenge free radicals. Their metal complexes are often more active in comparison with free ligands. They exhibit interesting biological properties, e.g. anticancer, antiphlogistic and antibacterial. The relationship between molecular structure and their biological properties was intensively studied using spectroscopic methods (UV-Vis, IR, Raman, NMR, ESI-MS). The aim of this paper is review on spectroscopic analyses of molecular structure and biological activity of hydroxyflavonol metal complexes.

  4. Syntheses of biologically active natural products and leading compounds for new pharmaceuticals employing effective construction of a polycyclic skeleton.

    Science.gov (United States)

    Ihara, Masataka

    2006-06-01

    Cascade reactions are useful methods for the construction of polycyclic skeletons, which are important cores for biological activities. A variety of cascade reactions carried out under multiple reaction conditions, such as pericyclic, polar, radical, and transition metal-catalyzed reaction conditions, have been investigated. Culmorin, pentalenene, pentalenic acid, deoxypentalenic acid, longiborneol, cedrandiol, 8,14-cedranoxide, atisirene, atisine, and estrane-type steroids were synthesized via the intramolecular double Michael reaction. Aza double Michael reaction was applied to the syntheses of tylophorine, epilupinine, tacamonine, and paroxetine. Furthermore, sequential Michael and aldol reactions were performed in both intramolecular and intermolecular manners, leading to the formation of polycyclic compounds fused to a four-membered ring. Synthesis of paesslerin A utilizing a multicomponent cascade reaction revealed an error in the proposed structure. Unique cascade reactions carried out under radical and transition metal-catalyzed reaction conditions were also investigated. With the combination of several cascade reactions, serofendic acids and methyl 7beta-hydroxykaurenoate, both of which have neuroprotective activity, were synthesized in a selective manner.

  5. Expression of the peroxisome proliferator activated receptor γ gene is repressed by DNA methylation in visceral adipose tissue of mouse models of diabetes

    Directory of Open Access Journals (Sweden)

    Shiota Kunio

    2009-07-01

    Full Text Available Abstract Background Adipose tissues serve not only as a store for energy in the form of lipid, but also as endocrine tissues that regulates metabolic activities of the organism by secreting various kinds of hormones. Peroxisome proliferator activated receptor γ (PPARγ is a key regulator of adipocyte differentiation that induces the expression of adipocyte-specific genes in preadipocytes and mediates their differentiation into adipocytes. Furthermore, PPARγ has an important role to maintain the physiological function of mature adipocyte by controlling expressions of various genes properly. Therefore, any reduction in amount and activity of PPARγ is linked to the pathogenesis of metabolic syndrome. Results In this study, we investigated the contribution of epigenetic transcriptional regulatory mechanisms, such as DNA methylation, to the expression of the PPARγ gene, and further evaluated the contribution of such epigenetic regulatory mechanisms to the pathogenesis of metabolic syndrome. In 3T3-L1 preadipocytes, the promoter of the PPARγ2 gene was hypermethylated, but was progressively demethylated upon induction of differentiation, which was accompanied by an increase of mRNA expression. Moreover, treatment of cells with 5'-aza-cytideine, an inhibitor of DNA methylation, increased expression of the PPARγ gene in a dose-dependent manner. Methylation in vitro of a PPARγ promoter-driven reporter construct also repressed the transcription of a downstream reporter gene. These results suggest that the expression of the PPARγ gene is inhibited by methylation of its promoter. We next compared the methylation status of the PPARγ promoters in adipocytes from wild-type (WT mice with those from two diabetic mouse models: +Leprdb/+Leprdb and diet-induced obesity mice. Interestingly, we found increased methylation of the PPARγ promoter in visceral adipose tissues (VAT of the mouse models of diabetes, compared to that observed in wild-type mice. We

  6. Biodegradation and anticholinesrerase activity of methyl isocyanate in the aquatic environment of Bhopal

    Digital Repository Service at National Institute of Oceanography (India)

    SenGupta, R.; Sarkar, A.; Kureishy, T.W.

    of Bhopal, Puntius ticto was found to be the most susceptible to MIC-poisoning. There is a change in the values of pH, ammonia-nitrogen and urea-nitrogen concentrations in the Lower Lake water. The cholinesterase activities of different tissues of various...

  7. Biological activity of alkaloids from Solanum dulcamara L.

    Science.gov (United States)

    Kumar, Padma; Sharma, Bindu; Bakshi, Nidhi

    2009-01-01

    Alkaloids are well known for their antimicrobial activity. Though all natural alkaloids come from plants, not all plants produce alkaloids. Plants of the Solanaceae family are known for their high alkaloid content. Alkaloids are found in all plant parts like roots, stems, leaves, flowers, fruits and seeds. In the present study, those plant parts of Solanum dulcamara were selected which have been reported to produce a high content of a specific alkaloid: solanine (from unripe fruits), solasodine (from flowers) and beta-solamarine (from roots). These alkaloids were extracted from various parts of S. dulcamara by well-established methods and were screened for their antibacterial activity. Human pathogenic bacteria, viz., Enterobacter aerogenes, Escherichia coli, Staphylococcus aureus, were selected for the study. All three alkaloids inhibited the growth of E. coli and S. aureus. However, no significant activity was observed against E. aerogenes. Minimum inhibitory concentration and minimum bactericidal concentration were also evaluated.

  8. Papaya seed represents a rich source of biologically active isothiocyanate.

    Science.gov (United States)

    Nakamura, Yoshimasa; Yoshimoto, Motoko; Murata, Yoshiyuki; Shimoishi, Yasuaki; Asai, Yumi; Park, Eun Young; Sato, Kenji; Nakamura, Yasushi

    2007-05-30

    In the present study, papaya (Carica papaya) seed and edible pulp were carefully separated and then the contents of benzyl isothiocyanate and the corresponding glucosinolate (benzyl glucosinolate, glucotropaeolin) quantified in each part. The papaya seed with myrosinase inactivation contained >1 mmol of benzyl glucosinolate in 100 g of fresh seed. This content is equivalent to that of Karami daikon (the hottest Japanese white radish) or that of cress. The papaya seed extract also showed a very high activity of myrosinase and, without myrosinase inactivation, produced 460 micromol of benzyl isothiocyanate in 100 g of seed. In contrast, papaya pulp contained an undetectable amount of benzyl glucosinolate and showed no significant myrosinase activity. The n-hexane extract of the papaya seed homogenate was highly effective in inhibiting superoxide generation and apoptosis induction in HL-60 cells, the activities of which are comparable to those of authentic benzyl isothiocyanate.

  9. Biological activity of Terminalia arjuna on Human Pathogenic Microorganisms

    Directory of Open Access Journals (Sweden)

    Tariq Javed

    2016-01-01

    Full Text Available World’s population relies chiefly on traditional medicinal plants, using their extracts or active constituents. Terminalia arjuna of family Combretaceae reported to be effective as aphrodisiac, expectorant, tonic, styptic, antidysenteric, sweet, acrid, purgative, laxative, astringent, diuretic, astringent, cirrhosis, cardioprotective and cancer treatment.   In present study, antibacterial, antifungal, brine shrimp lethality and phytotoxic effect of Terminalia arjuna was performed. Our results showed that methanolic extract of Terminalia arjuna leaves has moderate antifungal effect against Microsporm canis and fruit extract possess good antibacterial activity against Staphylococus aureus  and  Preudomonas aeroginosa. Moreover, Dichloromethane extract of Terminalia arjuna bark and fruit posses moderate phytotoxic activity

  10. Lysine methylation: beyond histones

    Institute of Scientific and Technical Information of China (English)

    Xi Zhang; Hong Wen; Xiaobing Shi

    2012-01-01

    Posttranslational modifications (PTMs) of histone proteins,such as acetylation,methylation,phosphorylation,and ubiquitylation,play essential roles in regulating chromatin dynamics.Combinations of different modifications on the histone proteins,termed 'histone code' in many cases,extend the information potential of the genetic code by regulating DNA at the epigenetic level.Many PTMs occur on non-histone proteins as well as histones,regulating protein-protein interactions,stability,localization,and/or enzymatic activities of proteins involved in diverse cellular processes.Although protein phosphorylation,ubiquitylation,and acetylation have been extensively studied,only a few proteins other than histones have been reported that can be modified by lysine methylation.This review summarizes the current progress on lysine methylation of nonhistone proteins,and we propose that lysine methylation,like phosphorylation and acetylation,is a common PTM that regulates proteins in diverse cellular processes.

  11. Synthesis and Biological Activities of Substituted Triazolethione Schiff Base

    Institute of Scientific and Technical Information of China (English)

    SUN, Xiao-Hong; TAO, Yan; LIU, Yuan-Fa; CHEN, Bang

    2007-01-01

    Six novel Schiff bases have been synthesized by the condensation reaction of 4-amino-5-(4-pyridyl)-2,4-dihydro-1,2,4-triazole-3-thione with various benzaldehydes. The structures of the compounds have been confirmed by 1H NMR, IR and elemental analysis. The preliminary bioassay indicated that the title compounds possessed good fungicidal activities to several vegetable pathogens.

  12. Biological activity of Schinus molle on Triatoma infestans.

    Science.gov (United States)

    Ferrero, A A; Werdin González, J O; Sánchez Chopa, C

    2006-07-01

    Hexanic extracts from leaves and fruits of Schinus molle were tested for repellent and insecticidal properties against first instar nymphs and eggs of Triatoma infestans, the vector of Chagas' disease. Leaf and fruit extracts were highly repellent for first nymphs. Fruit extracts had also ovicidal activity.

  13. Synthesis and biological activity of salinomycin conjugates with floxuridine.

    Science.gov (United States)

    Huczyński, Adam; Antoszczak, Michał; Kleczewska, Natalia; Lewandowska, Marta; Maj, Ewa; Stefańska, Joanna; Wietrzyk, Joanna; Janczak, Jan; Celewicz, Lech

    2015-03-26

    As part of our program to develop anticancer agents, we have synthesized new compounds, which are conjugates between well-known anticancer drug, floxuridine and salinomycin which is able to selectivity kill cancer stem cells. The conjugates were obtained in two ways i.e. by copper(I) catalysed click Huisgen cycloaddition reaction performed between 3'-azido-2',3'-dideoxy-5-fluorouridine and salinomycin propargyl amide, and by the ester synthesis starting from salinomycin and floxuridine under mild condition. The compounds obtained were characterized by spectroscopic methods and evaluated for their in vitro cytotoxicity against seven human cancer cell lines as well as antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). The conjugate obtained by esterification reaction showed a significantly higher antiproliferative activity against the drug-resistant cancer cells and lower toxicity than those of salinomycin and floxuridine towards normal cells, as well as standard anticancer drugs, such as cisplatin and doxorubicin. The conjugate compound revealed also moderate activity against MRSA and MRSE bacterial strains. Very high activity of floxuridine and 5-fluorouracil against MRSA and MRSE has been also observed.

  14. Programming biological operating systems: genome design, assembly and activation.

    Science.gov (United States)

    Gibson, Daniel G

    2014-05-01

    The DNA technologies developed over the past 20 years for reading and writing the genetic code converged when the first synthetic cell was created 4 years ago. An outcome of this work has been an extraordinary set of tools for synthesizing, assembling, engineering and transplanting whole bacterial genomes. Technical progress, options and applications for bacterial genome design, assembly and activation are discussed.

  15. Biologically active dibenzofurans from Pilidiostigma glabrum, an endemic Australian Myrtaceae.

    Science.gov (United States)

    Shou, Qingyao; Banbury, Linda K; Renshaw, Dane E; Lambley, Eleanore H; Mon, Htwe; Macfarlane, Graham A; Griesser, Hans J; Heinrich, Michael M; Wohlmuth, Hans

    2012-09-28

    In an effort to identify new anti-inflammatory and antibacterial agents with potential application in wound healing, five new dibenzofurans, 1,3,7,9-tetrahydroxy-2,8-dimethyl-4,6-di(2-methylbutanoyl)dibenzofuran (1), 1,3,7,9-tetrahydroxy-2,8-dimethyl-4-(2-methylbutanoyl)-6-(2-methylpropionyl)dibenzofuran (2), 1,3,7,9-tetrahydroxy-2,8-dimethyl-4,6-di(2-methylpropionyl)dibenzofuran (3), 1,3,7,9-tetrahydroxy-4,6-dimethyl-2-(2-methylbutanoyl)-8-(2-methylpropionyl)dibenzofuran (4), and 1,3,7,9-tetrahydroxy-4,6-dimethyl-2,8-di(2-methylpropionyl)dibenzofuran (5), were isolated from the leaves of Pilidiostigma glabrum together with one previously described dibenzofuran. Structure elucidation was achieved by way of spectroscopic measurements including 2D-NMR spectroscopy. Compounds with 2,8-acyl substitutions had potent antibacterial activity against several Gram-positive strains (MIC in the low micromolar range), while compounds with 4,6-acyl substitutions were less active. All compounds except 3 inhibited the synthesis of nitric oxide in RAW264 macrophages with IC(50) values in the low micromolar range. Compounds with 2,8-acyl substitutions also inhibited the synthesis of PGE(2) in 3T3 cells, whereas 4,6-acyl-substituted compounds were inactive. None of the compounds inhibited the synthesis of TNF-α in RAW264 cells. The compounds showed variable but modest antioxidant activity in the oxygen radical absorbance capacity assay. These findings highlight that much of the Australian flora remains unexplored and may yet yield many new compounds of interest. Initial clues are provided on structure/activity relationships for this class of bioactives, which may enable the design and synthesis of compounds with higher activity and/or selectivity.

  16. Synthesis and biological activity of some heterocyclic compounds containing benzimidazole and beta-lactam moiety

    Indian Academy of Sciences (India)

    K F Ansari; C Lal

    2009-11-01

    A number of 1-substituted-2-methyl benzimidazole derivatives have been synthesized and tested for their antibacterial activities. The chemical structures of the newly synthesized compounds were verified on the basis of spectral and elemental methods of analyses. Investigation of antimicrobial activity of the compounds was done by disc diffusion method using Gram-positive (S. aureus, S. mutans and B. subtilis), Gram-negative (E. coli, S. typhi and P. aeruginosa) bacteria and fungi (C. albicans, A. flavus and A. niger). Among the compounds tested 5a, 5b, 5d, 5i, 5j and 5k exhibited good antibacterial activities against Gram positive bacteria, while 5d and 5i also showed notable antifungal activity. Specially compounds 5a and 5b exhibited appreciable activity against S. aureus and B. subtilis comparable to reference drugs.

  17. Murine T cell activation is regulated by surfen (bis-2-methyl-4-amino-quinolyl-6-carbamide)

    Energy Technology Data Exchange (ETDEWEB)

    Warford, Jordan, E-mail: jordan.warford@dal.ca [Department of Pathology, Dalhousie University, Tupper Building, 5850 College Street, Halifax, Nova Scotia B3H 4R2 (Canada); Doucette, Carolyn D., E-mail: carolyn.doucette@dal.ca [Department of Microbiology and Immunology, Dalhousie University, Tupper Building, 5850 College Street, Halifax, Nova Scotia B3H 4R2 (Canada); Hoskin, David W., E-mail: d.w.hoskin@dal.ca [Department of Pathology, Dalhousie University, Tupper Building, 5850 College Street, Halifax, Nova Scotia B3H 4R2 (Canada); Department of Microbiology and Immunology, Dalhousie University, Tupper Building, 5850 College Street, Halifax, Nova Scotia B3H 4R2 (Canada); Easton, Alexander S., E-mail: alexander.easton@dal.ca [Department of Pathology, Dalhousie University, Tupper Building, 5850 College Street, Halifax, Nova Scotia B3H 4R2 (Canada); Department of Microbiology and Immunology, Dalhousie University, Tupper Building, 5850 College Street, Halifax, Nova Scotia B3H 4R2 (Canada); Department of Surgery (Neurosurgery), Dalhousie University, Tupper Building, 5850 College Street, Halifax, Nova Scotia B3H 4R2 (Canada)

    2014-01-10

    Highlights: •Surfen is the first inhibitor of glycosaminoglycan function to be studied in murine T cells. •Surfen reduces T cell proliferation stimulated in vitro and in vivo. •Surfen reduces CD25 expression in T cells activated in vivo but not in vitro. •Surfen increases T cell proliferation when T cell receptor activation is bypassed. •Surfen’s effects are blocked by co-administration of heparin sulfate. -- Abstract: Surfen (bis-2-methyl-4-amino-quinolyl-6-carbamide) binds to glycosaminoglycans (GAGs) and has been shown to influence their function, and the function of proteoglycans (complexes of GAGs linked to a core protein). T cells synthesize, secrete and express GAGs and proteoglycans which are involved in several aspects of T cell function. However, there are as yet no studies on the effect of GAG-binding agents such as surfen on T cell function. In this study, surfen was found to influence murine T cell activation. Doses between 2.5 and 20 μM produced a graduated reduction in the proliferation of T cells activated with anti-CD3/CD28 antibody-coated T cell expander beads. Surfen (20 mg/kg) was also administered to mice treated with anti-CD3 antibody to activate T cells in vivo. Lymphocytes from surfen-treated mice also showed reduced proliferation and lymph node cell counts were reduced. Surfen reduced labeling with a cell viability marker (7-ADD) but to a much lower extent than its effect on proliferation. Surfen also reduced CD25 (the α-subunit of the interleukin (IL)-2 receptor) expression with no effect on CD69 expression in T cells treated in vivo but not in vitro. When receptor activation was bypassed by treating T cells in vitro with phorbyl myristate acetate (10 ng/ml) and ionomycin (100 ng/ml), surfen treatment either increased proliferation (10 μM) or had no effect (2.5, 5 and 20 μM). In vitro treatment of T cells with surfen had no effect on IL-2 or interferon-γ synthesis and did not alter proliferation of the IL-2 dependent cell

  18. Henry's law constants and infinite dilution activity coefficients of cis-2-butene, dimethylether, chloroethane, and 1,1-difluoroethane in methanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, isobutanol, tert-butanol, 1-pentanol, 2-pentanol, 3-pentanol, 2-methyl-1-butanol, 3-methyl-1-butanol, and 2-methyl-2-butanol

    Energy Technology Data Exchange (ETDEWEB)

    Miyano, Yoshimori [Department of Chemistry and Bioscience, Kurashiki University of Science and the Arts, 2640 Nishinoura, Tsurajimacho, Kurashiki 712-8505 (Japan)]. E-mail: miyano@chem.kusa.ac.jp; Kobashi, Takahiro [Department of Chemistry and Bioscience, Kurashiki University of Science and the Arts, 2640 Nishinoura, Tsurajimacho, Kurashiki 712-8505 (Japan); Shinjo, Hiroshi [Department of Chemistry and Bioscience, Kurashiki University of Science and the Arts, 2640 Nishinoura, Tsurajimacho, Kurashiki 712-8505 (Japan); Kumada, Shinya [Department of Chemistry and Bioscience, Kurashiki University of Science and the Arts, 2640 Nishinoura, Tsurajimacho, Kurashiki 712-8505 (Japan); Watanabe, Yusuke [Department of Chemistry and Bioscience, Kurashiki University of Science and the Arts, 2640 Nishinoura, Tsurajimacho, Kurashiki 712-8505 (Japan); Niya, Wataru [Department of Chemistry and Bioscience, Kurashiki University of Science and the Arts, 2640 Nishinoura, Tsurajimacho, Kurashiki 712-8505 (Japan); Tateishi, Yoko [Department of Chemistry and Bioscience, Kurashiki University of Science and the Arts, 2640 Nishinoura, Tsurajimacho, Kurashiki 712-8505 (Japan)

    2006-06-15

    Henry's law constants and infinite dilution activity coefficients of cis-2-butene, dimethylether, chloroethane, and 1,1-difluoroethane in methanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, isobutanol, tert-butanol, 1-pentanol, 2-pentanol, 3-pentanol, 2-methyl-1-butanol, 3-methyl-1-butanol, and 2-methyl-2-butanol in the temperature range of 250 K to 330 K were measured by a gas stripping method and partial molar excess enthalpies were calculated from the activity coefficients. A rigorous formula for evaluating the Henry's law constants from the gas stripping measurements was used for the data reduction of these highly volatile mixtures. The uncertainty is about 2% for the Henry's law constants and 3% for the estimated infinite dilution activity coefficients. In the evaluation of the infinite dilution activity coefficients, the nonideality of the solute such as the fugacity coefficient and Poynting correction factor cannot be neglected, especially at higher temperatures. The estimated uncertainty of the infinite dilution activity coefficients includes 1% for nonideality.

  19. [Biological activity of selenorganic compounds at heavy metal salts intoxication].

    Science.gov (United States)

    Rusetskaya, N Y; Borodulin, V B

    2015-01-01

    Possible mechanisms of the antitoxic action of organoselenium compounds in heavy metal poisoning have been considered. Heavy metal toxicity associated with intensification of free radical oxidation, suppression of the antioxidant system, damage to macromolecules, mitochondria and the genetic material can cause apoptotic cell death or the development of carcinogenesis. Organic selenium compounds are effective antioxidants during heavy metal poisoning; they exhibit higher bioavailability in mammals than inorganic ones and they are able to activate antioxidant defense, bind heavy metal ions and reactive oxygen species formed during metal-induced oxidative stress. One of promising organoselenium compounds is diacetophenonyl selenide (DAPS-25), which is characterized by antioxidant and antitoxic activity, under conditions including heavy metal intoxication.

  20. Synthesis and biological activity studies of some thiazolidinones and azetidinones

    Directory of Open Access Journals (Sweden)

    Mehta P

    2006-01-01

    Full Text Available A series of 4-thiazolidinones and 2-azetidinones have been synthesized by condensation of 4,4′-diaminodiphenylsulphone with various aromatic or heterocyclic aldehydes to yield the Schiff′s bases. Cyclocondensation of Schiff′s bases with 2-mercaptopropionic acid afforded 4-thiazolidinone derivatives, and cyclocondensation of Schiff′s bases with chloroacetylchloride in presence of triethylamine afforded 2-azetidinone derivatives. The structures of the newly synthesized compounds were confirmed by analytical and spectral (IR, NMR, and Mass data. All these compounds were evaluated for their in vitro growth-inhibitory activity against several microbes. Compound 4b and 4c exhibited equipotent antibacterial activity with the reference standard ampicillin against Bacillus subtilis.