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Sample records for biologically active methyl

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

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    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.

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

    Science.gov (United States)

    Sangpheak, Waratchada; Kicuntod, Jintawee; Schuster, Roswitha; Rungrotmongkol, Thanyada; Wolschann, Peter; Kungwan, Nawee; Viernstein, Helmut

    2015-01-01

    Summary 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. PMID:26877798

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

    International Nuclear Information System (INIS)

    The essential oils of branches and leaves of Endlicheria citiodora were obtained by hydrodistillation and analysed using GC-FID, GC-MS and both NMR 13C and 1H, 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 μg/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)

  5. Synthesis, structure and biological activity of nickel(II) complexes of 5-methyl 2-furfural thiosemicarbazone.

    Science.gov (United States)

    Jouad, E M; Larcher, G; Allain, M; Riou, A; Bouet, G M; Khan, M A; Thanh, X D

    2001-09-01

    5-Methyl 2-furfuraldehyde thiosemicarbazone (M5HFTSC) with nickel(II) leads to three types of complexes: [Ni(M5HFTSC)(2)X(2)], [Ni(M5FTSC)(2)] and [Ni(M5FTSC)(2)] x 2DMF. In the first type the ligand remains in thione form, while in the two other, the anionic thiolato form is involved. The species [Ni(M5HFTSC)(2)X(2)] has been characterized spectroscopically. The structures of [Ni(M5FTSC)(2)] x 2DMF and [Ni(M5FTSC)(2)] have been solved using X-ray diffraction. Biological studies of [Ni(M5HFTSC)(2)Cl(2)] have been carried out in vitro for antifungal activity on human pathogenic fungi, Aspergillus fumigatus and Candida albicans, and in vivo for toxicity on mice. The results are compared to those of the ligand, the metal salt and a similar copper complex [Cu(M5HFTSC)Cl(2)]. PMID:11566328

  6. Synthesis, characterization and biological activity of 2-methyl-3-aminoquinazolin-4(3H)-ones Schiff bases

    International Nuclear Information System (INIS)

    The 3-amino-2-methyl quinazoline/6-bromo-2-methyl quinazoline-4(3H)-ones, 2a,b, on treatment with 2,3-indolinedione in the presence of traces of glacial acetic acid yielded 3-{(2'-oxo-1',2'-dihydroindole-3'-ylidene)amino}-2-methylquinazolin/6-bromo -2-methylquinazolin-4-(3H)- ones, 3a,b, which on condensation with various secondary amines and formaldehyde in ethanol afforded title compounds 3-{(1'-alkyl/arylaminomethyl-2'-oxo-1',2'-dihydroindole-3'-ylidene) amino}-2-methyl-6-quinazolin-4-(3H)-ones, 4a1-6 and 4b1-6. C, H, N analysis, infrared spectroscopy, 1H NMR, and mass spectroscopy allowed the identification of the synthesized compounds, which were investigated for their antimicrobial, analgesic, anti-inflammatory and antihelmintic activities. The results of the biological activities revealed that the compounds 4a3, 4a4 and 4b6 exhibited significant analgesic and anti-inflammatory activities. Compounds 4b5 and 4b6 showed antihelmintic activity when tested against Pheretima posthuma. (author)

  7. Synthesis, Structure and Biological Activity of Zn(II) Complex with Tris(benzimidazol-2-yl-methyl)amine Ligand

    Institute of Scientific and Technical Information of China (English)

    LIU,Xiao-Lan(刘小兰); ZHAO,Ru(赵茹); LIU,Xiao-Hong(刘晓红); YUE,Jun-Jie(岳俊杰); YIN,Yu-Xin(尹宇新); SUN,Yun(孙云); SUN,Ming(孙命)

    2004-01-01

    A new Zn(II) mononuclear complex with tris(benzimidazol-2-yl-methyl)amine (NTB) was synthesized with stoichiometry of [Zn(NTB)NO3]NO3·DIPY·DMF (DIPY∶4,4'-dipyridyl). The complex was characterized by elemental analysis, UV and IR spectra. The crystal structure was determined by using X-ray diffraction analysis. The crystal structure indicates that four N atoms and one O atom coordinate to zinc ion to construct a distorted trigonal-dipyramid configuration. Three nonprotonated N atoms from imidazole groups are in the equatorial plane, one alkylamino N atom and one O atom from in the axial directions. The biological activity assay shows that this complex presents certain biological activity by means of pyrogallol autoxidation and it can be called a model compound of superoxide dismutase (SOD).

  8. 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.

  9. 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.

  10. 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.

  11. 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

    bed reactor, was determined using a batch kinetic based approach. The procedure involved modeling of methyl tert-butyl ether removal rates from batch experiments followed by parameter estimations. It was estimated to be 5-14% (w/w) of the measured volatile suspended solids concentration in the reactor....

  12. 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.

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

    Science.gov (United States)

    Wongnate, Thanyaporn; Sliwa, Dariusz; Ginovska, Bojana; Smith, Dayle; Wolf, Matthew W; Lehnert, Nicolai; Raugei, Simone; Ragsdale, Stephen W

    2016-05-20

    Methyl-coenzyme M reductase, the rate-limiting enzyme in methanogenesis and anaerobic methane oxidation, is responsible for the biological production of more than 1 billion tons of methane per year. The mechanism of methane synthesis is thought to involve either methyl-nickel(III) or methyl radical/Ni(II)-thiolate intermediates. We employed transient kinetic, spectroscopic, and computational approaches to study the reaction between the active Ni(I) enzyme and substrates. Consistent with the methyl radical-based mechanism, there was no evidence for a methyl-Ni(III) species; furthermore, magnetic circular dichroism spectroscopy identified the Ni(II)-thiolate intermediate. Temperature-dependent transient kinetics also closely matched density functional theory predictions of the methyl radical mechanism. Identifying the key intermediate in methanogenesis provides fundamental insights to develop better catalysts for producing and activating an important fuel and potent greenhouse gas. PMID:27199421

  14. Synthesis and biological activity of analogs of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and its monoamine oxidase-derived metabolites

    International Nuclear Information System (INIS)

    The structure-activity relationship (SAR) of substituted tetrahydropyridines as a substrates for monoamine oxidase (MAO) was examined through the synthesis and evaluation of the two methyl substituted analogs of the neurotoxic tertiary amine 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Neither the 1,2-dimethyl-4-phenyl-1,2,3,6-tetrahydropyridine (17) nor the 1,6-dimethyl-4-phenyl-1,2,3,6-tetrahydropyridine (18) are substrates for either the A or B forms of MAO. It was also demonstrated that neither tetrahydropyridine analog shares the neurotoxic effect of MPTP. However, the chemically synthesized 2-electron and 4-electron oxidation products, 1,2-dimethyl-4-phenyl-1,2-dihydropyridinium ion (15) and 1,2-dimethyl-4-phenylpyridinium ion (60), respectively, which are methyl analogs of the MAO derived metabolites of MPTP share the toxic properties associated with these metabolites, MPDP+ and MPP+, respectively. Furthermore, the pyridinium ion is an effect inhibitor of mitochondrial respiration. Finally, the 1,2-dimethyl-4-phenylpyridinium species 60 is demonstrated to be an inhibitor of mouse striatal synaptosomal uptake of both [3H] dopamine and [3H] MPP+

  15. Synthesis of Some Novel Biologically Active Disperse Dyes Derived from 4-Methyl-2,6-dioxo-1-propyl-1,2,5,6-tetrahydro-pyridine-3-carbonitrile as Coupling Component and Their Colour Assessment on Polyester Fabrics

    Directory of Open Access Journals (Sweden)

    Mohamed H. Elnagdi

    2012-07-01

    Full Text Available A series of novel azo-disperse dyes containing alkylhydrazonopyridinone structures were synthesized. 4-Methyl-2,6-dioxo-1-propyl-1,2,5,6-tetrahydropyridine-3-carbonitrile (8 is synthesized by one-pot synthesis using ethyl cyanoacetate, propylamine, and ethyl acetoacetate. Compound 8 is then coupled with aromatic and heteroaromatic diazonium salts to afford the corresponding aryl- and heteroaryl-4-methyl-2,6-dioxo-1-propyl-1,2,5,6-tetrahydropyridine-3-carbonitriles 12a,b and 13a–c. Structural assignments to the dyes were made using NMR spectroscopic methods. A high temperature dyeing method was employed to apply these dyes to polyester fabrics. Most of the dyed fabrics tested displayed very good light fastness levels and good wash fastness. Finally, the biological activity of the prepared dyes against Gram positive bacteria and Gram negative bacteria were evaluated.

  16. Synthesis, crystal structure analysis, spectral investigations, DFT computations, Biological activities and molecular docking of methyl(2E)-2-{[N-(2-formylphenyl)(4-methylbenzene) sulfonamido]methyl}-3-(4-fluorophenyl)prop-2-enoate, a potential bioactive agent

    Science.gov (United States)

    Murugavel, S.; Vetri Velan, V.; Kannan, Damodharan; Bakthadoss, Manickam

    2016-03-01

    The title compound methyl(2E)-2-{[N-(2-formylphenyl) (4-methylbenzene)sulfonamido]methyl}-3-(4-fluorophenyl) prop-2-enoate (MFMSF) has been synthesized and single crystals were grown by slow evaporation solution growth technique at room temperature. The grown crystals were characterized by FTIR, 1H NMR, 13C NMR, and single crystal X-ray diffraction. In the crystal, molecules are linked by intermolecular C-H…O hydrogen bonds forming a two-dimensional supramolecular network along [110] direction. The molecular geometry was also optimized using density functional theory (DFT/B3LYP) method with the 6-311G (d,p) basis set in ground state and compared with the experimental data. The entire vibrational assignments of wave numbers were made on the basis of potential energy distribution (PED) by VEDA 4 programme. Stability of the molecule arising from hyper conjugative interactions, charge delocalization has been analyzed using natural bond orbital (NBO) analysis. In addition, NLO, MEP, Mulliken, thermodynamic properties, HOMO and LUMO energy gap were theoretically predicted. The global chemical reactivity descriptors are calculated for MFMSF and used to predict their relative stability and reactivity. The antibacterial activity of the compound was also tested against various pathogens. The molecular docking studies concede that title compound may exhibit PBP-2X inhibitor activity.

  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. Characterization of DNA methylation and its association with other biological systems in lymphoblastoid cell lines

    Science.gov (United States)

    Zhang, Zhe; Liu, Jinglan; Kaur, Maninder; Krantz, Ian D.

    2016-01-01

    Lymphoblastoid cell line (LCL) is a common tool to study genetic disorders. However, it has not been fully characterized to what degree LCLs preserve the in vivo status of non-genetic biological systems, such as DNA methylation and gene transcription. We previously reported that DNA methylation in LCLs is highly variable in a data set of ~27,000 CpG dinucleotide sites around transcription start site (TSS) and 63 human subjects including healthy controls and probands of genetic disorders. Disease-causing mutations are linked to differential methylation at some CpG sites, but account for a small proportion of the total variance. In this study, we repeated the experiments to ensure that the high variance is not due to technical error and scrutinized the characteristics of DNA methylation and its association with other biological systems. Using sequence information and ChIP-seq data, we conclude that local CpG density and histone modifications not only correlate to baseline methylation level, but also affect the direction of methylation change in LCLs. Integrative analysis of gene transcription and DNA methylation data of the same subjects shows that medium or high methylation around TSS blocks the transcription while low methylation is a necessary, but not sufficient condition of downstream gene transcription. We utilized epigenetic information around TSS to predict active gene transcription via logistic regression models. The multivariate model using DNA methylation, eight histone modifications, and two regulatory protein complexes (CTCF and cohesin) as predictors has better performance (accuracy = 95.1%) than any univariate models of single predictors. Linear regression analysis further shows that the transcriptional levels predicted by epigenetic markers have significant correlation to microarray measurements (p = 2.2e-10). This study provides new insights into the epigenetic systems of LCLs and suggests that more specifically designed experiments are needed to

  19. DNA Methylation

    OpenAIRE

    İzmirli, Müzeyyen; Tufan, Turan; Alptekin, Davut

    2012-01-01

    Methylation is a chemical reaction in biological systems for normal genome regulation and development. It is a well known type of epigenetic mechanism. Methylation which regulates gene expression via epigenetic events like gene activation, repression, and chromatin remodelling, consists of two methylation systems. One of these systems is DNA methylation whereas the other is protein (histone) methylation. These systems are associated with some fundamental abnormalities and diseases. This revi...

  20. DNA Methylation

    OpenAIRE

    Muzeyyen Izmirli; Turan Tufan; Davut Alptekin

    2012-01-01

    Methylation is a chemical reaction in biological systems for normal genome regulation and development. It is a well known type of epigenetic mechanism. Methylation which regulates gene expression via epigenetic events like gene activation, repression, and chromatin remodelling, consists of two methylation systems. One of these systems is DNA methylation whereas the other is protein (histone) methylation. These systems are associated with some fundamental abnormalities and diseases. This revie...

  1. Biological activity determination

    Czech Academy of Sciences Publication Activity Database

    Madronová, L.; Novák, J.; Kubíček, J.; Antošová, B.; Kozler, J.; Novák, František

    New York: Nova Science Publisher, 2011 - (Madronová, L.), s. 85-103. (Chemistry Research and Applications). ISBN 978-1-61668-965-0 Institutional research plan: CEZ:AV0Z60660521 Keywords : biological activity * determination * potassium humate samples Subject RIV: CB - Analytical Chemistry, Separation

  2. 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.

  3. X-ray Single Crystal Structure, DFT Calculations and Biological Activity of 2-(3-Methyl-5-(pyridin-2'-yl)-1H-pyrazol-1-yl) Ethanol.

    Science.gov (United States)

    Radi, Smaail; Attayibat, Ahmed; El-Massaoudi, Mohamed; Salhi, Amin; Eddike, Driss; Tillard, Monique; Mabkhot, Yahia N

    2016-01-01

    A pyridylpyrazole bearing a hydroxyethyl substituent group has been synthesized by condensation of (Z)-4-hydroxy-4-(pyridin-2-yl)but-3-en-2-one with 2-hydroxyethylhydrazine. The compound was well characterized and its structure confirmed by single crystal X-ray diffraction. Density functional calculations have been performed using DFT method with 6-31G* basis set. The HOMO-LUMO energy gap, binding energies and electron deformation densities are calculated at the DFT (BLYP, PW91, PWC) level. The electrophilic f(-) and nucleophilic f(+) Fukui functions and also the electrophilic and nucleophilic Parr functions are well adapted to find the electrophile and nucleophile centers in the molecule. The title compound has been tested for its DPPH radical scavenging activity which is involved in aging processes, anti-inflammatory, anticancer and wound healing activity. Compound is also found with a significant antioxidant activity, probably due to the ability to donate a hydrogen atom to the DPPH radical. PMID:27527141

  4. 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

    spectroscopy and supported by computer simulations and molecular mechanics calculations. While the trans forms of 2,3-PDA and 2,4-PDA and cis-2,5-PDA show NMDA receptor agonist activities, cis-2,3-PDA and cis-2,4-PDA are NMDA antagonists. The compounds trans-2,5-PDA and cis-2,6-PDA did not interact with NMDA...

  5. DNA methylation characteristics of primary melanomas with distinct biological behaviour.

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    Szilvia Ecsedi

    Full Text Available In melanoma, the presence of promoter related hypermethylation has previously been reported, however, no methylation-based distinction has been drawn among the diverse melanoma subtypes. Here, we investigated DNA methylation changes associated with melanoma progression and links between methylation patterns and other types of somatic alterations, including the most frequent mutations and DNA copy number changes. Our results revealed that the methylome, presenting in early stage samples and associated with the BRAF(V600E mutation, gradually decreased in the medium and late stages of the disease. An inverse relationship among the other predefined groups and promoter methylation was also revealed except for histologic subtype, whereas the more aggressive, nodular subtype melanomas exhibited hypermethylation as well. The Breslow thickness, which is a continuous variable, allowed for the most precise insight into how promoter methylation decreases from stage to stage. Integrating our methylation results with a high-throughput copy number alteration dataset, local correlations were detected in the MYB and EYA4 genes. With regard to the effects of DNA hypermethylation on melanoma patients' survival, correcting for clinical cofounders, only the KIT gene was associated with a lower overall survival rate. In this study, we demonstrate the strong influence of promoter localized DNA methylation changes on melanoma initiation and show how hypermethylation decreases in melanomas associated with less favourable clinical outcomes. Furthermore, we establish the methylation pattern as part of an integrated apparatus of somatic DNA alterations.

  6. Synthesis and pharmacological activities of 2-methyl-8-quinolyloxypropylamines

    Directory of Open Access Journals (Sweden)

    Reddy YSR

    2007-01-01

    Full Text Available Starting chloropropane derivative (2 was prepared by the reaction of 2-methyl-8-hydroxyquinoline (1 with 1- bromo-3-chloropropane in presence of a base. Various new 1-(2-methyl-8-quinolyloxy-3-propylamines (3a-3j have been synthesized by the condensation of 1-(2-methyl-8-quinolyloxy-3-chloropropane (2 with different amines. Compounds were screened for the possible central nervous system depressant activities. Some of them showed moderate central nervous system depressant activity.

  7. 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- 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...

  8. SECONDARY METABOLITES OF OCIMUM GRATISSIMUM AND THEIR BIOLOGICAL ACTIVITIES

    OpenAIRE

    Deeptanjali Sahoo; Ajay Kumar

    2013-01-01

    Ocimum gratissimum synthesizes and accumulates a variety of secondary metabolites. Some of the biologically active secondary metabolites such as eugenol, thymol, methyl cinnamate and geraniol are responsible for the antimicrobial activity of the well-known plant of this species and substantiate the claim in traditional system of medicine. The present review summarizes the information available on the secondary metabolites isolated from Ocimum gratissimum.

  9. Brassinosteroids: synthesis and biological activities

    Czech Academy of Sciences Publication Activity Database

    Oklešťková, Jana; Rárová, Lucie; Kvasnica, Miroslav; Strnad, Miroslav

    2015-01-01

    Roč. 14, č. 6 (2015), s. 1053-1072. ISSN 1568-7767 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Brassinosteroids * Chemical synthesis * Plant biological activity Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.407, year: 2014

  10. Pectin methyl esterase activity in apple and orange pulps

    International Nuclear Information System (INIS)

    The results of pectin methyl esterase activity from apple, orange pulp and orange peel depending of ph and temperature are discussed. It's shown that the methyl esterase activity form apple and orange pulps higher in range of temperatures from +37...+60digC. The analysis of dependence of its activity from ph has shown that in both case the enzyme activity increase with increase of ph

  11. The DNA methylation profile of activated human natural killer cells.

    Science.gov (United States)

    Wiencke, John K; Butler, Rondi; Hsuang, George; Eliot, Melissa; Kim, Stephanie; Sepulveda, Manuel A; Siegel, Derick; Houseman, E Andres; Kelsey, Karl T

    2016-05-01

    Natural killer (NK) cells are now recognized to exhibit characteristics akin to cells of the adaptive immune system. The generation of adaptive memory is linked to epigenetic reprogramming including alterations in DNA methylation. The study herein found reproducible genome wide DNA methylation changes associated with human NK cell activation. Activation led predominately to CpG hypomethylation (81% of significant loci). Bioinformatics analysis confirmed that non-coding and gene-associated differentially methylated sites (DMS) are enriched for immune related functions (i.e., immune cell activation). Known DNA methylation-regulated immune loci were also identified in activated NK cells (e.g., TNFA, LTA, IL13, CSF2). Twenty-one loci were designated high priority and further investigated as potential markers of NK activation. BHLHE40 was identified as a viable candidate for which a droplet digital PCR assay for demethylation was developed. The assay revealed high demethylation in activated NK cells and low demethylation in naïve NK, T- and B-cells. We conclude the NK cell methylome is plastic with potential for remodeling. The differentially methylated region signature of activated NKs revealed similarities with T cell activation, but also provided unique biomarker candidates of NK activation, which could be useful in epigenome-wide association studies to interrogate the role of NK subtypes in global methylation changes associated with exposures and/or disease states. PMID:26967308

  12. Allele-specific DNA methylation reinforces PEAR1 enhancer activity.

    Science.gov (United States)

    Izzi, Benedetta; Pistoni, Mariaelena; Cludts, Katrien; Akkor, Pinar; Lambrechts, Diether; Verfaillie, Catherine; Verhamme, Peter; Freson, Kathleen; Hoylaerts, Marc F

    2016-08-18

    Genetic variation in the PEAR1 locus is linked to platelet reactivity and cardiovascular disease. The major G allele of rs12041331, an intronic cytosine guanine dinucleotide-single-nucleotide polymorphism (CpG-SNP), is associated with higher PEAR1 expression in platelets and endothelial cells than the minor A allele. The molecular mechanism underlying this difference remains elusive. We have characterized the histone modification profiles of the intronic region surrounding rs12041331 and identified H3K4Me1 enhancer-specific enrichment for the region that covers the CpG-SNP. Interestingly, methylation studies revealed that the CpG site is fully methylated in leukocytes of GG carriers. Nuclear protein extracts from megakaryocytes, endothelial cells, vs control HEK-293 cells show a 3-fold higher affinity for the methylated G allele compared with nonmethylated G or A alleles in a gel electrophoretic mobility shift assay. To understand the positive relationship between methylation and gene expression, we studied DNA methylation at 4 different loci of PEAR1 during in vitro megakaryopoiesis. During differentiation, the CpG-SNP remained fully methylated, while we observed rapid methylation increases at the CpG-island overlapping the first 5'-untranslated region exon, paralleling the increased PEAR1 expression. In the same region, A-allele carriers of rs12041331 showed significantly lower DNA methylation at CGI1 compared with GG homozygote. This CpG-island contains binding sites for the methylation-sensitive transcription factor CTCF, whose binding is known to play a role in enhancer activation and/or repression. In conclusion, we report the molecular characterization of the first platelet function-related CpG-SNP, a genetic predisposition that reinforces PEAR1 enhancer activity through allele-specific DNA methylation. PMID:27313330

  13. Synthesis, Crystal Structure and Biological Activity of N-tert-butyl-N-(4-methyl-1,2,3-thiadiazole)-5-yl-N'-(4-methyl-1,2,3-thiadiazole)-5-formyl-N'-3,5-dichloropyridin-2-yl-diacylhydrazine

    Institute of Scientific and Technical Information of China (English)

    WANG Huan; FU Yi-Feng; FAN Zhi-Jin; SONG Hai-Bin; WU Qing-Jun; ZHANG You-Jun; Belskaya N. P.; Bakulev V. A.

    2011-01-01

    The title compound N-tert-butyl-N-(4-methyl-1,2,3-thiadiazole)-5-yl-N'-(4-me-thyl-1,2,3-thiadiazole)-5-formyl-N'-3,5-dichloropyrid-2-yl-diacylhydrazines (C18H17C12N7O3S2, Mr =514.41) has been synthesized by the reaction of N-tert-butyl-N'-3,6-dichloropyridine-2-formyl hydrazine with 4-methyl-1,2,3- thiadiazole-5-carbonyl chloride and triethylamine, and its strueture was characterized by 1H NMR, HR MS, and single-crystal X-ray diffraction.The crystal of the title compound belongs to monoclinic, space group C2/c with a = 27.726(8), b = 11.045(3), c = 14.507(4)(A), β = 96.758(4)°, Z = 8, V= 4412(2)(A)3, Dc = 1.549 g/cm3,μ = 0.521 mm-1, F(000) = 2112, R =0.0405 and wR = 0.1153.X-ray analysis indicates that all rings are non-planar in this molecule.The bioassay results indicate that both the title compound and the positive control RH-5992 have weak fungicide activities, while the title compound has good insecticidal activity against Plutella xylostella L.and no insecticidal activity against Culex pipiens pallens.

  14. Brassinosteroids and their Biological Activities

    Czech Academy of Sciences Publication Activity Database

    Oklešťková, Jana; Rárová, Lucie; Strnad, Miroslav

    Vol. Part XIII. Heidelberg: Springer Verlag, 2013 - (Ramawat, K.; Mérillon, J.), s. 3851-3871 ISBN 978-3-642-22143-9 R&D Projects: GA AV ČR IAA400550801 Grant ostatní: GA MŠk(CZ) ED0007/01/01 Institutional support: RVO:61389030 Keywords : Anticancer activity * apoptosis * bioassay Subject RIV: EB - Genetics ; Molecular Biology

  15. Affinity-based enrichment strategies to assay methyl-CpG binding activity and DNA methylation in early Xenopus embryos

    Directory of Open Access Journals (Sweden)

    Bogdanović Ozren

    2011-08-01

    Full Text Available Abstract Background DNA methylation is a widespread epigenetic modification in vertebrate genomes. Genomic sites of DNA methylation can be bound by methyl-CpG-binding domain proteins (MBDs and specific zinc finger proteins, which can recruit co-repressor complexes to silence transcription on targeted loci. The binding to methylated DNA may be regulated by post-translational MBD modifications. Findings A methylated DNA affinity precipitation method was implemented to assay binding of proteins to methylated DNA. Endogenous MeCP2 and MBD3 were precipitated from Xenopus oocyte extracts and conditions for methylation-specific binding were optimized. For a reverse experiment, DNA methylation in early Xenopus embryos was assessed by MBD affinity capture. Conclusions A methylated DNA affinity resin can be applied to probe for MBD activity in extracts. This assay has a broad application potential as it can be coupled to downstream procedures such as western blotting, fluorimetric HDAC assays and quantitative mass spectrometry. Methylated DNA affinity capture by methyl-CpG binding proteins produces fractions highly enriched for methylated DNA, suitable for coupling to next generation sequencing technologies. The two enrichment strategies allow probing of methyl-CpG protein interactions in early vertebrate oocytes and embryos.

  16. Biological activity of guanidino purines

    Czech Academy of Sciences Publication Activity Database

    Česnek, Michal; Holý, Antonín

    Marburg : University of Marburg, 2006. s. 85. ISBN 3-89703-685-1. [Joint Meeting of the Czech, German and Hungarian Pharmaceutical Societies. 04.10.2006-07.10.2006, Marburg] R&D Projects: GA MŠk(CZ) 1M0508 Grant ostatní: Descartes Prize(XE) HPAW-2002-100096 Institutional research plan: CEZ:AV0Z40550506 Keywords : biological activity * guanidino purines Subject RIV: CC - Organic Chemistry

  17. 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.

  18. 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.

  19. 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).

  20. 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.

  1. Adsorption of Gaseous Methyl Iodide by Active Carbons

    International Nuclear Information System (INIS)

    The impregnation of active carbons is known to be a useful means of improving the ability of these carbons to retain methyl iodide which might be formed during the accidental release of fission products from a reactor. Some basic work was done on both impregnated and unimpregnated materials, which involved: (a) the texture: (b) the reaction of Mel with the impregnants; (c) the adsorption of Mel on the carbons under dry and wet conditions at different temperatures. It was found that the carbons are highly microporous. A large part of this porosity disappears on impregnation with organic amine; These impregnants react chemically with the methyl iodide, which is thereby fixed on the carbon. For carbon which is impregnated with KI, a rapid exchange reaction takes place between the methyl iodide and KI under both dry and wet conditions. Consequently most of the iodine activity can be removed from the gas. (author)

  2. 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

  3. 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

  4. Biological Activities of Scolopendrid Pharmacopuncture

    Directory of Open Access Journals (Sweden)

    Kim Sung-Chul

    2010-09-01

    Full Text Available 2Reactive Oxygen Species(ROS are continuously produced at a high rate as a by- product of aerobic metabolism. Since tissue damage by free radical increases with age, the reactive oxygen species(ROS such as hydrogen peroxide(H2O2, nitric oxide(NO. Several lines of evidence provided that ROS appears to cause to develop aging-related various diseases such as cancer, arthritis, cardiovascular disease. Our reserch objective was to examine the in vitro biological activity of Scolopendrid Pharmacopuncture, including the total poly-phenol content, DPPH radical scavenging, ABTS radical scavenging, Superoxide dismutase(SOD-like activity, Nitrite scavenging ability. The total poly-phenol contents of Scolopendrid Pharmacopuncture was 35.859mg/L. Elctron donation ability on DPPH was 36.82%. The 2,2'-azinobis-3-ehtlbezothiazoline-6- sulfonic acid radical decolorization (ABTS was 84.7%. The superoxide dismutase (SOD-like activities of Scolopendrid Pharmacopuncture was 44.33%. The nitrite scavenging effects were pH dependent, and were highest at pH 1.5(45.2% and lowest at pH 6.0(11.3%. We conclude that Scolopendrid Pharmacopuncture may be useful as potential sources of antioxidant.

  5. Inhibition of Pectin Methyl Esterase Activity By Green Tea Catechins

    OpenAIRE

    Sagi, Irit; Lewis, Kristin; Tworowski, Dmitry; Shahar, Chen; Selzer, Tzvia

    2008-01-01

    Pectin methyl esterases (PMEs) and their endogenous inhibitors are involved in the regulation of many processes in plant physiology, ranging from tissue growth and fruit ripening to parasitic plant haustorial formation and host invasion. Thus, control of PME activity is critical for enhancing our understanding of plant physiological processes and regulation. Here we report on the identification of epigallocatechin gallate (EGCG), a green tea component, as a natural inhibitor for pectin ...

  6. Enzyme activities in agricultural soils fumigated with methyl bromide alternatives

    OpenAIRE

    Klose, Susanne; Ajwa, H A

    2004-01-01

    Pre-plant fumigation of agricultural soils with a combination of methyl bromide (MeBr) and chloropicrin (CP) to control nematodes, soil-borne pathogens and weeds has been a common practice in strawberry (Fragaria X ananassa Duchesne) production since the 1960s. MeBr will be phased out by 2005, but little is known about the impacts of alternative fumigants on soil microbial processes. We investigated the response of microbial biomass and enzyme activities in soils fumigated over two years with...

  7. 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.

  8. Daphnetin methylation stabilizes the activity of phosphoribulokinase in wheat during cold acclimation.

    Science.gov (United States)

    Kane, Khalil; Moheb, Amira; Fukushi, Yukihara; Roy, René; Hüner, Norman P A; Ibrahim, Ragai K; Sarhan, Fathey

    2012-10-01

    The methylation of daphnetin (7,8-dihydroxycoumarin) to its 8-methyl derivative is catalyzed by a wheat (Triticum aestivum L.) O-methyltransferase (TaOMT1). This enzyme is regulated by cold and photosystem II excitation pressure (plastid redox state). Here, we investigated the biological significance of this methylation and its potential role in modulating the activity of kinases in wheat. To identify the potential kinases that may interact with daphnetin in wheat, the soluble protein extract from aerial parts of cold-acclimated wheat was purified by DEAE-cellulose separation and affinity chromatography on a daphnetin derivative (7,8-dihydroxy-4-coumarin acetic acid)-EAH sepharose column. Mass spectrometric analysis indicated that wheat phosphoribulokinase (TaPRK) is the major kinase that binds to daphnetin. This TaPRK plays an important role in regulating the flow of carbon through the Calvin cycle, by catalyzing the final step in the regeneration of ribulose 1,5-bisphosphate from ribulose-5-phosphate (Ru5P) and ATP. The activities of TaPRK, endogenous or recombinant, are inhibited by daphnetin in a specific and dose-dependent manner, but not by its monomethyl derivative (7-methyl, 8-hydroxycoumarin). Furthermore, HPLC-MS analysis of wheat extracts reveals that 7,8-dimethoxycoumarin is more abundant than its monomethyl derivative. The results also show that cold acclimation does not alter the level of TaPRK mRNA or its enzyme activity, and thus ensures the stable generation of ribulose 1,5-biphosphate. PMID:22827600

  9. Phosphorylation, acetylation and methylation modification and the biological activity regulation of nuclear transcription factor NF-κB/RelA%核转录因子NF-κB/RelA的磷酸化、乙酰化和甲基化修饰与活性调控

    Institute of Scientific and Technical Information of China (English)

    王玲; 单保恩; 刘丽宏

    2012-01-01

    RelA是NF-κB家族的重要成员.它通过对靶基因的调节,参与细胞的增殖与转化、凋亡、炎症以及免疫应答等重要的生命活动,同时这些功能受到磷酸化、乙酰化、甲基化等多种翻译后修饰的调控.本文就Re1A的结构、功能及其活性调控做一综述,希望为人们认识RelA的网络调控机制提供新的认识.%RelA is an important transcription factor belonging to NF-KB family. RelA plays critical roles in various cellular responses by regulating the corresponding target genes, including cell proliferation and differentiation, apoptosis, inflammation, and immune response. Meanwhile, these functions of RelA are post-translationally regulated by phosphorylation, acetylation and methylation. Hence, this paper summarizes the current advances in study of the structure, biological functions and activity regulation of RelA. Hopefully, these researches can provide new insights into the network regulatory mechanisms of RelA.

  10. BIOLOGICALLY ACTIVE TRITERPENOIDS USABLE AS PRODRUGS

    Czech Academy of Sciences Publication Activity Database

    Urban, M.; Kvasnica, Miroslav; Dickinson, N.J.; Sarek, J.

    Hauppauge NY : Nova Science Pub. Inc, 2015, s. 25-49. ISBN 978-1-63463-656-8 R&D Projects: GA MŠk(CZ) LO1204; GA MŠk(CZ) LO1304 Institutional support: RVO:61389030 Keywords : triterpenoids * therapeutics * biological activity Subject RIV: EB - Genetics ; Molecular Biology http://site.ebrary.com/lib/alltitles/docDetail.action?docID=11006921

  11. Biologically active substance usable in organic agriculture

    OpenAIRE

    Šircová, Alena

    2012-01-01

    Organic farming system is a model of continuous agricultural activities, in that no synthetic pesticides, herbicides, growth regulators or GMOs may be used for plant protection. Such biological plant protection is allowed, where different antagonistic relationships between individual micro- and macro-organisms and pests occur. Certain biologically active substances contained in plants have a positive effect in protecting plants from pests and diseases as well as extracts from them functio...

  12. Biological Activities of Asparagus Racemosus

    OpenAIRE

    Potduang, Buppachart; Meeploy, Maneerat; Giwanon, Rattanasiri; Benmart, Yaowaluck; Kaewduang, Montree; Supatanakul, Winai

    2008-01-01

    Cytotoxic, antioxidant, tyrosinase inhibitory, antimicrobial activities of the crude ethanol extract of dry powdered roots of Asparagus racemosus (Liliaceae) were investigated. The LC50 to brine shrimp was 2189.49 µg/ml; the EC50 for DPPH radical scavenging was 381.91 µg/ml; the IC50 for tyrosinase inhibition was 7.98 mg/ml. The extract was active at 5–20 mg/ml against various pathogenic microbial (16 species, 18 strains) using the agar dilution assay, with the minimum inhibitory concentratio...

  13. SETD6 lysine methylation of RelA couples GLP activity at chromatin to tonic repression of NF-κB signaling

    OpenAIRE

    Levy, Dan; Kuo, Alex J.; Chang, Yanqi; Schaefer, Uwe; Kitson, Christopher; Cheung, Peggie; Espejo, Alexsandra; Zee, Barry M.; Liu, Chih Long; Tangsombatvisit, Stephanie; Tennen, Ruth I.; Kuo, Andrew Y.; Tanjing, Song; Cheung, Regina; Katrin F. Chua

    2010-01-01

    Protein lysine methylation signaling is implicated in diverse biological and disease processes. Yet the catalytic activity and substrate specificity are unknown for many human protein lysine methyltransferases (PKMTs). We screened over forty candidate PKMTs and identified SETD6 as a methyltransferase that monomethylates chromatin-associated NF-κB RelA at lysine 310 (RelAK310me1). SETD6-mediated methylation rendered RelA inert and attenuated RelA-driven transcriptional programs, including infl...

  14. Measurement of mercury methylation in lake water and sediment samples

    International Nuclear Information System (INIS)

    Biological mercury methylation was assayed by a new radiochemical technique in the water column and sediments of a mercury-contaminated lake. In 24 weeks during 1979, there were three episodes of methylating activity in surface floc and in water, each lasting 3 to 5 weeks. Periods of methylation in the water column coincided with surface sediment methylation and appeared to be related to overall microbial activity. Mercury was actively methylated in the presence of bound sulfide

  15. Erythrocyte membrane stabilization effect and antioxidant activity of methyl methacrylate

    International Nuclear Information System (INIS)

    Methyl methacrylate (MMK) is a synthetic product with mild impact on human health that is not well studied on cellular basis. Here, human erythrocytes were used to investigate the effects MMK exerts on acid and heat-induced hemolysis. Biphasic effect of MMK was observed for acid-induced hemolysis; i.e., protection at low (0 - 0.05% v/v) and stimulation at higher (0.1- 0.4% v/v) concentrations. The maximal protective effect was produced at 0.03% (v/v). At this concentration MMK increased the temperatures of heat denaturation of erythrocyte membrane proteins, spectrin and integral proteins, by about 20C and inhibited the heat-induced hemolysis by 20 %. This membrane stabilization effect of MMK is similar to that produced by some anti-inflammatory and antirheumatic drugs. The increased acid resistance possibly indicated anti-oxidant properties of MMK. The nonenzymatic antioxidant activity test evidenced that MMK has no superoxide dismutase-like activity but demonstrates strong catalase-like activity (about 900 kU/mmol at 0.05-0.1 mmol/l concentration). The results indicate that at low concentration MMK exerts benign effect on cellular membrane that could find therapeutic usage. (author)

  16. SYNTHESIS AND BIOLOGICAL ACTIVITY OF FURAN DERIVATIVES

    Directory of Open Access Journals (Sweden)

    Verma Anupam

    2011-04-01

    Full Text Available Furan derivative are an important class of heterocyclic compound that possess important biological properties. From last few decades a considerable amount of attention has been focussed on synthesis of Furan derivatives and screening them for different pharmacological activities.The furan ring system is the basic skeleton of numerous compounds possessing cardiovascular activities. An iodinated lipophilic furan derivative is widely used in the treatment of ventricular and atrial fibrillation. These moieties are widely employed as antibacterial, antiviral, anti-inflammatory, antifungal, antitumor, Antihyperglycemic, Analgesic, Anticonvulsant etc. Slight change in substitution pattern in furan nucleus causes distinguishable difference in their biological activities. In this review we are discussing about synthesis and various biological activities of newly synthesized furan derivatives.

  17. Xanthane sesquiterpenoids: structure, synthesis and biological activity.

    Science.gov (United States)

    Vasas, Andrea; Hohmann, Judit

    2011-04-01

    The aim of this review is to survey the naturally occurring xanthanes and xanthanolides, their structures, biological activities, structure–activity relationships and synthesis. There has been no comprehensive review of this topic previously. On the basis of 126 references, 112 compounds are summarized. PMID:21321751

  18. 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.

  19. Hemi-methylated DNA regulates DNA methylation inheritance through allosteric activation of H3 ubiquitylation by UHRF1

    Science.gov (United States)

    Harrison, Joseph S; Cornett, Evan M; Goldfarb, Dennis; DaRosa, Paul A; Li, Zimeng M; Yan, Feng; Dickson, Bradley M; Guo, Angela H; Cantu, Daniel V; Kaustov, Lilia; Brown, Peter J; Arrowsmith, Cheryl H; Erie, Dorothy A; Major, Michael B; Klevit, Rachel E; Krajewski, Krzysztof; Kuhlman, Brian; Strahl, Brian D; Rothbart, Scott B

    2016-01-01

    The epigenetic inheritance of DNA methylation requires UHRF1, a histone- and DNA-binding RING E3 ubiquitin ligase that recruits DNMT1 to sites of newly replicated DNA through ubiquitylation of histone H3. UHRF1 binds DNA with selectivity towards hemi-methylated CpGs (HeDNA); however, the contribution of HeDNA sensing to UHRF1 function remains elusive. Here, we reveal that the interaction of UHRF1 with HeDNA is required for DNA methylation but is dispensable for chromatin interaction, which is governed by reciprocal positive cooperativity between the UHRF1 histone- and DNA-binding domains. HeDNA recognition activates UHRF1 ubiquitylation towards multiple lysines on the H3 tail adjacent to the UHRF1 histone-binding site. Collectively, our studies are the first demonstrations of a DNA-protein interaction and an epigenetic modification directly regulating E3 ubiquitin ligase activity. They also define an orchestrated epigenetic control mechanism involving modifications both to histones and DNA that facilitate UHRF1 chromatin targeting, H3 ubiquitylation, and DNA methylation inheritance. DOI: http://dx.doi.org/10.7554/eLife.17101.001 PMID:27595565

  20. 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.

  1. Reactions of 3-formylchromone with active methylene and methyl compounds and some subsequent reactions of the resulting condensation products.

    Science.gov (United States)

    Gasparová, Renata; Lácová, Margita

    2005-01-01

    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 gamma-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. PMID:18007363

  2. 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-phenyl...

  3. Active sensitization and contact allergy to methyl 2-octynoate

    DEFF Research Database (Denmark)

    Heisterberg, Maria Vølund; Vigan, Martine; Johansen, Jeanne Duus

    2010-01-01

    Methyl 2-octynoate is a synthetic fragrance which was first described to have sensitizing properties in 1935. It is one of the 26 fragrances to be labelled on the ingredient list according to current European cosmetics regulation.......Methyl 2-octynoate is a synthetic fragrance which was first described to have sensitizing properties in 1935. It is one of the 26 fragrances to be labelled on the ingredient list according to current European cosmetics regulation....

  4. New biologically active hydrogen sulfide donors.

    Science.gov (United States)

    Roger, Thomas; Raynaud, Francoise; Bouillaud, Frédéric; Ransy, Céline; Simonet, Serge; Crespo, Christine; Bourguignon, Marie-Pierre; Villeneuve, Nicole; Vilaine, Jean-Paul; Artaud, Isabelle; Galardon, Erwan

    2013-11-25

    Generous donors: The dithioperoxyanhydrides (CH3 COS)2 , (PhCOS)2 , CH3 COSSCO2 Me and PhCOSSCO2 Me act as thiol-activated hydrogen sulfide donors in aqueous buffer solution. The most efficient donor (CH3 COS)2 can induce a biological response in cells, and advantageously replace hydrogen sulfide in ex vivo vascular studies. PMID:24115650

  5. 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

  6. BENZIMIDAZOLES: THE LATEST INFORMATION ON BIOLOGICAL ACTIVITIES

    OpenAIRE

    Singh Gurvinder; Kaur Maninderjit; Chander Mohan

    2013-01-01

    Benzimidazole is a heterocyclic aromatic organic compound. It is an important pharmacophore and a privileged structure in medicinal chemistry. Benzimidazole and its derivatives play an important role in medical field with large number of Pharmacological activities such as antimicrobial, antiviral, antidiabetic and anticancer activity. This review is summarized to know about the chemistry of different derivatives of benzimidazoles along with their biological actions such as antioxidant, antimi...

  7. BIOLOGICALLY ACTIVE SUBSTANCES OF SPIRIT PRODUCTION WASTE

    OpenAIRE

    A. S. Kayshev; N. S. Kaysheva

    2014-01-01

    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 ...

  8. Biological activity of SV40 DNA

    International Nuclear Information System (INIS)

    This thesis deals with a study on the biological activity of SV40 DNA. The transforming activity of SV40 DNA and DNA fragments is investigated in order to define as precisely as possible the area of the viral genome that is involved in the transformation. The infectivity of SV40 DNA is used to study the defective repair mechanisms of radiation damages of human xeroderma pigmentosum cells. (C.F.)

  9. Activated Carbon and Biochar Reduce Mercury Methylation Potentials in Aquatic Sediments.

    Science.gov (United States)

    Bussan, Derek D; Sessums, Ryan F; Cizdziel, James V

    2016-04-01

    Much of the toxic methylmercury (MeHg) that biomagnifies in the aquatic food chain and accumulates in fish and seafood is believed to originate from microbial methylation of inorganic Hg(+2) in anoxic sediments. We examined the effect amending wetland sediments with activated carbon and biochar on Hg methylation potentials using microcosms and Hg stable isotope tracers. The inorganic (200)Hg(+2) spike was methylated at ~0.37 %/day in the untreated sediment, but that rate decreased to amended sediments, with 80 % and 88 % reductions in methylation rates for activated carbon and biochar amendments, respectively. Demethylation rates were relatively unchanged. Our key finding is that amending contaminated sediment with activated carbon and biochar decreases bioavailable Hg, and thus may also decrease Hg transfer into food webs. However, further research is needed to evaluate exactly how the sorbents impact Hg methylation rates and for related field studies. PMID:26779648

  10. SYNTHESIS AND BIOLOGICAL ACTIVITY OF PHENOTHIAZINE DERIVATIVES

    Directory of Open Access Journals (Sweden)

    Sinha Shweta

    2011-04-01

    Full Text Available Phenothiazines are heterocyclic molecules containing two benzene rings linked in a tricyclic system through nitrogen and sulfur atoms.Phenothiazine derivatives having amino alkyl side chain and these are connected to the nitrogen atom of heterocyclic unit playing crucial role in medicinal chemistry.From last few decades a considerable amount of attention has been focussed on synthesis of phenothiazines derivatives and screening them for different pharmacological activities. The investigation of substituted 10H-Phenothiazines has steadily strong growth because they exhibit a wide range of applications. These moieties are widely employed as antibacterial, antiviral, anti-inflammatory, anticancer, sedatives, tranquilizers agents etc. Slight change in substitution pattern in phenothiazine nucleus causes distinguishable difference in their biological activities. In this review we are discussing about synthesis and various biological activities of newly synthesized Phenothiazine derivatives.

  11. 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.

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

    OpenAIRE

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

    2012-01-01

    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.

  13. 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. PMID:23015769

  14. Neutron activation analysis of biological substances

    International Nuclear Information System (INIS)

    A Bowen cabbage sample was used as a reference material for the neutron activation studies, and the method was checked by the analysis of other biological substances (blood or serum etc.). For nondestructive measurements also some non-trace elements were determined in order to decide whether the activation analysis is a useful means for such measurements. The new activation analysis procedure was used for biomedical studies as, e.g., for trace element determination in body fluids, and for the analysis of inorganic components in air samples. (R.P.)

  15. Biological activities of selected basidiomycetes from Yemen.

    Science.gov (United States)

    Al-Fatimi, M; Schröder, G; Kreisel, H; Lindequist, U

    2013-03-01

    In a previous paper we demonstrated the results of biological screening of Yemeni basidiomycetes. The present study was aimed to investigate the antimicrobial and the antioxidant activity of further basidiomycetes collected in Yemen. Dichloromethane, methanol and aqueous extracts of the fruiting bodies of 25 species were screened in vitro for their antibacterial activities against three Gram-positive bacteria (Staphyloccocus aureus, Bacillus subtilis, Micrococcus flavus) and two Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), against six human fungal pathogens (Candida albicans, Candida krusei, Aspergillus fumigatus, Mucor sp., Microsporum gypseum, Trichophyton mentagrophytes) and against one non human pathogenic fungus (Candida maltosa). The results indicated that 75 extracts exhibited activity against one or more of the bacteria. The methanol extracts of Agaricus cf. bernardii, Agrocybe pediades, Chlorophyllum molybdites, Coriolopsis polyzona, Ganoderma xylonoides, Pycnoporus sanguineus, Trametes lactinea and Trametes cingulata showed activity against all tested bacteria. The highest antibacterial activity was exhibited by methanol extracts from Chlorophyllum molybdites, Ganoderma xylonoides and Trametes cingulata and Agaricus cf. bernardii, Agrocybe pediades, Coriolopsis polyzona, Pycnoporus sanguineus and Trametes lactinea. The methanol extracts of Chlorophyllum molybdites, Ganoderma xylonoides and Pycnoporus sanguineus showed considerable antifungal activities against the tested fungal strains. Strong antioxidative effects employing the DPPH assay were exhibited by methanol extracts from Chlorophyllum molybdites, Ganoderma xylonoides, Hexagonia velutina, Pycnoporus sanguineus, Trametes lactinea and Trametes cingulata. Our previous and presented studies about 48 basidiomycetes collected in Yemen provide evidence that basidiomycetes from the Arabic region so far should attract more attention as potential source for new biologically active

  16. 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.

  17. 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.

  18. Litchi Flavonoids: Isolation, Identification and Biological Activity

    OpenAIRE

    Jiangrong Li; Yueming Jiang

    2007-01-01

    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 cyanindi...

  19. COTTAGE CHEESE PRODUCTS ENRICHED BIOLOGICALLY ACTIVE ADDITIVES

    OpenAIRE

    Салкинбаева Г. Т.; Байбалинова Г. М.; Смаилова М. Н.

    2015-01-01

    This article deals with a reliable means of improving the structure of supply and optimum balance of the diet of the population, is the use of biologically active additives in a daily diet of the people to food dietary supplements. Supplements such advantages as an expression of food oriented, high nutritional density, homogeneity, easy preparation and forms of transport, good taste allow us to use them successfully in catering.

  20. Alteration of membrane phospholipid methylation by adenosine analogs does not affect T lymphocyte activation

    International Nuclear Information System (INIS)

    Membrane phospholipid methylation has been described during activation of various immune cells. Moreover recent data indicated modulation of immune cells functions by adenosine. As S-adenosyl-methionine and S-adenosyl-homocysteine are adenosine analogs and modulators of transmethylation reactions, the effects of SAH and SAM were investigated on membrane phospholipid methylation and lymphocyte activation. SAM was shown to induce the membrane phospholipid methylation as assessed by the 3Hmethyl-incorporation in membrane extract. This effect was inhibited by SAH. In contrast SAM and SAH did not affect the phytohemagglutinin-induced proliferative response of peripheral blood mononuclear cells. SAH neither modified the early internalization of membrane CD3 antigens nor did it prevent the late expression of HLA-DR antigens on lymphocytes activated by phytohemagglutinin. These results indicate that in vitro alteration of phospholipid methylation does not affect subsequent steps of human T lymphocyte activation and proliferation

  1. Removal efficiency of radioactive methyl iodide on TEDA-impregnated activated carbons

    International Nuclear Information System (INIS)

    Activated carbons were prepared by different series of carbon dioxide and steam activation from walnut shells for their optimal use as radioactive methyl iodide adsorbents in Nuclear Plants. The knowledge of the most favourable textural characteristics of the activated carbons was possible by the previous study of the commercial activated carbon currently used for this purpose. In order to increase their methyl iodide affinity, the effect of triethylenediamine impregnation was studied at 5 and 10 wt.%. The results obtained indicated that in both cases the adsorption efficiency is markedly improved by the addition of impregnant, which allows the adsorbate uptake to occur not only by physical adsorption, via non-specific interactions (as in non-impregnated carbons) but also by the specific interaction of triethylenediamine with radioactive methyl iodide. Methyl iodide retention efficiencies up to 98.1% were achieved. (author)

  2. Removal efficiency of radioactive methyl iodide on TEDA-impregnated activated carbons

    Energy Technology Data Exchange (ETDEWEB)

    Gonzalez-Garcia, C.M.; Gonzalez, J.F.; Roman, S. [Extremadura Univ., Badajoz (Spain). Dept. de Fisica Aplicada

    2011-02-15

    Activated carbons were prepared by different series of carbon dioxide and steam activation from walnut shells for their optimal use as radioactive methyl iodide adsorbents in Nuclear Plants. The knowledge of the most favourable textural characteristics of the activated carbons was possible by the previous study of the commercial activated carbon currently used for this purpose. In order to increase their methyl iodide affinity, the effect of triethylenediamine impregnation was studied at 5 and 10 wt.%. The results obtained indicated that in both cases the adsorption efficiency is markedly improved by the addition of impregnant, which allows the adsorbate uptake to occur not only by physical adsorption, via non-specific interactions (as in non-impregnated carbons) but also by the specific interaction of triethylenediamine with radioactive methyl iodide. Methyl iodide retention efficiencies up to 98.1% were achieved. (author)

  3. Essential oil components and biological activities of Coleus parvifolius leaves

    Directory of Open Access Journals (Sweden)

    Supinya Tewtrakul

    2005-08-01

    Full Text Available The essential oil distilled from the leaves of Coleus parvifolius Benth. (Labiatae was studied by gas chromatography and mass spectrometry (GC-MS. The main components were found to be (E-phytol (42.77%, followed by eicosatrienoate (16.39%, n-tetradecanoic acid (14.42%, octoil (6.54%, 2-methyl-7- octadecyne (5.97%, nonadecane (3.25%, germacrene-D (2.19% and α-humulene (1.42%, respectively. Regarding biological activities, the ethanolic extract of C. parvifolius showed potent antimicrobial activity against gram positive bacteria (Staphylococcus aureus, Bacillus subtilis and B. cereus with inhibition zones of 7-11 mm at a concentration of 10 mg/disc and moderate activity against gram negative bacteria (Salmonella typhi, S. enteritidis and Escherichia coli with inhibition zones of 9-11 mm at 100 mg/disc, whereas it was inactive against fungus, Candida albicans at a concentration of 100 mg/disc. The extract also exhibited strong antioxidant activity (ED50 = 5.87±0.03 μg/ml three times higher than that of butylated hydroxytoluene (BHT, ED50 = 18.08±0.43 μg/ml. Moreover, it was non-toxic to brine shrimp with LC50 value > 1,000 μg/ml.

  4. Radiometallating antibodies and biologically active peptides

    International Nuclear Information System (INIS)

    We have developed methods to radiolabel large molecules, using porphyrins as bifunctional chelating agents for radiometals. The porphyrins are substituted with an N-benzyl group to activate them for radiometallation under mild reaction conditions. Porphyrins that have on functional group for covalent attachment to other molecules cannot cause crosslinking. We have examined the labeling chemistry for antibodies, and we have also developed methods to label smaller biologically active molecules, such as autoantigenic peptides. The autoantigenic peptides, fragments of the acetylcholine receptor, are under investigation for myasthenia gravis research. The methods of covalent attachment of these bifunctional chelating agents to large molecules and the radiometallation chemistry will be discussed

  5. Design and biological properties of iodine-123 labeled β-methyl-branched fatty acids

    International Nuclear Information System (INIS)

    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

  6. 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)

  7. 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.

  8. Transcriptional activity of acetylcholinesterase gene is regulated by DNA methylation during C2C12 myogenesis.

    Science.gov (United States)

    Lau, Kei M; Gong, Amy G W; Xu, Miranda L; Lam, Candy T W; Zhang, Laura M L; Bi, Cathy W C; Cui, D; Cheng, Anthony W M; Dong, Tina T X; Tsim, Karl W K; Lin, Huangquan

    2016-07-01

    The expression of acetylcholinesterase (AChE), an enzyme hydrolyzes neurotransmitter acetylcholine at vertebrate neuromuscular junction, is regulated during myogenesis, indicating the significance of muscle intrinsic factors in controlling the enzyme expression. DNA methylation is essential for temporal control of myogenic gene expression during myogenesis; however, its role in AChE regulation is not known. The promoter of vertebrate ACHE gene carries highly conserved CG-rich regions, implying its likeliness to be methylated for epigenetic regulation. A DNA methyltransferase inhibitor, 5-azacytidine (5-Aza), was applied onto C2C12 cells throughout the myotube formation. When DNA methylation was inhibited, the promoter activity, transcript expression and enzymatic activity of AChE were markedly increased after day 3 of differentiation, which indicated the putative role of DNA methylation. By bisulfite pyrosequencing, the overall methylation rate was found to peak at day 3 during C2C12 cell differentiation; a SP1 site located at -1826bp upstream of mouse ACHE gene was revealed to be heavily methylated. The involvement of transcriptional factor SP1 in epigenetic regulation of AChE was illustrated here: (i) the SP1-driven transcriptional activity was increased in 5-Aza-treated C2C12 culture; (ii) the binding of SP1 onto the SP1 site of ACHE gene was fully blocked by the DNA methylation; and (iii) the sequence flanking SP1 sites of ACHE gene was precipitated by chromatin immuno-precipitation assay. The findings suggested the role of DNA methylation on AChE transcriptional regulation and provided insight in elucidating the DNA methylation-mediated regulatory mechanism on AChE expression during muscle differentiation. PMID:27021952

  9. Biological activities of Curcuma longa L.

    Directory of Open Access Journals (Sweden)

    Araújo CAC

    2001-01-01

    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.

  10. 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

  11. Receiving of iodoinsulin with preserved biological activity

    International Nuclear Information System (INIS)

    The paper presents a method of receiving iodoinsulin with preserved biological activity. As a raw material recrystallized bovine insulin produced by ''Polfa'' was used. Chloramine T was used as an oxidizing agent in the iodize reaction. Insulin was marked with 125I or 127I in the rate of molar concentration of NaI and insulin 0.6. The obtained product contained about 0.3 of iodine atom per one insulin molecule. Specific radioactivity of the iodoinsulin was between 77 and 147 μCi/μg. Such an insulin was in over 95% precipitable with trichloroacetic acid. Its immunological reactivity varied from 89% to 100% while biological activity, determined with the consumption of glucose by the fatty tissue of epididymis of rat, was 92% +- 24% of the native insulin activity. Half-life time of 125I insulin in the rat blood circulation was determined. Curve of the isotope disappearance was biphasic. Half-life time of the first phase (shorter one) was 0.64 +- 0.2 minute while the longer phase 8.89 +- 2.16 minutes. (author)

  12. Phytochemistry and biological activities of Phlomis species.

    Science.gov (United States)

    Limem-Ben Amor, Ilef; Boubaker, Jihed; Ben Sgaier, Mohamed; Skandrani, Ines; Bhouri, Wissem; Neffati, Aicha; Kilani, Soumaya; Bouhlel, Ines; Ghedira, Kamel; Chekir-Ghedira, Leila

    2009-09-01

    The genus Phlomis L. belongs to the Lamiaceae family and encompasses 100 species native to Turkey, North Africa, Europe and Asia. It is a popular herbal tea enjoyed for its taste and aroma. Phlomis species are used to treat various conditions such as diabetes, gastric ulcer, hemorrhoids, inflammation, and wounds. This review aims to summarize recent research on the phytochemistry and pharmacological properties of the genus Phlomis, with particular emphasis on its ethnobotanical uses. The essential oil of Phomis is composed of four chemotypes dominated by monoterpenes (alpha-pinene, limonene and linalool), sesquiterpenes (germacrene D and beta-caryophyllene), aliphalic compounds (9,12,15-octadecatrienoic acid methyl ester), fatty acids (hexadecanoic acid) and other components (trans-phytol, 9,12,15-octadecatrien-1-ol). Flavonoids, iridoids and phenylethyl alcohol constitute the main compounds isolated from Phlomis extracts. The pharmacological activities of some Phlomis species have been investigated. They are described according to antidiabetic, antinociceptive, antiulcerogenic, protection of the vascular system, anti-inflammatory, antiallergic, anticancer, antimicrobial and antioxidant properties. PMID:19563875

  13. NLRP3 Activation Was Regulated by DNA Methylation Modification during Mycobacterium tuberculosis Infection

    Science.gov (United States)

    Wei, Meili; Wang, Lu; Wu, Tao; Xi, Jun; Han, Yuze; Yang, Xingxiang; Zhang, Ding; Fang, Qiang

    2016-01-01

    Mycobacterium tuberculosis (Mtb) infection activates the NLRP3 inflammasome in macrophages and dendritic cells. Much attention has been paid to the mechanisms for regulation of NLRP3 against Mtb. However, whether epigenetic mechanisms participated in NLRP3 activation is still little known. Here we showed that NLRP3 activation was regulated by DNA methylation modification. Mtb infection promoted NLRP3 activation and inflammatory cytokines expression. NLRP3 promoter was cloned and subsequently identified by Dual-Luciferase Reporter System. The results showed that NLRP3 promoter activity was decreased after methylation by DNA methylase Sss I in vitro. Meanwhile, DNA methyltransferases inhibitor DAC could upregulate the expression of NLRP3. Furthermore, promoter region of NLRP3 gene was demethylated after Mtb H37Rv strain infection. These data revealed that DNA methylation was involved in NLRP3 inflammasome activation during Mtb infection and provided a new insight into the relationship between host and pathogens. PMID:27366746

  14. 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.

  15. Reconstructing Causal Biological Networks through Active Learning.

    Science.gov (United States)

    Cho, Hyunghoon; Berger, Bonnie; Peng, Jian

    2016-01-01

    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. PMID:26930205

  16. 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.

  17. Biological activities of Morus celtidifolia leaf extracts.

    Science.gov (United States)

    Viveros-Valdez, Ezequiel; Oranday-Cárdenas, Azucena; Rivas-Morales, Catalina; Verde-Star, María Julia; Carranza-Rosales, Pilar

    2015-07-01

    The aims of this research were to examine the antibacterial, cytotoxic and antiradical/antioxidant activities of the organic extracts obtained from the leaves of the medicinal plant Morus celtidifolia (Family: Moraceae). To evaluate its antimicrobial properties, M. celtidifolia was tested against the bacteria of medical importance: Bacillus subtilis, Staphyloccocus aureus, Enterococcus faecalis, Escherichia coli, Enterobacter cloacae and Enterobacter aerogenes. Cytotoxic activity was assessed by using the brine shrimp (Artemia salina) lethality assay and also by toxicity screening against human cancer cell lines: MCF-7 (human breast adenocarcinoma) and HeLa (cervix adenocarcinoma). The free radical-scavenging activity was determined by the 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) assay. Results revealed that the hexanic extract has antibacterial activity only against Gram positive strains, while the methanolic extract showed better cytotoxic and antioxidant activities than the non- polar extract with a median lethal dose (LD₅₀) of 125μg/ml, 90μg/ml and 75μg/ml against A. salina, MCF-7 and HeLa cells respectively, and median effective concentration (EC₅₀) of 152μg/ml on radical scavenging assay. This is the first study reporting the biological activities of leaves of Morus celtidifolia. PMID:26142508

  18. Aminoderivatives of cycloalkanespirohydantoins: synthesis and biological activity.

    Science.gov (United States)

    Naydenova, Emilia; Pencheva, Nevena; Popova, Julita; Stoyanov, Neyko; Lazarova, Maria; Aleksiev, Boris

    2002-03-01

    3-Aminocycloalkanespiro-5-hydantoins were synthesized and their biological activity was studied. In contrast to hydantoins, these compounds failed to induce either anticonvulsive effects in the central nervous system or inhibitory effects on cholinergic contractions in the enteric nervous system. However, they exerted well pronounced, atropinsensitive, contractile effects on the guinea-pig ileum longitudinal muscle preparations. Structure-activity relationships established allow the assumption that: (i) the reduction of the ring size in the molecule of the spirohydantoins leads to an increase in the potency of the respective analogue to induce contractile effect; (ii) the introduction of -NH2 in position 3 increases the ability of all the compounds studied to exert contractions; (iii) the enlargement of the ring leads to: (1) an increase of the degree of desensitization of the preparations; and (2) a decrease (except 1a) of the potency of the analogues to exert contractile effects. PMID:11989796

  19. 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.

  20. Spectroscopic study of biologically active glasses

    Science.gov (United States)

    Szumera, M.; Wacławska, I.; Mozgawa, W.; Sitarz, M.

    2005-06-01

    It is known that the chemical activity phenomenon is characteristic for some inorganic glasses and they are able to participate in biological processes of living organisms (plants, animals and human bodies). An example here is the selective removal of silicate-phosphate glass components under the influence of biological solutions, which has been applied in designing glasses acting as ecological fertilizers of controlled release rate of the nutrients for plants. The structure of model silicate-phosphate glasses containing the different amounts of the glass network formers, i.e. Ca 2+ and Mg 2+, as a binding components were studied. These elements besides other are indispensable of the normal growth of plants. In order to establish the function and position occupied by the particular components in the glass structure, the glasses were examined by FTIR spectroscopy (with spectra decomposition) and XRD methods. It has been found that the increasing amount of MgO in the structure of silicate-phosphate glasses causes the formation of domains the structure of which changes systematically from a structure of the cristobalite type to a structure corresponding to forsterite type. Whilst the increasing content of CaO in the structure of silicate-phosphate glasses causes the formation of domains the structure of which changes from a structure typical for cristobalite through one similar to the structure of calcium orthophosphate, to a structure corresponding to calcium silicates. The changing character of domains structure is the reason of different chemical activity of glasses.

  1. In vivo activation of methyl-coenzyme M reductase by carbon monoxide

    OpenAIRE

    Zhou, Yuzhen; Dorchak, Alexandria E.; Ragsdale, Stephen W.

    2013-01-01

    Methyl-coenzyme M reductase (MCR) from methanogenic archaea catalyzes the rate-limiting and final step in methane biosynthesis. Using coenzyme B as the two-electron donor, MCR reduces methyl-coenzyme M (CH3-SCoM) to methane and the mixed disulfide, CoBS-SCoM. MCR contains an essential redox-active nickel tetrahydrocorphinoid cofactor, Coenzyme F430, at its active site. The active form of the enzyme (MCRred1) contains Ni(I)-F430. Rapid and efficient conversion of MCR to MCRred1 is important fo...

  2. In vivo activation of methyl-coenzyme M reductase by carbon monoxide

    OpenAIRE

    StephenWileyRagsdale

    2013-01-01

    Methyl-coenzyme M reductase (MCR) from methanogenic archaea catalyzes the rate-limiting and final step in methane biosynthesis. Using coenzyme B (CoBSH) as the two-electron donor, MCR reduces methyl-coenzyme M (CH3-SCoM) to methane and the mixed disulfide, CoBS-SCoM. MCR contains an essential redox-active nickel tetrahydro¬corphinoid cofactor, Coenzyme F430, at its active site. The active form of the enzyme (MCRred1) contains Ni(I)-F430. Rapid and efficient conversion of MCR to MCRred1 i...

  3. 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)

  4. Synthesis and cytotoxic activity of N-((2-methyl-4(3H)-quinazolinon-6-yl)methyl)dithiocarbamates.

    Science.gov (United States)

    Cao, Sheng-Li; Wang, Yao; Zhu, Lin; Liao, Ji; Guo, Yan-Wen; Chen, Lin-Lin; Liu, Hong-Qin; Xu, Xingzhi

    2010-09-01

    A series of N-((2-methyl-4(3H)-quinazolinon-6-yl)methyl)dithiocarbamates 5a-w were synthesized and evaluated for their cytotoxic activity against five human cancer cell lines. We found that compound 5k inhibited proliferation of A549, MCF-7, HeLa, HT29 and HCT-116 cells with IC(50) values of 5.44, 7.15, 12.16, 10.35 and 11.44 microM, respectively. Compound 5i was the most potent with an IC(50) value of 3.65 microM against proliferation of MCF-7 cells, while 5n was the most potent with an IC(50) value of 5.09 microM against proliferation of A549 cells. Cell cycle analysis showed that both 5i and 5k arrested A549 cells at S and G2/M phases, suggesting that these compounds act through mechanisms different from 5-fluorouracil, which arrests cells at S phase only. PMID:20538385

  5. 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.

  6. Biological activity of ruthenium nitrosyl complexes.

    Science.gov (United States)

    Tfouni, Elia; Truzzi, Daniela Ramos; Tavares, Aline; Gomes, Anderson Jesus; Figueiredo, Leonardo Elias; Franco, Douglas Wagner

    2012-01-01

    Nitric oxide plays an important role in various biological processes, such as neurotransmission, blood pressure control, immunological responses, and antioxidant action. The control of its local concentration, which is crucial for obtaining the desired effect, can be achieved with exogenous NO-carriers. Coordination compounds, in particular ruthenium(III) and (II) amines, are good NO-captors and -deliverers. The chemical and photochemical properties of several ruthenium amine complexes as NO-carriers in vitro and in vivo have been reviewed. These nitrosyl complexes can stimulate mice hippocampus slices, promote the lowering of blood pressure in several in vitro and in vivo models, and control Trypanosoma cruzi and Leishmania major infections, and they are also effective against tumor cells in different models of cancer. These complexes can be activated chemically or photochemically, and the observed biological effects can be attributed to the presence of NO in the compound. Their efficiencies are explained on the basis of the [Ru(II)NO(+)](3+)/[Ru(II)NO(0)](2+) reduction potential, the specific rate constant for NO liberation from the [RuNO](2+) moiety, and the quantum yield of NO release. PMID:22178685

  7. 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.

  8. Effect of pesticide applications on soil microbial activity and on 14C-methyl parathion dissipation

    International Nuclear Information System (INIS)

    Some crops, as cotton, need different pesticide application to control pests and diseases. These compounds reach soil and may affect the soil microbial activity. As the microorganisms play important role on the nutrient cycling, changes in their activities may affect the soil fertility. The influence of several pesticides on soil microbial activity of the 0-15 cm and 15-30 cm depth of the soil profile, and the 14C-methyl parathion dissipation was studied under influence of other pesticide applications. The influence of pesticides on the microorganisms was followed in an experimental area of the Instituto Biologico, that was divided in two subareas, both under cotton crop. Columns of PVC was buried in both subareas and a solution of 14C-methyl parathion diluted in the technical compound was applied on the soil surface of each column. One subarea received all the recommended pesticides for the cotton crop besides the 14C-methyl parathion. The other subarea received only 14C-methyl parathion solution on the columns soil surface. The soil microbial activity of both subareas was estimated by measurements of dehydrogenase, arylsulfatase and arginine deaminase enzymes. Further, the availability of total nitrogen in the soil was also measured. The dissipation of 14C-methyl parathion was studied by radiocarbon recovery in soil extracts and combustion of extracted soil and quantification by radiometric techniques. (author)

  9. Nonexercise activity thermogenesis (NEAT): environment and biology.

    Science.gov (United States)

    Levine, James A

    2004-05-01

    Nonexercise activity thermogenesis (NEAT) is the energy expended for everything that is not sleeping, eating, or sports-like exercise. It includes the energy expended walking to work, typing, performing yard work, undertaking agricultural tasks, and fidgeting. NEAT can be measured by one of two approaches. The first is to measure or estimate total NEAT. Here, total daily energy expenditure is measured, and from it "basal metabolic rate-plus-thermic effect of food" is subtracted. The second is the factoral approach, whereby the components of NEAT are quantified, and total NEAT is calculated by summing these components. The amount of NEAT that humans perform represents the product of the amount and types of physical activities and the thermogenic cost of each activity. The factors that impact a human's NEAT are readily divisible into environmental factors, such as occupation or dwelling within a "concrete jungle," and biological factors such as weight, gender, and body composition. The combined impact of these factors explains the substantial variance in human NEAT. The variability in NEAT might be viewed as random, but human and animal data contradict this. It appears that changes in NEAT subtly accompany experimentally induced changes in energy balance and are important in the physiology of weight change. Inadequate modulation of NEAT plus a sedentary lifestyle may thus be important in obesity. It then becomes intriguing to dissect mechanistic studies that delineate how NEAT is regulated into neural, peripheral, and humoral factors. A scheme is described in this review in which NEAT corresponds to a carefully regulated "tank" of physical activity that is crucial for weight control. PMID:15102614

  10. 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.

  11. Activity of cell wall degrading glycanases in methyl jasmonate-induced leaf abscission in Kalanchoe blossfeldiana

    Directory of Open Access Journals (Sweden)

    Marian Saniewski

    2013-12-01

    Full Text Available It was found previously that methyl jasmonate (JA-Me induced leaf abscission in Kalanchoe blossfeldiana. In present studies it was shown that JA-Me markedly increased the total activities of cellulase, polygalacturonase, pectinase and xylanase in petioles, but did not affect activities of these enzymes in the blades and apical part of shoots of K. blossfeldiana. These results suggest that methyl jasmonate promotes the degradation of cell wall polysaccharides in the abscission zone and in this way induces leaf abscission in Kalanchoe blossfeldiana.

  12. The Pharmacological Activities of the Metabolites of N-[(Trimethylamineboryl)-Carbonyl]-L-Phenylalanine Methyl Ester

    OpenAIRE

    Miller, M. C.III; Sood, A.; Spielvogel, B. F.; Shrewsbury, R. P.; Hall, I. H.

    1996-01-01

    The metabolites of N-[(trimethylamineboryl)-carbonyl]-L-phenylalanine methyl ester 1 proved to be active in a number of pharmacological screens where the parent had previously demonstrated potent activity. The proposed metabolites demonstrated significant activity as cytotoxic, hypolipidemic, and anti-inflammatory agents. In cytotoxicity screens several of the proposed metabolites afforded better activity than the parent compound against the growth of suspended and solid tumor cell lines. Eva...

  13. Potential biological activity of acacia honey.

    Science.gov (United States)

    Muhammad, Aliyu; Odunola, Oyeronke A; Ibrahim, Mohammed A; Sallau, Abdullahi B; Erukainure, Ochuko L; Aimola, Idown A; Malami, Ibrahim

    2016-01-01

    Recent advances in functional foods-based research have increasingly become an area of major interest because it affects human health and activities. Functional foods are classes of foods with health promoting and disease preventing properties in addition to multiple nutritional values and of such type is honey. Acacia honey is a type of honey produced by bees (Apis mellifera) fed on Acacia flowers, hence the name. This review focuses on the potential biological activities of Acacia honey which includes quality, antioxidant, immuno-modulatory, antiproliferative and neurological properties at in vitro and in vivo levels. Based on our review, Acacia honey used from various researches is of high purity, contains some bioactive compounds ranging from vitamins, phenolics, flavonoids and fatty acids. It's highly nutritional with strong antioxidant and immuno-modulatory potentials which may therefore be considered a potential candidate for both cancer prevention and treatment. Neurologically, it may be considered as a viable therapeutic agent in the management of Alzheimer's disease. PMID:26709666

  14. Biological Activities of Plant Pigments Betalains.

    Science.gov (United States)

    Gandía-Herrero, Fernando; Escribano, Josefa; García-Carmona, Francisco

    2016-04-25

    Betalains are a family of natural pigments present in most plants of the order Caryophyllales. They provide colors ranging from yellow to violet to structures that in other plants are colored by anthocyanins. These include not only edible fruits and roots but also flowers, stems, and bracts. The recent characterization of different bioactivities in experiments with betalain containing extracts and purified pigments has renewed the interest of the research community in these molecules used by the food industry as natural colorants. Studies with multiple cancer cell lines have demonstrated a high chemopreventive potential that finds in vitro support in a strong antiradical and antioxidant activity. Experiments in vivo with model animals and bioavailability studies reinforce the possible role played by betalains in the diet. This work provides a critical review of all the claimed biological activities of betalains, showing that the bioactivities described might be supported by the high antiradical capacity of their structural unit, betalamic acid. Although more investigations with purified compounds are needed, the current evidences suggest a strong health-promoting potential. PMID:25118005

  15. 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.

  16. 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

  17. 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.

  18. Biological implications and therapeutic significance of DNA methylation regulated genes in cervical cancer.

    Science.gov (United States)

    Bhat, Samatha; Kabekkodu, Shama Prasada; Noronha, Ashish; Satyamoorthy, Kapaettu

    2016-02-01

    Cervical cancer is the second most common cancer among women worldwide. About 528,000 women are diagnosed with cervical cancer contributing to around 266,000 deaths, across the globe every year. Out of these, the burden of 226,000 (85%) deaths occurs in the developing countries, who are less resource intensive to manage the disease. This is despite the fact that cervical cancer is amenable for early detection due to its long and relatively well-known natural history prior to its culmination as invasive disease. Infection with high risk human papillomavirus (hrHPVs) is essential but not sufficient to cause cervical cancer. Although it was thought that genetic mutations alone was sufficient to cause cervical cancer, the current epidemiological and molecular studies have shown that HPV infection along with genetic and epigenetic changes are frequently associated and essential for initiation, development and progression of the disease. Moreover, aberrant DNA methylation in host and HPV genome can be utilized not only as biomarkers for early detection, disease progression, diagnosis and prognosis of cervical cancer but also to design effective therapeutic strategies. In this review, we focus on recent studies on DNA methylation changes in cervical cancer and their potential role as biomarkers for early diagnosis, prognosis and targeted therapy. PMID:26743075

  19. Protease activated receptors (PARS) mediation in gyroxin biological activity

    International Nuclear Information System (INIS)

    Gyroxin is a serine protease enzyme from the South American rattlesnake (Crotalus durissus terrificus) venom; it is only partially characterized and has multiple activities. Gyroxin induces blood coagulation, blood pressure decrease and a neurotoxic behavior named barrel rotation. The mechanisms involved in this neurotoxic activity are not known. Whereas gyroxin is a member of enzymes with high potential to become a new drug with clinical applications such as thrombin, batroxobin, ancrod, tripsyn and kalicrein, it is important to find out how gyroxin works. The analysis on agarose gel electrophoresis and circular dichroism confirmed the molecules' integrity and purity. The gyroxin intravenous administration in mice proved its neurotoxicity (barrel rotation). In vivo studies employing intravital microscopy proved that gyroxin induces vasodilation with the participation of protease activated receptors (PARs), nitric oxide and Na+K+ATPase. The leukocytes' adherence and rolling counting indicated that gyroxin has no pro inflammatory activity. Gyroxin induced platelet aggregation, which was blocked by inhibitors of PAR1 and PAR4 receptors (SCH 79797 and tcY-NH2, respectively). Finally, it was proved that the gyroxin temporarily alter the permeability of the blood brain barrier (BBB). Our study has shown that both the protease-activated receptors and nitric oxide are mediators involved in the biological activities of gyroxin. (author)

  20. 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...

  1. Synthesis, Characterization and Antimicrobial Activity of Methyl 1-(-2-amine-alkylcarbonyl piperidine-4-carboxylate

    Directory of Open Access Journals (Sweden)

    Nimavat K

    2013-04-01

    Full Text Available A series of Methyl 1-(-2-amine-alkylcarbonyl piperidine-4-carboxylate derivatives of amino acids (3aewas synthesized. These new derivative was achieved by treating Isonipecotic acid methyl ester (1with Boc-protected amino acids (2a-e using CDI as coupling reagent in MDC at room temperature.Further deprotection with HCl/Dioxane gives the desired product. Structures of the synthesizedcompounds were established on the basis of spectral and elemental analysis. The synthesizedcompounds were screened for antimicrobial activity.

  2. Anti-Inflammatory Activity of Methyl Salicylate Glycosides Isolated from Gaultheria yunnanensis (Franch. Rehder

    Directory of Open Access Journals (Sweden)

    Guan-Hua Du

    2011-05-01

    Full Text Available Gaultheria yunnanensis (Franch. Rehder is a kind of traditional Chinese herbal medicine used for the treatments of rheumatoid arthritis, swelling and pain. Two methyl salicylate glycosides, namely methyl benzoate-2-O-b-D-xylopyranosyl(1-6-O-b-D-gluco-pyranoside (J12122 and methyl benzoate-2-O-β-D-xylopyranosyl(1-2[O-β-D-xylopyranosyl(1-6]-O-β-D-glucopyranoside (J12123, are natural salicylic derivatives isolated from Gaultheria yunnanensis. In this study, we investigated the anti-inflammatory activity of J12122 and J12123 on LPS-induced RAW264.7 macrophage cells by measuring the production of pro-inflammatory cytokines, accumulation of nitric oxide (NO, and level of reactive oxygen species (ROS. The results showed that both methyl salicylate glycosides dose-dependently inhibited the production of tumor necrosis factor-α (TNF-α, interleukin-1β (IL-1β, and IL-6, respectively. Consistent with these observations, J12122 and J12123 significantly suppressed the accumulation of NO, with an inhibitory rate of 56.20% and 51.72% at 3.0 μg/mL concentration, respectively. Furthermore, the two methyl salicylate glycosides reduced the level of ROS induced by LPS. These results showed that the isolated compounds possess anti-inflammatory properties through inhibition the production pro-inflammatory cytokines, NO, and ROS.

  3. Anti-inflammatory activity of methyl salicylate glycosides isolated from Gaultheria yunnanensis (Franch.) Rehder.

    Science.gov (United States)

    Zhang, Dan; Liu, Rui; Sun, Lan; Huang, Chao; Wang, Chao; Zhang, Dong-Ming; Zhang, Tian-Tai; Du, Guan-Hua

    2011-01-01

    Gaultheria yunnanensis (Franch.) Rehder is a kind of traditional Chinese herbal medicine used for the treatments of rheumatoid arthritis, swelling and pain. Two methyl salicylate glycosides, namely methyl benzoate-2-O-β-D-xylopyranosyl(1-6)-O-β-D-gluco-pyranoside (J12122) and methyl benzoate-2-O-β-D-xylopyranosyl(1-2)[O-β-D-xylopyranosyl(1-6)]-O-β-D-glucopyranoside (J12123), are natural salicylic derivatives isolated from Gaultheria yunnanensis. In this study, we investigated the anti-inflammatory activity of J12122 and J12123 on LPS-induced RAW264.7 macrophage cells by measuring the production of pro-inflammatory cytokines, accumulation of nitric oxide (NO), and level of reactive oxygen species (ROS). The results showed that both methyl salicylate glycosides dose-dependently inhibited the production of tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and IL-6, respectively. Consistent with these observations, J12122 and J12123 significantly suppressed the accumulation of NO, with an inhibitory rate of 56.20% and 51.72% at 3.0 μg/mL concentration, respectively. Furthermore, the two methyl salicylate glycosides reduced the level of ROS induced by LPS. These results showed that the isolated compounds possess anti-inflammatory properties through inhibition the production pro-inflammatory cytokines, NO, and ROS. PMID:21555977

  4. Process optimization for methyl ester production from waste cooking oil using activated carbon supported potassium fluoride

    Energy Technology Data Exchange (ETDEWEB)

    Hameed, B.H.; Goh, C.S.; Chin, L.H. [School of Chemical Engineering, Engineering Campus, Universiti Sains Malaysia, 14300 Nibong Tebal, Penang (Malaysia)

    2009-12-15

    This paper presents the transesterification of waste cooking palm oil (WCO) using activated carbon supported potassium fluoride catalyst. A central composite rotatable design was used to optimize the effect of molar ratio of methanol to oil, reaction period, catalyst loading and reaction temperature on the transesterification process. The reactor was pressurized up to 10 bar using nitrogen gas. All the variables were found to affect significantly the methyl ester yield where the most effective factors being the amount of catalyst and reaction temperature, followed by methanol to oil ratio. A quadratic polynomial equation was obtained for methyl ester yield by multiple regression analysis using response surface methodology (RSM). The optimum condition for transesterification of WCO to methyl ester was obtained at 3 wt.% amount of catalyst, 175 C temperature, 8.85 methanol to oil molar ratio and 1 h reaction time. At the optimum condition, the predicted methyl ester yield was 83.00 wt.%. The experimental value was well within the estimated value of the model. The catalyst showed good performance with a high yield of methyl ester and the separation of the catalyst from the liquid mixture is easy. (author)

  5. Lysine methylation of HIV-1 Tat regulates transcriptional activity of the viral LTR

    Directory of Open Access Journals (Sweden)

    Flynn Elizabeth K

    2008-05-01

    Full Text Available Abstract Background The rate of transcription of the HIV-1 viral genome is mediated by the interaction of the viral protein Tat with the LTR and other transcriptional machinery. These specific interactions can be affected by the state of post-translational modifications on Tat. Previously, we have shown that Tat can be phosphorylated and acetylated in vivo resulting in an increase in the rate of transcription. In the present study, we investigated whether Tat could be methylated on lysine residues, specifically on lysine 50 and 51, and whether this modification resulted in a decrease of viral transcription from the LTR. Results We analyzed the association of Tat with histone methyltransferases of the SUV39-family of SET domain containing proteins in vitro. Tat was found to associate with both SETDB1 and SETDB2, two enzymes which exhibit methyltransferase activity. siRNA against SETDB1 transfected into cell systems with both transient and integrated LTR reporter genes resulted in an increase in transcription of the HIV-LTR in the presence of suboptimal levels of Tat. In vitro methylation assays with Tat peptides containing point mutations at lysines 50 and 51 showed an increased incorporation of methyl groups on lysine 51, however, both residues indicated susceptibility for methylation. Conclusion The association of Tat with histone methyltransferases and the ability for Tat to be methylated suggests an interesting mechanism of transcriptional regulation through the recruitment of chromatin remodeling proteins to the HIV-1 promoter.

  6. 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.

  7. Parametric study on removal efficiency of impregnated activated charcoal and silver zeolite for radioactive methyl iodide

    International Nuclear Information System (INIS)

    The removal efficiency of impregnated activated charcoal and silver zeolite for radioactive methyl iodide is influenced by various parameters such as temperature, relative humidity, face velocity and packing density. This study is to evaluate the dependency of the removal efficiency on each parameter and these combined parameters, quantitatively. Four types of adsorbents, BC-727, AgX, CHC-50 and SS 208C 5KI3, were tested. From experimental data and mass transfer theory, an experimental equation for evaluating the removal efficiency of adsorbents was derived under a series of experiments for radioactive methyl iodine-131. It was concluded that the removal efficiency calculated from the experimental equation agreed well with the experimental value. Effects of experimental specific parameters, such as Pre-flow time, methyl iodide injection time and After-flow time, on the removal efficiency of adsorbent are also described

  8. Syntheses and biological activities of 13-substituted avermectin aglycons.

    Science.gov (United States)

    Mrozik, H; Linn, B O; Eskola, P; Lusi, A; Matzuk, A; Preiser, F A; Ostlind, D A; Schaeffer, J M; Fisher, M H

    1989-02-01

    The reactions of sulfonate esters of the allylic/homoallylic 13-alcohol of 5-O-(tert-butyldimethylsilyl)-22,23-dihydroavermectin B1a aglycon (1a) were investigated. Nucleophilic substitution gave 13 beta-chloro and 13 beta-iodo derivatives, while solvolytic reaction conditions yielded 13 alpha-methoxy, 13 alpha-fluoro, and 13 alpha-chloro products. A mixture of 13 alpha- and 13 beta-fluorides was obtained upon reaction with DAST. The 13 beta-iodide gave, upon elimination with lutidine, the 8(9),10(11),12(13),14(15)-tetraene. The 13 beta-alcohol and the rearranged 15-ol 13(14)-ene and 15-amino 13(14)-ene derivatives were obtained by substitution via the allylic carbonium ion. MEM ethers 11 and 12 of the two epimeric 13-ols were prepared by alkylation with MEM chloride. In contrast, methylation of 1a with MeI and Ag2O in CH2Cl2 occurred exclusively at the tertiary 7-hydroxy group and not at the secondary 13 alpha-ol. Oxidation of the allylic alcohol 1a proceeded under Swern conditions but not with MnO2 to the 13-oxo aglycon, which was reduced by NaBH4 exclusively to the natural 13 alpha-ol, while reductive amination with NaCNBH3-NH4OAc gave the 13 alpha-amine. The methoxime derivative was obtained in the form of the two geometric isomers. Anthelmintic activities against the sheep nematode Trichostrongylus colubriformis, miticidal activities against the two-spotted spider mite (Tetranychus urticae), and insecticidal activities against the southern armyworm (Spodoptera eridania) as well as the binding constants to a free living nematode (Caenorhabditis elegans) derived receptor assay were obtained and compared to avermectin B1a, 22,23-dihydroavermectin B1a, and the 13-deoxy-22,23-dihydroavermectin B1 aglycon related to the milbemycins. None of the newly prepared derivatives exceeded the potency of the three reference compounds. Lipophilic 13-substituents such as halogen, alkoxy, and methoxime retained high biological activities in all assays, while the more polar

  9. 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.

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

    International Nuclear Information System (INIS)

    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. 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. 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. 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 methylation at these repressive regions may provide an attractive

  11. Reconstructing Causal Biological Networks through Active Learning

    OpenAIRE

    Cho, Hyunghoon; Berger, Bonnie; Peng, Jian

    2016-01-01

    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 ...

  12. Methionine sulfoxide reductase regulates brain catechol-O-methyl transferase activity

    OpenAIRE

    Moskovitz, Jackob; Walss-Bass, Consuelo; Cruz, Dianne A.; Thompson, Peter M.; Bortolato, Marco

    2014-01-01

    Catechol-O-methyl transferase (COMT) plays a key role in the degradation of brain dopamine (DA). Specifically, low COMT activity results in higher DA levels in the prefrontal cortex (PFC), thereby reducing the vulnerability for attentional and cognitive deficits in both psychotic and healthy individuals. COMT activity is markedly reduced by a non-synonymous SNP that generates a valine-to-methionine substitution on the residue 108/158, by means of as-yet incompletely understood posttranslation...

  13. Adsorption of doxorubicin on poly (methyl methacrylate) -chitosan-heparin coated activated carbon beads

    OpenAIRE

    Miao, Jianjun; Zhang, Fuming; Takieddin, Majde; Mousa, Shaker; Linhardt, Robert J.

    2012-01-01

    Extracorporeal filter cartridges, filled with activated carbon bead (ACB) adsorbent, have been used for removal of overdosed cancer drugs from the blood. Coatings on adsorbent matrices, poly (methyl methacrylate) (PMMA)/activated carbon bead and PMMA/chitosan/heparin/ACB composites, were tested to improve their biocompatibility and blood compatibility. PMMA coating on ACBs was accomplished in a straightforward manner using a PMMA solution in ethyl acetate. One-step hybrid coating of ACBs with...

  14. 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. PMID:25496282

  15. Endogenous neurotransmitter activates N-methyl-D-aspartate receptors on differentiating neurons in embryonic cortex.

    OpenAIRE

    Blanton, M G; Lo Turco, J J; Kriegstein, A R

    1990-01-01

    Before synapses form in embryonic turtle cerebral cortex, an endogenous neurotransmitter activates N-methyl-D-aspartate (NMDA) channels on neurons in the cortical plate. Throughout cortical development, these channels exhibit voltage-dependent Mg2+ blockade and are antagonized by D-2-amino-5-phosphonovaleric acid, a selective NMDA receptor antagonist. The activation in situ of these nonsynaptic NMDA channels demonstrates a potential physiological substrate for control of early neuronal differ...

  16. Parametric investigations on the retention of methyl iodide by a KI-impregnated activated carbon

    International Nuclear Information System (INIS)

    Investigations are described on the retention of methyl iodide (CH3I-131) by a typical batch of the activated carbon 207B (KI) which is mostly used in the iodine filters of German nuclear power plants. The results obtained with variation of about ten parameters are relevant both for the testing of activated carbons and for the design, operation and surveillance of iodine filters. (orig./HP)

  17. 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.

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

    Science.gov (United States)

    Howard, Timothy D; Mathias, Rasika A; Seeds, Michael C; Herrington, David M; Hixson, James E; Shimmin, Lawrence C; Hawkins, Greg A; Sellers, Matthew; Ainsworth, Hannah C; Sergeant, Susan; Miller, Leslie R; Chilton, Floyd H

    2014-01-01

    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. PMID:24842322

  19. Chlropyrifos-methyl shows anti-androgenic activity without estrogenic activity in rats

    International Nuclear Information System (INIS)

    Chlorpyrifos-methyl (CPM), an organophosphate insecticide, widely used for grain storage and agriculture, has been suspected as endocrine disrupter by a few in vitro studies. This study was performed to investigate the (anti-) estrogenicity and (anti-) androgenicity of CPM in vivo using immature rat uterotrophic assay and rat Hershberger assay. CPM with or without 17β-estradiol were administered to 20 days old female rats to investigate its (anti-) estrogenic activity. Uterine and vaginal weight, uterine epithelial cell height were not affected by the treatment of CPM (2, 10, 50, 250 mg/kg). CPM 250 mg/kg potentiated relative vagina weight in 17β-estradiol treated immature female rats without any changing of uterine weight. Relative liver weight was increased with decrease of body weight by CPM 250 mg/kg treatment. Uterine cell proliferation tested with bromodeoxyuridine labeling index was not observed in CPM treated rats. CPM with or without testosterone propionate were administered to castrated rat of 51 days old for 10 days to investigate the (anti-)androgenic activity,. The weight of relative and absolute androgen-dependent accessory sex organs; seminal vesicle with coagulating glands (SV/CG), ventral prostate gland (VP), glans penis (GP), levator ani plus bulbocarvernosus muscle (LABC) and Cowper's gland (CG,) were unchanged by the treatment of CPM alone. While CPM induced the increase of relative adrenal gland weight, CPM 50 mg/kg decreased the weights of CV/CG, VP, CG and LABC without change of GP without changing of GP when it was treated with TP. In conclusion, CPM dose not show estrogenic and anti-estrogenic activity in immature female rats, but it represents anti-androgenic activity by inhibition of the TP-stimulated increase of the weight of accessory sex organs

  20. Kinetic modeling of the purging of activated carbon after short term methyl iodide loading

    International Nuclear Information System (INIS)

    A bimolecular reaction model containing the physico-chemical parameters of the adsorption and desorption was developed earlier to describe the kinetics of methyl iodide retention by activated carbon adsorber. Both theoretical model and experimental investigations postulated constant upstream methyl iodide concentration till the maximum break-through. The work reported here includes the extension of the theoretical model to the general case when the concentration of the challenging gas may change in time. The effect of short term loading followed by purging with air, and an impulse-like increase in upstream gas concentration has been simulated. The case of short term loading and subsequent purging has been experimentally studied to validate the model. The investigations were carried out on non-impregnated activated carbon. A 4 cm deep carbon bed had been challenged by methyl iodide for 30, 90, 120 and 180 min and then purged with air, downstream methyl iodide concentration had been measured continuously. The main characteristics of the observed downstream concentration curves (time and slope of break-through, time and amplitude of maximum values) showed acceptable agreement with those predicted by the model

  1. 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

  2. Activation and transfer of sulfate in biological systems (1960)

    International Nuclear Information System (INIS)

    It examines in this review the successive stages of active sulfate formation and its role in biological synthesis of sulfuric esters. The possible role of active sulfate as intermediary in sulfate reduction is also discussed. (author)

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

    Czech Academy of Sciences Publication Activity Database

    Loza-Muller, L.; Rodriguez-Corona, U.; Sobol, Margaryta; Rodriguez-Zapata, L.C.; Hozák, Pavel; Castano, E.

    2015-01-01

    Roč. 6, Nov 6 (2015). ISSN 1664-462X R&D Projects: GA ČR GAP305/11/2232; GA ČR GA15-08738S; GA MPO FR-TI3/588; GA TA ČR(CZ) TE01020118; GA MŠk(CZ) ED1.1.00/02.0109 Institutional support: RVO:68378050 Keywords : histones * methylation * RNA polymerase I * Brassica * phosphoinositide Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 3.948, year: 2014

  4. 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.

  5. Preparation, spectral, thermal, and biological properties of zinc(II) 4-chloro- and 5-chlorosalicylate complexes with methyl 3-pyridylcarbamate and phenazone

    Czech Academy of Sciences Publication Activity Database

    Bujdošová, Z.; Gyoryova, K.; Hudecová, D.; Kovářová, Jana; Halás, L.

    2010-01-01

    Roč. 64, č. 5 (2010), s. 584-591. ISSN 0366-6352 Institutional research plan: CEZ:AV0Z40500505 Keywords : zinc(II) chlorosalicylate * methyl 3-pyridylcarbamate * phenazone * thermal stability * biological properties Subject RIV: CD - Macromolecular Chemistry Impact factor: 0.754, year: 2010

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

    OpenAIRE

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

    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 signific...

  7. 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

  8. Studies on the Synthesis, Characterization, DNA Binding, Cytotoxicity and Antioxidant activity of 2-methyl-4-nitrophenylferrocene

    International Nuclear Information System (INIS)

    We report herein the synthesis, structural characterization, DNA binding, BamH1 digestion, cytotoxicity and antioxidant activity of 2-methyl-4-nitrophenylferrocene. Structural characterization is based on multinuclear (1H and 13C) NMR, FT-IR spectroscopy and elemental analysis. Interaction of 2-methyl-4-nitrophenylferrocene with pBR322 plasmid DNA shows noncovalent interactions however these noncovalent interactions reveal the prevention of BamH1 restriction site (g/ggtcc). In the voltammogram, a negative shift in peak potential has been observed on addition of increasing concentration of CT-DNA, which shows electrostatic interaction for 2-methyl-4-nitrophenylferro with negatively charged phosphate of DNA backbone. The binding ratio, binding constant, binding free energy and diffusion coefficient of free and bound drug were calculated to understand the mechanism. The high negative value of -delta G signifies the spontaneity and high conformational stability of 2-methyl-4-nitrophenylferro with CT-DNA. The compound has the ability to scavenge free radicals as have been revealed by DPPH findings. (author)

  9. 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.

  10. 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.

  11. Tissue culture-induced transpositional activity of mPing is correlated with cytosine methylation in rice

    Directory of Open Access Journals (Sweden)

    Pang Jinsong

    2009-07-01

    Full Text Available Abstract Background mPing is an endogenous MITE in the rice genome, which is quiescent under normal conditions but can be induced towards mobilization under various stresses. The cellular mechanism responsible for modulating the activity of mPing remains unknown. Cytosine methylation is a major epigenetic modification in most eukaryotes, and the primary function of which is to serve as a genome defense system including taming activity of transposable elements (TEs. Given that tissue-culture is capable of inducing both methylation alteration and mPing transposition in certain rice genotypes, it provides a tractable system to investigate the possible relationship between the two phenomena. Results mPing transposition and cytosine methylation alteration were measured in callus and regenerated plants in three rice (ssp. indica genotypes, V14, V27 and R09. All three genotypes showed transposition of mPing, though at various frequencies. Cytosine methylation alteration occurred both at the mPing-flanks and at random loci sampled globally in callus and regenerated plants of all three genotypes. However, a sharp difference in the changing patterns was noted between the mPing-flanks and random genomic loci, with a particular type of methylation modification, i.e., CNG hypermethylation, occurred predominantly at the mPing-flanks. Pearson's test on pairwise correlations indicated that mPing activity is positively correlated with specific patterns of methylation alteration at random genomic loci, while the element's immobility is positively correlated with methylation levels of the mPing's 5'-flanks. Bisulfite sequencing of two mPing-containing loci showed that whereas for the immobile locus loss of CG methylation in the 5'-flank was accompanied by an increase in CHG methylation, together with an overall increase in methylation of all three types (CG, CHG and CHH in the mPing-body region, for the active locus erasure of CG methylation in the 5'-flank was

  12. First synthesis of racemic saphenamycin and its enantiomers. Investigation of biological activity

    DEFF Research Database (Denmark)

    Laursen, Jane B.; Jorgensen, C.G.; Nielsen, John

    2003-01-01

    The natural antibiotic saphenamycin, 6-[1-(2-hydroxy-6-methyl-benzoyloxy)-ethyl]-phenazine-1-carboxylic acid, was synthesized from saphenic acid using temporary ally] protection of carboxy and phenoxy functionalities. Resolution of racemic saphenic acid was performed by crystallization of the...... and screened against a range of skin flora and resistant Staphylococcus aureus strains. Biological activities of saphenamycin enantiomers were compared with that of the synthetic racemate as well as earlier reported activities of saphenamycin isolated from natural sources. No significant difference...... was observed in activity of the enantiomers of saphenamycin, which revealed that the chirality of saphenamycin has no consequences for the antibiotic activity. Saphenamycin proved to be a potent antibiotic against fusidic acid and rifampicin resistant S. aureus strains showing MIC of 0.1-0.2 mug/mL....

  13. Syntheses, biological activities and SAR studies of novel carboxamide compounds containing piperazine and arylsulfonyl moieties.

    Science.gov (United States)

    Wang, Bao-Lei; Shi, Yan-Xia; Zhang, Shu-Jun; Ma, Yi; Wang, Hong-Xue; Zhang, Li-Yuan; Wei, Wei; Liu, Xing-Hai; Li, Yong-Hong; Li, Zheng-Ming; Li, Bao-Ju

    2016-07-19

    A series of novel carboxamide compounds 19a-19j, 20a-20j and 22a-22d containing piperazine and arylsulfonyl moieties have been synthesized. The bioassay results showed that some compounds exhibited favorable herbicidal activities against dicotyledonous plants and many of them possessed excellent antifungal activities. Among 24 novel compounds, some showed superiority over the commercial fungicides Chlorothalonil, Dimethomorph, Thiophanate-methyl, Iprodione, and Zhongshengmycin at 500 mg/L concentration. Some compounds also exhibited high KARI inhibitory activity at 100 μg/mL concentration and could be used as new KARI lead inhibitors for further studies. Moreover, SAR of these new compounds were comprehensively investigated using different computational methods in which 3D-QSAR model obtained provided useful information for further structural optimization for the discovery of new fungicides. The results of this research will contribute to explore comprehensive biological activities of piperazine-containing compounds in different areas of chemistry. PMID:27092414

  14. 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.

  15. 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.

  16. Biological Activities of a Thai Luminescent Mushroom

    OpenAIRE

    Jiraporn BURAKORN; Trong Binh NGUEYN; Rueankeaw PRAPHRUET

    2015-01-01

    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 inf...

  17. Biologically active secondary metabolites from marine cyanobacteria

    OpenAIRE

    Nunnery, Joshawna K.; Mevers, Emily; Gerwick, William H

    2010-01-01

    Marine cyanobacteria are a rich source of complex bioactive secondary metabolites which derive from mixed biosynthetic pathways. Recently, several marine cyanobacterial natural products have garnered much attention due to their intriguing structures and exciting anti-proliferative or cancer cell toxic activities. Several other recently discovered secondary metabolites exhibit insightful neurotoxic activities whereas others are showing pronounced anti-inflammatory activity. A number of anti-in...

  18. 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.

  19. 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.

  20. 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

  1. Synthetic Approaches and Biological Activities of 4-Hydroxycoumarin Derivatives

    OpenAIRE

    Oee-Sook Park; Jae-Chul Jung

    2009-01-01

    The main purpose of this review is to summarize recent chemical syntheses and structural modifications of 4-hydroxycoumarin and its derivatives, of interest due to their characteristic conjugated molecular architecture and biological activities.

  2. Synthetic Approaches and Biological Activities of 4-Hydroxycoumarin Derivatives

    Directory of Open Access Journals (Sweden)

    Oee-Sook Park

    2009-11-01

    Full Text Available The main purpose of this review is to summarize recent chemical syntheses and structural modifications of 4-hydroxycoumarin and its derivatives, of interest due to their characteristic conjugated molecular architecture and biological activities.

  3. Antimicrobial activity of methyl australate from Ganoderma australe Atividade antimicrobiana do australato de metila de Ganoderma australe

    OpenAIRE

    Elza de Fatima Albino Smania; Franco Delle Monache; Rosendo Augusto Yunes; Roberta Paulert; Artur Smania Junior

    2007-01-01

    In addition to nine known steroidal compounds, australic acid and the new methyl australate have been isolated from the Brazilian fungus Ganoderma australe. Both methyl australate and its corresponding acid were shown to be active against fungi and Gram-positive bacteria, the methyl ester being also active against Gram-negative bacteria.Do fungo brasileiro Ganoderma australe foram isolados o ácido austrálico e o novo composto australado de metila, além de outros 9 compostos já conhecidos. Tan...

  4. PHYTOCHEMICALS AND BIOLOGICAL ACTIVITIES OF FAGONIA INDICA

    Directory of Open Access Journals (Sweden)

    Goyal Manoj

    2012-06-01

    Full Text Available Fagonia Indica (family Zygophyllaceae is a small spiny under-shrub, mostly found in the deserts of Asia and Africa. It is widely used is Ayurvedic system of medicine to treat vitiated conditions since this plant was antioxidant, analgesic, anti-inflammatory, antimicrobial, astringent, febrifuge and prophylactic against small-pox agents.There are reports providing scientific evidences for antimicrobial, analgesic, anti-inflammatory, and antioxidant activities of this plant. These activities were attributed to the presence of a variety of active ingredients including triterpenoidal saponins , flavonol glycosides, ursolic and oleanolic acids either alone or with their derivatives. A comprehensive account of the morphology, photochemical constituents, ethanobotanical uses and pharmacological activities reported are included in this review for exploring the immense medicinal potential of this plant.

  5. Biological Activity of Curcuminoids Isolated from Curcuma longa

    OpenAIRE

    Simay Çıkrıkçı; Erkan Mozioğlu; Hasibe Yılmaz

    2008-01-01

    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.

  6. 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.

  7. Saponins from Swartzia langsdorffii: biological activities

    OpenAIRE

    2003-01-01

    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...

  8. PHYTOCHEMICALS AND BIOLOGICAL ACTIVITIES OF FAGONIA INDICA

    OpenAIRE

    Goyal Manoj; Pareek Anil; Batra Nikhil; Nagori Badri Prakash

    2012-01-01

    Fagonia Indica (family Zygophyllaceae) is a small spiny under-shrub, mostly found in the deserts of Asia and Africa. It is widely used is Ayurvedic system of medicine to treat vitiated conditions since this plant was antioxidant, analgesic, anti-inflammatory, antimicrobial, astringent, febrifuge and prophylactic against small-pox agents.There are reports providing scientific evidences for antimicrobial, analgesic, anti-inflammatory, and antioxidant activities of this plant. These activities w...

  9. SYNTHESIS AND BIOLOGICAL EVALUTION OF 3-CHLORO 2- METHYL PHENYL CARBAMOYL SUBSTITUTED SEMICARBAZONE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS

    Directory of Open Access Journals (Sweden)

    Laxmi Banjare

    2012-01-01

    Full Text Available A series of 3- chloro 2- methyl phenyl carbamoyl substituted semicarbazones (4-21 was synthesized and evaluated for anticonvulsant and CNS activities. The anticonvulsant activity of the synthesized compounds was established after intraperitoneal administration in three seizure models in mice which include maximalelectroshock seizure, subcutaneous pentylenetetrazole, and subcutaneous strychnine-induced seizure screens. All the test compounds were administered at doses of 30, 100, and 300 mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration . . Aryl semicarbazides have also been reported to display excellent anticonvulsant activity in mice and rats . In terms of interaction at the binding site, as proposed previously by Dimmock et al. the pharma-cophoric elements were thought to be a lipophilic aryl ring and hydrogen bonding semicarbazone moiety. The attach- ment of a second aryl ring designated as the distal ring to the proximal aryl ring to increase the van der Waal’s bonding at the binding site and to increase potency have also been reported. Substitutions in the aryl ring by halogens have been found to increase potency in the MES screen .

  10. 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

  11. 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.

  12. Activation of endocrine-related gene expression in placental choriocarcinoma cell lines following DNA methylation knock-down.

    Science.gov (United States)

    Hogg, K; Robinson, W P; Beristain, A G

    2014-07-01

    Increasingly, placental DNA methylation is assessed as a factor in pregnancy-related complications, yet the transcriptional impact of such findings is not always clear. Using a proliferative in vitro placental model, the effect of DNA methylation loss on gene activation was evaluated at a number of genes selected for being differentially methylated in pre-eclampsia-associated placentae in vivo. We aimed to determine whether reduced DNA methylation at specific loci was associated with transcriptional changes at the corresponding gene, thus providing mechanistic underpinnings for previous clinical findings and to assess the degree of transcriptional response amongst our candidate genes. BeWo and JEG3 choriocarcinoma cells were exposed to 1 μM 5-Aza-2'-deoxycytidine (5-Aza-CdR) or vehicle control for 48 h, and re-plated and cultured for a further 72 h in normal media before cells were harvested for RNA and DNA. Bisulphite pyrosequencing confirmed that DNA methylation was reduced by ∼30-50% points at the selected loci studied in both cell lines. Gene activation, measured by qRT-PCR, was highly variable and transcript specific, indicating differential sensitivity to DNA methylation. Most notably, loss of DNA methylation at the leptin (LEP) promoter corresponded to a 200-fold and 40-fold increase in LEP expression in BeWo and JEG3 cells, respectively (P < 0.01). Transcripts of steroidogenic pathway enzymes CYP11A1 and HSD3B1 were up-regulated ∼40-fold in response to 5-Aza-CdR exposure in BeWo cells (P < 0.01). Other transcripts, including aromatase (CYP19), HSD11B2, inhibin (INHBA) and glucocorticoid receptor (NR3C1) were more moderately, although significantly, affected by loss of associated DNA methylation. These data present a mixed effect of DNA methylation changes at selected loci supporting cautionary interpretation of DNA methylation results in the absence of functional data. PMID:24623739

  13. In vivo activation of methyl-coenzyme M reductase by carbon monoxide

    Directory of Open Access Journals (Sweden)

    StephenWileyRagsdale

    2013-04-01

    Full Text Available Methyl-coenzyme M reductase (MCR from methanogenic archaea catalyzes the rate-limiting and final step in methane biosynthesis. Using coenzyme B (CoBSH as the two-electron donor, MCR reduces methyl-coenzyme M (CH3-SCoM to methane and the mixed disulfide, CoBS-SCoM. MCR contains an essential redox-active nickel tetrahydro¬corphinoid cofactor, Coenzyme F430, at its active site. The active form of the enzyme (MCRred1 contains Ni(I-F430. Rapid and efficient conversion of MCR to MCRred1 is important for elucidating the enzymatic mechanism, yet this reduction is difficult because the Ni(I state is subject to oxidative inactivation. Furthermore, no in vitro methods have yet been described to convert Ni(II forms into MCRred1. Since 1991, it has been known that MCRred1 from Methanothermobacter marburgensis can be generated in vivo when cells are purged with 100% H2. Here we show that purging cells or cell extracts with CO can also activate MCR. The rate of in vivo activation by CO is about 15 times faster than by H2 (130 min-1 and 8 min-1, respectively and CO leads to two-fold higher MCRred1 than H2. Unlike H2-dependent activation, which exhibits a 10-h lag time, there is no lag for CO-dependent activation. Based on cyanide inhibition experiments, CODH is required for the CO-dependent activation. Formate, which also is a strong reductant, cannot activate MCR in M. marburgensis in vivo.

  14. Characterization and Antioxidant Activity of Quercetin/Methyl-β-Cyclodextrin Complexes.

    Science.gov (United States)

    Güleç, Kadri; Demirel, Müzeyyen

    2016-01-01

    Quercetin (Qu), a polyphenolic flavonoid, is one of the most effective plant originated antioxidants. Despite the potential use of Qu in clinical trials, low water solubility, stability problems and the scarcity of cellular bioavailability limit its applications. The purpose of this study was to enhance aqueous solubility, dissolution rate and antioxidant activity of Qu by complexation with Methyl-β- cyclodextrin (M-β-CD). Analyses results showed that the aqueous solubility, dissolution rate and antioxidant activity of the complex were increased 254-fold, ~3-fold and 10% respectively compared to the pure Qu. Complexes were prepared by freeze-drying and evaporation method. The characteristics of the complexes were evaluated by DSC, XRD, (1)H-NMR, FT-IR, SEM, encapsulation efficacy, in-vitro dissolution rate analyses. Antioxidant activity studies on complexes carried out with DPPH tests. Analyses results showed that the formation of the complexes resulted in enhanced solubility with increased its antioxidant activity of Qu. PMID:26521654

  15. 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.

  16. Kinetic for Adsorption of Dye Methyl Orange by the Modified Activated Carbon from Rice Husk

    Directory of Open Access Journals (Sweden)

    Muqing Qiu

    2015-08-01

    Full Text Available In this study, the modified activated carbon from rice husk is used as the low cost material to absorb dye Methyl Orange in aqueous solution. The effects of different process parameters like pH, initial dye concentration and contact time on the adsorption of dye are investigated. The kinetic data of adsorption studies are discussed by the pseudo first-order, pseudo second-order and intraparticle diffusion. The results were shown that the adsorption process is chemisorption, which involves a sharing of electrons between the adsorbate and the surface of the adsorbent.

  17. 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.

  18. 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.

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

    OpenAIRE

    Yoon-Ha Kim; Gauhar Rehman; Shabir Ahmad; Syed Abdullah Gilani; Muhammad Hamayun; Javid Hussain; Abdul Latif Khan; Sang-Mo Kang; In-Jung Lee

    2010-01-01

    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 ...

  20. DACT2 is frequently methylated in human gastric cancer and methylation of DACT2 activated Wnt signaling

    OpenAIRE

    Yu, Yuanzi; Yan, Wenji; Liu, Xuefeng; Jia, Yan; Cao, Baoping; YU, YINGYAN; Lv, Youyong; Brock, Malcolm V; Herman, Jame G; Licchesi, Julien; Yang, Yunsheng; Guo, Mingzhou

    2014-01-01

    Dapper, Dishevelled-associated antagonist of β-catenin (DACT), is a key regulator of Wnt signaling pathway. The purpose of this study is to explore the epigenetic changes and the function ofDACT2 in human gastric cancer (GC). Eight human gastric cancer cell lines, 167 cases of primary gastric cancer and 8 cases of normal gastric mucosa were involved in this study. In addition, methylation Specific PCR (MSP), semi-quantitative RT-PCR, colony formation assay, flow cytometry assay, siRNA, immuno...

  1. 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.

  2. Design, synthesis, and in vitro biological evaluation of novel 6-methyl-7-substituted-7-deaza purine nucleoside analogs as anti-influenza A agents.

    Science.gov (United States)

    Lin, Cai; Sun, Chenghai; Liu, Xiao; Zhou, Yiqian; Hussain, Muzammal; Wan, Junting; Li, Minke; Li, Xue; Jin, Ruiliang; Tu, Zhengchao; Zhang, Jiancun

    2016-05-01

    Among many subtypes of influenza A viruses, influenza A(H1N1) and A(H3N2) subtypes are currently circulating among humans (WHO report 2014-15). Therapeutically, the emergence of viral resistance to currently available drugs (adamantanes and neuraminidase inhibitors) has heightened alarms for developing novel drugs that could address diverse targets in the viral replication cycle in order to improve treatment outcomes. To this regard, the design and synthesis of nucleoside analog inhibitors as potential anti-influenza A agents is a very active field of research nowadays. In this study, we designed and synthesized a series of hitherto unknown 6-methyl-7-substituted-7-deaza purine nucleoside analogs, and evaluated for their biological activities against influenza A virus strains, H1N1 and H3N2. From the viral inhibition assay, we identified some effective compounds, among which, compounds 5x (IC50 = 5.88 μM and 6.95 μM for H1N1 and H3N2, respectively) and 5z (IC50 = 3.95 μM and 3.61 μM for H1N1 and H3N2, respectively) demonstrated potent anti-influenza A activity. On the basis of selectivity index, we conceive that compound 5x may serve as a chemical probe of interest for further lead optimization studies with a general aim of developing novel and effective anti-influenza A virus agents. PMID:26802557

  3. 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.

  4. Biological models for active vision: Towards a unified architecture

    OpenAIRE

    Terzic K.; Lobato D.; Saleiro M.; Martins J; Farrajota M.; Rodrigues J.M.F.; Du Buf J.M.H.

    2013-01-01

    Building a general-purpose, real-time active vision system completely based on biological models is a great challenge. We apply a number of biologically plausible algorithms which address different aspects of vision, such as edge and keypoint detection, feature extraction,optical flow and disparity, shape detection, object recognition and scene modelling into a complete system. We present some of the experiments from our ongoing work, where our system leverages a combination of algorithms to ...

  5. Biological activities of radiation-degraded carrageenan

    International Nuclear Information System (INIS)

    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)

  6. 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)

  7. [Oregano: properties, composition and biological activity].

    Science.gov (United States)

    Arcila-Lozano, Cynthia Cristina; Loarca-Piña, Guadalupe; Lecona-Uribe, Salvador; González de Mejía, Elvira

    2004-03-01

    The oregano spice includes various plant species. The most common are the genus Origanum, native of Europe, and the Lippia, native of Mexico. Among the species of Origanum. their most important components are the limonene, gamma-cariofilene, rho-cymenene, canfor, linalol, alpha-pinene, carvacrol and thymol. In the genus Lippia, the same compounds can be found. The oregano composition depends on the specie, climate, altitude, time of recollection and the stage of growth. Some of the properties of this plant's extracts are being currently studied due to the growing interest for substituting synthetic additives commonly found in foods. Oregano has a good antioxidant capacity and also presents antimicrobial activity against pathogenic microorganisms like Salmonella typhimurium, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, among others. These are all characteristics of interest for the food industry because they may enhance the safety and stability of foods. There are also some reports regarding the antimutagenic and anticarcinogenic effect of oregano; representing an alternative for the potential treatment and/or prevention of certain chronic ailments, like cancer. PMID:15332363

  8. 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.

  9. SET7/9 catalytic mutants reveal the role of active site water molecules in lysine multiple methylation.

    Science.gov (United States)

    Del Rizzo, Paul A; Couture, Jean-François; Dirk, Lynnette M A; Strunk, Bethany S; Roiko, Marijo S; Brunzelle, Joseph S; Houtz, Robert L; Trievel, Raymond C

    2010-10-01

    SET domain lysine methyltransferases (KMTs) methylate specific lysine residues in histone and non-histone substrates. These enzymes also display product specificity by catalyzing distinct degrees of methylation of the lysine ε-amino group. To elucidate the molecular mechanism underlying this specificity, we have characterized the Y245A and Y305F mutants of the human KMT SET7/9 (also known as KMT7) that alter its product specificity from a monomethyltransferase to a di- and a trimethyltransferase, respectively. Crystal structures of these mutants in complex with peptides bearing unmodified, mono-, di-, and trimethylated lysines illustrate the roles of active site water molecules in aligning the lysine ε-amino group for methyl transfer with S-adenosylmethionine. Displacement or dissociation of these solvent molecules enlarges the diameter of the active site, accommodating the increasing size of the methylated ε-amino group during successive methyl transfer reactions. Together, these results furnish new insights into the roles of active site water molecules in modulating lysine multiple methylation by SET domain KMTs and provide the first molecular snapshots of the mono-, di-, and trimethyl transfer reactions catalyzed by these enzymes. PMID:20675860

  10. SET7/9 Catalytic Mutants Reveal the Role of Active Site Water Molecules in Lysine Multiple Methylation*

    Science.gov (United States)

    Del Rizzo, Paul A.; Couture, Jean-François; Dirk, Lynnette M. A.; Strunk, Bethany S.; Roiko, Marijo S.; Brunzelle, Joseph S.; Houtz, Robert L.; Trievel, Raymond C.

    2010-01-01

    SET domain lysine methyltransferases (KMTs) methylate specific lysine residues in histone and non-histone substrates. These enzymes also display product specificity by catalyzing distinct degrees of methylation of the lysine ϵ-amino group. To elucidate the molecular mechanism underlying this specificity, we have characterized the Y245A and Y305F mutants of the human KMT SET7/9 (also known as KMT7) that alter its product specificity from a monomethyltransferase to a di- and a trimethyltransferase, respectively. Crystal structures of these mutants in complex with peptides bearing unmodified, mono-, di-, and trimethylated lysines illustrate the roles of active site water molecules in aligning the lysine ϵ-amino group for methyl transfer with S-adenosylmethionine. Displacement or dissociation of these solvent molecules enlarges the diameter of the active site, accommodating the increasing size of the methylated ϵ-amino group during successive methyl transfer reactions. Together, these results furnish new insights into the roles of active site water molecules in modulating lysine multiple methylation by SET domain KMTs and provide the first molecular snapshots of the mono-, di-, and trimethyl transfer reactions catalyzed by these enzymes. PMID:20675860

  11. SET7/9 Catalytic Mutants Reveal the Role of Active Site Water Molecules in Lysine Multiple Methylation

    Energy Technology Data Exchange (ETDEWEB)

    Del Rizzo, Paul A.; Couture, Jean-François; Dirk, Lynnette M.A.; Strunk, Bethany S.; Roiko, Marijo S.; Brunzelle, Joseph S.; Houtz, Robert L.; Trievel, Raymond C. (Michigan); (NWU); (Kentucky)

    2010-11-15

    SET domain lysine methyltransferases (KMTs) methylate specific lysine residues in histone and non-histone substrates. These enzymes also display product specificity by catalyzing distinct degrees of methylation of the lysine {epsilon}-amino group. To elucidate the molecular mechanism underlying this specificity, we have characterized the Y245A and Y305F mutants of the human KMT SET7/9 (also known as KMT7) that alter its product specificity from a monomethyltransferase to a di- and a trimethyltransferase, respectively. Crystal structures of these mutants in complex with peptides bearing unmodified, mono-, di-, and trimethylated lysines illustrate the roles of active site water molecules in aligning the lysine {epsilon}-amino group for methyl transfer with S-adenosylmethionine. Displacement or dissociation of these solvent molecules enlarges the diameter of the active site, accommodating the increasing size of the methylated {epsilon}-amino group during successive methyl transfer reactions. Together, these results furnish new insights into the roles of active site water molecules in modulating lysine multiple methylation by SET domain KMTs and provide the first molecular snapshots of the mono-, di-, and trimethyl transfer reactions catalyzed by these enzymes.

  12. Phenolic Compounds Characterization and Biological Activities of Citrus aurantium Bloom

    OpenAIRE

    Armin Oskoueian; Jaafar, Hawa Z. E.; Rudi Hendra; Ehsan Oskoueian; Ehsan Karimi

    2012-01-01

    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 fla...

  13. 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

  14. 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.

  15. 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

  16. 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.

  17. Methionine sulfoxide reductase regulates brain catechol-O-methyl transferase activity.

    Science.gov (United States)

    Moskovitz, Jackob; Walss-Bass, Consuelo; Cruz, Dianne A; Thompson, Peter M; Bortolato, Marco

    2014-10-01

    Catechol-O-methyl transferase (COMT) plays a key role in the degradation of brain dopamine (DA). Specifically, low COMT activity results in higher DA levels in the prefrontal cortex (PFC), thereby reducing the vulnerability for attentional and cognitive deficits in both psychotic and healthy individuals. COMT activity is markedly reduced by a non-synonymous single-nucleotide polymorphism (SNP) that generates a valine-to-methionine substitution on the residue 108/158, by means of as-yet incompletely understood post-translational mechanisms. One post-translational modification is methionine sulfoxide, which can be reduced by the methionine sulfoxide reductase (Msr) A and B enzymes. We used recombinant COMT proteins (Val/Met108) and mice (wild-type (WT) and MsrA knockout) to determine the effect of methionine oxidation on COMT activity and COMT interaction with Msr, through a combination of enzymatic activity and Western blot assays. Recombinant COMT activity is positively regulated by MsrA, especially under oxidative conditions, whereas brains of MsrA knockout mice exhibited lower COMT activity (as compared with their WT counterparts). These results suggest that COMT activity may be reduced by methionine oxidation, and point to Msr as a key molecular determinant for the modulation of COMT activity in the brain. The role of Msr in modulating cognitive functions in healthy individuals and schizophrenia patients is yet to be determined. PMID:24735585

  18. 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.

  19. Antimicrobial activity of nerolidol and its derivatives against airborne microbes and further biological activities.

    Science.gov (United States)

    Krist, Sabine; Banovac, Daniel; Tabanca, Nurhayat; Wedge, David E; Gochev, Velizar K; Wanner, Jürgen; Schmidt, Erich; Jirovetz, Leopold

    2015-01-01

    Nerolidol and its derivatives, namely cis-nerolidol, O-methyl-nerolidol, O-ethyl-nerolidol, (-)-α-bisabolol, trans,trans-farnesol and its main natural source cabreuva essential oil, were tested for their antimicrobial activity against airborne microbes and antifungal properties against plant pathogens. Among the tested compounds, α-bisabolol was the most effective antimicrobial agent and trans,trans-farnesol showed the best antifungal activity. PMID:25920237

  20. 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.

  1. Polymeric functional nanostructures for in vivo delivery of biologically active proteins

    International Nuclear Information System (INIS)

    Poly(methyl methacrylate) core-shell particles in the submicron scale range were prepared by dispersion polymerization through an appropriate selection of the experimental parameters. Due to the versatility of this reaction, the macromolecular design can be directed towards the preparation of nano/microspheres with extensively hydrophilic and protein-friendly surfaces with low non-specific interactions. If the steric stabilizer is soluble in physiologic medium, the formation of a core shell structure, constituted by a soft outer shell, made up of long soluble arms able to fix the protein, anchored to an inner hard insoluble core can be envisaged. In the presence of commercial polymeric stabilizers Eudragit L100-55 and Eudragit E100, acid and basic microspheres can be obtained, able to interact with biologically active proteins. (author)

  2. Affinity-based enrichment strategies to assay methyl-CpG binding activity and DNA methylation in early Xenopus embryos

    OpenAIRE

    Bogdanović Ozren; Veenstra Gert Jan C

    2011-01-01

    Abstract Background DNA methylation is a widespread epigenetic modification in vertebrate genomes. Genomic sites of DNA methylation can be bound by methyl-CpG-binding domain proteins (MBDs) and specific zinc finger proteins, which can recruit co-repressor complexes to silence transcription on targeted loci. The binding to methylated DNA may be regulated by post-translational MBD modifications. Findings A methylated DNA affinity precipitation method was implemented to assay binding of proteins...

  3. Methyl Jasmonate Enhances Antioxidant Activity, Flavonoid Content and Antiproliferation of Human Cancer Cells in Blackberries (Rubus spp.)

    Science.gov (United States)

    The effects of preharvest methyl jasmonate (MJ) application on fruit quality, antioxidant activity and flavonoid content in blackberries (Rubus spp.) were determined. Anticancer activity against human lung A549 cells and HL-60 leukemia cells was also evaluated. Three blackberry cultivars (Chester T...

  4. 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.

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

    DEFF Research Database (Denmark)

    Nielsen, O H; Vainer, B; Madsen, S M; Seidelin, J B; Heegaard, Niels Henrik Helweg

    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 dis...

  6. 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

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

    OpenAIRE

    Kozarski Maja S.; Klaus Anita S.; Nikšić Miomir P.; van Griensven Leo J.L.D.; Vrvić Miroslav M.; Jakovljević Dragica M.

    2014-01-01

    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 pr...

  8. Modeling Radial Holoblastic Cleavage: A Laboratory Activity for Developmental Biology.

    Science.gov (United States)

    Ellis, Linda K.

    2000-01-01

    Introduces a laboratory activity designed for an undergraduate developmental biology course. Uses Play-Doh (plastic modeling clay) to build a multicellular embryo in order to provide a 3-D demonstration of cleavage. Includes notes for the instructor and student directions. (YDS)

  9. Obtaining of biologically active substances from dandelion (Taraxacum officinale Wigg.)

    OpenAIRE

    Яблонська, К.М.; Національний авіаційний університет; Косоголова, Л. О.; Національний авіаційний університет; Мосюк, Л. І.; Національний авіаційний університет

    2015-01-01

    An aqueous extracts of dandelion (Taraxacum oficinale Wigg.) for the needs of diet. The optimum conditions for extraction of biologically active substances dandelion, namely the ratio of raw materials: extractant 1:20, extraction time – 30 minutes, the temperature – 55 °C. Extraction was carried out with distilled water.

  10. 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

  11. Biological activity of phenolic compounds present in buckwheat plants

    Czech Academy of Sciences Publication Activity Database

    Kalinová, J.; Tříska, Jan; Vrchotová, Naděžda

    2005-01-01

    Roč. 16, č. 1 (2005), s. 123-129. ISSN 0971-4693 Institutional research plan: CEZ:AV0Z60870520 Keywords : biological activity, extract, Fagopyrum esculenthum Subject RIV: CB - Analytical Chemistry, Separation Impact factor: 0.686, year: 2005

  12. 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...

  13. 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)

  14. 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.

  15. Secondary metabolites from Inula britannica L. and their biological activities.

    Science.gov (United States)

    Khan, Abdul Latif; Hussain, Javid; Hamayun, Muhammad; Gilani, Syed Abdullah; Ahmad, Shabir; Rehman, Gauhar; Kim, Yoon-Ha; Kang, Sang-Mo; Lee, In-Jung

    2010-03-01

    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. PMID:20336001

  16. 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.

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

    Science.gov (United States)

    Chen, Yongcan; Zhu, Wei-Guo

    2016-07-01

    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 proline-tryptophan-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. PMID:27217472

  18. 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

  19. 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.

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

    Science.gov (United States)

    Jiu-Fu, Lu; Hong-Guang, Ge; Juan, Shi

    2015-12-01

    Reaction of 2-(1-methyl-1,2-dihydroimidazol-3-yl)acetonitrile tetrafluoroborate with silver oxide in dichloromethane readily yields [Ag( DIM)2]BF4, 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) Å3, Z = 4, D x = 1.771 g/cm3, F (000) = 864, µ(Mo K α) = 1.278 mm-1. The final R 1 = 0.0711 and wR 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.

  1. AHPG: 9-[(1-amino-3-hydroxy-2-propoxy)methyl]guanine. Synthesis, biological evaluation, and biochemical mechanism of action in the L1210 cell system

    International Nuclear Information System (INIS)

    This thesis involved the synthesis, biological evaluation, and determination of the mechanism of cytotoxicity of 9-[(1-amino-3-hydroxy-2-propoxy)methyl]guanine, AHPG. This acyclic nucleoside was synthesized by a novel route and purified by state-of-the-art chromatography. The antimetabolite was screened for cytotoxic activity and was found to be most effective against L1210 cells among those systems tested. Initial biochemical studies in this system indicated that AHPG significantly decreased the incorporation of amino acids into L1210 acid-insoluble material without altering the incorporation of precursor molecules into DNA or RNA. Electrophoretic analysis of the nuclear and cytoplasmic proteins formed in the presence of drug indicated that this effect was a generalized phenomenon. Additionally, AHPG was found not to alter amino acid transport into L1210 cells. Since AHPG is a modified precursor of DNA and RNA, it was essential to evaluate the influence of this agent on these macromolecules. DNA and RNA were isolated from L1210 cells which had been treated with radiolabeled AHPG (tritium in the guanine base). HPLC analysis indicated that native AHPG was not present in the nucleic acids and phosphorylated AHPG was not found in cytosolic fractions. Since all the data suggested that the primary effect of AHPG might be directed at the level of translation, ribosomes and polysomes were isolated in the presence and absence of drug. After sixty minutes of exposure to AHPG there was a significant decrease in the levels of these complexes, suggesting that AHPG invokes its initial cytotoxic action directly at the level of protein synthesis. In summary, AHPG produces toxicity in L1210 cells by altering protein metabolism

  2. Chemical and structural features influencing the biological activity of curcumin.

    Science.gov (United States)

    Priyadarsini, K Indira

    2013-01-01

    Curcumin, a polyphenolic natural product, exhibits therapeutic activity against a number of diseases, attributed mainly to its chemical structure and unique physical, chemical, and biological properties. It is a diferuloyl methane molecule [1,7-bis (4-hydroxy-3- methoxyphenyl)-1,6-heptadiene-3,5-dione)] containing two ferulic acid residues joined by a methylene bridge. It has three important functionalities: an aromatic o-methoxy phenolic group, α, β-unsaturated β-diketo moiety and a seven carbon linker. Extensive research in the last two decades has provided evidence for the role of these different functional groups in its crucial biological activities. A few highlights of chemical structural features associated with the biological activity of curcumin are: The o-methoxyphenol group and methylenic hydrogen are responsible for the antioxidant activity of curcumin, and curcumin donates an electron/ hydrogen atom to reactive oxygen species. Curcumin interacts with a number of biomolecules through non-covalent and covalent binding. The hydrogen bonding and hydrophobicity of curcumin, arising from the aromatic and tautomeric structures along with the flexibility of the linker group are responsible for the non-covalent interactions. The α, β-unsaturated β-diketone moiety covalently interacts with protein thiols, through Michael reaction. The β-diketo group forms chelates with transition metals, there by reducing the metal induced toxicity and some of the metal complexes exhibit improved antioxidant activity as enzyme mimics. New analogues with improved activity are being developed with modifications on specific functional groups of curcumin. The physico-chemical and structural features associated with some of the biological activities of curcumin and important analogues are summarized in this article. PMID:23116315

  3. Stereochemical Assignment of Strigolactone Analogues Confirms Their Selective Biological Activity.

    Science.gov (United States)

    Artuso, Emma; Ghibaudi, Elena; Lace, Beatrice; Marabello, Domenica; Vinciguerra, Daniele; Lombardi, Chiara; Koltai, Hinanit; Kapulnik, Yoram; Novero, Mara; Occhiato, Ernesto G; Scarpi, Dina; Parisotto, Stefano; Deagostino, Annamaria; Venturello, Paolo; Mayzlish-Gati, Einav; Bier, Ariel; Prandi, Cristina

    2015-11-25

    Strigolactones (SLs) are new plant hormones with various developmental functions. They are also soil signaling chemicals that are required for establishing beneficial mycorrhizal plant/fungus symbiosis. In addition, SLs play an essential role in inducing seed germination in root-parasitic weeds, which are one of the seven most serious biological threats to food security. There are around 20 natural SLs that are produced by plants in very low quantities. Therefore, most of the knowledge on SL signal transduction and associated molecular events is based on the application of synthetic analogues. Stereochemistry plays a crucial role in the structure-activity relationship of SLs, as compounds with an unnatural D-ring configuration may induce biological effects that are unrelated to SLs. We have synthesized a series of strigolactone analogues, whose absolute configuration has been elucidated and related with their biological activity, thus confirming the high specificity of the response. Analogues bearing the R-configured butenolide moiety showed enhanced biological activity, which highlights the importance of this stereochemical motif. PMID:26502774

  4. 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)

  5. 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.

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

    Directory of Open Access Journals (Sweden)

    Russell Keast

    2010-02-01

    Full Text Available 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 traditional Mediterranean diet. Studies (human, animal, in vivo and in vitro have demonstrated that olive oil phenolic compounds have positive effects on certain physiological parameters, such as plasma lipoproteins, oxidative damage, inflammatory markers, platelet and cellular function, antimicrobial activity and bone health. This paper summarizes current knowledge on the bioavailability and biological activities of olive oil phenolic compounds.

  7. 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.

  8. 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.

  9. 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.

  10. 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.

  11. Methyl jasmonate effectively enhanced some defense enzymes activity and Total Antioxidant content in harvested "Sabrosa" strawberry fruit.

    Science.gov (United States)

    Asghari, Mohammadreza; Hasanlooe, Ali Rashid

    2016-05-01

    The use of chemicals in postharvest technology of horticultural crops is highly restricted and it is necessary to introduce safe food preserving methods. Strawberry is very susceptible to postharvest losses and more than 50% of harvested fruit is lost in Iran. Effect of postharvest treatment with methyl jasmonate (at 0, 8, and 16 μmol L(-1)) on some quality attributes of Sabrosa strawberry fruit during storage at 1 ± 0.5°C with 90-95% RH for 14 days followed by 24 h at 20°C was studied. Methyl jasmonate, at both concentrations, decreased weight loss and retained marketability of fruits. Catalase activity of treated fruits was decreased during the first days, but showed a substantial increase during the second week. Methyl jasmonate, in a concentration-dependent manner, enhanced peroxidase activity. Fruit total antioxidant capacity was enhanced by methyl jasmonate treatment. The results indicated that methyl jasmonate plays a key role in establishing resistance against stresses, enhancing fruit defense systems, antioxidant capacity, and storage life leading to decreased postharvest losses. This phytochemical has a good potential to be used in postharvest technology of Sabrosa strawberry fruit and enhance the fruit postharvest life. PMID:27247768

  12. Set7 mediated Gli3 methylation plays a positive role in the activation of Sonic Hedgehog pathway in mammals

    Science.gov (United States)

    Fu, Lin; Wu, Hailong; Cheng, Steven Y; Gao, Daming; Zhang, Lei; Zhao, Yun

    2016-01-01

    Hedgehog signaling plays very important roles in development and cancers. Vertebrates have three transcriptional factors, Gli1, Gli2 and Gli3. Among them, Gli3 is a very special transcriptional factor which closely resembles Cubitus interruptus (Ci, in Drosophila) structurally and functionally as a ‘double agent’ for Shh target gene expression. Here we show that Gli3 full-length, but not the truncated form, can be methylated at K436 and K595. This methylation is specifically catalyzed by Set7, a lysine methyltransferase (KMT). Methylation at K436 and K595 respectively increases the stability and DNA binding ability of Gli3, resulting in an enhancement of Shh signaling activation. Furthermore, functional experiments indicate that the Gli3 methylation contributes to the tumor growth and metastasis in non-small cell lung cancer in vitro and in vivo. Therefore, we propose that Set7 mediated methylation is a novel PTM of Gli3, which positively regulates the transactivity of Gli3 and the activation of Shh signaling. DOI: http://dx.doi.org/10.7554/eLife.15690.001 PMID:27146893

  13. Biological activities of xanthatin from Xanthium strumarium leaves.

    Science.gov (United States)

    Nibret, Endalkachew; Youns, Mahamoud; Krauth-Siegel, R Luise; Wink, Michael

    2011-12-01

    The objective of the present work was to evaluate the biological activities of the major bioactive compound, xanthatin, and other compounds from Xanthium strumarium (Asteraceae) leaves. Inhibition of bloodstream forms of Trypanosoma brucei brucei and leukaemia HL-60 cell proliferation was assessed using resazurin as a vital stain. Xanthatin was found to be the major and most active compound against T. b. brucei with an IC(50) value of 2.63 µg/mL and a selectivity index of 20. The possible mode of action of xanthatin was further evaluated. Xanthatin showed antiinflammatory activity by inhibiting both PGE(2) synthesis (24% inhibition) and 5-lipoxygenase activity (92% inhibition) at concentrations of 100 µg/mL and 97 µg/mL, respectively. Xanthatin exhibited weak irreversible inhibition of parasite specific trypanothione reductase. Unlike xanthatin, diminazene aceturate and ethidium bromide showed strong DNA intercalation with IC(50) values of 26.04 µg/mL and 44.70 µg/mL, respectively. Substantial induction of caspase 3/7 activity in MIA PaCa-2 cells was observed after 6 h of treatment with 100 µg/mL of xanthatin. All these data taken together suggest that xanthatin exerts its biological activity by inducing apoptosis and inhibiting both PGE(2) synthesis and 5-lipoxygenase activity thereby avoiding unwanted inflammation commonly observed in diseases such as trypanosomiasis. PMID:21953905

  14. 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.

  15. 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.

  16. Recent insight into the biological activities of synthetic xanthone derivatives.

    Science.gov (United States)

    Shagufta; Ahmad, Irshad

    2016-06-30

    Xanthones are a class of oxygen containing heterocyclic compounds with a broad range of biological activities, and they have prominent significance in the field of medicinal chemistry. Xanthone is an attractive scaffold for the design and development of new drugs due to its promising biological activities, primarily as anticancer, antimalarial, antimicrobial, anti-HIV, anticonvulsant, anticholinesterase, antioxidant, anti-inflammatory, and as inhibitors of several enzymes like α-glycosidase, topoisomerase, protein kinase, aromatase, etc. In this review, we have compiled and discussed recent developments on the pharmacological profile of synthetic xanthone derivatives for different therapeutic targets. The review highlights the therapeutic significance of xanthones and offers support in the development of new xanthone derivatives as therapeutic agents. PMID:27111599

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

    Science.gov (United States)

    Pal, Dilipkumar; Mishra, Pragya; Sachan, Neetu; Ghosh, Ashoke K

    2011-10-01

    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. PMID:22247887

  18. 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.

  19. Milk kefir: composition, microbial cultures, biological activities, and related products.

    Science.gov (United States)

    Prado, Maria R; Blandón, Lina Marcela; Vandenberghe, Luciana P S; Rodrigues, Cristine; Castro, Guillermo R; Thomaz-Soccol, Vanete; Soccol, Carlos R

    2015-01-01

    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. PMID:26579086

  20. 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.

  1. 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.

    isolated by Histopaque™ (Sigma- Aldrich, St. Louis, USA) flotation. Isolated PBMC were stained supravitally with fluorescent CFSE (Carboxyfluorescein succinimidyl ester) dye according to the method described by Witkowski (2008), re-suspended in culture..., from bacteria and viruses to aquatic animals (Rohrlack et al., 2004; Sedmak et al., 2008; Sønstebø & Rohrlack, 2011). As many cyanobacterial products are characterized by a unique biological activity, they have become a focus of high interest...

  2. Processed Vietnamese ginseng: Preliminary results in chemistry and biological activity

    OpenAIRE

    Le, Thi Hong Van; Lee, Seo Young; Kim, Tae Ryong; Kim, Jae Young; Kwon, Sung Won; NGUYEN, NGOC KHOI; Park, Jeong Hill; Nguyen, Minh Duc

    2013-01-01

    Background This study was carried out to investigate the effect of the steaming process on chemical constituents, free radical scavenging activity, and antiproliferative effect of Vietnamese ginseng. Methods Samples of powdered Vietnamese ginseng were steamed at 120°C for various times and their extracts were subjected to chemical and biological studies. Results Upon steaming, contents of polar ginsenosides, such as Rb1, Rc, Rd, Re, and Rg1, were rapidly decreased, whereas less polar ginsenos...

  3. Secondary metabolites in grasses: characterization and biological activity

    OpenAIRE

    Aldo Tava

    2007-01-01

    In a series of studies dealing on the nutritional value of forage species, more attention was focussed on several compounds, named secondary metabolites, that are important in determining nutritional characteristics. Secondary metabolites are compounds detected in the green materials in low concentration compared to primary metabolites (proteins, sugars, lipids, fibers), but of fundamental importance for the plant physiology. The possess several biological activities and this contribute to th...

  4. Simaroubaceae family: botany, chemical composition and biological activities

    OpenAIRE

    Iasmine A.B.S. Alves; Henrique M. Miranda; Luiz A. L. Soares; Karina P. Randau

    2014-01-01

    The Simaroubaceae family includes 32 genera and more than 170 species of trees and brushes of pantropical distribution. The main distribution hot spots are located at tropical areas of America, extending to Africa, Madagascar and regions of Australia bathed by the Pacific. This family is characterized by the presence of quassinoids, secondary metabolites responsible of a wide spectrum of biological activities such as antitumor, antimalarial, antiviral, insecticide, feeding deterrent, amebicid...

  5. Electronic structure and biological activity: Barbiturates vs. thiobarbiturates

    Science.gov (United States)

    Novak, Igor; Kovač, Branka

    2010-06-01

    The electronic structure of the derivatives of thiobarbituric acid: 1,3-diethyl-2-thiobarbituric acid ( I) and 1,3-dibutyl-2-thiobarbituric acid ( II) has been investigated by HeI and HeII UV photoelectron spectroscopy (UPS) and quantum chemical calculations. We discuss their electronic structures and compare them with barbituric acid. We also relate the difference in electronic structure between barbituric and thiobarbituric acids to difference in biological activity of their derivatives.

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

    OpenAIRE

    Shukranul Mawa; Khairana Husain; Ibrahim Jantan

    2013-01-01

    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 l...

  7. 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...

  8. Polyphosphate Kinase from Activated Sludge Performing Enhanced Biological Phosphorus Removal†

    OpenAIRE

    Katherine D McMahon; Dojka, Michael A.; Pace, Norman R.; Jenkins, David; Keasling, Jay D.

    2002-01-01

    A novel polyphosphate kinase (PPK) was retrieved from an uncultivated organism in activated sludge carrying out enhanced biological phosphorus removal (EBPR). Acetate-fed laboratory-scale sequencing batch reactors were used to maintain sludge with a high phosphorus content (approximately 11% of the biomass). PCR-based clone libraries of small subunit rRNA genes and fluorescent in situ hybridization (FISH) were used to verify that the sludge was enriched in Rhodocyclus-like β-Proteobacteria kn...

  9. Biological activity of selected essential oils of the Lamiaceae family

    OpenAIRE

    Havlová, Kateřina

    2013-01-01

    The Lamiaceae family (the mints) is one of the large groups of plants. These herbs are important for their biological active substances, such as essential oils, tannins, bitter principles, etc. The properties of selected plants from this family are used in many industries. Many of them have been used long due to their medicinal properties and simultaneously they form an indispensable part of many products used for cosmetic purposes. The important ingredients are first of all essential oils, w...

  10. 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.

  11. Biological activities and phytochemicals of Swietenia macrophylla King.

    Science.gov (United States)

    Moghadamtousi, Soheil Zorofchian; Goh, Bey Hing; Chan, Chim Kei; Shabab, Tara; Kadir, Habsah Abdul

    2013-01-01

    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. PMID:23999722

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

    OpenAIRE

    M. M. Habashy; M. H. Nassar; Mahmoud, M. R.; H. M. F. Madkour

    2000-01-01

    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.

  13. Lewis base activation of Lewis acids. Catalytic enantioselective addition of silyl enol ethers of achiral methyl ketones to aldehydes.

    Science.gov (United States)

    Denmark, Scott E; Heemstra, John R

    2003-06-26

    A highly enantioselective addition of silyl enol ethers derived from simple methyl ketones is described. The catalyst system of silicon tetrachloride activated by a chiral bisphosphoramide (R,R)-7 effectively promotes the addition of a variety of unsubstituted silyl enol ethers to aromatic, olefinic, and heteroaromatic aldehydes in excellent yield. [reaction: see text] PMID:12816434

  14. Integrity and Biological Activity of DNA after UV Exposure

    Science.gov (United States)

    Lyon, Delina Y.; Monier, Jean-Michel; Dupraz, Sébastien; Freissinet, Caroline; Simonet, Pascal; Vogel, Timothy M.

    2010-04-01

    The field of astrobiology lacks a universal marker with which to indicate the presence of life. This study supports the proposal to use nucleic acids, specifically DNA, as a signature of life (biosignature). In addition to its specificity to living organisms, DNA is a functional molecule that can confer new activities and characteristics to other organisms, following the molecular biology dogma, that is, DNA is transcribed to RNA, which is translated into proteins. Previous criticisms of the use of DNA as a biosignature have asserted that DNA molecules would be destroyed by UV radiation in space. To address this concern, DNA in plasmid form was deposited onto different surfaces and exposed to UVC radiation. The surviving DNA was quantified via the quantitative polymerase chain reaction (qPCR). Results demonstrate increased survivability of DNA attached to surfaces versus non-adsorbed DNA. The DNA was also tested for biological activity via transformation into the bacterium Acinetobacter sp. and assaying for antibiotic resistance conferred by genes encoded by the plasmid. The success of these methods to detect DNA and its gene products after UV exposure (254 nm, 3.5 J/m2s) not only supports the use of the DNA molecule as a biosignature on mineral surfaces but also demonstrates that the DNA retained biological activity.

  15. 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.

  16. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF SOME NOVEL ARYL AND HETROARYL CHALCONE ANALOGUES

    OpenAIRE

    Tribhuvan Singh; R Lavanya; Srikanth Merugu; P.Sudhakar; Syeda Sana Yasmeen

    2012-01-01

    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.

  17. Extracts from hardwood trees used in commercial paper mills contain biologically active neurochemical disruptors.

    Science.gov (United States)

    Basu, Niladri; Waye, Andrew; Trudeau, Vance L; Arnason, John T

    2012-01-01

    Following on our discovery that pulp and paper mill effluents can interact with, and disrupt, various neurotransmitter receptors and enzymes important to fish reproduction, we tested wood and bark extracts of 14 Eastern North American hardwood trees used in pulp and paper production. Radioligand binding to neurotransmitter receptors, including the dopamine-2 receptor (D2), the gamma aminobutyric acid receptor A (GABA(A)), N-methyl-D-aspartic acid (NMDA) receptor, and muscarinic cholinergic receptor (mACh-R), were significantly changed following in vitro incubations with many but not all extracts. Activities of neurotransmitter-related enzymes monoamine oxidase (MAO), GABA-transaminase (GABA-T), acetylcholinesterase (AChE) and glutamic acid decarboxylase (GAD) were also significantly altered. Butternut wood extracts and the isolated compound juglone significantly inhibited the enzymatic activities of MAO and GAD which we suggest may be part of a mechanism that may negatively affect fish reproduction. Besides giving credence to the hypothesis that neuroactive compounds in pulp and paper effluent may originate in the trees used by mills, the results reported here also indicate important neuropharmacological activities in hardwoods which may help identify new sources of biologically active natural products. PMID:22137476

  18. 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)

  19. 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.

  20. Radiation degradation of carbohydrates and their biological activities for plants

    Energy Technology Data Exchange (ETDEWEB)

    Kume, T.; Nagasawa, N.; Matsuhashi, S. [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment] [and others

    2000-03-01

    Radiation effects on carbohydrates such as chitosan, sodium alginate, carrageenan, cellulose, pectin have been investigated to improve the biological activities. These carbohydrates were easily degraded by irradiation and induced various kinds of biological activities such as anti-bacterial activity, promotion of plant growth, suppression of heavy metal stress, phytoalexins induction. Pectic fragments obtained from degraded pectin induced the phytoalexins such as glyceollins in soybean and pisatin in pea. The irradiated chitosan shows the higher elicitor activity for pisatin than that of pectin. For the plant growth promotion, alginate derived from brown marine algae, chitosan and ligno-cellulosic extracts show a strong activity. Kappa and iota carrageenan derived from red marine algae can promote growth of rice and the highest effect was obtained with kappa irradiated at 100 kGy. Some radiation degraded carbohydrates suppressed the damage of heavy metals on plants. The effects of irradiated carbohydrates on transportation of heavy metals have been investigated by PETIS (Positron Emitting Tracer Imaging System) and autoradiography using {sup 48}V and {sup 62}Zn. (author)

  1. Radiation degradation of carbohydrates and their biological activities for plants

    International Nuclear Information System (INIS)

    Radiation effects on carbohydrates such as chitosan, sodium alginate, carrageenan, cellulose, pectin have been investigated to improve the biological activities. These carbohydrates were easily degraded by irradiation and induced various kinds of biological activities such as anti-bacterial activity, promotion of plant growth, suppression of heavy metal stress, phytoalexins induction. Pectic fragments obtained from degraded pectin induced the phytoalexins such as glyceollins in soybean and pisatin in pea. The irradiated chitosan shows the higher elicitor activity for pisatin than that of pectin. For the plant growth promotion, alginate derived from brown marine algae, chitosan and ligno-cellulosic extracts show a strong activity. Kappa and iota carrageenan derived from red marine algae can promote growth of rice and the highest effect was obtained with kappa irradiated at 100 kGy. Some radiation degraded carbohydrates suppressed the damage of heavy metals on plants. The effects of irradiated carbohydrates on transportation of heavy metals have been investigated by PETIS (Positron Emitting Tracer Imaging System) and autoradiography using 48V and 62Zn. (author)

  2. On the mechanism of biological activation by tritium.

    Science.gov (United States)

    Rozhko, T V; Badun, G A; Razzhivina, I A; Guseynov, O A; Guseynova, V E; Kudryasheva, N S

    2016-06-01

    The mechanism of biological activation by beta-emitting radionuclide tritium was studied. Luminous marine bacteria were used as a bioassay to monitor the biological effect of tritium with luminescence intensity as the physiological parameter tested. Two different types of tritium sources were used: HTO molecules distributed regularly in the surrounding aqueous medium, and a solid source with tritium atoms fixed on its surface (tritium-labeled films, 0.11, 0.28, 0.91, and 2.36 MBq/cm(2)). When using the tritium-labeled films, tritium penetration into the cells was prevented. The both types of tritium sources revealed similar changes in the bacterial luminescence kinetics: a delay period followed by bioluminescence activation. No monotonic dependences of bioluminescence activation efficiency on specific radioactivities of the films were found. A 15-day exposure to tritiated water (100 MBq/L) did not reveal mutations in bacterial DNA. The results obtained give preference to a "non-genomic" mechanism of bioluminescence activation by tritium. An activation of the intracellular bioluminescence process develops without penetration of tritium atoms into the cells and can be caused by intensification of trans-membrane cellular processes stimulated by ionization and radiolysis of aqueous media. PMID:27035890

  3. 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

    2013-01-01

    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. PMID:26784660

  4. 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.

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

    International Nuclear Information System (INIS)

    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.

  6. 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.

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

    Science.gov (United States)

    Saeed, Noha M; El-Demerdash, Ebtehal; Abdel-Rahman, Hanaa M; Algandaby, Mardi M; Al-Abbasi, Fahad A; Abdel-Naim, Ashraf B

    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. PMID:22842335

  8. Adsorption of doxorubicin on poly(methyl methacrylate)-chitosan-heparin-coated activated carbon beads.

    Science.gov (United States)

    Miao, Jianjun; Zhang, Fuming; Takieddin, Majde; Mousa, Shaker; Linhardt, Robert J

    2012-03-01

    Extracorporeal filter cartridges, filled with an activated carbon bead (ACB) adsorbent, have been used for removal of overdosed cancer drugs from the blood. Coatings on adsorbent matrices, poly(methyl methacrylate) (PMMA)/activated carbon bead and PMMA/chitosan/heparin/ACB composites, were tested to improve their biocompatibility and blood compatibility. PMMA coating on ACBs was accomplished in a straightforward manner using a PMMA solution in ethyl acetate. A one-step hybrid coating of ACBs with PMMA-anticoagulant heparin required the use of acetone and water co-solvents. Multilayer coatings with three components, PMMA, chitosan, and heparin, involved three steps: PMMA was first coated on ACBs; chitosan was then coated on the PMMA-coated surface; and finally, heparin was covalently attached to the chitosan coating. Surface morphologies were studied by scanning electron microscopy. X-ray photoelectron spectroscopy confirmed the -SO(3)(-) group. Adsorption, of a chemotherapy drug (doxorubicin) from both water and phosphate-buffered saline, by the coated ACBs was examined. The adsorption isotherm curves were fitted using the Freundlich model. The current adsorption system might find potential applications in the removal of high-dose regional chemotherapy drugs while maintaining high efficiency, biocompatibility, and blood compatibility. PMID:22313019

  9. 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. PMID:25305245

  10. 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. PMID:26748373

  11. TWO-PARAMETER ISOTHERMS OF METHYL ORANGE SORPTION BY PINECONE DERIVED ACTIVATED CARBON

    Directory of Open Access Journals (Sweden)

    M. R. Samarghandi ، M. Hadi ، S. Moayedi ، F. Barjasteh Askari

    2009-10-01

    Full Text Available The adsorption of a mono azo dye methyl-orange (MeO onto granular pinecone derived activated carbon (GPAC, from aqueous solutions, was studied in a batch system. Seven two-parameter isotherm models Langmuir, Freundlich, Dubinin-Radushkevic, Temkin, Halsey, Jovanovic and Hurkins-Jura were used to fit the experimental data. The results revealed that the adsorption isotherm models fitted the data in the order of Jovanovic (X2=1.374 > Langmuir > Dubinin-Radushkevic > Temkin > Freundlich > Halsey > Hurkins-Jura isotherms. Adsorption isotherms modeling showed that the interaction of dye with activated carbon surface is localized monolayer adsorption. A comparison of kinetic models was evaluated for the pseudo-second order, Elovich and Lagergren kinetic models. Lagergren first order model was found to agree well with the experimental data (X2=9.231. In order to determine the best-fit isotherm and kinetic models, two error analysis methods of Residual Mean Square Error and Chi-square statistic (X2 were used to evaluate the data.

  12. Summary of diamino pyrazoles derived and study their biological activities

    International Nuclear Information System (INIS)

    The work involves the synthesis of new heterocyclic structures diamino pyrazoles derivatives that are present in many natural products and products of pharmacological and therapeutic interests and study their biological activities. In order to develop a radiotracer interest and use in diagnostic nuclear medicine, we are interested to synthesis a pyrazole derivative with the precursor [Re(CO)5Br] and studying the antibacterial and antifungal activity of 3.5-diamino pyrazole and even thioamide complex rhenium. The objectives of our workout: 1/ Synthesis of molecules 3,5-diamino pyrazole and thioamide. 2/ Synthesis of 3,5-diamino pyrazole-rhenium complex. 3/ The in vitro study: Bacteriological Tests (Study of antibacterial and antifungal activity of 3,5-diamino pyrazole and thioamide). The first part of this work concerns the chemical synthesis of molecules such as: thioamide, Amp z1 Ampz2 and then we had synthesized the complex 3,5-diamino pyrazole-rhenium. Similarly we determined the physicochemical characteristics of the compounds synthesized by CLHP, CCM and RMN (1H, 13C). The second part is devoted to the study in vitro of biological activities of the synthesized molecules and complex 3,5 diaminopyrazole-rhenium with concentration 1 mg/mL and 2 mg/mL. The results allow us to say that the thioamide and Ampz2 have antibacterial activity against S. enterica and Ampz2 has low activity against S. aureus and P. aeruginossa. Other pyrazole derivatives have no significant antibacterial and antifungal activity. The results also show that the synthesized compounds of concentration 2 mg/mL in relation to the inhibition zones of amoxicillin and DMSO: 1/ Escherichia coli, there is antibacterial activity for thioamide, and the Amp z1-Re Ampz2 compound. 2/ Staphylococcus aureus, the complex Ampz 1-Re and the thioamide have significant antibacterial activity. 3/ Salmonella, we observe that the thioamide molecules, Ampz2 and Amp z1-Re have significant antibacterial activity while

  13. 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.

  14. Biological activities of water-soluble fullerene derivatives

    Science.gov (United States)

    Nakamura, S.; Mashino, T.

    2009-04-01

    Three types of water-soluble fullerene derivatives were synthesized and their biological activities were investigated. C60-dimalonic acid, an anionic fullerene derivative, showed antioxidant activity such as quenching of superoxide and relief from growth inhibition of E. coli by paraquat. C60-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 IC50 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. Biological activities of water-soluble fullerene derivatives

    International Nuclear Information System (INIS)

    Three types of water-soluble fullerene derivatives were synthesized and their biological activities were investigated. C60-dimalonic acid, an anionic fullerene derivative, showed antioxidant activity such as quenching of superoxide and relief from growth inhibition of E. coli by paraquat. C60-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 IC50 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.

  16. Chemical Composition and Biological Activities of Gerbera anandria

    Directory of Open Access Journals (Sweden)

    Fa He

    2014-04-01

    Full Text Available Gerbera anandria (Compositae was extracted with 75% ethanol and the residue was fractionated using light petroleum, chloroform and ethyl acetate. The constituents of the extracts were separated by column chromatography employing solvents of different polarity. Column chromatography of the light petroleum fraction resulted in the isolation of methyl hexadecanoate, while the chloroform fraction afforded xanthotoxin, 2-hydroxy-6-methylbenzoic acid, 7-hydroxy-1(3H-isobenzofuranone, a mixture of β-sitosterol and stigmasterol, and 8-methoxysmyrindiol and the ethyl acetate fraction gave gerberinside, apigenin-7-O-β-d-glucopyranoside and quercetin. A new coumarin, 8-methoxysmyrindiol, was found. The chemical structures of the isolated compounds were established by MS and NMR (HSQC, HMBC. Free radical scavenging and cytotoxic activities of crude extracts and 8-methoxysmyrindiol were further investigated. The ethyl acetate phase exerted the strongest DPPH free radical scavenging activity in comparison to the other fractions. The coumarin 8-methoxysmyrindiol demonstrated cytotoxicity against multiple human cancer cell lines, with the highest potency in HepG2 cells.

  17. 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.

  18. Pearson versus Spearman, Kendall's Tau Correlation Analysis on Structure-Activity Relationships of Biologic Active Compounds

    OpenAIRE

    Jäntschi, Lorentz; Sorana-Daniela BOLBOACĂ

    2006-01-01

    A sample of sixty-seven pyrimidine derivatives with inhibitory activity on E. coli dihydrofolate reductase (DHFR) was studied by the use of molecular descriptors family on structure-activity relationships. Starting from the results obtained by applying of MDF-SAR methodology on pyrimidine derivatives and from the assumption that the measured activity (compounds’ inhibitory activity) of a biologically active compounds is a semi-quantitative outcome (can be related with the type of equipment us...

  19. 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

  20. Perceived causality influences brain activity evoked by biological motion.

    Science.gov (United States)

    Morris, James P; Pelphrey, Kevin A; McCarthy, Gregory

    2008-01-01

    Using functional magnetic resonance imaging (fMRI), we investigated brain activity in an observer who watched the hand and arm motions of an individual when that individual was, or was not, the cause of the motion. Subjects viewed a realistic animated 3D character who sat at a table containing four pistons. On Intended Motion trials, the character raised his hand and arm upwards. On Unintended Motion trials, the piston under one of the character's hands pushed the hand and arm upward with the same motion. Finally, during Non-Biological Motion control trials, a piston pushed a coffee mug upward in the same smooth motion. Hand and arm motions, regardless of intention, evoked significantly more activity than control trials in a bilateral region that extended ventrally from the posterior superior temporal sulcus (pSTS) region and which was more spatially extensive in the right hemisphere. The left pSTS near the temporal-parietal junction, robustly differentiated between the Intended Motion and Unintended Motion conditions. Here, strong activity was observed for Intended Motion trials, while Unintended Motion trials evoked similar activity as the coffee mug trials. Our results demonstrate a strong hemispheric bias in the role of the pSTS in the perception of causality of biological motion. PMID:18633843

  1. Ion exchange defines the biological activity of titanate nanotubes.

    Science.gov (United States)

    Rónavári, Andrea; Kovács, Dávid; Vágvölgyi, Csaba; Kónya, Zoltán; Kiricsi, Mónika; Pfeiffer, Ilona

    2016-05-01

    One-dimensional titanate nanotubes (TiONTs) were subjected to systematic ion exchange to determine the impact of these modifications on biological activities. Ion exchanged TiONTs (with Ag, Mg, Bi, Sb, Ca, K, Sr, Fe, and Cu ions) were successfully synthesized and the presence of the substituted ions was verified by energy dispersive X-ray spectroscopy (EDS). A complex screening was carried out to reveal differences in toxicity to human cells, as well as in antibacterial, antifungal, and antiviral activities between the various modified nanotubes. Our results demonstrated that Ag ion exchanged TiONTs exerted potent antibacterial and antifungal effects against all examined microbial species but were ineffective on viruses. Surprisingly, the antibacterial activity of Cu/TiONTs was restricted to Micrococcus luteus. Most ion exchanged TiONTs did not show antimicrobial activity against the tested bacterial and fungal species. Incorporation of various ions into nanotube architectures lead to mild, moderate, or even to a massive loss of human cell viability; therefore, this type of biological effect exerted by TiONTs can be greatly modulated by ion exchange. These findings further emphasize the contribution of ion exchange in determining not only the physical and chemical characteristics but also the bioactivity of TiONT against different types of living cells. PMID:26972521

  2. 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.

  3. 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.

  4. European activities in space radiation biology and exobiology

    Energy Technology Data Exchange (ETDEWEB)

    Horneck, G. [Deutsche Forschungsanstalt fuer Luft- und Raumfahrt e.V. (DLR), Koeln (Germany)

    1996-12-31

    In view of the space station era, the European Space Agency has initiated a review and planning document for space life sciences. Radiation biology includes dosimetry of the radiation field and its modification by mass shielding, studies on the biological responses to radiation in space, on the potential impact of space flight environment on radiation effects, and assessing the radiation risks and establishing radiation protection guidelines. To reach a better understanding of the processes leading to the origin, evolution and distribution of life, exobiological activities include the exploration of the solar system, the collection and analysis of extraterrestrial samples and the utilization of space as a tool for testing the impact of space environment on organics and resistant life forms. (author)

  5. Buckwheat (Fagopyrum esculentum M.) Sprout Treated with Methyl Jasmonate (MeJA) Improved Anti-Adipogenic Activity Associated with the Oxidative Stress System in 3T3-L1 Adipocytes

    OpenAIRE

    Jeong-Ho Lim; Kee-Jai Park; Bo-Ra Yoon; Kui-Jin Kim; Young-Jun Lee; Ok-Hwan Lee

    2013-01-01

    Buckwheat sprouts contain various bioactive compounds including rutin which have a number of biological activities. We have previously shown that buckwheat sprouts (TBWE) treated with methyl jasmonate (MeJA) significantly increased the amount of phenolics and the antioxidant activity. The aim of this study was to demonstrate the effect of TBWE on anti-adipogenesis and pro-oxidant enzyme in 3T3-L1 adipocytes. We also evaluated the anti-oxidative activity of TBWE in adipocytes by using the nitr...

  6. Anti-Inflammatory Activity of Methyl Salicylate Glycosides Isolated from Gaultheria yunnanensis (Franch.) Rehder

    OpenAIRE

    Guan-Hua Du; Tian-Tai Zhang; Dong-Ming Zhang; Chao Wang; Chao Huang; Lan Sun; Rui Liu; Dan Zhang

    2011-01-01

    Gaultheria yunnanensis (Franch.) Rehder is a kind of traditional Chinese herbal medicine used for the treatments of rheumatoid arthritis, swelling and pain. Two methyl salicylate glycosides, namely methyl benzoate-2-O-b-D-xylopyranosyl(1-6)-O-b-D-gluco-pyranoside (J12122) and methyl benzoate-2-O-β-D-xylopyranosyl(1-2)[O-β-D-xylopyranosyl(1-6)]-O-β-D-glucopyranoside (J12123), are natural salicylic derivatives isolated from Gaultheria yunnanensis. In this study, we investigated the anti-inflamm...

  7. 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.

  8. Glucuronoyl esterases are active on the polymeric substrate methyl esterified glucuronoxylan.

    Science.gov (United States)

    Biely, Peter; Malovíková, Anna; Uhliariková, Iveta; Li, Xin-Liang; Wong, Dominic W S

    2015-08-19

    Alkali extracted beechwood glucuronoxylan methyl ester prepared by esterification of 4-O-methyl-D-glucuronic acid side residues by methanol was found to serve as substrate of microbial glucuronoyl esterases from Ruminococcus flavefaciens, Schizophyllum commune and Trichoderma reesei. The enzymatic deesterification was monitored by (1)H NMR spectroscopy and evaluated on the basis of the decrease of the signal of the ester methyl group and increase of the signal of methanol. The results show for the first time the action of enzymes on polymeric substrate, which imitates more closely the natural substrate in plant cell walls than the low molecular mass artificial substrates used up to present. PMID:26216754

  9. 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

  10. Biological activities of aqueous extract from Cinnamomum porrectum

    Science.gov (United States)

    Farah, H. Siti; Nazlina, I.; Yaacob, W. A.

    2013-11-01

    A study was carried out to evaluate biological activities of an extract obtained from Cinnamomum porrectum under reflux using water. Aqueous extract of Cinnamomum porrectum was tested for antibacterial activity against six Gram-positive and eight Gram-negative bacteria as well as MRSA. The results confirmed that the aqueous extract of Cinnamomum porrectum was bactericidal. Cytotoxic tests on Vero cell culture revealed that Cinnamomum porrectum was non-toxic which IC50 value higher than 0.02 mg/mL. Antiviral activity was tested based on the above IC50 values together with the measured EC50 values to obtain Therapeutic Index. The result showed that Cinnamomum porrectum has the ability to inhibit viral replication of HSV-1 in Vero cells.

  11. Biochemical studies on certain biologically active nitrogenous compounds

    International Nuclear Information System (INIS)

    Certain biologically active nitrogenous compounds such as alkaloids are widely distributed in many wild and medicinal plants such as peganum harmala L. (Phycophyllaceae). However, less literature cited on the natural compounds was extracted from the aerial parts of this plant; therefore this study was conducted on harmal leaves using several solvents. Data indicated that methanol extract was the inhibitoriest effect against some pathogenic bacteria, particularly Streptococcus pyogenus. Chromatographic separation illustrated that presence of four compounds; the most active one was the third compound (3). Elementary analysis (C, H, N) revealed that the primary chemical structure of the active antibacterial compound (C3) was: C17 H21 N3 O7 S with molecular weight 411. Spectroscopic analysis proved that coninical structure was = 1- thioformyl, 8?- D glucoperanoside- Bis- 2, 3 dihydroisopyridino pyrrol. This new compound is represented as a noval ?- carboline alkaloid compound

  12. CANTHARELLUS CIBARIUS - CULINARY-MEDICINAL MUSHROOM CONTENT AND BIOLOGICAL ACTIVITY.

    Science.gov (United States)

    Muszyńska, Bozena; Kała, Katarzyna; Firlej, Anna; Sułkowska-Ziaja, Katarzyna

    2016-01-01

    One of the most frequently harvested mushrooms in Polish forests is Yellow chanterelle (chanterelle) - Cantharellus cibarius Fr. from the Cantharellaceae family. Chanterelle is an ectomycorrhizal mushroom occurring in Poland. Chanterelle lives in symbiosis with pine, spruce, oak and hombeam. In cookery, chanterelle is appreciated because of the aroma, taste, firmness and crunchiness of its fruiting bodies. Wild edible mushrooms are widely consumed in Asia, Western Europe and Central America. Chanterelle contains a great number of carbohydrates and proteins and a low amount of fat. Actual review presents the main groups of physiologically active primary and secondary metabolites in the fruiting bodies of chanterelle such as indole and phenolic compounds, carbohydrates, fatty acids, proteins, free amino acids, sterols, carotenoids, enzymes, vitamins and elements with biological activity. The presence of these compounds and elements conditions the nutrient and therapeutic activity of chanterelle, e.g., immunomodulatory, anti-inflammatory, antioxidant, antiviral, antimicrobial and antigenotoxic properties. PMID:27476275

  13. 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

  14. 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.

  15. 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.

  16. 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.

  17. 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.

  18. 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.

  19. Biological activity of lactoferrin-functionalized biomimetic hydroxyapatite nanocrystals

    Directory of Open Access Journals (Sweden)

    Nocerino N

    2014-03-01

    Full Text Available Nunzia Nocerino,1 Andrea Fulgione,1 Marco Iannaccone,1 Laura Tomasetta,1 Flora Ianniello,1 Francesca Martora,1 Marco Lelli,2 Norberto Roveri,2 Federico Capuano,3 Rosanna Capparelli1 1Department of Agriculture Special Biotechnology Center Federico II, CeBIOTEC Biotechnology, University of Naples Federico II, Naples, 2Department of Chemistry, G Ciamician, Alma Mater Studiorum, University of Bologna, Bologna, 3Department of Food Inspection IZS ME, Naples, Italy Abstract: The emergence of bacterial strains resistant to antibiotics is a general public health problem. Progress in developing new molecules with antimicrobial properties has been made. In this study, we evaluated the biological activity of a hybrid nanocomposite composed of synthetic biomimetic hydroxyapatite surface-functionalized by lactoferrin (LF-HA. We evaluated the antimicrobial, anti-inflammatory, and antioxidant properties of LF-HA and found that the composite was active against both Gram-positive and Gram-negative bacteria, and that it modulated proinflammatory and anti-inflammatory responses and enhanced antioxidant properties as compared with LF alone. These results indicate the possibility of using LF-HA as an antimicrobial system and biomimetic hydroxyapatite as a candidate for innovative biomedical applications. Keywords: lactoferrin, hydroxyapatite nanocrystals, biomimetism, biological activity, drug delivery

  20. Structure of Biologically Active Organotin(IV) Dithiocarbamates

    Science.gov (United States)

    Farina, Y.; Sanuddin, M.; Yamin, B. M.

    2008-03-01

    The diorganotin(IV) complexes of dithiocarbamates derived from from N-ethyl-n-propylamine (EtPrdtc), 2-dimethylaminoethylamine (Me2Etdtc), 3-dimethlyamino-1-propylamine (Me2Prdtc), p-tolylmethanamine (TylMetdtc) and N-methyl-1-phenylmethanamine (MePhMetdtc) have been synthesized and characterized. Single crystal X-ray diffraction studies on Ph3Sn(EtPrdtc), Me2Sn(MePhMetdtc)2 and Bu2Sn(MePhMetdtc)2 showed that the complexes adopted a monoclinic system with space group P(2)/n, P21/n and C2/c, respectively. The Ph3Sn(EtPrdtc) complex adopted a trigonal pyramidal structure while the Me2Sn(MePhMetdtc)2 and Bu2Sn(MePhMetdtc)2 complexes displayed structures which may be described as distorted octahedrons. Cytotoxicity test using HL60 cells (human promyelocytic leukemic) showed that only Me2Sn(Me2Etdtc), Me2Sn(MePhMetdtc)2 and Bu2Sn(MePhMetdtc)2 complexes were active. The rest of the complexes did not show cytotoxicity behaviour towards HL60 cells.

  1. 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. PMID:27311502

  2. High-resolution methylation analysis of the human hypoxanthine phosphoribosyltransferase gene 5{prime} region on the active and inactive X chromosomes: Correlation with binding sites for transcription factors

    Energy Technology Data Exchange (ETDEWEB)

    Hornstra, I.K.; Yang, T.P. [Univ. of Florida College of Medicine, Gainesville, FL (United States)

    1994-02-01

    DNA methylation within GC-rich promoters of constitutively expressed X-linked genes is correlated with transcriptional silencing on the inactive X chromosome in female mammals. For most X-linked genes, X chromosome inactivation results in transcriptionally active and inactive alleles occupying each female nucleus. To examine mechanisms responsible for maintaining this unique system of differential gene expression, we have analyzed the methylation of individual cytosine residues in the 5{prime} CpG island of the human hypoxanthine phosphoribosyltransferase (HPRT) gene on the active and inactive X chromosomes. These studies demonstrate the 5{prime} CpG islands of active and 5-azacytidine-reactivated alleles are essentially unmethylated while the inactive allele is hypermethylated. The inactive allele is completely methylated at nearly all CpG dinucleotides except in a 68-bp region containing four adjacent GC boxes where most CpG dinucleotides are either unmethylated or partially methylated. Curiously, these GC boxes exhibit in vivo footprints only on the active X chromosome, not on the inactive X. The methylation pattern of the inactive HPRT gene is strikingly different from that reported for the inactive X-linked human phosphoglycerate kinase gene which exhibits methylation at all CpG sites in the 5{prime} CpG island. These results suggest that the position of methylated CpG dinucleotides, the density of methylated CpGs, the length of methylated regions, and/or chromatin structure associated with methylated DNA may have a role in repressing the activity of housekeeping promoters on the inactive X chromosome. The pattern of DNA methylation on the inactive human HPRT gene may also provide insight into the process of inactivating the gene early in female embryogenesis. 55 refs., 7 figs.

  3. 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...

  4. Physicochemical Characteristics and Biological Activity of Irradiated Pectin Solution

    International Nuclear Information System (INIS)

    Pectin was dissolved in HCI, citric acid, and deionized distilled water (DW, 2%, v/v) and irradiated at different irradiation doses (2.5-50 kGy) by gamma ray to investigate its physicochemical characteristics and biological activity. Viscosity of pectin solution was significantly decreased by irradiation up to 10 kGy, then remained constant thereafter. Gamma-irradiation increased monosaccharide and polysaccharide levels up to 30-40 kDa. Electron donating ability of pectin solution was highest when DW was added was increased by increasing irradiation dose (p less than 0.05)

  5. Nanodiamonds as Carriers for Address Delivery of Biologically Active Substances.

    Science.gov (United States)

    Purtov, K V; Petunin, A I; Burov, A E; Puzyr, A P; Bondar, V S

    2010-01-01

    Surface of detonation nanodiamonds was functionalized for the covalent attachment of immunoglobulin, and simultaneously bovine serum albumin and Rabbit Anti-Mouse Antibody. The nanodiamond-IgG(I125) and RAM-nanodiamond-BSA(I125) complexes are stable in blood serum and the immobilized proteins retain their biological activity. It was shown that the RAM-nanodiamond-BSA(I125) complex is able to bind to the target antigen immobilized on the Sepharose 6B matrix through antibody-antigen interaction. The idea can be extended to use nanodiamonds as carriers for delivery of bioactive substances (i.e., drugs) to various targets in vivo. PMID:20672079

  6. Nanodiamonds as Carriers for Address Delivery of Biologically Active Substances

    Directory of Open Access Journals (Sweden)

    Petunin AI

    2010-01-01

    Full Text Available Abstract Surface of detonation nanodiamonds was functionalized for the covalent attachment of immunoglobulin, and simultaneously bovine serum albumin and Rabbit Anti-Mouse Antibody. The nanodiamond-IgGI125 and RAM-nanodiamond-BSAI125 complexes are stable in blood serum and the immobilized proteins retain their biological activity. It was shown that the RAM-nanodiamond-BSAI125 complex is able to bind to the target antigen immobilized on the Sepharose 6B matrix through antibody–antigen interaction. The idea can be extended to use nanodiamonds as carriers for delivery of bioactive substances (i.e., drugs to various targets in vivo.

  7. 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.

  8. Activation Analysis of Biological Samples of Forensic Interest

    International Nuclear Information System (INIS)

    In forensic (crime investigation) studies, samples of a biological origin are frequently used as evidence. Often it is necessary to compare one sample (associated with a victim or the scene of a crime) with another sample of the same general type (associated with a suspect in some way). The purpose of such comparisons is to establish, if possible, that - to a high degree of probability - the two samples have a common origin. Typically, all available relevant methods of comparison are utilized in such cases by the criminalist: microscopic examination; X-ray diffraction; infra-red, visible, and ultra-violet spectrometry; and various methods of elemental analysis. The forensic applications of high-flux thermal-neutron activation analysis (NAA) have shown great promise and are attracting considerable attention. The authors' laboratory has been engaged in such forensic NAA research and development studies for the past five years. (It also operates a non-profit Forensic Activation Analysis Service, available to all law enforcement agencies, for the NAA comparison of evidence samples involved in actual criminal cases. Samples from many actual cases have been thus examined.) In the United States, NAA results have now been successfully presented in court in some 20 actual cases. Some of the evidence-type materials of interest are non-biological; others are biological. Only the latter will be discussed in this paper. The principal evidence-type materials of a biological nature that have been examined in this laboratory by high-flux thermal-NAA to date are the following: hair, blood, faeces, urine, fingernails, skin, wood, tobacco, whisky, green plants, and marijuana. (In addition, a number of these evidence-type materials have also been studied in this laboratory by high-flux photonuclear activation analysis (PNAA); attention in this paper will be largely devoted to the thermal-NAA forensic studies.) The main topics to be reported upon in this paper are: (1) limits of

  9. 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).

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

    International Nuclear Information System (INIS)

    Labdane derivatives obtained from the diterpenoid labdanediol suppressed NO and PGE2 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 PGE2 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 PGE2 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).

  11. Efficient Synthesis of 3-Methyl-flavanones and Evaluation of Their Anti-bacterial Activity

    Institute of Scientific and Technical Information of China (English)

    Nawghare Beena; Funde Sharad; Raheem Abdul; Lokhande Pradeep

    2012-01-01

    A series of 2-phenyl-2,3-dihydrochromon-4-one derivatives (flavanone derivatives) were synthesized by silica gel assisted isomerization of several a-methyl-2'-hydroxy chalcones in 74%--88% yield. These flavanones were further oxidized to 3-methyl flavones by using iodine in dimethyl sulphoxide at 60℃ in presence of acid. The newly synthesized derivatives were evaluated for in vitro study against Staphylococcus aureus, Micrococcus luteus and Staphylococcus epidermis.

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

    OpenAIRE

    Moser, Dominik A.; Ariane Paoloni-Giacobino; Ludwig Stenz; Wafae Adouan; Aurélia Manini; Francesca Suardi; Cordero, Maria I.; Marylene Vital; Ana Sancho Rossignol; Sandra Rusconi-Serpa; François Ansermet; Dayer, Alexandre G.; Schechter, Daniel S.

    2015-01-01

    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 ex...

  13. Chemical composition and biological activities of leaves of ziziphus mauritiana l. native to pakistan

    International Nuclear Information System (INIS)

    Ziziphus mauritiana L., is a fruit tree well known for its nutritional and medicinal benefits. The aim of the current study was to investigate the chemical composition as well as biological (antioxidant, antimicrobial, antitumor and anticancer) attributes of different solvent extracts from the leaves of Ziziphus mauritiana. It was established by colorimetric method that chloroform extract had greater amount of total phenolics (84.69 +- 0.92 micro g GAE/mg of extract), while methanol extract contained higher content of total flavonoids (46.94+-1.55 micro g QE/mg of extract). Meanwhile, methanol extract exhibited higher DPPH free radical scavenging potential (IC50 = 0.11 mg/mL) and antimicrobial (antibacterial and antifungal) activity among others. Overall, E. coli was noted to be the most resistant microbial strain against all the tested extracts. Chloroform extract showed strongest antitumor (IC50 = 70.74 micro g/mL) and anticancer activity (IC50 values of 27.78 and 18.32 micro g/mL against human cancer cell lines U937 and HCT-116, respectively) and significantly inhibited the viability of these cell lines. According to GC-MS analysis methyl stearate (15.59%), plamitic acid (38.55%) and micro-linolenic acid (26.45%) were identified as the major components of methanol, chloroform and hexane extracts, respectively in addition to presence of several other bioactives. The results of this study conclude that Z. mauritiana leaves extract with efficient biological activities can be explored for potential uses as antioxidant, antitumor and anticancer agents for pharmaceutical industry. (author)

  14. CpG methylation suppresses transcriptional activity of human syncytin-1 in non-placental tissues

    International Nuclear Information System (INIS)

    Syncytin-1 is a captive envelope glycoprotein encoded by one of human endogenous retroviruses W. It is expressed exclusively in the placental trophoblast where it participates in cell-to-cell fusion during differentiation of syncytiotrophobast. In other tissues, however, syncytin-1 expression must be kept in check because inadvertent cell fusion might be dangerous for tissue organization and integrity. We describe here an inverse correlation between CpG methylation of syncytin-1 5' long terminal repeat and its expression. Hypomethylation of the syncytin-1 5' long terminal repeat in the placenta and in the choriocarcinoma-derived cell line BeWo was detected. However, other analyzed primary cells and cell lines non-expressing syncytin-1 contain proviruses heavily methylated in this sequence. CpG methylation of syncytin-1 is resistant to the effect of the demethylating agent 5-azacytidine. The inhibitory role of CpG methylation is further confirmed by transient transfection of in-vitro-methylated syncytin-1 promoter-driven reporter construct. Altogether, we conclude that CpG methylation plays a principal role in the transcriptional suppression of syncytin-1 in non-placental tissues, and, in contrast, demethylation of the syncytin-1 promoter in trophoblast is a prerequisite for its expression and differentiation of multinucleated syncytiotrophoblast

  15. Analytical Methodologies for Detection of Gamma-valerolactone, Delta-valerolactone, Acephate, and Azinphos Methyl and their Associated Metabolites in Complex Biological Matrices

    Energy Technology Data Exchange (ETDEWEB)

    Zink, Erika M.; Clark, Ryan J.; Grant, Karen E.; Campbell, James A.; Hoppe, Eric W.

    2005-01-01

    Non-invasive biomonitoring for chemicals of interest in law enforcement and similar monitoring of pesticides together with their metabolites can not only save money but can lead to faster medical attention for individuals exposed to these chemicals. This study describes methods developed for the analysis of gamma-valerolactone (GVL), delta-valerolactone (DVL), acephate, and azinphos methyl in saliva and serum. Liquid chromatography/mass spectrometry (LC/MS) operated in the negative ion mode and in the positive ion mode and gas chromatography/mass spectrometry (GC/MS) were used to analyze GVL and DVL. Although both analytical techniques worked well, lower detection limits were obtained with GC/MS. The lactones and their corresponding sodium salts were spiked into both saliva and serum. The lactones were isolated from saliva or serum using newly developed extraction techniques and then subsequently analyzed using GC/MS. The sodium salts of the lactones are nonvolatile and require derivatization prior to analysis by this method. N-methyl-N-(t-butyldimethylsilyl)-trifluoroacetamide (MTBSTFA) was ultimately selected as the reagent for derivatization because the acidic conditions required for reactions with diazomethane caused the salts to undergo intramolecular cyclization to the corresponding lactones. In vitro studies were conducted using rat liver microsomes to determine other metabolites associated with these compounds. Azinphos methyl and acephate are classified as organophosphate pesticides, and are known to be cholinesterase inhibitors in humans and insects, causing neurotoxicity. For this reason they have both exposure and environmental impact implications. These compounds were spiked into serum and saliva and prepared for analysis by GC/MS. Continuation of this research would include analysis by GC/MS under positive ion mode to determine the parent ions of the unknown metabolites. Further research is planned through an in vivo analysis of the lactones and

  16. O6-methylguanine-DNA methyltransferase activity is associated with response to alkylating agent therapy and with MGMT promoter methylation in glioblastoma and anaplastic glioma

    Science.gov (United States)

    Bobola, Michael S.; Alnoor, Mohammad; Chen, John Y.-S.; Kolstoe, Douglas D.; Silbergeld, Daniel L.; Rostomily, Robert C.; Blank, A.; Chamberlain, Marc C.; Silber, John R.

    2014-01-01

    Background CpG methylation in the O6-methylguanine-DNA methyltransferase (MGMT) promoter is associated with better outcome following alkylating agent chemotherapy in glioblastoma (GBM) and anaplastic glioma (AG). To what extent improved response reflects low or absent MGMT activity in glioma tissue has not been unequivocally assessed. This information is central to developing anti-resistance therapies. Methods We examined the relationship of MGMT activity in 91 GBMs and 84 AGs with progression-free survival (PFS) following alkylator therapy and with promoter methylation status determined by methylation-specific PCR (MSP). Results Cox regression analysis revealed that GBMs with high activity had a significantly greater risk for progression in dichotomous (P ≤ 0.001) and continuous (P ≤ 0.003) models, an association observed for different alkylator regimens, including concurrent chemo-radiation with temozolomide. Analysis of MGMT promoter methylation status in 47 of the GBMs revealed that methylated tumors had significantly lower activity (P ≤ 0.005) and longer PFS (P ≤ 0.036) compared to unmethylated tumors, despite overlapping activities. PFS was also significantly greater in methylated vs. unmethylated GBMs with comparable activity (P ≤ 0.005), and among unmethylated tumors with less than median activity (P ≤ 0.026), suggesting that mechanisms in addition to MGMT promote alkylator resistance. Similar associations of MGMT activity with PFS and promoter methylation status were observed for AGs. Conclusions Our results provide strong support for the hypotheses that MGMT activity promotes alkylator resistance and reflects promoter methylation status in malignant gliomas. General significance MGMT activity is an attractive target for anti-resistance therapy regardless of methylation status. PMID:25558448

  17. Nitrogen-Containing Apigenin Analogs: Preparation and Biological Activity

    Directory of Open Access Journals (Sweden)

    Jinyi Wang

    2012-12-01

    Full Text Available A series of nitrogen-containing apigenin analogs 4a–j was synthesized via Mannich reactions to develop anticancer, antibacterial, and antioxidant agents from plant-derived flavonoids. The chemical structures of these compounds were confirmed using 1H-NMR, 13C-NMR, and ESI-MS. The in vitro biological activities of the analogs were evaluated via assays of their antiproliferative, antibacterial, and antioxidant activities. The prepared apigenin analogs exhibited different antiproliferative activities against four human cancer cell lines, namely human cervical (HeLa, human hepatocellular liver (HepG2, human lung (A549, and human breast (MCF-7 cancer cells. Compound 4i showed the most favorable in vitro antiproliferative activity with IC50 values of 40, 40, 223, and 166 μg/mL against HeLa, HepG2, A549, and MCF-7, respectively. The 1,1-diphenyl-2-picrylhydrazyl (DPPH free radical scavenging activity assay also showed that 4i had the most potent antioxidant activity, with the smallest IC50 value (334.8 μg/mL. The antibacterial activities of the analogs were determined using a two-fold serial dilution technique against four pathogenic bacteria, namely Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. All the prepared apigenin analogs exhibited more potent activities than the parent apigenin. Compounds 4h and 4j, in particular, exhibited the best inhibitory activities against the Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis with MIC values of 3.91 and 1.95 μg/mL, respectively.

  18. Activation of Tag1 transposable elements in Arabidopsis dedifferentiating cells and their regulation by CHROMOMETHYLASE 3-mediated CHG methylation.

    Science.gov (United States)

    Khan, Asif; Yadav, Narendra Singh; Morgenstern, Yaakov; Zemach, Assaf; Grafi, Gideon

    2016-10-01

    Dedifferentiation, that is, the acquisition of stem cell-like state, commonly induced by stress (e.g., protoplasting), is characterized by open chromatin conformation, a chromatin state that could lead to activation of transposable elements (TEs). Here, we studied the activation of the Arabidopsis class II TE Tag1, in which two copies, situated close to each other (near genes) on chromosome 1 are found in Landsberg erecta (Ler) but not in Columbia (Col). We first transformed protoplasts with a construct in which a truncated Tag1 (ΔTag1 non-autonomous) blocks the expression of a reporter gene AtMBD5-GFP and found a relatively high ectopic excision of ΔTag1 accompanied by expression of AtMBD5-GFP in protoplasts derived from Ler compared to Col; further increase was observed in ddm1 (decrease in DNA methylation1) protoplasts (Ler background). Ectopic excision was associated with transcription of the endogenous Tag1 and changes in histone H3 methylation at the promoter region. Focusing on the endogenous Tag1 elements we found low level of excision in Ler protoplasts, which was slightly and strongly enhanced in ddm1 and cmt3 (chromomethylase3) protoplasts, respectively, concomitantly with reduction in Tag1 gene body (GB) CHG methylation and increased Tag1 transcription; strong activation of Tag1 was also observed in cmt3 leaves. Notably, in cmt3, but not in ddm1, Tag1 elements were excised out from their original sites and transposed elsewhere in the genome. Our results suggest that dedifferentiation is associated with Tag1 activation and that CMT3 rather than DDM1 plays a central role in restraining Tag1 activation via inducing GB CHG methylation. PMID:27475038

  19. 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.

  20. Isolation and identification of 5-hydroxyl-5-methyl-2-hexenoic acid from Actinoplanes sp. HBDN08 with antifungal activity.

    Science.gov (United States)

    Zhang, Ji; Wang, Xiang-Jing; Yan, Yi-Jun; Jiang, Ling; Wang, Ji-Dong; Li, Bao-Ju; Xiang, Wen-Sheng

    2010-11-01

    A bioactivity-guided approach was employed to isolate and determine the chemical identity of bioactive constituents with antifungal activity from Actinoplanes sp. HBDN08. The structure of the antifungal metabolite was elucidated as 5-hydroxyl-5-methyl-2-hexenoic acid on the basis of spectral analysis. This compound showed strong in vitro antifungal activity against Botrytis cinerea, Cladosporium cucumerinum and Corynespora cassiicola, with an IC(50) of 32.45, 27.17, and 30.66 mg/L, respectively; however, it only moderately inhibited hyphal growth of Rhizoctonia solani with an IC(50) of 61.64 mg/L. The in vivo antifungal activity under greenhouse conditions demonstrated that 5-hydroxyl-5-methyl-2-hexenoic acid could effectively control the diseases caused by B. cinerea, C. cucumerinum and C. cassiicola with 71.42%, 78.63% and 65.13% control values at 350 mg/L, respectively. This strong antifungal activity suggests that 5-hydroxyl-5-methyl-2-hexenoic acid might be a promising candidate for new antifungal agents. PMID:20584599

  1. 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.

  2. Biological activities of an extract from Cleome viscosa L. (Capparaceae).

    Science.gov (United States)

    Williams, L A D; Vasques, E; Reid, W; Porter, R; Kraus, W

    2003-10-01

    Electron micrograph examination of the leaf and stem surfaces of Cleome viscosa L (Family Capparaceae) revealed the presence of secretory glandular trichomes with club-cylinder and cylinder morphologies. In the present study, the leaves and stems of C. viscosa were extracted with hexane and the extract was evaluated for the following biological activities: anti-bacterial, anti-fungal, contact insecticidal and nematicidal. The extract was found to be a potent anti-bacterial agent according to the thin layer chromatography autobiographic assay. Activity-directed isolation studies of the anti-bacterially active compounds led to a 14-member ring cembranoid diterpene being identified as one of the effective agents. Minimum inhibitory concentration (MIC) values (microg/spot) of 5.0 microg/spot and 1.0 microg/spot were found for the diterpene on Bacillus subtilis (Gram-positive) and Pseudomonas fluorescens (Gram-negative), respectively. The diterpene did not inhibit the growth of the fungus Cladosporium cucumerinum. The extract demonstrated a pyrethroid type of contact insecticidal activity on adult Cylas formicarius elegantulus Summer (Coleoptera: Curculionidae). The extract also had high nematicidal activity with a percentage Abbott's value of 72.69 on the plant parasitic nematode Meloidogyne incognita Chitwood; however, the extract lost its potency upon subfractionation. PMID:14564407

  3. 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.

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

    OpenAIRE

    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

    2010-01-01

    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 m...

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

    OpenAIRE

    M. Lácova; R. Gasparová

    2005-01-01

    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 reac...

  6. Activation of N-Methyl-d-aspartate (NMDA) Receptors in the Dorsal Vagal Complex Lowers Glucose Production*

    OpenAIRE

    Lam, Carol K. L.; Chari, Madhu; Su, Brenda B.; Cheung, Grace W.C.; Kokorovic, Andrea; Yang, Clair S.; Wang, Penny Y. T.; Lai, Teresa Y.Y.; Lam, Tony K.T.

    2010-01-01

    Diabetes is characterized by hyperglycemia due partly to increased hepatic glucose production. The hypothalamus regulates hepatic glucose production in rodents. However, it is currently unknown whether other regions of the brain are sufficient in glucose production regulation. The N-methyl-d-aspartate (NMDA) receptor is composed of NR1 and NR2 subunits, which are activated by co-agonist glycine and glutamate or aspartate, respectively. Here we report that direct administration of either co-ag...

  7. [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.

  8. 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

    2016-03-01

    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. PMID:26894797

  9. Biological activity of soil contaminated with cobalt, tin, and molybdenum.

    Science.gov (United States)

    Zaborowska, Magdalena; Kucharski, Jan; Wyszkowska, Jadwiga

    2016-07-01

    In this age of intensive industrialization and urbanization, mankind's highest concern should be to analyze the effect of all metals accumulating in the environment, both those considered toxic and trace elements. With this aim in mind, a unique study was conducted to determine the potentially negative impact of Sn(2+), Co(2+), and Mo(5+) in optimal and increased doses on soil biological properties. These metals were applied in the form of aqueous solutions of Sn(2+) (SnCl2 (.)2H2O), Co(2+) (CoCl2 · 6H2O), and Mo(5+) (MoCl5), each in the doses of 0, 25, 50, 100, 200, 400, and 800 mg kg(-1) soil DM. The activity of dehydrogenases, urease, acid phosphatase, alkaline phosphatase, arylsulfatase, and catalase and the counts of twelve microorganism groups were determined on the 25th and 50th day of experiment duration. Moreover, to present the studied problem comprehensively, changes in the biochemical activity and yield of spring barley were shown using soil and plant resistance indices-RS. The study shows that Sn(2+), Co(2+), and Mo(5+) disturb the state of soil homeostasis. Co(2+) and Mo(5+) proved the greatest soil biological activity inhibitors. The residence of these metals in soil, particularly Co(2+), also generated a drastic decrease in the value of spring barley resistance. Only Sn(2+) did not disrupt its yielding. The studied enzymes can be arranged as follows for their sensitivity to Sn(2+), Co(2+), Mo(5+): Deh > Ure > Aryl > Pal > Pac > Cat. Dehydrogenases and urease may be reliable soil health indicators. PMID:27277093

  10. 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. PMID:26887328

  11. Biological and Nonbiological Antioxidant Activity of Some Essential Oils.

    Science.gov (United States)

    Pérez-Rosés, Renato; Risco, Ester; Vila, Roser; Peñalver, Pedro; Cañigueral, Salvador

    2016-06-15

    Fifteen essential oils, four essential oil fractions, and three pure compounds (thymol, carvacrol, and eugenol), characterized by gas chromatography and gas chromatography-mass spectrometry, were investigated for biological and nonbiological antioxidant activity. Clove oil and eugenol showed strong DPPH (2,2-diphenyl-1-picrylhydrazyl) free-radical scavenging activity (IC50 = 13.2 μg/mL and 11.7 μg/mL, respectively) and powerfully inhibited reactive oxygen species (ROS) production in human neutrophils stimulated by PMA (phorbol 12-myristate 13-acetate) (IC50 = 7.5 μg/mL and 1.6 μg/mL) or H2O2 (IC50 = 22.6 μg/mL and 27.1 μg/mL). Nutmeg, ginger, and palmarosa oils were also highly active on this test. Essential oils from clove and ginger, as well as eugenol, carvacrol, and bornyl acetate inhibited NO (nitric oxide) production (IC50 oils of clove, red thyme, and Spanish oregano, together with eugenol, thymol, and carvacrol showed the highest myeloperoxidase inhibitory activity. Isomers carvacrol and thymol displayed a disparate behavior in some tests. All in all, clove oil and eugenol offered the best antioxidant profile. PMID:27214068

  12. Colloidal mesoporous silica nanoparticles enhance the biological activity of resveratrol.

    Science.gov (United States)

    Summerlin, Natalie; Qu, Zhi; Pujara, Naisarg; Sheng, Yong; Jambhrunkar, Siddharth; McGuckin, Michael; Popat, Amirali

    2016-08-01

    The naturally occurring polyphenol resveratrol (RES) has attracted increasing attention in recent years due to its antioxidant, anti-inflammatory, and anticancer activity. However, resveratrol's promising potential as a nutraceutical is hindered by its poor aqueous solubility, which limits its biological activity. Here we show that encapsulating resveratrol in colloidal mesoporous silica nanoparticles (MCM-48-RES) enhances its saturated solubility by ∼95% and increases its in vitro release kinetics compared to pure resveratrol. MCM-48-RES showed high loading capacity (20% w/w) and excellent encapsulation efficiency (100%). When tested against HT-29 and LS147T colon cancer cell lines, MCM-48-RES-mediated in vitro cell death was higher than that of pure resveratrol, mediated via the PARP and cIAP1 pathways. Finally, MCM-48-RES treatment also inhibited lipopolysaccharide-induced NF-κB activation in RAW264.7 cells, demonstrating improved anti-inflammatory activity. More broadly, our observations demonstrate the potential of colloidal mesoporous silica nanoparticles as next generation delivery carriers for hydrophobic nutraceuticals. PMID:27060664

  13. [The biological activity of macrophages in health and disease].

    Science.gov (United States)

    Nazimek, Katarzyna; Bryniarski, Krzysztof

    2012-01-01

    Macrophages are involved in immune response as phagocytes, antigen presenting cells and as effector cells of delayed-type hypersensitivity. Moreover, the activity of macrophages is associated with modulation of many biological processes during the whole life and depends on the actual macrophage phenotype induced under the influence of various microenvironmental stimuli. In pregnancy, placental macrophages induce the development of maternal tolerance to fetal antigens, while fetal macrophages are responsible for proper formation of tissues and organs. Residual macrophages play a very important role in tissue homeostasis, apoptotic cell clearance to prevent autoimmunization and first defense in infections. The inflammatory response of macrophages may be modulated by pathogens. Their suppressive activity is observed in immunologically privileged organs such as testes. In pathologies, macrophages are responsible for tissue damage in a case of nonspecific activation followed by overproduction of proinflammatory factors. Suppression of a specific immune response against tumors is mainly the effect of tumor associated macrophage (TAM) action. On the other hand, presentation of allergens or self-antigens by macrophages and their nonspecific activation by necrotic adipocytes leads to the induction of a chronic inflammatory response and impairment of immunity. Therefore, modulation of macrophage functions may be the key for improvement of therapy of cancer and allergic, autoimmune, metabolic, cardiovascular and Alzheimer's diseases. PMID:22922151

  14. Biological Activities of the Essential Oil from Erigeron floribundus

    Directory of Open Access Journals (Sweden)

    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.

  15. 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.

  16. 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.

  17. Biological surface-active compounds from marine bacteria.

    Science.gov (United States)

    Dang, Nga Phuong; Landfald, Bjarne; Willassen, Nils Peder

    2016-01-01

    Surface-active compounds (SACs) are widely used in different industries as well as in many daily consumption products. However, with the increasing concern for their environmental acceptability, attention has turned towards biological SACs which are biodegradable, less toxic and more environmentally friendly. In this work, 176 marine hydrocarbon-degrading bacterial isolates from petroleum-contaminated sites along the Norwegian coastline were isolated and screened for their capacity to produce biological SACs. Among them, 18 isolates were capable of reducing the surface tension of the culture medium by at least 20 mN m(-1) and/or capable of maintaining more than 40% of the emulsion volume after 24 h when growing on glucose or kerosene as carbon and energy source. These isolates were members of the genera Pseudomonas, Pseudoalteromonas, Rhodococcus, Catenovulum, Cobetia, Glaciecola, Serratia, Marinomonas and Psychromonas. Two isolates, Rhodococcus sp. LF-13 and Rhodococcus sp. LF-22, reduced surface tension of culture medium by more than 40 mN m(-1) when growing on kerosene, n-hexadecane or rapeseed oil. The biosurfactants were produced by resting cells of the two Rhodococcus strains suggesting the biosynthesis of the biosurfactants was not necessarily associated with their growth on hydrocarbons. PMID:26506920

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

    OpenAIRE

    Lisa Markenstein; Antje Appelt-Menzel; Marco Metzger; Gerhard Wenz

    2014-01-01

    The mono-6-deoxy-6-azides of 2,6-di-O-methyl-beta-cyclodextrin (DIMEB) and randomly methylated-beta-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 degrees C (DIMEB-HES) and 84.5 degrees C (RAMEB-HES), respectively. LCST phase separations could be completely avoided by the introduction of a small amount of carboxylate groups at...

  19. Production of biologically active recombinant human lactoferrin in Aspergillus oryzae.

    Science.gov (United States)

    Ward, P P; Lo, J Y; Duke, M; May, G S; Headon, D R; Conneely, O M

    1992-07-01

    We report the production of recombinant human lactoferrin in Aspergillus oryzae. Expression of human lactoferrin (hLF), a 78 kD glycoprotein, was achieved by placing the cDNA under the control of the A. oryzae alpha-amylase promoter and the 3' flanking region of the A. niger glucoamylase gene. Using this system, hLF is expressed and secreted into the growth medium at levels up to 25 mg/l. The recombinant lactoferrin is indistinguishable from human milk lactoferrin with respect to its size, immunoreactivity, and iron-binding capacity. The recombinant protein appears to be appropriately N-linked glycosylated and correctly processed at the N-terminus by the A. oryzae secretory apparatus. Lactoferrin is the largest heterologous protein and the first mammalian glycoprotein expressed in the Aspergillus system to date. Hence, this expression system appears suitable for the large-scale production and secretion of biologically active mammalian glycoproteins. PMID:1368268

  20. Inactivation efficiencies of radical reactions with biologically active DNA

    Science.gov (United States)

    Lafleur, M. V. M.; Retèl, J.; Loman, H.

    Dilute aqueous solutions of biologically active θX174 DNA may serve as a simplified model system of the cell. Damage to the DNA after irradiation with γ-rays, may be ascribed to reactions with .OH, .H and e -aq or secondary radicals, arising from reactions of water radicals with added scavengers. Conversion of primary (water) radicals into secondary (scavenger) radicals leads to a considerable protection of the DNA, which, however, would have been larger if these secondary radicals did not contribute to DNA inactivation. The inactivation yield due to isopropanol or formate (secondary) radicals depends on dose rate as well as DNA concentration. Furthermore the inactivation efficiencies of the reactions of both the primary and the secondary radicals with single-stranded DNA could be established.

  1. Inactivation efficiencies of radical reactions with biologically active DNA

    International Nuclear Information System (INIS)

    Dilute aqueous solutions of biologically active ΦX174 DNA may serve as a simplified model system of the cell. Damage to the DNA after irradiation with γ-rays, may be ascribed to reactions with radical OH, radical H and esub(aq)- or secondary radicals, arising from reactions of water radicals with added scavengers. Conversion of primary (water) radicals into secondary (scavenger) radicals leads to a considerable protection of the DNA, which however, would have been larger if these secondary radicals did not contribute to DNA inactivation. The inactivation yield due to isopropanol or formate (secondary) radicals depends on dose rate as well as DNA concentration. Furthermore the inactivation efficiencies of the reactions of both the primary and the secondary radicals with single-stranded DNA could be established. (author)

  2. Simaroubaceae family: botany, chemical composition and biological activities

    Directory of Open Access Journals (Sweden)

    Iasmine A.B.S. Alves

    2014-08-01

    Full Text Available The Simaroubaceae family includes 32 genera and more than 170 species of trees and brushes of pantropical distribution. The main distribution hot spots are located at tropical areas of America, extending to Africa, Madagascar and regions of Australia bathed by the Pacific. This family is characterized by the presence of quassinoids, secondary metabolites responsible of a wide spectrum of biological activities such as antitumor, antimalarial, antiviral, insecticide, feeding deterrent, amebicide, antiparasitic and herbicidal. Although the chemical and pharmacological potential of Simaroubaceae family as well as its participation in official compendia; such as British, German, French and Brazilian pharmacopoeias, and patent registration, many of its species have not been studied yet. In order to direct further investigation to approach detailed botanical, chemical and pharmacological aspects of the Simaroubaceae, the present work reviews the information regarding the main genera of the family up to 2013.

  3. Constituents and Biological Activities of some Iranian Artemisia species

    Directory of Open Access Journals (Sweden)

    Abdolhossein Rustaiyan

    2014-09-01

    Full Text Available Plants play a vital role in maintaining human health and contribute towards improvement of human life. They are important components of medicines, cosmetics, dyes, beverages etc. Plants have been one of the important sources of medicines even since the dawn of human civilization. In spite of tremendous development in the field of allopathy during the 20th century, plants still remain one of the major sources of drug in the modern as well as traditional system of medicine throughout the world. Over 60% of all pharmaceuticals are plant-based. Plants are considered as state-of-art chemical laboratories capable of biosynthesizing number of biomolecules of different chemical classes. The present review describes the chemical and biological activities of some Iranian Artemisia species: A. aucheri Boiss., A. austriaca Jacq., A. chamaemelifolia Vill, A. ciniformis Krasch, A. deserti Krasch and A. diffusa. Krasch.

  4. 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. PMID:27357404

  5. [The release of biologically active compounds from peat peloids].

    Science.gov (United States)

    Babaskin, D V

    2011-01-01

    This work had the objective to study kinetics of the release of flavonoides from peat peloid compositions containing extracts of medicinal herbs in model systems.The key parameters of the process are defined. The rate of liberation of flavonoides is shown to depend on their initial concentration in the compositions being used. The influence of the flavonoide composition of the tested extracts and dimethylsulfoxide on the release of biologically active compounds contained in the starting material in the model environment is estimated. The possibility of the layer-by-layer deposition of the compositions and peat peloids in order to increase the efficacy of flavonoide release from the starting composition and to ensure more rational utilization of the extracts of medicinal plants is demonstrated. PMID:22165149

  6. Radiation degradation of polysaccharides and induced biological activity

    Energy Technology Data Exchange (ETDEWEB)

    Nagasawa, Naotsugu; Yoshii, Fumio; Makuuchi Keizo; Kume Tamikazu [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment; Mitomo, Hiroshi [Gunma Univ., Kiryu (Japan). Faculty of Engineering

    1999-09-01

    Relationship between irradiation effect of polysaccharides and induced biological activity for plants has been investigated. Sodium alginate was irradiated by gamma-rays from a Co-60 source in liquid state (aqueous solution) and in solid state (powder form). Measurement of molecular weight and analysis of UV spectra of irradiated sodium alginate have been carried out. The molecular weight was decreased by irradiation in both conditions. New absorbance peak derived from double bond or/and carbonyl group was appeared at close to 267 nm by irradiation in UV spectra. It was found that alginate having molecular weight about 10,000 is most suitable to used as growth promoter in plants. To obtain the molecular weight of 10,000 by irradiation, the necessary doses are 100 kGy in liquid state and 500 kGy in solid state, respectively. (author)

  7. Synthesis, spectroscopic characterization and biological evaluation studies of Schiff's base derived from naphthofuran-2-carbohydrazide with 8-formyl-7-hydroxy-4-methyl coumarin and its metal complexes

    Science.gov (United States)

    Halli, M. B.; Sumathi, R. B.; Kinni, Mallikarjun

    2012-12-01

    Metal complexes of the type ML2, where M = Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II) and L = Schiff's base derived from the condensation of naphthofuran-2-carbohydrazide with 8-formyl-7-hydroxy-4-methyl coumarin have been synthesized. The chelation of the complexes have been elucidated in the light of analytical, IR, UV-vis, 1H NMR, mass, ESR spectral data, thermal and magnetic studies. The measured molar conductance values indicate that, the complexes are non-electrolytic in nature. The redox behavior of one of the synthesized metal complexes was investigated by cyclic voltammetry. The Schiff's base and its metal complexes have been screened for their in vitro antibacterial and antifungal activities by MIC method. The DNA cleavage activities of all the complexes were studied by agarose gel electrophoresis method. In addition, the free ligand along with its complexes has been studied for their antioxidant activity.

  8. The long-term fertilization effect on biological activity of different genesis soils

    OpenAIRE

    Grigaliūnienė, Kristina

    2006-01-01

    The effect of organic and mineral fertilizers on biological activity of different genesis soils in long-term crop rotation trials was determined. Biological activity was diverse in the soils of different genesis and it activity correlated with some soil chemical properties. Organic and mineral fertilizers and their combinations more increased biological activity in the soil than only mineral fertilizers. Mineral fertilizers suppressed dehydrogenase and alkaline phosphatase activity (180 kg ha...

  9. 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.

  10. BIOLOGICAL ACTIVITY OF APPLE JUICE ENRICHED BY HERBAL EXTRACTS

    Directory of Open Access Journals (Sweden)

    Eva Ivanišová

    2015-02-01

    Full Text Available Herbal phytochemicals have recently become an attractive subject for scientists in many different research areas. The aim of this study was to determine antioxidant activity, total polyphenol and flavonoid content of apple juice enriched by water herbal extracts. Secondary was to evaluate sensory characteristic of enriched apple juice. It was found that applications of water herbal extracts to apple juice increase antioxidant activities, and also total polyphenol and flavonoid content with compare to pure apple juice. The highest biological activities were detected in apple juice with addition of lemon balm (14.42 mg TEAC/L; 84.38 mg TEAC/L; 50.88 mg GAE/L; 36.26 μg QE/L, oregano (14.92 mg TEAC/L; 79.97 mg TEAC/L; 50.51 mg GAE/L; 31.02 μg QE/L and salvia (8.40 mg TEAC/L; 30.40 mg TEAC/L; 23.33 mg GAE/L; 27.67 μg QE/L water extract. Sensorial analysis of samples showed, that enriched juices had better properties for evaluators with compared to pure juice. The aim of this study was also to mention the potential use of medicinal herbs in food industry, because plant bioactive compounds can play an important role in preventing cardiovascular diseases, cancers and reduction inflammatory action.

  11. 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.

  12. In vitro biological activities of alkaloids from Cryptolepis sanguinolenta.

    Science.gov (United States)

    Cimanga, K; De Bruyne, T; Lasure, A; Van Poel, B; Pieters, L; Claeys, M; Berghe, D V; Kambu, K; Tona, L; Vlietinck, A J

    1996-02-01

    In our biological screening of higher plants, an aqueous and an 80% EtOH extract from the root bark of Cryptolepis sanguinolenta showed potent antibacterial, anticomplementary, and moderate antiviral activities, but no antifungal effect could be detected. Bioassay-guided fractionation of the 80% EtOH extract led to the isolation of three alkaloids: quindoline (1), hydroxycryptolepine (2), cryptolepine.HCl (3), and the corresponding base cryptolepine (4). All compounds strongly inhibited the growth of Gram-positive bacteria (MIC 500 micrograms/ml) against selected Gram-negative bacteria. They also possessed a bactericidal effect depending on the bacterial strain. Compounds 1, 2 and 3 displayed a dose-dependent inhibitory effect on the classical pathway of the complement system while compounds 2 and 3 activated the alternative pathway, except for compound 1. Compound 3 was found to possess an antiherpetic activity. Compounds 1 and 4 showed no antiviral effect, but were quite cytotoxic in the antiviral test system down to a concentration of 1 microgram/ml. PMID:8720383

  13. Cholinesterase activity of muscle tissue from freshwater fishes: characterization and sensitivity analysis to the organophosphate methyl-paraoxon.

    Science.gov (United States)

    Lopes, Renato Matos; Filho, Moacelio Veranio Silva; de Salles, João Bosco; Bastos, Vera Lúcia Freire Cunha; Bastos, Jayme Cunha

    2014-06-01

    The biochemical characterization of cholinesterases (ChE) from different teleost species has been a critical step in ensuring the proper use of ChE activity levels as biomarkers in environmental monitoring programs. In the present study, ChE from Oreochromis niloticus, Piaractus mesopotamicus, Leporinus macrocephalus, and Prochilodus lineatus was biochemically characterized by specific substrates and inhibitors. Moreover, muscle tissue ChE sensitivity to the organophosphate pesticide methyl-paraoxon was evaluated by determining the inhibition kinetic constants for its progressive irreversible inhibition by methyl-paraoxon as well as the 50% inhibitory concentration (IC50) for 30 min for each species. The present results indicate that acetylcholinesterase (AChE) must be present in the muscle from P. mesopotamicus, L. macrocephalus, and P. lineatus and that O. niloticus possesses an atypical cholinesterase or AChE and butyrylcholinesterase (BChE). Furthermore, there is a large difference regarding the sensitivity of these enzymes to methyl-paraoxon. The determined IC50 values for 30 min were 70 nM (O. niloticus), 258 nM (P. lineatus), 319 nM (L. macrocephalus), and 1578 nM (P. mesopotamicus). The results of the present study also indicate that the use of efficient methods for extracting these enzymes, their kinetic characterization, and determination of sensitivity differences between AChE and BChE to organophosphate compounds are essential for the determination of accurate ChE activity levels for environmental monitoring programs. PMID:24648156

  14. 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

  15. Synthesis and evaluation of alpha-[[(2-haloethyl)amino]methyl]-2- nitro-1H-imidazole-1-ethanols as prodrugs of alpha-[(1-aziridinyl)methyl]-2- nitro-1H-imidazole-1-ethanol (RSU-1069) and its analogues which are radiosensitizers and bioreductively activated cytotoxins

    International Nuclear Information System (INIS)

    alpha-[(1-Aziridinyl)methyl]-2-nitro-1H-imidazole-1-ethanols, of general formula ImCH2CH(OH)CH2NCR1R2CR3R4, where Im = 2-nitroimidazole and R1, R2, R3, R4 = H, Me, are radiosensitizers and selective bioreductively activated cytotoxins toward hypoxic tumor cells in vitro and in vivo. Treatment of the aziridines with hydrogen halide in acetone or aqueous acetone gave the corresponding 2-haloethylamines of general formula ImCH2CH(OH)CH2(+)-NH2CR1R2CR3R4X X-, where R1, R2, R3, R4 = H, Me, and X = F, Cl, Br, I. These 2-haloethylamines were evaluated as prodrugs of the parent aziridines. The rates of ring closure in aqueous solution at pH approximately 6 were found to increase with increasing methyl substitution and to depend on the nature of the leaving group (I approximately Br greater than Cl much greater than F). A competing reaction of ImCH2CH(OH)CH2+NH2CH2CH2X X- (X = Cl, Br) with aqueous HCO3- ions gives 3-[2-hyroxy-3-(2-nitro-1H-imidazol-1-yl)propyl]-2-oxazolidinone. The activities of these prodrugs as radiosensitizers or as bioreductively activated cytotoxins were consistent with the proportion converted to the parent aziridine during the course of the experiment. alpha-[[(2-Bromoethyl)amino]methyl]-2-nitro-1H-imidazole-1- ethanol (RB 6145, 10), the prodrug of alpha-[(1-aziridinyl)methyl]-2-nitro-1H-imidazole-1-ethanol (RSU-1069, 3), is identified as the most useful compound in terms of biological activity and rate of ring closure under physiological conditions

  16. Biological activity of terpene compounds produced by biotechnological methods.

    Science.gov (United States)

    Paduch, Roman; Trytek, Mariusz; Król, Sylwia K; Kud, Joanna; Frant, Maciej; Kandefer-Szerszeń, Martyna; Fiedurek, Jan

    2016-06-01

    Context Biotransformation systems are profitable tools for structural modification of bioactive natural compounds into valuable biologically active terpenoids. Objective This study determines the biological effect of (R)-(+)-limonene and (-)-α-pinene, and their oxygenated derivatives, (a) perillyl alcohol and (S)-(+)- and (R)-(-)-carvone enantiomers and (b) linalool, trans-verbenol and verbenone, respectively, on human colon tumour cells and normal colonic epithelium. Materials and methods Biotransformation procedures and in vitro cell culture tests were used in this work. Cells were incubated for 24 h with terpenes at concentrations of 5-500 μg/mL for NR, MTT, DPPH, and NO assays. IL-6 was determined by ELISA with/without 2 h pre-activation with 10 μg/mL LPS. Results trans-Verbenol and perillyl alcohol, obtained via biotransformation, produced in vitro effect against tumour cells at lower concentrations (IC50 value = 77.8 and 98.8 μg/mL, respectively) than their monoterpene precursors, (R)-(+)-limonene (IC50 value = 171.4 μg/mL) and (-)-α-pinene (IC50 value = 206.3 μg/mL). They also showed lower cytotoxicity against normal cells (IC50 > 500 and > 200 μg/mL, respectively). (S)-(+)-Carvone was 59.4% and 27.1% more toxic to tumour and normal cells, respectively, than the (R)-(-)-enantiomer. (R)-(+)-limonene derivatives decreased IL-6 production from normal cells in media with or without LPS (30.2% and 13.9%, respectively), while (-)-α-pinene derivatives induced IL-6 (verbenone had the strongest effect, 60.2% and 29.1% above control, respectively). None of the terpenes had antioxidative activity below 500 μg/mL. Discussion and conclusions Bioactivity against tumour cells decreased in the following order: alcohols > ketones > hydrocarbons. (R)-(+)-limonene, (-)-α-pinene, and their derivatives expressed diverse activity towards normal and tumour cells with noticeable enantiomeric differences. PMID:26808720

  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

    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. 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

    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...

  19. Phenolic Compounds Characterization and Biological Activities of Citrus aurantium Bloom

    Directory of Open Access Journals (Sweden)

    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

  20. 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…

  1. Teaching Systems Biology: An Active-Learning Approach

    Science.gov (United States)

    Kumar, Anuj

    2005-01-01

    With genomics well established in modern molecular biology, recent studies have sought to further the discipline by integrating complementary methodologies into a holistic depiction of the molecular mechanisms underpinning cell function. This genomic subdiscipline, loosely termed "systems biology," presents the biology educator with both…

  2. Synthesis, Characterization and Biological Activities of Organotin (IV Methylcyclohexyldithiocarbamate Compounds

    Directory of Open Access Journals (Sweden)

    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.

  3. Increased intragenic IGF2 methylation is associated with repression of insulator activity and elevated expression in serous ovarian carcinoma

    Directory of Open Access Journals (Sweden)

    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

  4. Chemistry, biogenesis, and biological activities of Cinnamomum zeylanicum.

    Science.gov (United States)

    Jayaprakasha, G K; Rao, L Jagan Mohan

    2011-07-01

    The genus Cinnamomum comprises of several hundreds of species, which are distributed in Asia and Australia. Cinnamomum zeylanicum, the source of cinnamon bark and leaf oils, is an indigenous tree of Sri Lanka, although most oil now comes from cultivated areas. C. zeylanicum is an important spice and aromatic crop having wide applications in flavoring, perfumery, beverages, and medicines. Volatile oils from different parts of cinnamon such as leaves, bark, fruits, root bark, flowers, and buds have been isolated by hydro distillation/steam distillation and supercritical fluid extraction. The chemical compositions of the volatile oils have been identified by GC and GC-MS. More than 80 compounds were identified from different parts of cinnamon. The leaf oil has a major component called eugenol. Cinnamaldehyde and camphor have been reported to be the major components of volatile oils from stem bark and root bark, respectively. Trans-cinnamyl acetate was found to be the major compound in fruits, flowers, and fruit stalks. These volatile oils were found to exhibit antioxidant, antimicrobial, and antidiabetic activities. C. zeylanicum bark and fruits were found to contain proanthocyandins with doubly linked bis-flavan-3-ol units in the molecule. The present review provides a coherent presentation of scattered literature on the chemistry, biogenesis, and biological activities of cinnamon. PMID:21929331

  5. 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.

  6. Hen's egg as a source of valuable biologically active substances.

    Science.gov (United States)

    Zdrojewicz, Zygmunt; Herman, Marta; Starostecka, Ewa

    2016-01-01

    The aim of this article is to show current knowledge concerning valuable substances biologically active present in hen eggs and underline important nutritive role of hen eggs. Hen egg is a good source of nutrients such as proteins, vitamins (A, B2, B6, B12, D, E, K), minerals and lipids. The significant part of lipids is a group of unsaturated phospholipids, which are components of cell membranes, act protectively on the cardiovascular system and contribute to a decrease of cholesterol level and blood pressure. Therefore, the consumption of unsaturated phospholipids is recommended especially in patients suffering from diseases of the cardiovascular system. Another important substance is egg cystatin, which has a wide spectrum of biological functions, for example the ability to stimulate cell growth, inhibit inflammatory processes and has antibacterial and antiviral properties. Other substance presented in the egg white which helps fight bacteria is lysozyme. It is used in medicine as an aid in antibiotic therapy and analgesic in the course of infection, as well as in tumor malignancies. Among the components contained in the egg yolk there is also immunoglobulin Y which due to its therapeutic importance deserves special attention. Its use offers the possibility of replacing chemotherapeutic agents in the treatment of bacterial infections of digestive system, as well as an opportunity for the development of medicine associated with passive immunization of patients. The egg is a rich source of retinol which gradual depletion in the organism causes many eye pathologies. A very important and useful part of the egg, used in medicine is a shell and its membranes, due to the high collagen content relevant in the treatment of connective tissue diseases. PMID:27383572

  7. 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.

  8. DNA Methylation and Cancer Diagnosis

    Directory of Open Access Journals (Sweden)

    Jérôme Torrisani

    2013-07-01

    Full Text Available DNA methylation is a major epigenetic modification that is strongly involved in the physiological control of genome expression. DNA methylation patterns are largely modified in cancer cells and can therefore be used to distinguish cancer cells from normal tissues. This review describes the main technologies available for the detection and the discovery of aberrantly methylated DNA patterns. It also presents the different sources of biological samples suitable for DNA methylation studies. We discuss the interest and perspectives on the use of DNA methylation measurements for cancer diagnosis through examples of methylated genes commonly documented in the literature. The discussion leads to our consideration for why DNA methylation is not commonly used in clinical practice through an examination of the main requirements that constitute a reliable biomarker. Finally, we describe the main DNA methylation inhibitors currently used in clinical trials and those that exhibit promising results.

  9. Development of Methods for the Hot Synthesis of S35-Labelled Biologically Active Substances

    International Nuclear Information System (INIS)

    It was found in investigations with model systems that sulphur-35 recoil atoms are capable of entering atom and atom-group substitution reactions through interaction with cyclic and heterocyclic compounds, as well as by way of the C-C bond. We therefore considered that it would be interesting to use the specific properties of hot sulphur atoms for the synthesis of labelled biologically active compounds. We selected 4-methyl-5β-hydroxyethyl thiazole (an intermediate product of vitamin B1 synthesis), triethylenimine thiophosphoramide and amino acids (methionine, norvaline and norleucine) for investigation. Binary systems containing the compounds enumerated above, as well as CCI4 or HCl (donors of hot S35 atoms) were investigated. Irradiation was carried out in an IRT-1000 reactor channel at a thermal neutron flux of 1011-1012 n/cm2 * s. The S35 recoil atoms, formed by the reaction Cl35 (n, p) S35 with a recoil energy of 16 keV, interact with the thiazole giving thiazole-S35. The yield of labelled product is highly dependent on the composition of the system, reaching a maximum of 20-25%. The addition of benzene (acceptor of the excitation energy) increases the yield of product, the maximum yield being reached when the ratio of CCl4, thiazole and benzene is 1:1:1. When the mixture of triethylenimine thiophosphoramide and CCl4 is irradiated, an initial product labelled with S35 and P32 is obtained, the P32 being formed by the reactions Cl35(n, α)P32, S32 and P31(n, γ)P32. Methionine-S35 is obtained by irradiating methionine and HCl in an aqueous solution. The labelled product formed is usually diluted by a carrier, although it is possible to obtain compounds without a carrier by selecting the initial compounds appropriately. Thus, by irradiating systems of norvaline-HCl and norleucine-HCl one obtains methionine-S35 without a carrier, due to the entry of S35 by way of the C-C bond into the norvaline molecule or the substitution of the CH2 group in the norleucine. In

  10. Placental DNA methylation of peroxisome-proliferator-activated receptor-γ co-activator-1α promoter is associated with maternal gestational glucose level.

    Science.gov (United States)

    Xie, Xuemei; Gao, Hongjie; Zeng, Wanjiang; Chen, Suhua; Feng, Ling; Deng, Dongrui; Qiao, Fu-yuan; Liao, Lihong; McCormick, Kenneth; Ning, Qin; Luo, Xiaoping

    2015-08-01

    Intrauterine exposure to hyperglycaemia may increase the risk of later-life metabolic disorders. Although the underlying mechanism is not fully understood, epigenetic dysregulation in fetal programming has been implicated. With regard to energy homoeostasis, PGC-1α (peroxisome-proliferator-activated receptor γ co-activator-1α, encoded by the PPARGC1A gene) plays a regulatory role in several biochemical processes. We hypothesized that maternal gestational glucose levels would positively correlate with DNA methylation of the PPARGC1A promoter in placental tissue. We undertook a cross-sectional study of 58 mothers who underwent uncomplicated Caesarean delivery in a university hospital. Maternal gestational glucose concentration was determined after a 75-g OGTT (oral glucose tolerance test) at 24-28 weeks of gestation. Placenta tissue and cord blood were collected immediately after delivery. Genomic DNA was extracted and thereafter bisulfite conversion was performed. After PCR amplification, the DNA methylation of the PPARGC1A promoter was quantified using a pyrosequencing technique. The protein level of PGC-1α was evaluated by Western blotting. For all participants as a whole, including the GDM (gestational diabetes mellitus) and normoglycaemia groups, the maternal gestational glucose level was positively correlated with placental DNA methylation, and negatively correlated with cord blood DNA methylation of the PPARGC1A promoter in a CpG site-specific manner. In the GDM group alone, the placental CpG site-specific methylation of the PPARGC1A promoter strongly correlated with gestational 2-h post-OGTT glycaemia. Epigenetic alteration of the PPAGRC1A promoter may be one of the potential mechanisms underlying the metabolic programming in offspring exposed to intrauterine hyperglycaemia. PMID:25875376

  11. Synthesis of SnO2-activated carbon fiber hybrid catalyst for the removal of methyl violet from water

    International Nuclear Information System (INIS)

    Graphical abstract: - Highlights: • A new biomass route for the synthesis of SnO2/ACF hybrid catalyst was proposed. • The original fibrous structure of kapok fiber was retained in the SnO2/ACF hybrid catalyst. • SnO2/ACF hybrid catalyst exhibited high BET surface area (647–897 m2/g) and large pore volume (0.36–0.56 cm3 g−1). • High microwave-induced catalytic activity for methyl violet degradation was obtained. - Abstract: SnO2/activated carbon fiber (ACF) hybrid catalyst was synthesized from kapok precursor via a two-step process involving pore-fabricating and self-assembly of SnO2 nanoparticles. The morphology and phase structure of the obtained samples were characterized by X-ray diffraction, field emission scanning electron microscope, high resolution transmission electron microscopy and N2 adsorption-desorption isotherm. These results demonstrated that the synthesized SnO2/ACF retained the hollow-fiber structure of kapok fibers. SnO2 nanoparticles dispersed uniformly over the ACF support. The obtained hybrid catalyst showed porous structure with high surface area (647–897 m2/g) and large pore volume (0.36–0.56 cm3 g−1). In addition, the catalytic activities of the obtained samples for methyl violet degradation under microwave irradiation were also evaluated. It was found that the SnO2/ACF catalyst exhibited high catalytic activity for methyl violet degradation due to the synergistic effect of microwave and SnO2/ACF catalyst

  12. Nanoencapsulation of Biologically Active Peptides from Whey Proteins

    Directory of Open Access Journals (Sweden)

    Sebnem Tellioglu Harsa

    2014-06-01

    Full Text Available "Now a days consumers, in order to feed with balanced diet, prefer healthy and reliable foods. In this respect food manufacturers are trying to respond the demands of consumers by developing new types of foods such as diet foods ( low calorie foods, modified foods (organic foods and functional foods (probiotic and prebiotics. Thus, production of nutritious, functional and beneficial foods has become a growing sector in the United States and European countries. Proteins are major source of many bioactive peptides. Bioactive peptides have been defined as specific protein fragments that have a positive impact on body functions and may ultimately influence human health. These peptides stay inactive within the main protein structure and activated by the enzymatic hydrolysis. These bioactive peptides, derived from proteins, are able to influence basic body systems (cardiovascular, nervous, gastrointestinal and immune systems and show multi-functional character. Due to these properties, studies have recently been focused on milk proteins and their bioactive peptides. Such peptides are inactive within the sequence of the milk protein. Whey contains a multitude of biologically active proteins and peptides. Physiologically active serum proteins are serum albumin, immunoglobulins, proteose-peptone, lactoferrin, lactoperoxidase and growth factors. In addition to these, enzymatic degradation of serum proteins releases a number of bioactive peptides such as alfa-lactophorin, beta-lactophorin, beta- lactotensin, lactokinin, albutensin, serophorin and lactoferricin. One of the common qualities of bioactive substances is their sensitivity to the physical and chemical properties of the environment. For this reason, the usefulness of bioactive components in food is limited by the structure. In order to sustain bioavailibility of these peptides, limiting its relationship with the media by encapsulation technology is one of them osthotly debated issues on in recent

  13. 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. PMID:22456234

  14. Blockade of N-methyl-d-aspartate receptor activation suppresses learning-induced synaptic elimination

    OpenAIRE

    Bock, Jörg; Braun, Katharina

    1999-01-01

    Auditory filial imprinting in the domestic chicken is accompanied by a dramatic loss of spine synapses in two higher associative forebrain areas, the mediorostral neostriatum/hyperstriatum ventrale (MNH) and the dorsocaudal neostriatum (Ndc). The cellular mechanisms that underlie this learning-induced synaptic reorganization are unclear. We found that local pharmacological blockade of N-methyl-d-aspartate (NMDA) receptors in the MNH, a manipulation that has been shown previously to impair aud...

  15. Activation of water soluble amines by halogens for trapping methyl radioactive iodine from air streams

    Science.gov (United States)

    Deitz, Victor R.; Blachly, Charles H.

    1977-01-01

    Gas adsorbent charcoals impregnated with an aqueous solution of the reaction product of a tertiary amine and elemental iodine or bromine are better than 99 per cent efficient in trapping methyl iodine.sup.131. The chemical addition of iodine or bromine to the tertiary amine molecule increases the efficiency of the impregnated charcoal as a trapping agent, and in conjunction with the high flash point of the tertiary amine raises the ignition temperature of the impregnated charcoal.

  16. 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.

  17. CMTM5 exhibits tumor suppressor activity through promoter methylation in oral squamous cell carcinoma

    International Nuclear Information System (INIS)

    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

  18. PREDICTION OF BIOLOGICAL ACTIVITY SPECTRA FOR SECONDARY METABOLITES FROM MARINE MACROALGAE CAULERPA SPP (CHLOROPHYTA – CAULERPALS

    Directory of Open Access Journals (Sweden)

    R. Azhaguraj

    2012-05-01

    Full Text Available This study aims to evaluate the biological activity of Caulerpin β-Sitosterol, Taraxerol and Palmtic acid isolated from the marine macro algae Caulerpa spp. The PASS computer program was used in this study to predict the biological activity profile of the four Phenazine derivates. The results were analyzed to show various biological activities like pharmacological (Kinase inhibitor, Neuroprotector and Antiviral, Effects (Oxidoreductase inhibitor, Acid Phosphatase inhibitor and toxicological activity (Teratogen of these compounds. The PASS software is useful for the study of biological activity of secondary metabolites.

  19. Results of activated sludge plants applying enhanced biological phosphorus removal

    Energy Technology Data Exchange (ETDEWEB)

    Machado, A.; Pinto, M.; Neder, K.; Hoffmann, H.

    1989-02-01

    To stop the eutrophication in lakes and rivers, the input of nutrient and phosphorus compounds must be limited. The biological elimination of phosphorus describes a possibility, to reduce phosphorus in the biological stage of a treatment plant to a considerable extent. In this paper the process-system and the operation-results of a pilot plant and two municipal treatment plants are presented, where biological phosphorus reduction about 80% takes place without any constructional modifications.

  20. Computational Systems Biology Analysis of Cell Reprogramming and Activation Dynamics

    OpenAIRE

    Fu, Yan

    2012-01-01

    In the past two decades, molecular cell biology has transitioned from a traditional descriptive science into a quantitative science that systematically measures cellular dynamics on different levels of genome, transcriptome and proteome. Along with this transition emerges the interdisciplinary field of systems biology, which aims to unravel complex interactions in biological systems through integrating experimental data into qualitative or quantitative models and computer simulations. In th...

  1. STUDIES OF RELATIONSHIPS BETWEEN MOLECULAR STRUCTURE AND BIOLOGICAL ACTIVITY BY PATTERN RECOGNITION METHODS

    Science.gov (United States)

    The attempt to rationalize the connections between the molecular structures of organic compounds and their biological activities comprises the field of structure-activity relations (SAR) studies. Correlations between structure and activity are important for the understanding and ...

  2. Nonoxidized, biologically active parathyroid hormone determines mortality in hemodialysis patients

    DEFF Research Database (Denmark)

    Tepel, Martin; Armbruster, Franz Paul; Grön, Hans Jürgen; Scholze, Alexandra; Reichetzeder, Christoph; Roth, Heinz Jürgen; Hocher, Berthold

    2013-01-01

    Background: It was shown that nonoxidized PTH (n-oxPTH) is bioactive, whereas the oxidation of PTH results in a loss of biological activity. Methods: In this study we analyzed the association of n-oxPTH on mortality in hemodialysis patients using a recently developed assay system. Results......: Hemodialysis patients (224 men, 116 women) had a median age of 66 years. One hundred seventy patients (50%) died during the follow-up period of 5 years. Median n-oxPTH levels were higher in survivors (7.2 ng/L) compared with deceased patients (5.0 ng/L; P = .002). Survival analysis showed an increased survival......-oxPTH levels. Conclusions: The predictive power of n-oxPTH and iPTH on the mortality of hemodialysis patients differs substantially. Measurements of n-oxPTH may reflect the hormone status more precisely. The iPTH-associated mortality is most likely describing oxidative stress-related mortality....

  3. Biological activity of harpin produced by Pantoea stewartii subsp. stewartii.

    Science.gov (United States)

    Ahmad, M; Majerczak, D R; Pike, S; Hoyos, M E; Novacky, A; Coplin, D L

    2001-10-01

    Pantoea stewartii subsp. stewartii causes Stewart's wilt of sweet corn. A hypersensitive response and pathogenicity (Hrp) secretion system is needed to produce water-soaking and wilting symptoms in corn and to cause a hypersensitive response (HR) in tobacco. Sequencing of the hrp cluster revealed a putative harpin gene, hrpN. The product of this gene was overexpressed in Escherichia coli and shown to elicit the HR in tobacco and systemic resistance in radishes. The protein was designated HrpN(Pnss). Like other harpins, it was heat stable and protease sensitive, although it was three- to fourfold less active biologically than Erwinia amylovora harpin. We used antibodies to purified HrpN(Pnss) to verify that hrpN mutants could not produce harpin. This protein was secreted into the culture supernatant and was produced by strains of P. stewartii subsp. indologenes. In order to determine the importance of HrpN(Pnss) in pathogenesis on sweet corn, three hrpN::Tn5 mutants were compared with the wild-type strain with 50% effective dose, disease severity, response time, and growth rate in planta as parameters. In all tests, HrpN(Pnss) was not required for infection, growth, or virulence in corn or endophytic growth in related grasses. PMID:11605962

  4. TEAK: topology enrichment analysis framework for detecting activated biological subpathways.

    Science.gov (United States)

    Judeh, Thair; Johnson, Cole; Kumar, Anuj; Zhu, Dongxiao

    2013-02-01

    To mine gene expression data sets effectively, analysis frameworks need to incorporate methods that identify intergenic relationships within enriched biologically relevant subpathways. For this purpose, we developed the Topology Enrichment Analysis frameworK (TEAK). TEAK employs a novel in-house algorithm and a tailor-made Clique Percolation Method to extract linear and nonlinear KEGG subpathways, respectively. TEAK scores subpathways using the Bayesian Information Criterion for context specific data and the Kullback-Leibler divergence for case-control data. In this article, we utilized TEAK with experimental studies to analyze microarray data sets profiling stress responses in the model eukaryote Saccharomyces cerevisiae. Using a public microarray data set, we identified via TEAK linear sphingolipid metabolic subpathways activated during the yeast response to nitrogen stress, and phenotypic analyses of the corresponding deletion strains indicated previously unreported fitness defects for the dpl1Δ and lag1Δ mutants under conditions of nitrogen limitation. In addition, we studied the yeast filamentous response to nitrogen stress by profiling changes in transcript levels upon deletion of two key filamentous growth transcription factors, FLO8 and MSS11. Via TEAK we identified a nonlinear glycerophospholipid metabolism subpathway involving the SLC1 gene, which we found via mutational analysis to be required for yeast filamentous growth. PMID:23268448

  5. Solar activity, magnetic storms and their effects on biological systems

    International Nuclear Information System (INIS)

    Full text: In the present time much attention is spent on the electromagnetic waves, solar radiation and magnetic storms on biological systems, including on person. However, there are few publications describing the mechanism of these influences on human. First of all it is necessary to point out that electromagnetic waves, the flow of particles in space and magnetic storms, acting on person human-all is connected with biophysical processes. So approach to influence of these factors on organism follows the processes of influence of these waves on bio system. Magnetic storms are phenomena continuously connected with solar activity. Investigation of cosmic space has intensified the practical importance of the problem of interaction with natural factors of external ambience. Much attention deserves the cosmic radiation, geomagnetic field, elements of climate and weathers. However the mechanism of bio tropic action of these factors is not enough studied. Beginning XXI century was already signified the successes in investigation of Mars. The Space shuttles 'Spirit' and 'Opportunity' successfully have carried out some work on examining and finding of water on Mars. A flight of person to Mars is being considered. One of the important mechanisms of influence on human organism is, in our opinion, the rising of the resonance at coincidence of frequencies and their more important factor is a phenomena of electromagnetic induction and forming the radicals in the organism

  6. Role of Calcium Signaling in B Cell Activation and Biology.

    Science.gov (United States)

    Baba, Yoshihiro; Kurosaki, Tomohiro

    2016-01-01

    Increase in intracellular levels of calcium ions (Ca2+) is one of the key triggering signals for the development of B cell response to the antigen. The diverse Ca2+ signals finely controlled by multiple factors participate in the regulation of gene expression, B cell development, and effector functions. B cell receptor (BCR)-initiated Ca2+ mobilization is sourced from two pathways: one is the release of Ca2+ from the intracellular stores, endoplasmic reticulum (ER), and other is the prolonged influx of extracellular Ca2+ induced by depleting the stores via store-operated calcium entry (SOCE) and calcium release-activated calcium (CRAC) channels. The identification of stromal interaction molecule 1(STIM1), the ER Ca2+ sensor, and Orai1, a key subunit of the CRAC channel pore, has now provided the tools to understand the mode of Ca2+ influx regulation and physiological relevance. Herein, we discuss our current understanding of the molecular mechanisms underlying BCR-triggered Ca2+ signaling as well as its contribution to the B cell biological processes and diseases. PMID:26369772

  7. 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.

  8. Methyl Jasmonate and 1-Methylcyclopropene Treatment Effects on Quinone Reductase Inducing Activity and Post-Harvest Quality of Broccoli

    OpenAIRE

    Ku, Kang Mo; Choi, Jeong Hee; Kim, Hyoung Seok; Kushad, Mosbah M.; Jeffery, Elizabeth H.; Juvik, John A.

    2013-01-01

    Effect of pre-harvest methyl jasmonate (MeJA) and post-harvest 1-methylcyclopropene (1-MCP) treatments on broccoli floret glucosinolate (GS) concentrations and quinone reductase (QR, an in vitro anti-cancer biomarker) inducing activity were evaluated two days prior to harvest, at harvest and at 10, 20, and 30 days of post-harvest storage at 4 °C. MeJA treatments four days prior to harvest of broccoli heads was observed to significantly increase floret ethylene biosynthesis resulting in chloro...

  9. 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.

  10. 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

  11. Microbial Survey of a Full-Scale, Biologically Active Filter for Treatment of Drinking Water

    OpenAIRE

    White, Colin P.; DeBry, Ronald W.; Lytle, Darren A.

    2012-01-01

    The microbial community of a full-scale, biologically active drinking water filter was surveyed using molecular techniques. Nitrosomonas, Nitrospira, Sphingomonadales, and Rhizobiales dominated the clone libraries. The results elucidate the microbial ecology of biological filters and demonstrate that biological treatment of drinking water should be considered a viable alternative to physicochemical methods.

  12. Synthesis and Antimicrobial and Antioxidant Activities of Some New 5-(2-Methyl-1H-indol-3-yl-1,3,4-oxadiazol-2-amine Derivatives

    Directory of Open Access Journals (Sweden)

    Anand R. Saundane

    2013-01-01

    Full Text Available A series of 5-(2-methyl-1H-indol-3-yl-1,3,4-oxadiazol-2-amine derivatives (3–5 were synthesized. These previously unknown compounds were characterized by spectral studies and elemental analysis. These compounds were evaluated for their antimicrobial and antioxidant activities. Among all the compounds tested 5d exhibited promising antibacterial, antifungal, radical scavenging, and ferric ions (Fe3+ reducing antioxidant power (FRAP activities, whereas the compounds 3b, 4c, and 5e exhibited good FRAP and metal chelating activities. In general compounds containing chloro and methyl substituent exhibited better antimicrobial and antioxidant activities.

  13. Synthesis and Herbicidal Activities of Novel 4-(4-(5-methyl-3-arylisoxazol-4-ylthiazol-2-ylpiperidyl Carboxamides and Thiocarboxamides

    Directory of Open Access Journals (Sweden)

    Ai-Dong Zhang

    2009-03-01

    Full Text Available A series of novel 4-(4-(5-methyl-3-arylisoxazol-4-ylthiazol-2-ylpiperidyl carboxamides and thiocarboxamides were synthesized as potential lead compounds of inhibitors targeting D1 protease in plants. These compounds were designed on the basis of a D1 protease inhibitor hit structure identified by homology modeling and virtual screening. The syntheses of these compounds were accomplished via a four-step procedure including the isoxazole ring formation, a-bromination of acetyl group, thiazole ring formation, and carboxamide/thiocarboxamide attachment. The in vivo herbicidal activity tests show that most compounds possess moderate to good herbicidal activities. The enzyme activity of one compound against the native spinach D1 protease exhibits a competitive inhibition. The results suggest that these compounds are indeed potential inhibitors for targeting D1 protease in plants.

  14. Redox Activation of Dicarbonyl (.eta.5-Cyclopentadienyl) Methyl Iron within the Cavity of .beta.-Cyclodextrin: Carbon Monoxide Insertion in Iron -Methyl Bond

    Czech Academy of Sciences Publication Activity Database

    Pospíšil, Lubomír; Hromadová, Magdaléna; Fiedler, Jan; Amatore, C.; Verpeaux, J. N.

    COST, 2004. s. 6. [Workshop on Interfacial Chemistry and Catalysis /4./. 20.10.2004-22.10.2004, La Cole sur Loup] R&D Projects: GA MŠk 1P04OCD15.10 Keywords : dicarbonyl * iron-methyl * carbon Subject RIV: CF - Physical ; Theoretical Chemistry

  15. 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.

  16. 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.

  17. Humin-based complexes and study of their biological activity under irradiation

    International Nuclear Information System (INIS)

    Full text : Several experimental studies have indicated that humin acids has features such as antioxidant activity, antiradiation activity and other. It is known that the humin acids are biologically active organic compounds with characteristics of high polyfunctional and complexing acids. The biological activity of these compounds is connected with presence of phenolic and hydroxyl groups. The main goal of this research is to increase biological activity and sorption properties of humin acids and obtaining of their modified and enriched forms with organic minerals and their analysis on model plant objects. Humin acids solutions can stimulate the life activity of irradiated plants with critical doses and plants growing in the polluted soils with radionuclides

  18. Cyclopenta[c]phenanthrenes--chemistry and biological activity.

    Science.gov (United States)

    Brzuzan, Paweł; Góra, Maciej; Luczyński, Michał K; Woźny, Maciej

    2013-06-25

    Despite cyclopenta-fused polycyclic aromatic hydrocarbons (CP-PAHs) having been detected in the environment, the ability of these compounds to induce cellular and tissue responses remains poorly characterized. In this review, we look at the chemistry and biological activity of the cyclopenta[c]phenanthrenes (CP[c]Phs) as potential chemicals of concern in the process of risk assessment. The first part of the review deals with the environmental occurrence and chemistry of CP-PAHs, focusing on available methods of CP[c]Ph chemical synthesis. The most interesting structural feature of the CP[c]Ph is the presence of a pseudo fjord-region constructed by the cyclopentane ring. This compound can be treated either as a structurally similar one to B[c]Ph, or as a phenanthrene skeleton with an electrodonating alkyl substituent in the bay-region of the molecule. The second thread, providing available data on the adverse effects of CP[c]Ph compounds on cells and tissues of living organisms, mainly fish, improves our understanding of these possible environmental hazards. The data show that CP[c]Ph is less potent at inducing CYP1A gene expression in rainbow trout than benzo[a]pyrene (B[a]P), a well-known Ah-receptor agonist. Interestingly, the CP[c]Ph dependent up-regulation of CYP1A mRNA is positively correlated with the incidences of clastogenic changes in rainbow trout erythrocytes. CP[c]Ph has, comparably to B[a]P, a potential to repress expression of tumor suppressor p53, in the head kidney of rainbow trout. Furthermore, estrogen responsive genes in fish liver, ERα and VTG, are not induced by CP[c]Ph, suggesting that the compound has no endocrine disrupting potential. However, some CP[c]Phs show mutagenic activity when investigated in the Ames test, and exhibit genotoxic properties in in vitro micronucleus assay. The above characteristics suggest that CP-PAHs are chemicals of concern for which potential pathways of exposure should be further identified. PMID:23628509

  19. 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.

  20. Mutant p53: Multiple Mechanisms Define Biologic Activity in Cancer

    OpenAIRE

    Kim, Michael Paul; Zhang, Yun; Lozano, Guillermina

    2015-01-01

    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 alterations involve p53 missense mutations that result in the production of mutant p53 proteins. Such mutant p53 proteins lack normal p53 function and may concomitantly gain novel functions, often with deleterious effects. Here, we rev...

  1. 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

  2. Synthesis and biological screening of 5-{[(4,6-disubstituted pyrimidine-2-ylthio]methyl}-N-phenyl-1,3,4-thiadiazol-2-amines

    Directory of Open Access Journals (Sweden)

    Azam M

    2008-01-01

    Full Text Available A number of substituted-a,β -unsaturated carbonyl compounds (1a-i were prepared by Claisen-Schmidt condensation of substituted acetophenone with selected araldehydes, which on cycloaddition with thiourea furnished 4,6-disubstituted pyrimidine-2-thiols (2a-i. Reaction of (2a-i with ethyl chloroacetate followed by condensation with hydrazine hydrate yielded 2-[(4,6-disubstituted pyrimidine-2-yl thio] acetohydrazides (4a-c. Condensation of compounds (4a-c with phenyl isothiocyanate gave 2-{[(4,6-disubstituted pyrimidine-2-yl thio] acetyl}-N-phenylhydrazinecarbothioamides (5a-c which on treatment with concentrated sulphuric acid afforded titled compounds 5-{(4,6-disubstituted pyrimidine-2-yl thio] methyl}-N-phenyl-1,3,4-thiadiazole-2-amines (6a-c. These compounds have been characterized on the basis of elemental analysis, IR, 1 H NMR and MS. Compounds have been evaluated for their anticancer and antioxidant activities. Compounds 2b, 2c and 6b exhibited significant antitumor activity against human breast cancer MCF 7 cell line. However, moderate antioxidant activity was observed with compounds 2c, 2d, 2g and 6b.

  3. 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

    2015-01-01

    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. PMID:26528563

  4. Biologically active polymers from spontaneous carotenoid oxidation: a new frontier in carotenoid activity.

    Directory of Open Access Journals (Sweden)

    James B Johnston

    Full Text Available In animals carotenoids show biological activity unrelated to vitamin A that has been considered to arise directly from the behavior of the parent compound, particularly as an antioxidant. However, the very property that confers antioxidant activity on some carotenoids in plants also confers susceptibility to oxidative transformation. As an alternative, it has been suggested that carotenoid oxidative breakdown or metabolic products could be the actual agents of activity in animals. However, an important and neglected aspect of the behavior of the highly unsaturated carotenoids is their potential to undergo addition of oxygen to form copolymers. Recently we reported that spontaneous oxidation of ß-carotene transforms it into a product dominated by ß-carotene-oxygen copolymers. We now report that the polymeric product is biologically active. Results suggest an overall ability to prime innate immune function to more rapidly respond to subsequent microbial challenges. An underlying structural resemblance to sporopollenin, found in the outer shell of spores and pollen, may allow the polymer to modulate innate immune responses through interactions with the pattern recognition receptor system. Oxygen copolymer formation appears common to all carotenoids, is anticipated to be widespread, and the products may contribute to the health benefits of carotenoid-rich fruits and vegetables.

  5. Activation of chemical biological defense mechanisms and alleviation of in vivo oxidation injury by low dose radiation

    International Nuclear Information System (INIS)

    We clarified that adequate oxygen stress induced by low dose radiation activates not only chemical biological protective function, such as induction of the synthesis of superoxide dismutase (SOD), glutathione peroxidase (GPX) and heat shock protein 70 (HSP70), but also the biomembrane function, such as enhanced membrane fluidity and ATPase activity. It is possible that activation of these mechanisms alleviates in vivo oxidation injuries resulting in alleviation of pathologic condition, such as ferric-nitrilotriacetate (Fe3+-NTA) or CCl4-induced liver damage, 1-methyl-4-phenyl 1,2,3,6-tetrahydro-pyridine (MPTP)-induced brain damage and diabetes mellitus. Namely, in contrast to the toxic effects of high dose irradiation, adequate activation of the functions of the living body by low dose radiation or inhalation of an appropriate amount of radon can contribute to suppressing aging and to preventing or reducing active oxygen species related diseases which are thought to involve peroxidation and have been regarded as the diseases for which radon spring water is an effective treatment. In future, clarification in detail of the mechanisms of these phenomena is required to understand the effects of low dose radiation on the functions of the living body, including adaptive response. (author)

  6. Oxoaporphine alkaloids: conversion of lysicamine into liriodendronine and its 2-O-methyl ether, and antifungal activity.

    Science.gov (United States)

    Pabuccuoglu, V; Rozwadowska, M D; Brossi, A; Clark, A; Hufford, C D; George, C; Flippen-Anderson, J L

    1991-01-01

    Pschorr reaction of diazonium salt 7 in aqueous methanolic sulfuric acid afforded, besides lysicamine 2, the orange colored sulfate of oxodibenzopyrrocoline (8). The structure is fully supported by an X-ray analysis of its picrate salt. Selective ether cleavage of lysicamine (2) with 48% HBr afforded a hydrobromide of 9, and free betaine 9 on treatment with pyridine-water. Both compounds methylated on treatment with etherial diazomethane on nitrogen to give the known 2-O,N-dimethylliriodendronine (11). Liriodendronine (10) was obtained from lysicamine (2) on heating with pyridine HBr at 189 degrees C, and treatment with pyridine-water, as a dark violet betaine. Betaine 12 was obtained by heating 11.HCl to 200 degrees C. The quaternary salts of lysicamine, lysicamine methiodide (3) and lysicamine methosulfate (4) were comparable in anticandidal activity to liriodenine (1), but were not as active as liriodenine methiodide (13). PMID:2043039

  7. 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...

  8. Current research and service activities of AFRRI's biological dosimetry program

    International Nuclear Information System (INIS)

    Full text: The long-range goal of the Armed Forces Radiobiology Research Institute's (AFRRI) Biological Dosimetry Team is to develop validated radiation bio dosimeters. Our objectives are (1) to establish definitive clinical bioassays for rapid, high-throughput radiation exposure analyses and (2) to develop complimentary triage-type radiation exposure assessment bioassays to support medical treatment decisions. The experimental approach involves two steps. The first is to establish a reference laboratory that uses conventional bioassays for definitive analyses of biological samples. The second step is to develop a validated and forward deployable biological dosimetry capability for rapid radiation dose assessment with an emphasis on the use of molecular biology-based diagnostic platforms. The conventional lymphocyte metaphase-spread dicentric assay was established at AFRRI in accordance with international harmonized protocols and applied to estimate radiation exposure doses in several overexposure accidents. Currently, novel interphase cell-based cytological bioassay that detects cells with chromosomal type aberrations and radiation responsive molecular bio markers (i.e., gene expression, protein) are being validated and optimized for rapid radiation exposure assessment applications. In addition the Biological Assessment Tool (BAT), a radiation casualty management software application, was developed. Available at AFRRI's website (www.afrri.usuhs.mil), BAT permits the recording and communication of relevant radiological and medical information for radiation accidents. These research and service efforts contribute to an improved diagnostic response for accidental overexposures and also have applications in other research fields including radiation therapy and toxicology

  9. Synthesis and Microbial Activity of Novel 3-Methyl-2-pyrazolin-5-one Derivatives

    Directory of Open Access Journals (Sweden)

    Mohamed S. Mostafa

    2013-01-01

    Full Text Available 2-Oxo-2H-chromene-3-carbohydrazide derivatives 2a,b react with 2-{[4-(substituted thiazol-2-yliminoethyl-phenyl]hydrazono}-3-oxo-butyric acid ethyl esters 4a–c to give 3-methyl-1-[(2-oxo-2H-chromen-3-yl carbonyl]-4-{[4-(substituted thiazol-2-yliminoethyl-phenyl]hydrazono}]-2-pyrazolin-5-one derivatives 5a–f. A considerable increase in the reaction rate had been observed with better yield using microwave irradiation for the synthesis of compounds 2a, b, 3a–c, and 5a–f. The synthesized products were tested against B. subtilis, S. aureus, and E. coli as well as C. albicans compared with tetracycline and nystatin as reference drugs.

  10. Effect of the fungicides carbendazim and metalaxyl on the biological activity of soils

    International Nuclear Information System (INIS)

    Metalaxyl and carbendazim at 10 and 100 ppm concentration have no influence on the biological activity of Humic Gley and Yellow Red Latosol soils as measured by respirometry. Carbendazim added to the Humic Gley soil at concentration of 500 ppm showed an inhibitory influence on the biological activity of this soil. (Author)

  11. Biological Activity of Autochthonic Bacterial Community in Oil-Contaminated Soil

    OpenAIRE

    Wolińska, Agnieszka; Kuźniar, Agnieszka; Szafranek-Nakonieczna, Anna; Jastrzębska, Natalia; Roguska, Eliza; Stępniewska, Zofia

    2016-01-01

    Soil microbial communities play an important role in the biodegradation of different petroleum derivates, including hydrocarbons. Also other biological factors such as enzyme and respiration activities and microbial abundance are sensitive to contamination with petroleum derivates. The aim of this study was to evaluate the response of autochthonic microbial community and biological parameters (respiration, dehydrogenase and catalase activities, total microorganisms count) on contamination wit...

  12. Simultaneous Determination of Arsenic, Manganese, and Selenium in Biological Materials by Neutron-Activation Analysis

    DEFF Research Database (Denmark)

    Heydorn, Kaj; Damsgaard, Else

    1973-01-01

    A new method was developed for the simultaneous determination of arsenic, manganese, and selenium in biological material by thermal-neutron activation analysis. The use of 81 mSe as indicator for selenium permitted a reduction of activation time to 1 hr for a 1 g sample, and the possibility of loss...... the ppM level in samples of biological tissue....

  13. Diversity of Secondary Metabolites from Marine Bacillus Species: Chemistry and Biological Activity

    OpenAIRE

    Hee Jae Shin; Muhammad Abdul Mojid Mondol; Mohammad Tofazzal Islam

    2013-01-01

    Marine Bacillus species produce versatile secondary metabolites including lipopeptides, polypeptides, macrolactones, fatty acids, polyketides, and isocoumarins. These structurally diverse compounds exhibit a wide range of biological activities, such as antimicrobial, anticancer, and antialgal activities. Some marine Bacillus strains can detoxify heavy metals through reduction processes and have the ability to produce carotenoids. The present article reviews the chemistry and biological activi...

  14. Activation of the H-ras oncogene in hepatocellular carcinomas initiated with diethylnitrosamine and promoted by a dietary methyl deficiency

    International Nuclear Information System (INIS)

    High molecular weight DNA was isolated from control livers and from hepatocellular carcinomas produced in F344 rats initiated with diethylnitrosamine (20 mg/kg body weight) then fed a methyl-deficient diet. The DNAs were used to transfect NIH 3T3 cells by the calcium phosphate precipitation technique. Cultures were scored for foci of morphologically transformed cells after 21 days. Three of 24 DNAs isolated from tumors initiated with diethylnitrosamine were able to transform NIH 3T3 cells (frequency = 0.01 to 0.04 foci/μg DNA). Secondary transformants were produced when DNA isolated from transformed foci were used in the transfection assay. The presence of rat DNA sequences in the primary transformants was demonstrated using a probe specific for rat repetitive sequences. High molecular weight DNA isolated from each of the 3 primary transformants was digested with BamH1 and was subjected to Southern blot analysis using a 32P-labelled probe for the H-ras gene. Each transformant tested exhibited a fragment not present in 3T3 DNA that hybridized with the H-ras probe. Twelve control DNAs isolated from livers of tumor-free animals were negative in the transfection assay. The results are consistent with the involvement of the activated H-ras gene in the development of these chemically-initiated carcinomas in methyl-deficient animals

  15. Conclusion on the peer review of the pesticide risk assessment of the active substance ethametsulfuron (evaluated variant ethametsulfuron-methyl

    Directory of Open Access Journals (Sweden)

    European Food Safety Authority

    2014-07-01

    Full Text Available The conclusions of the European Food Safety Authority (EFSA following the peer review of the initial risk assessments carried out by the competent authority of the rapporteur Member State the United Kingdom, for the pesticide active substance ethametsulfuron (evaluated variant ethametsulfuron-methyl are reported. The context of the peer review was that required by Commission Regulation (EU No 188/2011 and Article 56 of Regulation (EC No 1107/2009. The conclusions were reached on the basis of the evaluation of the representative uses of ethametsulfuron-methyl as a herbicide on oilseed rape. The reliable endpoints concluded as being appropriate for use in regulatory risk assessment, derived from the available studies and literature in the dossier peer reviewed, are presented. Missing information identified as being required by the regulatory framework as well as assessments that could not be finalised based on the available data are listed. Concerns are identified as regards the potential for groundwater contamination by some toxicologically relevant metabolites and the risk assessment for aquatic organisms.

  16. Synthesis and Photodynamic Activities of Pyrazolyl and Cyclopropyl Derivatives of Purpurin-18 Methyl Ester and Purpurin-18-N-butylimide

    International Nuclear Information System (INIS)

    The synthesis of new pyrazolyl and cyclopropyl derivatives of purpurin-18 methyl ester and purpurin-18-N-butylimide 1a, 1b, 2a, 2b and 8 is described. The new compounds were characterized by NMR, UV-vis spectroscopy and mass spectrometry. UV-vis spectra of the new compounds showed long wavelength absorption of ranges 692 - 708 nm (λmax). Photodynamic effects of the chlorin derivatives 1a, 1b, 2a and 2b were investigated by WST-1 assay in A549 cells, and showed good photodynamic activities with high photocytotoxicity and low cytotoxicity in the dark. In comparison between pyrazolyl and cyclopropyl derivatives, purpurin-18 methyl ester compounds 1a and 1b showed comparable photocytotoxicity result of the cell viabilities, otherwise, pyrazolyl derivative of purpurin-18-N-butylimide 2a showed better cell viabilities than those of cyclopropyl derivative 2b. And cyclopropyl derivative of purpurin-18-N-butylimide 2b showed higher dark cytotoxicity than that of others

  17. 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. PMID:26269460

  18. Activities in biological radiation research at the AGF

    International Nuclear Information System (INIS)

    The AGF is working on a wide spectrum of biological radiation research, with the different scientific disciplines contributing different methodologies to long-term research projects. The following fields are studied: 1. Molecular and cellular modes of action of radiation. 2. Detection and characterisation of biological radiation damage, especially in humans. 3. Medical applications of radiation effects. 4. Concepts and methods of radiation protection. The studies will lead to suggestions for radiation protection and improved radiotherapy. They may also contribute to the development of environmental protection strategies. (orig./MG)

  19. DNA methylation in ES cells requires the lysine methyltransferase G9a but not its catalytic activity

    OpenAIRE

    Dong, Kevin B; Maksakova, Irina A.; Mohn, Fabio; Leung, Danny; Appanah, Ruth; Lee, Sandra; Yang, Hao W; Lam, Lucia L.; Mager, Dixie L; Schübeler, Dirk; Tachibana, Makoto; Shinkai, Yoichi; Lorincz, Matthew C.

    2008-01-01

    Histone H3K9 methylation is required for DNA methylation and silencing of repetitive elements in plants and filamentous fungi. In mammalian cells however, deletion of the H3K9 histone methyltransferases (HMTases) Suv39h1 and Suv39h2 does not affect DNA methylation of the endogenous retrovirus murine leukaemia virus, indicating that H3K9 methylation is dispensable for DNA methylation of retrotransposons, or that a different HMTase is involved. We demonstrate that embryonic stem (ES) cells lack...

  20. Asymmetric Total Synthesis of (+)- and (−)-Clusianone and (+)- and (−)Clusianone Methyl Enol Ether via ACC Alkylation and Evaluation of their Anti-HIV Activity

    OpenAIRE

    Garnsey, Michelle R.; Matous, James A.; Kwiek, Jesse J; Coltart, Don M.

    2011-01-01

    The total asymmetric synthesis of (+)- and (−)-clusianone and (+)- and (−)-clusianone methyl enol ether is reported. Asymmetric induction is achieved through the use of ACC alkylation, providing the key intermediates with an er of 99:1. The four synthetic compounds were evaluated for their anti-HIV activity. Both (+)- and (−)-clusianone displayed significant anti-HIV activity.

  1. Synthesis, molecular modeling and biological evaluation of novel 2-allyl amino 4-methyl sulfanyl butyric acid as α-amylase and α-glucosidase inhibitor

    Science.gov (United States)

    Balan, Kannan; Perumal, Perumal; Sundarabaalaji, Narayanan; Palvannan, Thayumanavan

    2015-02-01

    In the present study 2-allyl amino 4-methyl sulfanyl butyric acid (AMSB) was synthesized in good yield. AMSB was characterized by Fourier transforms infrared spectroscopy (FTIR), Nuclear magnetic resonance (NMR) (1H and 13C) and Liquid chromatography mass spectrometry (LCMS). The radical scavenging activity and reducing power assay of AMSB was assessed using 1-1-diphenyl 2-picryl hydrazyl (DPPH), 2,2‧-azino-bis (3-ethyl benzothiazoline-6-sulfonic acid) (ABTS) and ferric ion reducing antioxidant power assay (FRAP) and was found to be 44.1, 34.71 and 41.7 μg/ml respectively. The compound showed effective inhibition against α-amylase and α-glucosidase. AMSB was identified to be a reversible mixed noncompetitive inhibitor of α-amylase and α-glucosidase. The molecular docking study was carried out to evaluate the specific groove binding properties and affords valuable information of AMSB binding mode in the active site of α-glucosidase the study may lead to the which leads to the rational design of new class of antidiabetic drugs targeting α-glucosidase based on AMSB in near future.

  2. 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.

  3. The biological activity and the using areas of glycerin derivatives

    International Nuclear Information System (INIS)

    The glycerin and its derivatives carry out several important biological functions in alive organism. Glycero lipids related to the neutral lipid groups thanks to presence of polar and hydrophobic groups take part in the developing of structure biogical membranes and in the processes, connected with transfer of matters and ions throw the membranes, energy supply of cell and defense reactions of organism

  4. Synthesis and biological activity of new homolupanes and homolupane saponins

    Czech Academy of Sciences Publication Activity Database

    Sidoryk, K.; Korda, A.; Rárová, Lucie; Oklešťková, Jana; Strnad, Miroslav; Cmoch, P.; Pakulski, Z.; Gwardiak, K.; Karczewski, R.; Luboradzki, R.

    2015-01-01

    Roč. 71, č. 13 (2015), s. 2004-2012. ISSN 0040-4020 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Homobetulin * Homobetulinic acid * Glycosylation Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.641, year: 2014

  5. The half-lives of biological activity of some pesticides in water

    OpenAIRE

    Kyaw Myint Oo,

    2001-01-01

    In the absence of analytical methods, the half-lives of biological activity of pesticides can be estimated by bioassays. To determine the half-lives of biological acivity of pesticides to fish, static bioassays were conducted in the laboratory with ten different formulations of pesticides using Labeo rohita as a bio-indicator. The half-lives of biological activity for ten different pesticides in soft water at pH 7.5 and 27░C, ranged from 4.6 days to 11.8 days. The half-life of biological acti...

  6. N-methyl-D-aspartate receptor activation increases cAMP levels and voltage-gated Ca2+ channel activity in area CA1 of hippocampus.

    OpenAIRE

    Chetkovich, D.M.; Gray., R; Johnston, D.; Sweatt, J D

    1991-01-01

    Tetanic stimulation of the Schaffer collateral inputs into area CA1 of the hippocampus causes N-methyl-D-aspartate (NMDA) receptor activation, an effect that contributes to the induction of long-term potentiation (LTP) in this region. The present studies demonstrate that LTP-inducing tetanic stimulation in rat hippocampal area CA1 elicited increased levels of cAMP. The elevation of cAMP was blocked by the NMDA receptor antagonist DL-2-amino-5-phosphonovaleric acid (APV). Bath application of N...

  7. Polycyclic Xanthone Natural Products: Structure, Biological Activity and Chemical Synthesis

    OpenAIRE

    Winter, Dana K.; Sloman, David L.; Porco, John A.

    2013-01-01

    Polycyclic xanthone natural products are a family of polyketides which are characterized by highly oxygenated, angular hexacyclic frameworks. In the last decade, this novel class of molecules has attracted noticeable attention from the synthetic and biological communities due to emerging reports of their potential use as antitumour agents. The aim of this article is to highlight the most recent developments of this subset of the xanthone family by detailing the innate challenges of the constr...

  8. ACTIVE AND PARTICIPATORY METHODS IN BIOLOGY: PROBLEM-SOLVING

    OpenAIRE

    Adela NEMEŞ; Nicoleta IANOVICI

    2010-01-01

    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 id...

  9. Residual matrix from different separation techniques impacts exosome biological activity

    OpenAIRE

    Lucia Paolini; Andrea Zendrini; Giuseppe Di Noto; Sara Busatto; Elisabetta Lottini; Annalisa Radeghieri; Alessandra Dossi; Andrea Caneschi; Doris Ricotta; Paolo Bergese

    2016-01-01

    Exosomes are gaining a prominent role in research due to their intriguing biology and several therapeutic opportunities. However, their accurate purification from body fluids and detailed physicochemical characterization remain open issues. We isolated exosomes from serum of patients with Multiple Myeloma by four of the most popular purification methods and assessed the presence of residual contaminants in the preparations through an ad hoc combination of biochemical and biophysical technique...

  10. 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.

  11. Hyperpigmentation mechanism of methyl 3,5-di-caffeoylquinate through activation of p38 and MITF induction of tyrosinase.

    Science.gov (United States)

    Kim, Hyo Jung; Kim, Jin Sook; Woo, Je-Tae; Lee, Ik-Soo; Cha, Byung-Yoon

    2015-07-01

    Methyl 3,5-di-caffeoylquinate (3,5-diCQM) has been used for the treatment of various diseases in oriental medicine, but its effect on melanogenesis has not been reported yet. In this study, the molecular mechanism of 3,5-diCQM-induced melanogenesis was investigated. It was found that 3,5-diCQM induced synthesis of melanin pigments in murine B16F10 melanoma cells in a concentration-dependent manner. Treatment of cells with 3,5-diCQM for 48 h increased extracellular and intracellular melanin production and tyrosinase activity. The expressions of tyrosinase, tyrosinase-related protein 1 (TRP1), and TRP2 were up-regulated in a dose-dependent manner 48 h after 3,5-diCQM treatment. Western blot analysis showed that 3,5-diCQM increased the phosphorylation of p38 mitogen-activated protein kinase and cAMP responsive element binding as well as the expression of microphthalmia-associated transcription factor. In addition, 3,5-diCQM-stimulated cAMP production, and 3,5-diCQM-induced tyrosinase activity and melanin synthesis were attenuated by H89, a protein kinase A inhibitor. These results suggested that 3,5-diCQM-mediated activation of the p38 pathway may represent a novel approach for an effective therapy for vitiligo and hair graying. PMID:26018825

  12. Activated carbon/Fe(3)O(4) nanoparticle composite: fabrication, methyl orange removal and regeneration by hydrogen peroxide.

    Science.gov (United States)

    Do, Manh Huy; Phan, Ngoc Hoa; Nguyen, Thi Dung; Pham, Thi Thu Suong; Nguyen, Van Khoa; Vu, Thi Thuy Trang; Nguyen, Thi Kim Phuong

    2011-11-01

    In the water treatment field, activated carbons (ACs) have wide applications in adsorptions. However, the applications are limited by difficulties encountered in separation and regeneration processes. Here, activated carbon/Fe(3)O(4) nanoparticle composites, which combine the adsorption features of powdered activated carbon (PAC) with the magnetic and excellent catalytic properties of Fe(3)O(4) nanoparticles, were fabricated by a modified impregnation method using HNO(3) as the carbon modifying agent. The obtained composites were characterized by X-ray diffraction, scanning and transmission electron microscopy, nitrogen adsorption isotherms and vibrating sample magnetometer. Their performance for methyl orange (MO) removal by adsorption was evaluated. The regeneration of the composite and PAC-HNO(3) (powdered activated carbon modified by HNO(3)) adsorbed MO by hydrogen peroxide was investigated. The composites had a high specific surface area and porosity and a superparamagnetic property that shows they can be manipulated by an external magnetic field. Adsorption experiments showed that the MO sorption process on the composites followed pseudo-second order kinetic model and the adsorption isotherm date could be simulated with both the Freundlich and Langmuir models. The regeneration indicated that the presence of the Fe(3)O(4) nanoparticles is important for a achieving high regeneration efficiency by hydrogen peroxide. PMID:21840037

  13. 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.

  14. High molar activity of [11C]TCH346 via [11C]methyl triflate using the 'wet' [11C]CO2 reduction method

    International Nuclear Information System (INIS)

    [11C]TCH346, a compound acting on the glycolytic enzyme, glycerol-aldehyde-3-phosphate dehydrogenase, was produced under optimised conditions by methylation of the desmethyl compound with no-carrier added (n.c.a.) [11C]methyl triflate. An i.v. injectable solution of n.c.a. [11C]TCH346 containing 4040±1550 MBq (n=6) containing a molar activity between 40 and 5700 GBq/μmol and a radiochemical purity of >99% was obtained within 30 min (after EOB) by irradiation of nitrogen gas containing 0.5% oxygen with 16.5 MeV protons at 45 μA for 30 min. The alkylation reagent [11C]methyl triflate was prepared via on-line conversion of [11C]methyl iodide. For the formation of [11C]methyl iodide, [11C]carbon dioxide from the target chamber was reduced by a lithium aluminium hydride solution, and the methanol obtained on-line was converted using triphenylphosphine diiodide. The molar activity of [11C]TCH346 could be improved from 40 up to nearly 5700 GBq/μmol during the optimisation of the synthesis using the same stock solution of lithium aluminium hydride solution in tetrahydrofuran

  15. Estimation of the methylation pattern distribution from deep sequencing data

    OpenAIRE

    Lin, Peijie; Forêt, Sylvain; Wilson, Susan R; Burden, Conrad J.

    2015-01-01

    Background Bisulphite sequencing enables the detection of cytosine methylation. The sequence of the methylation states of cytosines on any given read forms a methylation pattern that carries substantially more information than merely studying the average methylation level at individual positions. In order to understand better the complexity of DNA methylation landscapes in biological samples, it is important to study the diversity of these methylation patterns. However, the accurate quantific...

  16. Biological research of Grabia River - fifty years of activity

    OpenAIRE

    Siciński, Jacek; Tończyk, Grzegorz

    2005-01-01

    Grabia, a small still close to natural conditions lowland river, has been an object of special interest for Łódź hydrobiologists for more than 50 years. Over 100 scientific papers and over 100 master theses were produced in the Faculty of Biology and Environmental Protection University of Łódź. The initiator was Prof.L.K. Pawłowski who spent many years conducting research into the river. The ground and the first research objective was to recognize the fauna diversity. The checklis...

  17. Epithermal neutron activation analysis of trace elements in biological materials

    International Nuclear Information System (INIS)

    The detection limits of 24 important minor and trace elements were studied in NBS SRM-1571 Orchard Leaves, NBS SRM-1577 Bovine Liver, Bowen's kale and IAEA H-4 Animal Muscle using ENAA method with cadmium and cadmium-boron filter. The lower detection limits have been found for elements As, Au, Ba, Br, Cd, Mo, Ni, Sb, Se, Sm and U by ENAA with cadmium filter and for elements As, Cd, Mo and Ni by ENAA with cadmium-boron filter, respectively, in comparison with INAA method. The results of the determination of elements studied in the above mentioned biological materials are also presented. (author)

  18. Electronic transport in methylated fragments of DNA

    Science.gov (United States)

    de Almeida, M. L.; Oliveira, J. I. N.; Lima Neto, J. X.; Gomes, C. E. M.; Fulco, U. L.; Albuquerque, E. L.; Freire, V. N.; Caetano, E. W. S.; de Moura, F. A. B. F.; Lyra, M. L.

    2015-11-01

    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.

  19. 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.

  20. An Introduction to Biological Modeling Using Coin Flips to Predict the Outcome of a Diffusion Activity

    Science.gov (United States)

    Butcher, Greg Q.; Rodriguez, Juan; Chirhart, Scott; Messina, Troy C.

    2016-01-01

    In order to increase students' awareness for and comfort with mathematical modeling of biological processes, and increase their understanding of diffusion, the following lab was developed for use in 100-level, majors/non-majors biology and neuroscience courses. The activity begins with generation of a data set that uses coin-flips to replicate…

  1. Harnessing microbial metabolic exchange for the discovery of biologically active molecules

    OpenAIRE

    Liu, Wei-Ting

    2012-01-01

    Microbial metabolic exchange mediates microbial interactions and plays key roles in regulating biology and has shaped modern healthcare, agriculture and other commercial processes. In this thesis, cutting edge mass spectrometry techniques, new genome mining approaches, and innovative bioinformatics tools were coupled and developed into investigating microbial metabolic exchange and led to the identification and characterization of biological active molecules that may have therapeutic values. ...

  2. 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 ...

  3. Genome-wide DNA methylation identifies trophoblast invasion-related genes: Claudin-4 and Fucosyltransferase IV control mobility via altering matrix metalloproteinase activity.

    Science.gov (United States)

    Hu, Yuxiang; Blair, John D; Yuen, Ryan K C; Robinson, Wendy P; von Dadelszen, Peter

    2015-05-01

    Previously we showed that extravillous cytotrophoblast (EVT) outgrowth and migration on a collagen gel explant model were affected by exposure to decidual natural killer cells (dNK). This study investigates the molecular causes behind this phenomenon. Genome wide DNA methylation of exposed and unexposed EVT was assessed using the Illumina Infinium HumanMethylation450 BeadChip array (450 K array). We identified 444 differentially methylated CpG loci in dNK-treated EVT compared with medium control (P EVT. Among these genes, CLDN4 (encoding claudin-4) and FUT4 (encoding fucosyltransferase IV) were chosen for follow-up studies because of their biological relevance from research on tumor cells. The results showed that the mRNA and protein expressions of both CLDN4 and FUT4 in dNK-treated EVT were significantly reduced compared with control (P EVT mobility at least partially in association with an alteration of DNA methylation profile. Hypermethylation of CLDN4 and FUT4 reduces protein expression. CLDN4 and FUT4 are representative genes that participate in modulating trophoblast mobility. PMID:25697377

  4. Design, Synthesis and Anti-Tobacco Mosaic Virus (TMV Activity of 5-Chloro-N-(4-cyano-1-aryl-1H-pyrazol-5-yl-1-aryl-3-methyl-1H-pyrazole-4-carboxamide Derivatives

    Directory of Open Access Journals (Sweden)

    Jin-Jing Xiao

    2015-01-01

    Full Text Available A series of novel pyrazole amide derivatives 3a–3p which take TMV PC protein as the target has been designed and synthesized by the reactions of 5-chloro-1-aryl-3-methyl-1H-pyrazole-4-carboxylic acids with 5-amino-1-aryl-1H-pyrazole-4-carbonitriles. All the compounds were characterized by 1H-NMR, mass spectroscopy and elemental analysis. Preliminary bioassays indicated that all the compounds acted against the tobacco mosaic virus (TMV with different in vivo and in vitro modes at 500 μg/mL and were found to possess promising activity. Especially, compound 3p showed the most potent biological activity against tobacco mosaic virus (TMV compared to ningnanmycin, and a molecular docking study was performed and the binding model revealed that the pyrazole amide moiety was tightly embedded in the binding sites of TMV PC (PDB code: 2OM3.

  5. Methyl Iodide

    Science.gov (United States)

    Methyl iodide (MeI, iodomethane, CH3I) was reported as a potential alternative to the stratospheric ozone-depleting fumigant methyl bromide (MeBr) in the mid-1990s (Sims et al., 1995; Ohr et al., 1996). It has since received significant research attention to determine its environmental fate and tran...

  6. 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.

  7. Synthesis, biological activities and structure-activity relationships for new avermectin analogues.

    Science.gov (United States)

    Zhang, Jian; Nan, Xiang; Yu, Hai-Tao; Cheng, Pi-Le; Zhang, Yan; Liu, Ying-Qian; Zhang, Shao-Yong; Hu, Guan-Fang; Liu, Huanxiang; Chen, An-Liang

    2016-10-01

    In an effort to discover new molecules with good insecticidal activities, more than 40 new avermectin derivatives were synthesized and evaluated for their biological activities against three species of arachnids, insects and nematodes, namely, Tetranychus Cinnabarinus, Aphis craccivora and Bursaphelenchus xylophilus. All the tested compounds showed potent inhibitory activities against three insect species. Notably, the majority of compounds exhibited high selectivity against T. cinnabarinus, some of which were much better in comparison with avermectin. Especially compounds 9j (LC50: 0.005 μM) and 16d (LC50: 0.002 μM) were 2.5- and 4.7-fold more active than avermectin (LC50: 0.013 μM), respectively, against T. cinnabarinus. Moreover, compounds 9b, 9d-f, 9h, 9j, 9l, 9n, 9p, 9r, 9v and 17d showed superior activities with LC50 values of 2.959-5.013 μM compared to that of 1 (LC50: 6.746 μM) against B. xylophilus. Meanwhile, the insecticidal activities of compounds 9f, 9g, 9h, and 9m against A. craccivora were 7-8 times better than that of avermectin, with LC50 values of 7.744, 5.634, 6.809, 7.939 and 52.234 μM, respectively. Furthermore, QSAR analysis showed that the molecular shape, size, connectivity degree and electronic distribution of avermectin analogues had substantial effects on insecticidal potency. These preliminary results provided useful insight in guiding further modifications of avermectin in the development of potential new insecticides. PMID:27318119

  8. 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.

  9. 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.

  10. 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.

  11. BIOLOGICAL VALUE OF PUNY FRUITS RELATED TO THEIR ANTIRADICAL ACTIVITY

    Directory of Open Access Journals (Sweden)

    PAULOVICSOVÁ B.

    2007-05-01

    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.

  12. 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...

  13. 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.

  14. Some biologically active oxovanadium(IV) complexes of triazole derived Schiff bases: their synthesis, characterization and biological properties.

    Science.gov (United States)

    Chohan, Zahid H; Sumrra, Sajjad H

    2010-10-01

    A series of biologically active oxovanadium(IV) complexes of triazole derived Schiff bases L(1)-L(5) have been synthesized and characterized by their physical, analytical, and spectral data. The synthesized ligands potentially act as bidentate, in which the oxygen of furfural and nitrogen of azomethine coordinate with the oxovanadium atom to give a stoichiometry of vanadyl complexes 1:2 (M:L) in a square-pyramidal geometry. In vitro antibacterial and antifungal activities on different species of pathogenic bacteria (E. coli, S. flexneri, P. aeruginosa, S. typhi, S. aureus, and B. subtilis) and fungi (T. longifusus, C. albicans, A. flavus, M. canis, F. solani, and C. glabrata) have been studied. All compounds showed moderate to significant antibacterial activity against one or more bacterial strains and good antifungal activity against most of the fungal strains. The brine shrimp bioassay was also carried out to check the cytotoxicity of coordinated and uncoordinated synthesized compounds. PMID:20429776

  15. Ha-ras oncogene activation in mammary glands of N-methyl-N-nitrosourea-treated rats genetically resistant to mammary adenocarcinogenesis.

    OpenAIRE

    Lu, S J; Archer, M.C.

    1992-01-01

    A single dose of N-methyl-N-nitrosourea given to sexually immature female Buf/N rats produces a high incidence of mammary adenocarcinomas. A large percentage of these tumors contain the Ha-ras oncogene, activated by a G----A transition at the second nucleotide of codon 12. Copenhagen rats, on the other hand, are completely resistant to mammary tumor induction by a number of carcinogens, including N-methyl-N-nitrosourea. Here we show, using a sensitive method involving PCR, that codon 12 Ha-ra...

  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. Stable heterologous expression of biologically active terpenoids in green plant cells

    DEFF Research Database (Denmark)

    Binti Khairul Ikram, Nur Kusaira; Zhan, Xin; Pan, Xiwu;

    2015-01-01

    Plants biosynthesize a great diversity of biologically active small molecules of interest for fragrances, flavors, and pharmaceuticals. Among specialized metabolites, terpenoids represent the greatest molecular diversity. Many terpenoids are very complex, and total chemical synthesis often requir...

  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. Synthesis and antiplatelet activity of antithrombotic thiourea compounds: biological and structure-activity relationship studies.

    Science.gov (United States)

    Lourenço, André Luiz; Saito, Max Seidy; Dorneles, Luís Eduardo Gomes; Viana, Gil Mendes; Sathler, Plínio Cunha; Aguiar, Lúcia Cruz de Sequeira; de Pádula, Marcelo; Domingos, Thaisa Francielle Souza; Fraga, Aline Guerra Manssour; Rodrigues, Carlos Rangel; de Sousa, Valeria Pereira; Castro, Helena Carla; Cabral, Lucio Mendes

    2015-01-01

    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. PMID:25903367

  20. 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.

  1. 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.

  2. 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. PMID:26833854

  3. 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.

  4. 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...

  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. 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. PMID:26716226

  7. Biologically active collagen-based scaffolds: advances in processing and characterization

    OpenAIRE

    Yannas, I.V.; Tzeranis, D. S.; Harley, B A; So, P. T. C.

    2010-01-01

    A small number of type I collagen–glycosaminoglycan scaffolds (collagen–GAG scaffolds; CGSs) have unusual biological activity consisting primarily in inducing partial regeneration of organs in the adult mammal. Two of these are currently in use in a variety of clinical settings. CGSs appear to induce regeneration by blocking the adult healing response, following trauma, consisting of wound contraction and scar formation. Several structural determinants of biological activity have been identif...

  8. Evaluation of Biologically Active Compounds from Calendula officinalis Flowers using Spectrophotometry

    OpenAIRE

    Butnariu Monica; Coradini Cristina

    2012-01-01

    Abstract Background This study aimed to quantify the active biological compounds in C. officinalis flowers. Based on the active principles and biological properties of marigolds flowers reported in the literature, we sought to obtain and characterize the molecular composition of extracts prepared using different solvents. The antioxidant capacities of extracts were assessed by using spectrophotometry to measure both absorbance of the colorimetric free radical scavenger 2,2-diphenyl-1-picrylhy...

  9. Target enhanced 2D similarity search by using explicit biological activity annotations and profiles

    OpenAIRE

    Yu, Xiang; Geer, Lewis Y.; Han, Lianyi; Bryant, Stephen H

    2015-01-01

    Background The enriched biological activity information of compounds in large and freely-accessible chemical databases like the PubChem Bioassay Database has become a powerful research resource for the scientific research community. Currently, 2D fingerprint based conventional similarity search (CSS) is the most common widely used approach for database screening, but it does not typically incorporate the relative importance of fingerprint bits to biological activity. Results In this study, a ...

  10. Synthesis and biological activity of pyrimido [1, 2-a] quinoline moiety and its 2-substituted derivatives

    Science.gov (United States)

    Jadhav, A. G.; Halikar, N. K.

    2013-04-01

    2-Amino-3-cyano quinoline (1) and bis (methylthio) methylene malononitrile (2) were refluxed in N,N-dimethyl formamide (DMF) in presence of catalytic amount of anhydrous potassium carbonate to afforded 3, 11-dicyano-4-imino-2-methylthio -4H-pyrimido [1, 2-a] quinoline (3). The latter were further reacted with different substituted aniline, phenol, hetryl amine and compound containing active methyl group. Afforded to 3, 11-dicyano-4-imino -4H-pyrimido [1, 2-a] quinoline and their 2-substuited derivatives (4a-7c). All these newly synthesized compounds were characterized by elemental analysis and spectral data, and screened for their antimicrobial activities.

  11. Screening of biological activities of a series of chalcone derivatives against human pathogenic microorganisms.

    Science.gov (United States)

    Karaman, Isa; Gezegen, Hayreddin; Gürdere, M Burcu; Dingil, Alparslan; Ceylan, Mustafa

    2010-02-01

    In an effort to develop new antimicrobial agents, a series of chalcone derivatives, 3-60, were prepared by Claisen-Schmidt condensation of appropriate acetophenones and 2-furyl methyl ketones with appropriate aromatic aldehydes, furfural, and thiophene-2-carbaldehyde in an aqueous solution of NaOH and EtOH at room temperature. The synthesized compounds were characterized by means of their IR- and NMR-spectral data, and elemental analysis. All compounds were tested for their antibacterial and antifungal activities by the disc diffusion method. For the most active compounds, also minimum inhibitory concentrations (MICs) were determined. PMID:20151389

  12. VOLATILE CONSTITUENTS AND BIOLOGICAL ACTIVITIES OF ESSENTIAL OIL FROM Securidaca longepedunculata Fers. GROWING IN BENIN

    Directory of Open Access Journals (Sweden)

    Dominique C.K. Sohounhloue

    2012-03-01

    Full Text Available The essential oil obtained by hydrodistillation of roots bark of Securidacaca longepedunculata Fers. (Polygalaceae growing in Savalou, Biguinan and Gbegrou (Benin were analyzed using capillary GC and GC/MS. Seven compounds representing (99.5%; 99.1%; 99.3% respectively of the oils were identified. The major compound was found to be methyl salicylate respectively (98.0%; 98.6%; 98.7%. The antimicrobial activity of these oils was found to be high, and medium antiradical activity was observed.

  13. Assessing the Biological Activity of the Glucan Phosphatase Laforin.

    Science.gov (United States)

    Romá-Mateo, Carlos; Raththagala, Madushi; Gentry, Mathew S; Sanz, Pascual

    2016-01-01

    Glucan phosphatases are a recently discovered family of enzymes that dephosphorylate either starch or glycogen and are essential for proper starch metabolism in plants and glycogen metabolism in humans. Mutations in the gene encoding the only human glucan phosphatase, laforin, result in the fatal, neurodegenerative, epilepsy known as Lafora disease. Here, we describe phosphatase assays to assess both generic laforin phosphatase activity and laforin's unique glycogen phosphatase activity. PMID:27514803

  14. The Role of Protease Activity in ErbB Biology

    OpenAIRE

    Blobel, Carl P; Carpenter, Graham; Freeman, Matthew

    2008-01-01

    Proteases are now recognized as having an active role in a variety of processes aside from their recognized metabolic role in protein degradation. Within the ErbB system of ligands and receptors proteases are known to be necessary for the generation of soluble ligands from transmembrane precursers and for the processing of the ErbB4 receptor, such that its intracellular domain is translocated to the nucleus. There are two protease activities involved in the events: proteases that cleave withi...

  15. 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…

  16. Low Budget Biology. A Collection of Low Cost Labs and Activities.

    Science.gov (United States)

    Wartski, Bert; Wartski, Lynn Marie

    This document contains a collection of low cost labs and activities. The activities are organized into the following units: Chemistry; Microbiology; DNA to Chromosomes; Genetics; Evolution; Classification, Protist, and Fungus; Plant; Invertebrate; Human Biology; and Ecology and Miscellaneous. Some of the activities within these units include: (1)…

  17. Biological activity of three alkyl cinnamates on young larvae of Tuta absoluta.

    Science.gov (United States)

    Perez, M E; Haramboure, M; Mirande, L; Romanelli, G P; Schneider, M I; Autino, J C

    2013-01-01

    The "tomato moth," Tuto absoluta (Meyrick) (Lepidoptera: Gelechiidae), is a neotropical oligophagous insect considered a key pest of tomato crops. It was detected in Europe seven years ago and quickly spread to several regions of Asia and North Africa. In Argentina, its control is done by chemical pesticides mainly. The indiscriminate use of chemical broad spectrum pesticides have caused several problems in the control of this pest due to resistance mechanism involved to several insecticides including pyrethroids, organophosphates and biopesticides. In this context, the searching and evaluation of new compounds- compatible with integrated pest management programs- has become relevant. Within the phenylpropanoids, alkyl cinnamates, whether natural or synthetic, have been reported with biological activity: repellence, antifeedant and insecticide. Therefore, the cinnamates could be a valuable alternative to replace the conventional insecticides. The aim of this work was to study the antifeedant effect of three alkyl cinnamates (methyl, ethyl and propyl cinnamate) on the consumption rate patterns of second instar larvae of T. absoluta. A series of concentrations of each compound (100, 250 and 500 micrograms/milliliter) were prepared using acetone (analytical grade) - distilled water as solvent and a surfactant (Tween 80) was added to each solution to improve the wet of leaves. Tomato leaf disks of 2 cm diameter were treated by immersion in each solution during 15 seconds. Afterward, the treated discs were dried under fume hood and each disk was placed in a plastic capsule. A larva with 6-8 hours of starvation was added to each experimental unit. Each treatment was replicated between 24-30 times. The area consumed by each larva was measured after 24, 48 and 72 hours post-treatment. We also evaluated development time, weight of the pupa, adult emergence, fecundity and fertility as sublethal effects. The results were analyzed using ANOVA test. None of the compounds tested

  18. Is kinase activity essential for biological functions of BRI1?

    Institute of Scientific and Technical Information of China (English)

    Weihui Xu; Juan Huang; Baohua Li; Jiayang Li; Yonghong Wang

    2008-01-01

    Brassinosteroids (BRs) are a major group of plant hormones that regulate plant growth and development. BRI1, a protein localized to the plasma membrane, functions as a BR receptor and it has been proposed that its kinase activity has an essential role in BR-regulated plant growth and development. Here we report the isolation and molecular characterization of a new allele of bril, bril-301, which shows moderate morphological phenotypes and a reduced response to BRs under normal growth conditions. Sequence analysis identified a two-base alteration from GG to AT, resulting in a conversion of 989G to 9891 in the BRI1 kinase domain. An in vitro assay of kinase activity showed that bril-301 has no detectable autophosphorylation activity or phosphorylation activity towards the BRI1 substrates TTL and BAK1. Furthermore, our results suggest that bril-301, even with extremely impaired kinase activity, still retains partial function in regulating plant growth and development, which raises the question of whether BRI1 kinase activity is essential for BR-mediated growth and development in higher plants.

  19. Biological Activities of Aerial Parts Extracts of Euphorbia characias

    Science.gov (United States)

    Pisano, Maria Barbara; Cosentino, Sofia; Viale, Silvia; Spanò, Delia; Corona, Angela; Esposito, Francesca; Tramontano, Enzo; Montoro, Paola; Tuberoso, Carlo Ignazio Giovanni; Medda, Rosaria; Pintus, Francesca

    2016-01-01

    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. PMID:27314007

  20. (Accumulation of methyl-deficient rat liver messenger ribonucleic acid on ethionine administration). Progress report. [Methyltransferase activity in Ehrlich ascites tumor cells and effects of phorbol ester on methyltransferase activity

    Energy Technology Data Exchange (ETDEWEB)

    Borek, E.

    1980-01-01

    Enzyme fractions were isolated from Ehrlich ascites cells which introduced methyl groups into methyl deficient rat liver mRNA and unmethylated vaccinia mRNA. The methyl groups were incorporated at the 5' end into cap 1 structures by the viral enzyme, whereas both cap 0 and cap 1 structures were formed by the Ehrlich ascites cell enzymes. Preliminary results indicate the presence of adenine N/sup 6/-methyltransferase activity in Ehrlich ascites cells. These results indicate that mRNA deficient in 5'-cap methylation and in internal methylation of adenine accumulated in rats on exposure to ethionine. The methyl-deficient mRNA isolated from the liver of ethionine-fed rats differed in its translational properties from mRNA isolated from control animals. Preliminary experiments indicate that single topical application of 17n moles of TPA to mouse skin altered tRNA methyltransferases. The extent of methylation was increased over 2-fold in mouse skin treated with TPA for 48 hours. These changes have been observed as early as 12 hours following TPA treatment. In contrast, the application of initiating dose of DMBA had no effect on these enzymes. It should be emphasized that the changes in tRNA methyltransferases produced by TPA are not merely an increase of the concentration of the enzyme, rather that they represent alterations of specificity of a battery of enzymes. In turn the change in enzyme specificity can produce alterations in the structure of tRNA. (ERB)

  1. 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. PMID:26272388

  2. 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. PMID:25099154

  3. 125I radiolabelling of 1-34 N-terminal tetratiacontapeptide of bPTH with high specific activity and without destroying biological activity

    International Nuclear Information System (INIS)

    Radiolabelling of 1-34 N terminal synthetic biological active fragment of bovine parathormone (1-34 b PTH) with high specific activity and without loss of biological activity was studied. Chloramine T and lactoperoxydase methods were used. To assess biological activity of 125I 1-34 bPTH labelled fragment, their ability to activate renal cortical adenylate cyclase was used. The results show that enzymatic labelling method preserved the biological activity. With the chloramine T method it is possible to keep the biological activity by using DMSO

  4. 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

  5. Synthesis and biological activities of some benzimidazolone derivatives

    Directory of Open Access Journals (Sweden)

    B K Karale

    2015-01-01

    Full Text Available The reaction of 5-nitrobenzimidazolone with phenoxyethyl bromide in presence of potassium carbonate in dimethyl formamide obtained 6-nitro-1,3-bis(2-phenoxyethyl-1,3-dihydro-2H-benzimidazol-2-one. It was reduced using stannous chloride to get 6-amino -1,3-bis(2-phenoxyethyl-1, 3-dihydro-2H-benzimidazol -2-one, which was further treated with aromatic sulphonyl chloride to obtain benzimidazolone derivatives, 6a-k. These compounds were tested for antibacterial, antituberculosis and antifungal activity. Most of them have shown very good activity against some gram positive and gram negative microorganisms and fungal strains. Some of them have shown moderate activity against Mycobacterium tuberculosis.

  6. 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.

  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. PMID:10622109

  8. Activation methods of retrospective dosimetry using biological samples

    International Nuclear Information System (INIS)

    23Na and 32S are stable isotopes which are present in humans - 23Na in blood and other tissues, 32S in hair. When human body is irradiated by neutrons, nuclear reactions 23Na(n,γ)24Na and 32S(n,p)32P occur, the products, 24Na and 32P, being radioactive. The induced activity can be used for retrospective assessment of the neutron dose. The principle of this dosimetry application is described. As a particular case, the relations between the activity and neutron dose were derived for irradiation of a human by the fission neutron spectrum. (orig.)

  9. Withanolides: Biologically Active Constituents in the Treatment of Alzheimer's Disease.

    Science.gov (United States)

    Khan, Shahid A; Khan, Sher B; Shah, Zarbad; Asiri, Abdullah M

    2016-01-01

    The use of natural products in drug discovery and development have an important history. Several therapeutic agents have been investigated during the biological screenings of natural compounds. It is well documented that plants are possibly the core of novel substances that led to the discovery of new, novel, and effective therapeutic agents. Therefore, in the last few decades, scientists were thoroughly attempting for the search of benevolent drugs to protect mankind from various diseases and discomforts. The diverse chemical structures of natural products are the key element of their success in modern drug discovery. Cholinesterase enzyme inhibitors (ChEI) are chemicals which inhibit the splitting of cholinesterase enzymes (acetylcholinesterase and butyrylcholinesterase). Acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) are two types of cholinesterase enzymes that have been identified in vertebrates that are responsible for Alzheimer's disease and related dementia. Withanolides are affective plant secondary metabolites which inhibit acetylcholinesterase and butyrylcholinesterase enzyme and thus possibly will be the future drug for Alzheimer's disease. By viewing the importance of natural products in drug discovery and development, we present here, the importance of withanolides in the treatment of Alzheimer's disease. In this article, we also describe the classification and structural characterization of withanolides. This review comprises of 114 compounds. PMID:26527154

  10. Biological activity of Terminalia arjuna on Human Pathogenic Microorganisms

    OpenAIRE

    Tariq Javed; Sana Riaz; Muhammad Uzair; Gulam Mustafa; Ayesha Mohyuddin; Bashir Ahmad Ch.

    2016-01-01

    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...

  11. Chemical constituents and biological activities of Garcinia cowa Roxb.

    Directory of Open Access Journals (Sweden)

    Thunwadee Ritthiwigrom

    2013-06-01

    Full Text Available Garcinia cowa is an abundant source of bioactive phytochemicals. Phytochemical investigations of the plant parts indicated that the fruit, twig and stem are the best source of secondary metabolites, providing flavonoids, phloroglucinols and xanthones respectively. Seventy-eight of these compounds have been identified from the plant and several have interesting pharmacological activities.

  12. Chemical constituents and biological activities of Garcinia cowa Roxb.

    OpenAIRE

    Thunwadee Ritthiwigrom

    2013-01-01

    Garcinia cowa is an abundant source of bioactive phytochemicals. Phytochemical investigations of the plant parts indicated that the fruit, twig and stem are the best source of secondary metabolites, providing flavonoids, phloroglucinols and xanthones respectively. Seventy-eight of these compounds have been identified from the plant and several have interesting pharmacological activities.

  13. Densification of oil sands tailings by biological activity

    Energy Technology Data Exchange (ETDEWEB)

    Guo, C.; Chalaturnyk, R.J.; Scott, J.D. [Alberta Univ., Edmonton, AB (Canada). Dept. of Civil and Environmental Engineering; Mackinnon, M. [Syncrude Canada Ltd., Edmonton, AB (Canada). Edmonton Research Centre

    2004-07-01

    Syncrude's Mildred Lake Settling Basin (MLSB) has been accumulating mature fine tailings (MFT) since 1978 with the start of oilsand extraction. The MFT is an aqueous solution of silts, clays and unrecovered bitumen. This suspension was expected to densify to MFT slowly with full consolidation taking decades. However, the MFT densification in the MLSB has accelerated due to increased microbial activity and biogas accumulation and efflux from the MFT. This study examined the mechanism leading to this rapid densification. Small-scale column tests were performed to observe the gas evolution and to measure the changes of the geotechnical parameters under different microbial activities. This paper described the column test device and procedures which revealed the role of microbial activity in accelerating densification and provided a better understanding of the rapid water drainage from the MFT during microbial activity and gas generation. The relationship between the gas migration pathways in the MFT and the densification and strength within the MFT was also examined. The study is continuing on comprehensive consolidation tests of MFT under different conditions. 8 refs., 4 tabs., 16 figs.

  14. Synthesis of radioactively methyl-labelled (1)-carnitine

    Energy Technology Data Exchange (ETDEWEB)

    Ingalls, S.T.; Hoppel, C.L.; Turkaly, J.S. (Case Western Reserve Univ., Cleveland, OH (USA). School of Medicine)

    1982-04-01

    Commercial (l)-carnitine chloride was N-demethylated by the action of sodium benzenemercaptide in warm N,N-dimethylformamide. The product 4-(N,N-dimethylammonio)-3-hydroxybutanoic acid chloride salt was isolated in good yield by ion exchange chromatography. Methylation of the product by /sup 14/C-iodomethane in dry methanol produced biologically active 4-N-Me-/sup 14/C-(l)-carnitine chloride of high specific activity in excellent yield.

  15. Synthesis of radioactively methyl-labelled (1)-carnitine

    International Nuclear Information System (INIS)

    Commercial (l)-carnitine chloride was N-demethylated by the action of sodium benzenemercaptide in warm N,N-dimethylformamide. The product 4-(N,N-dimethylammonio)-3-hydroxybutanoic acid chloride salt was isolated in good yield by ion exchange chromatography. Methylation of the product by 14C -iodomethane in dry methanol produced biologically active 4-N-Me-14C -(l)-carnitine chloride of high specific activity in excellent yield. (author)

  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. Asymmetric Total Synthesis of (+)- and (−)-Clusianone and (+)- and (−)Clusianone Methyl Enol Ether via ACC Alkylation and Evaluation of their Anti-HIV Activity

    Science.gov (United States)

    Garnsey, Michelle R.; Matous, James A.; Kwiek, Jesse J.; Coltart, Don M.

    2011-01-01

    The total asymmetric synthesis of (+)- and (−)-clusianone and (+)- and (−)-clusianone methyl enol ether is reported. Asymmetric induction is achieved through the use of ACC alkylation, providing the key intermediates with an er of 99:1. The four synthetic compounds were evaluated for their anti-HIV activity. Both (+)- and (−)-clusianone displayed significant anti-HIV activity. PMID:21414776

  18. Biologically Inspired Photocatalytically Active Membranes for Water Treatment

    Science.gov (United States)

    Kinsinger, Nichola M.

    There is an alarming increase of a variety of new chemicals that are now being discharged into the wastewater system causing increased concern for public health and safety because many are not removed by typical wastewater treatment practices. Titanium Dioxide (TiO2) is a heterogeneous photocatalytic material that rapidly and completely mineralizing organics without harmful byproducts. TiO2 is synthesized by various methods, which lack the necessary control of crystal size, phase, and morphological features that yield optimized semiconductor materials. Mineralizing organisms demonstrate how nature can produce elegant structures at room temperature through controlled organic-mineral interactions. Here, we utilize biologically-inspired scaffolds to template the nucleation and growth of inorganic materials such as TiO2, which aid in controlling the size and phase of these particles and ultimately, their properties. Nanosized rutile and anatase particles were synthesized under solution conditions at relatively low temperatures and mild pH conditions. The effects of reaction conditions on phase and grain size were investigated and discussed from coordination chemistry and coarsening mechanisms. Photocatalytic characterization of TiO2 phase mixtures was performed to investigate their synergistic effect. The suspension conditions of these catalytic nanomaterials were modulated to optimize the degradation rate of organic analytes. Through the addition of an organic scaffold during the synthesis reaction, a mechanically robust (elastic) composite material containing TiO2 nanoparticles was produced. This composite was subsequently heat-treated to produce a porous, high surface area TiO2 nanoparticulate membrane. Processing conditions were investigated to characterize the growth and phase transformation of TiO2, which ultimately impacts photocatalytic performance. These bulk porous TiO2 structures can be fabricated and tailored to act as stand-alone photocatalytic membranes

  19. 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

    International Nuclear Information System (INIS)

    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

  20. 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