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Sample records for cyclic-imide peptidomimetics derivative

  1. The Synthesis of Unsubstituted Cyclic Imides Using Hydroxylamine under Microwave Irradiation

    Directory of Open Access Journals (Sweden)

    Yousef Hijji

    2008-01-01

    Full Text Available Unsubstituted cyclic imides were synthesized from a series of cyclic anhydrides,hydroxylamine hydrochloride (NH2OH·HCl, and 4-N,N-dimethylamino-pyridine (DMAP,base catalyst under microwave irradiation in monomode and multimode microwaves. Thisnovel microwave synthesis produced high yields of the unsubstituted cyclic imides forboth the monomode (61 - 81% and multimode (84 - 97% microwaves.

  2. New glyme-cyclic imide lithium salt complexes as thermally stable electrolytes for lithium batteries

    Science.gov (United States)

    Tamura, Takashi; Hachida, Takeshi; Yoshida, Kazuki; Tachikawa, Naoki; Dokko, Kaoru; Watanabe, Masayoshi

    New glyme-Li salt complexes were prepared by mixing equimolar amounts of a novel cyclic imide lithium salt LiN(C 2F 4S 2O 4) (LiCTFSI) and a glyme (triglyme (G3) or tetraglyme (G4)). The glyme-Li salt complexes, [Li(G3)][CTFSI] and [Li(G4)][CTFSI], are solid and liquid, respectively, at room temperature. The thermal stability of [Li(G4)][CTFSI] is much higher than that of pure G4, and the vapor pressure of [Li(G4)][CTFSI] is negligible at temperatures lower than 100 °C. Although the viscosity of [Li(G4)][CTFSI] is high (132.0 mPa s at 30 °C), because of its high molar concentration (ca. 3 mol dm -3), its ionic conductivity at 30 °C is relatively high, i.e., 0.8 mS cm -1, which is slightly lower than that of a conventional organic electrolyte solution (1 mol dm -3 LiTFSI dissolved in propylene carbonate). The self-diffusion coefficients of a Li + cation, a CTFSI - anion, and a glyme molecule were measured by the pulsed gradient spin-echo NMR method (PGSE-NMR). The ionicity (dissociativity) of [Li(G4)][CTFSI] at 30 °C is ca. 0.5, as estimated from the PGSE-NMR diffusivity measurements and the ionic conductivity measurements. Results of linear sweep voltammetry revealed that [Li(G4)][CTFSI] is electrochemically stable in an electrode potential range of 0-4.5 V vs. Li/Li +. The reversible deposition-stripping behavior of lithium was observed by cyclic voltammetry. The [LiCoO 2|[Li(G4)][CTFSI]|Li metal] cell showed a stable charge-discharge cycling behavior during 50 cycles, indicating that the [Li(G4)][CTFSI] complex is applicable to a 4 V class lithium secondary battery.

  3. Discovery of novel histidine-derived lipo-amino acids: applied in the synthesis of ultra-short antimicrobial peptidomimetics having potent antimicrobial activity, salt resistance and protease stability.

    Science.gov (United States)

    Ahn, Mija; Murugan, Ravichandran N; Jacob, Binu; Hyun, Jae-Kyung; Cheong, Chaejoon; Hwang, Eunha; Park, Hyo-Nam; Seo, Ji-Hyung; Srinivasrao, G; Lee, Kyung S; Shin, Song Yub; Bang, Jeong Kyu

    2013-10-01

    Here we report for the first time the synthesis of Histidine (His) derived lipo-amino acids having pendant lipid tails at N(τ)- and N(π)-positions on imidazole group of His and applied it into synthesis of lipo-peptides. The attachment of His-derived lipo-amino acid into the very short inactive cationic peptides endows potent antimicrobial activity against Gram-positive and Gram-negative bacteria without hemolytic activity. Furthermore, our designed His-derived lipo-peptidomimetics (HDLPs) consisting of two or three residues displayed strong anti-MRSA activity and protease stability as well as retained potent antimicrobial activity under high salt concentration. Our results demonstrate that the novel lipo-amino acid is highly flexible to synthesize and carry out the extensive structure-activity relationship (SAR) on lipo-antimicrobial peptidomimetics and represents a unique amenable platform for modifying parameters important for antimicrobial activity. Through this study, we proved that the discovery of His-derived lipo-amino acid and the corresponding HDLPs are an excellent candidate as a lead compound for the development of novel antimicrobial agents. Copyright © 2013 Elsevier Masson SAS. All rights reserved.

  4. Small ring constrained peptidomimetics. Synthesis of epoxy peptidomimetics, inhibitors of cysteine proteases.

    Science.gov (United States)

    Demarcus, M; Ganadu, M L; Mura, G M; Porcheddu, A; Quaranta, L; Reginato, G; Taddei, M

    2001-02-09

    Different dipeptide analogues containing an oxirane ring in the place of the peptidic bond were prepared starting from naturally occurring amino acids. N-Fmoc-amino aldehydes were transformed into the corresponding methoxyvinyl derivatives through a Wittig reaction, and the addition of PhSeCl gave a series of different alpha-phenylselenyl aldehydes. Mukajiama reaction with silylketene acetals gave an intermediate product that was finally transformed into the desired oxiranyl peptidomimetics. Following this strategy we were able to control three new contiguous stereocenters starting from the enantiomerically pure amino acid. The dipeptide analogues could be used in SPPS on a SASRIN resin as the final epoxides were relatively unstable under acidic conditions. Moreover the synthesis of the single dipeptide mimetics was carried out on solid phase to generate a small library of epoxy peptidomimetics. Some of the products prepared in this work resulted as time-dependent reversible inhibitors of cysteine protease.

  5. A diversity-oriented synthesis strategy enabling the combinatorial-type variation of macrocyclic peptidomimetic scaffolds.

    Science.gov (United States)

    Isidro-Llobet, Albert; Hadje Georgiou, Kathy; Galloway, Warren R J D; Giacomini, Elisa; Hansen, Mette R; Méndez-Abt, Gabriela; Tan, Yaw Sing; Carro, Laura; Sore, Hannah F; Spring, David R

    2015-04-21

    Macrocyclic peptidomimetics are associated with a broad range of biological activities. However, despite such potentially valuable properties, the macrocyclic peptidomimetic structural class is generally considered as being poorly explored within drug discovery. This has been attributed to the lack of general methods for producing collections of macrocyclic peptidomimetics with high levels of structural, and thus shape, diversity. In particular, there is a lack of scaffold diversity in current macrocyclic peptidomimetic libraries; indeed, the efficient construction of diverse molecular scaffolds presents a formidable general challenge to the synthetic chemist. Herein we describe a new, advanced strategy for the diversity-oriented synthesis (DOS) of macrocyclic peptidomimetics that enables the combinatorial variation of molecular scaffolds (core macrocyclic ring architectures). The generality and robustness of this DOS strategy is demonstrated by the step-efficient synthesis of a structurally diverse library of over 200 macrocyclic peptidomimetic compounds, each based around a distinct molecular scaffold and isolated in milligram quantities, from readily available building-blocks. To the best of our knowledge this represents an unprecedented level of scaffold diversity in a synthetically derived library of macrocyclic peptidomimetics. Cheminformatic analysis indicated that the library compounds access regions of chemical space that are distinct from those addressed by top-selling brand-name drugs and macrocyclic natural products, illustrating the value of our DOS approach to sample regions of chemical space underexploited in current drug discovery efforts. An analysis of three-dimensional molecular shapes illustrated that the DOS library has a relatively high level of shape diversity.

  6. KBE009: An antimalarial bestatin-like inhibitor of the Plasmodium falciparum M1 aminopeptidase discovered in an Ugi multicomponent reaction-derived peptidomimetic library.

    Science.gov (United States)

    González-Bacerio, Jorge; Maluf, Sarah El Chamy; Méndez, Yanira; Pascual, Isel; Florent, Isabelle; Melo, Pollyana M S; Budu, Alexandre; Ferreira, Juliana C; Moreno, Ernesto; Carmona, Adriana K; Rivera, Daniel G; Alonso Del Rivero, Maday; Gazarini, Marcos L

    2017-09-01

    Malaria is a global human parasitic disease mainly caused by the protozoon Plasmodium falciparum. Increased parasite resistance to current drugs determines the relevance of finding new treatments against new targets. A novel target is the M1 alanyl-aminopeptidase from P. falciparum (PfA-M1), which is essential for parasite development in human erythrocytes and is inhibited by the pseudo-peptide bestatin. In this work, we used a combinatorial multicomponent approach to produce a library of peptidomimetics and screened it for the inhibition of recombinant PfA-M1 (rPfA-M1) and the in vitro growth of P. falciparum erythrocytic stages (3D7 and FcB1 strains). Dose-response studies with selected compounds allowed identifying the bestatin-based peptidomimetic KBE009 as a submicromolar rPfA-M1 inhibitor (K i =0.4μM) and an in vitro antimalarial compound as potent as bestatin (IC 50 =18μM; without promoting erythrocyte lysis). At therapeutic-relevant concentrations, KBE009 is selective for rPfA-M1 over porcine APN (a model of these enzymes from mammals), and is not cytotoxic against HUVEC cells. Docking simulations indicate that this compound binds PfA-M1 without Zn 2+ coordination, establishing mainly hydrophobic interactions and showing a remarkable shape complementarity with the active site of the enzyme. Moreover, KBE009 inhibits the M1-type aminopeptidase activity (Ala-7-amido-4-methylcoumarin substrate) in isolated live parasites with a potency similar to that of the antimalarial activity (IC 50 =82μM), strongly suggesting that the antimalarial effect is directly related to the inhibition of the endogenous PfA-M1. These results support the value of this multicomponent strategy to identify PfA-M1 inhibitors, and make KBE009 a promising hit for drug development against malaria. Copyright © 2017 Elsevier Ltd. All rights reserved.

  7. Virtual Screening of Peptide and Peptidomimetic Fragments Targeted to Inhibit Bacterial Dithiol Oxidase DsbA.

    Directory of Open Access Journals (Sweden)

    Wilko Duprez

    Full Text Available Antibacterial drugs with novel scaffolds and new mechanisms of action are desperately needed to address the growing problem of antibiotic resistance. The periplasmic oxidative folding system in Gram-negative bacteria represents a possible target for anti-virulence antibacterials. By targeting virulence rather than viability, development of resistance and side effects (through killing host native microbiota might be minimized. Here, we undertook the design of peptidomimetic inhibitors targeting the interaction between the two key enzymes of oxidative folding, DsbA and DsbB, with the ultimate goal of preventing virulence factor assembly. Structures of DsbB--or peptides--complexed with DsbA revealed key interactions with the DsbA active site cysteine, and with a hydrophobic groove adjacent to the active site. The present work aimed to discover peptidomimetics that target the hydrophobic groove to generate non-covalent DsbA inhibitors. The previously reported structure of a Proteus mirabilis DsbA active site cysteine mutant, in a non-covalent complex with the heptapeptide PWATCDS, was used as an in silico template for virtual screening of a peptidomimetic fragment library. The highest scoring fragment compound and nine derivatives were synthesized and evaluated for DsbA binding and inhibition. These experiments discovered peptidomimetic fragments with inhibitory activity at millimolar concentrations. Although only weakly potent relative to larger covalent peptide inhibitors that interact through the active site cysteine, these fragments offer new opportunities as templates to build non-covalent inhibitors. The results suggest that non-covalent peptidomimetics may need to interact with sites beyond the hydrophobic groove in order to produce potent DsbA inhibitors.

  8. Development of Peptidomimetic Inhibitors of the ERG Gene Fusion Product in Prostate Cancer.

    Science.gov (United States)

    Wang, Xiaoju; Qiao, Yuanyuan; Asangani, Irfan A; Ateeq, Bushra; Poliakov, Anton; Cieślik, Marcin; Pitchiaya, Sethuramasundaram; Chakravarthi, Balabhadrapatruni V S K; Cao, Xuhong; Jing, Xiaojun; Wang, Cynthia X; Apel, Ingrid J; Wang, Rui; Tien, Jean Ching-Yi; Juckette, Kristin M; Yan, Wei; Jiang, Hui; Wang, Shaomeng; Varambally, Sooryanarayana; Chinnaiyan, Arul M

    2017-04-10

    Transcription factors play a key role in the development of diverse cancers, and therapeutically targeting them has remained a challenge. In prostate cancer, the gene encoding the transcription factor ERG is recurrently rearranged and plays a critical role in prostate oncogenesis. Here, we identified a series of peptides that interact specifically with the DNA binding domain of ERG. ERG inhibitory peptides (EIPs) and derived peptidomimetics bound ERG with high affinity and specificity, leading to proteolytic degradation of the ERG protein. The EIPs attenuated ERG-mediated transcription, chromatin recruitment, protein-protein interactions, cell invasion and proliferation, and tumor growth. Thus, peptidomimetic targeting of transcription factor fusion products may provide a promising therapeutic strategy for prostate cancer as well as other malignancies. Copyright © 2017 Elsevier Inc. All rights reserved.

  9. Rational Design of Nanobody80 Loop Peptidomimetics

    DEFF Research Database (Denmark)

    Martin, Charlotte; Moors, Samuel L C; Danielsen, Mia

    2017-01-01

    G protein-coupled receptors (GPCRs) play an important role in many cellular responses; as such, their mechanism of action is of utmost interest. To gain insight into the active conformation of GPCRs, the X-ray crystal structures of nanobody (Nb)-stabilized β2 -adrenergic receptor (β2 AR) have been......-hairpin conformation. Syntheses, conformational analysis, binding and functional in vitro assays, as well as internalization experiments, were performed. We demonstrate that peptidomimetics can structurally mimic the CDR3 loop of a nanobody and its function by inhibiting G protein coupling as measured by partial...

  10. Olefin Metathesis in Peptidomimetics, Dynamic Combinatorial Chemistry, and Molecular Imprinting

    National Research Council Canada - National Science Library

    Low, Tammy K

    2006-01-01

    .... Our research goals consisted of employing olefin metathesis in the synthesis of peptidomimetics, and studying the feasibility of this method in dynamic combinatorial chemistry and molecular imprinting of nerve agents...

  11. Synthesis of conformationally constrained peptidomimetics using multicomponent reactions

    NARCIS (Netherlands)

    Scheffelaar, R.; Klein Nijenhuis, R.A.; Paravidino, M.; Lutz, M.; Spek, A.L.; Ehlers, A.W.; de Kanter, F.J.J.; Groen, M.B.; Orru, R.V.A.; Ruijter, E.

    2009-01-01

    A novel modular synthetic approach toward constrained peptidomimetics is reported. The approach involves a highly efficient three-step sequence including two multicomponent reactions, thus allowing unprecedented diversification of both the peptide moieties and the turn-inducing scaffold. The

  12. Interferon gamma peptidomimetic targeted to hepatic stellate cells ameliorates acute and chronic liver fibrosis in vivo.

    Science.gov (United States)

    Bansal, Ruchi; Prakash, Jai; De Ruiter, Marieke; Poelstra, Klaas

    2014-04-10

    Hepatic stellate cells play a crucial role in the pathogenesis of hepatic fibrosis. Thus, pharmacological inhibition of pro-fibrotic activities of these cells might lead to an effective therapy for this disease. Among the potent anti-fibrotics, interferon gamma (IFNγ), a proinflammatory cytokine, is highly efficacious but it failed in clinical trials due to the poor efficacy and multiple adverse effects attributed to the ubiquitous IFNγ receptor (IFNγR) expression. To resolve these drawbacks, we chemically synthesized a chimeric molecule containing (a) IFNγ signaling peptide (IFNγ peptidomimetic, mimγ) that retains the agonistic activities of IFNγ but lacks an extracellular receptor recognition sequence for IFNγR; coupled via heterobifunctional PEG linker to (b) bicyclic platelet derived growth factor beta receptor (PDGFβR)-binding peptide (BiPPB) to induce internalization into the stellate cells that express PDGFβR. The synthesized targeted IFNγ peptidomimetic (mimγ-BiPPB) was extensively investigated for its anti-fibrotic and adverse effects in acute and chronic CCl4-induced liver fibrosis models in mice. Treatment with mimγ-BiPPB, after the onset of disease, markedly inhibited both early and established hepatic fibrosis as reflected by a reduced intrahepatic α-SMA, desmin and collagen-I mRNA expression and protein levels. While untargeted mimγ and BiPPB had no effect, and native IFNγ only induced a moderate reduction. Additionally, no off-target effects, e.g. systemic inflammation, were found with mimγ-BiPPB, which were substantially observed in mice treated with native IFNγ. The present study highlights the beneficial effects of a novel BiPPB mediated cell-specific targeting of IFNγ peptidomimetic to the disease-inducing cells and therefore represents a highly potential therapeutic approach to treat fibrotic diseases. Copyright © 2014 Elsevier B.V. All rights reserved.

  13. A diversity-oriented synthesis strategy enabling the combinatorial-type variation of macrocyclic peptidomimetic scaffolds† †Electronic supplementary information (ESI) available: Experimental procedures, characterization data and details of the computational analyses. See DOI: 10.1039/c5ob00371g Click here for additional data file.

    Science.gov (United States)

    Isidro-Llobet, Albert; Hadje Georgiou, Kathy; Galloway, Warren R. J. D.; Giacomini, Elisa; Hansen, Mette R.; Méndez-Abt, Gabriela; Tan, Yaw Sing; Carro, Laura; Sore, Hannah F.

    2015-01-01

    Macrocyclic peptidomimetics are associated with a broad range of biological activities. However, despite such potentially valuable properties, the macrocyclic peptidomimetic structural class is generally considered as being poorly explored within drug discovery. This has been attributed to the lack of general methods for producing collections of macrocyclic peptidomimetics with high levels of structural, and thus shape, diversity. In particular, there is a lack of scaffold diversity in current macrocyclic peptidomimetic libraries; indeed, the efficient construction of diverse molecular scaffolds presents a formidable general challenge to the synthetic chemist. Herein we describe a new, advanced strategy for the diversity-oriented synthesis (DOS) of macrocyclic peptidomimetics that enables the combinatorial variation of molecular scaffolds (core macrocyclic ring architectures). The generality and robustness of this DOS strategy is demonstrated by the step-efficient synthesis of a structurally diverse library of over 200 macrocyclic peptidomimetic compounds, each based around a distinct molecular scaffold and isolated in milligram quantities, from readily available building-blocks. To the best of our knowledge this represents an unprecedented level of scaffold diversity in a synthetically derived library of macrocyclic peptidomimetics. Cheminformatic analysis indicated that the library compounds access regions of chemical space that are distinct from those addressed by top-selling brand-name drugs and macrocyclic natural products, illustrating the value of our DOS approach to sample regions of chemical space underexploited in current drug discovery efforts. An analysis of three-dimensional molecular shapes illustrated that the DOS library has a relatively high level of shape diversity. PMID:25778821

  14. Adding diverse noncanonical backbones to rosetta: enabling peptidomimetic design.

    Directory of Open Access Journals (Sweden)

    Kevin Drew

    Full Text Available Peptidomimetics are classes of molecules that mimic structural and functional attributes of polypeptides. Peptidomimetic oligomers can frequently be synthesized using efficient solid phase synthesis procedures similar to peptide synthesis. Conformationally ordered peptidomimetic oligomers are finding broad applications for molecular recognition and for inhibiting protein-protein interactions. One critical limitation is the limited set of design tools for identifying oligomer sequences that can adopt desired conformations. Here, we present expansions to the ROSETTA platform that enable structure prediction and design of five non-peptidic oligomer scaffolds (noncanonical backbones, oligooxopiperazines, oligo-peptoids, [Formula: see text]-peptides, hydrogen bond surrogate helices and oligosaccharides. This work is complementary to prior additions to model noncanonical protein side chains in ROSETTA. The main purpose of our manuscript is to give a detailed description to current and future developers of how each of these noncanonical backbones was implemented. Furthermore, we provide a general outline for implementation of new backbone types not discussed here. To illustrate the utility of this approach, we describe the first tests of the ROSETTA molecular mechanics energy function in the context of oligooxopiperazines, using quantum mechanical calculations as comparison points, scanning through backbone and side chain torsion angles for a model peptidomimetic. Finally, as an example of a novel design application, we describe the automated design of an oligooxopiperazine that inhibits the p53-MDM2 protein-protein interaction. For the general biological and bioengineering community, several noncanonical backbones have been incorporated into web applications that allow users to freely and rapidly test the presented protocols (http://rosie.rosettacommons.org. This work helps address the peptidomimetic community's need for an automated and expandable

  15. Advances in Development of Antimicrobial Peptidomimetics as Potential Drugs.

    Science.gov (United States)

    Molchanova, Natalia; Hansen, Paul R; Franzyk, Henrik

    2017-08-29

    The rapid emergence of multidrug-resistant pathogens has evolved into a global health problem as current treatment options are failing for infections caused by pan-resistant bacteria. Hence, novel antibiotics are in high demand, and for this reason antimicrobial peptides (AMPs) have attracted considerable interest, since they often show broad-spectrum activity, fast killing and high cell selectivity. However, the therapeutic potential of natural AMPs is limited by their short plasma half-life. Antimicrobial peptidomimetics mimic the structure and biological activity of AMPs, but display extended stability in the presence of biological matrices. In the present review, focus is on the developments reported in the last decade with respect to their design, synthesis, antimicrobial activity, cytotoxic side effects as well as their potential applications as anti-infective agents. Specifically, only peptidomimetics with a modular structure of residues connected via amide linkages will be discussed. These comprise the classes of α-peptoids ( N -alkylated glycine oligomers), β-peptoids ( N -alkylated β-alanine oligomers), β³-peptides, α/β³-peptides, α-peptide/β-peptoid hybrids, α/γ N -acylated N -aminoethylpeptides (AApeptides), and oligoacyllysines (OAKs). Such peptidomimetics are of particular interest due to their potent antimicrobial activity, versatile design, and convenient optimization via assembly by standard solid-phase procedures.

  16. Selectivity in the potentiation of antibacterial activity of α-peptide/β-peptoid peptidomimetics and antimicrobial peptides by human blood plasma

    DEFF Research Database (Denmark)

    Hein-Kristensen, Line; Knapp, Kolja M.; Franzyk, Henrik

    2013-01-01

    Antimicrobial peptides (AMPs) are promising leads for novel antibiotics; however, their activity is often compromised under physiological conditions. The purpose of this study was to determine the activity of alpha-peptide/beta-peptoid peptidomimetics and AMPs against Escherichia coli and Staphyl......Antimicrobial peptides (AMPs) are promising leads for novel antibiotics; however, their activity is often compromised under physiological conditions. The purpose of this study was to determine the activity of alpha-peptide/beta-peptoid peptidomimetics and AMPs against Escherichia coli...... and Staphylococcus aureus in the presence of human blood-derived matrices and immune effectors. The minimum inhibitory concentration (MIC) of two peptidomimetics against E. coli decreased by up to one order of magnitude when determined in 50% blood plasma as compared to MHB media. The MIC of a membrane-active AMP......, LL-I/3, also decreased, whereas two intracellularly acting AMPs were not potentiated by plasma. Blood serum had no effect on activity against E. coli and neither matrix had an effect on activity against S. aureus. Unexpectedly, physiological concentrations of human serum albumin did not influence...

  17. Programming peptidomimetic syntheses by translating genetic codes designed de novo.

    Science.gov (United States)

    Forster, Anthony C; Tan, Zhongping; Nalam, Madhavi N L; Lin, Hening; Qu, Hui; Cornish, Virginia W; Blacklow, Stephen C

    2003-05-27

    Although the universal genetic code exhibits only minor variations in nature, Francis Crick proposed in 1955 that "the adaptor hypothesis allows one to construct, in theory, codes of bewildering variety." The existing code has been expanded to enable incorporation of a variety of unnatural amino acids at one or two nonadjacent sites within a protein by using nonsense or frameshift suppressor aminoacyl-tRNAs (aa-tRNAs) as adaptors. However, the suppressor strategy is inherently limited by compatibility with only a small subset of codons, by the ways such codons can be combined, and by variation in the efficiency of incorporation. Here, by preventing competing reactions with aa-tRNA synthetases, aa-tRNAs, and release factors during translation and by using nonsuppressor aa-tRNA substrates, we realize a potentially generalizable approach for template-encoded polymer synthesis that unmasks the substantially broader versatility of the core translation apparatus as a catalyst. We show that several adjacent, arbitrarily chosen sense codons can be completely reassigned to various unnatural amino acids according to de novo genetic codes by translating mRNAs into specific peptide analog polymers (peptidomimetics). Unnatural aa-tRNA substrates do not uniformly function as well as natural substrates, revealing important recognition elements for the translation apparatus. Genetic programming of peptidomimetic synthesis should facilitate mechanistic studies of translation and may ultimately enable the directed evolution of small molecules with desirable catalytic or pharmacological properties.

  18. Characterization of a proteolytically stable multifunctional host defense peptidomimetic

    DEFF Research Database (Denmark)

    Jahnsen, Rasmus D; Haney, Evan F; Franzyk, Henrik

    2013-01-01

    The in vitro activity of a host defense peptidomimetic (HDM-4) was investigated. The compound exhibited an antimicrobial activity profile against a range of Gram-negative bacteria. HDM-4 permeabilized the outer membrane and partly depolarized the inner membrane at its minimal inhibitory...... concentration (MIC). Moreover, it was demonstrated that HDM-4 was distributed widely in the bacterial cell at lethal concentrations, and that it could bind to DNA. It was confirmed that the multimodal action of HDM-4 resulted in it being less likely to lead to resistance development as compared to single......-target antibiotics. HDM-4 exhibited multispecies anti-biofilm activity at sub-MIC levels. Furthermore, HDM-4 modulated the immune response by inducing the release of the chemoattractants interleukin-8 (IL-8), monocyte chemotactic protein-1 (MCP-1), and MCP-3 from human peripheral blood mononuclear cells. In addition...

  19. The Synthetic Amphipathic Peptidomimetic LTX109 Is a Potent Fungicide That Disturbs Plasma Membrane Integrity in a Sphingolipid Dependent Manner

    DEFF Research Database (Denmark)

    Bojsen, Rasmus; Torbensen, Rasmus; Larsen, Camilla Eggert

    2013-01-01

    The peptidomimetic LTX109 (arginine-tertbutyl tryptophan-arginine-phenylethan) was previously shown to have antibacterial properties. Here, we investigated the activity of this novel antimicrobial peptidomimetic on the yeast Saccharomyces cerevisiae. We found that LTX109 was an efficient fungicid...

  20. Gs protein peptidomimetics as allosteric modulators of the β2-adrenergic receptor

    DEFF Research Database (Denmark)

    Boyhus, Lotte Emilie; Danielsen, Mia; Bengtson, Nina Smidt

    2018-01-01

    A series of Gs protein peptidomimetics were designed and synthesised based on the published X-ray crystal structure of the active state β2-Adrenergic receptor (β2AR) in complex with the Gs protein (PDB 3SN6). We hypothesised that such peptidomimetics may function as allosteric modulators...... that target the intracellular Gs protein binding site of the β2AR. Peptidomimetics were designed to mimic the 15 residue C-Terminal α-helix of the Gs protein and were pre-organised in a helical conformation by (i, i + 4)-stapling using copper catalysed azide alkyne cycloaddition. Linear and stapled...... be able to compete with the native Gs protein for the intracellular binding site to block ISO-induced cAMP formation, but are unable to stabilise an active-like receptor conformation....

  1. Lack of interaction between the peptidomimetic substrates captopril and cephradine.

    Science.gov (United States)

    Foster, David R; Yee, Shiyin; Bleske, Barry E; Carver, Peggy L; Shea, Michael J; Menon, Sujatha S; Ramachandran, Chandrasekharan; Welage, Lynda S; Amidon, Gordon L

    2009-03-01

    Intestinal peptide transporters, including hPEPT1, facilitate the absorption of cephalosporins and angiotensin-converting enzyme inhibitors, and have been investigated as a means to improve oral drug absorption. Renal peptide transporters including hPEPT2, may also facilitate renal reabsorption of such compounds. In vitro and animal studies suggest that co-administration of peptidomimetic compounds may alter oral pharmacokinetics, although this has not been well studied in humans. The purpose of this study was to determine whether co-administration of the hPEPT substrates captopril and cephradine alters the oral pharmacokinetics of either agent. Nine healthy male volunteers received a single oral 25-mg dose of captopril, a single oral 500-mg dose of cephradine, or concurrent ingestion of captopril and cephradine in a cross-over manner. Venous blood samples were taken and captopril and cephradine pharmacokinetics were determined using noncompartmental analyses. No significant differences were observed in captopril or cephradine pharmacokinetics when administered together as compared to each agent alone (a marginal decrease in C(max) was observed for both captopril and cephradine during co-administration [5-15%]; however, differences were not statistically significant). The results of our study suggest that hPEPT1 and hPEPT2 are unlikely to contribute to clinically important drug interactions in humans.

  2. Modulation of prion polymerization and toxicity by rationally designed peptidomimetics.

    Science.gov (United States)

    Srivastava, Ankit; Sharma, Sakshi; Sadanandan, Sandhya; Gupta, Sakshi; Singh, Jasdeep; Gupta, Sarika; Haridas, V; Kundu, Bishwajit

    2017-01-01

    Misfolding and aggregation of cellular prion protein is associated with a large array of neurological disorders commonly called the transmissible spongiform encephalopathies. Designing inhibitors against prions has remained a daunting task owing to limited information about mechanism(s) of their pathogenic self-assembly. Here, we explore the anti-prion properties of a combinatorial library of bispidine-based peptidomimetics (BPMs) that conjugate amino acids with hydrophobic and aromatic side chains. Keeping the bispidine unit unaltered, a series of structurally diverse BPMs were synthesized and tested for their prion-modulating properties. Administration of Leu- and Trp-BPMs delayed and completely inhibited the amyloidogenic conversion of human prion protein (HuPrP), respectively. We found that each BPM induced the HuPrP to form unique oligomeric nanostructures differing in their biophysical properties, cellular toxicities and response to conformation-specific antibodies. While Leu-BPMs were found to stabilize the oligomers, Trp-BPMs effected transient oligomerization, resulting in the formation of non-toxic, non-fibrillar aggregates. Yet another aromatic residue, Phe, however, accelerated the aggregation process in HuPrP. Molecular insights obtained through MD (molecular dynamics) simulations suggested that each BPM differently engages a conserved Tyr 169 residue at the α2-β2 loop of HuPrP and affects the stability of α2 and α3 helices. Our results demonstrate that this new class of molecules having chemical scaffolds conjugating hydrophobic/aromatic residues could effectively modulate prion aggregation and toxicity. © 2017 The Author(s); published by Portland Press Limited on behalf of the Biochemical Society.

  3. Tailoring Cytotoxicity of Antimicrobial Peptidomimetics with High Activity against Multidrug-Resistant Escherichia coli

    DEFF Research Database (Denmark)

    Jahnsen, Rasmus D; Sandberg-Schaal, Anne; Vissing, Karina Juul

    2014-01-01

    Infections with multidrug-resistant pathogens are an increasing concern for public health. Recently, subtypes of peptide-peptoid hybrids were demonstrated to display potent activity against multidrug-resistant Gram-negative bacteria. Here, structural variation of these antibacterial peptidomimetics...... cells. Thus, lead compounds with a high selectivity toward killing of clinically important multidrug-resistant E. coli were identified....

  4. Anti-virulence approaches and novel peptidomimetics for combating resistant and biofilm associated bacteria

    DEFF Research Database (Denmark)

    Liu, Yang

    Anti-virulence approaches and novel peptidomimetics for combating resistant and biofilm associated bacteria The misuse and overuse of antibiotics has a broad impact on the environment. Antibiotic resistance has become a major threat for modern medical treatment of infectious diseases. There are m......Anti-virulence approaches and novel peptidomimetics for combating resistant and biofilm associated bacteria The misuse and overuse of antibiotics has a broad impact on the environment. Antibiotic resistance has become a major threat for modern medical treatment of infectious diseases...... consisting of microcolonies embedded in self-produced extracellular polymer substances (EPS). EPS can contribute to cell-cell adhesion and restrict antibiotic penetration. Biofilm cells show much greater resistance to stressful conditions than their free-living counterparts. Conventional treatment strategies...

  5. Multivalent Peptidomimetic Conjugates as Inhibitors of Androgen Receptor Function in Therapy-Resistant Prostate Cancer

    Science.gov (United States)

    2016-10-01

    findings in the journal Cancer Research. 15. SUBJECT TERMS androgen receptor, prostate cancer, peptidomimetic conjugates, 16. SECURITY CLASSIFICATION OF...CAN-16-0385. Epub 2016 Aug 3, which is widely read by basic and clinical oncologists. The study was also highlighted in the journal Nature Reviews...This article must therefore be hereby marked advertisement in accordance with 18 U.S.C. Section 1734 solely to indicate this fact. Received February 11

  6. Multivalent Peptidomimetic Conjugates as Inhibitors of Androgen Receptor Function in Therapy-Resistant Prostate Cancer

    Science.gov (United States)

    2017-10-01

    treat patients with prostate cancer, over time the tumors become resistant to the drugs, leaving few treatment options. The goal of this proposal is to...interactions with the AR. 15. SUBJECT TERMS androgen receptor, prostate cancer, peptidomimetic conjugates, 16. SECURITY CLASSIFICATION OF: 17...used successfully to treat patients with prostate cancer, over time the tumors become resistant to the drugs, leaving few treatment options. The goal

  7. Peptidomimetic inhibitors of APC-Asef interaction block colorectal cancer migration.

    Science.gov (United States)

    Jiang, Haiming; Deng, Rong; Yang, Xiuyan; Shang, Jialin; Lu, Shaoyong; Zhao, Yanlong; Song, Kun; Liu, Xinyi; Zhang, Qiufen; Chen, Yu; Chinn, Y Eugene; Wu, Geng; Li, Jian; Chen, Guoqiang; Yu, Jianxiu; Zhang, Jian

    2017-09-01

    The binding of adenomatous polyposis coli (APC) to its receptor Asef relieves the negative intramolecular regulation of Asef and leads to aberrant cell migration in human colorectal cancer. Because of its crucial role in metastatic dissemination, the interaction between APC and Asef is an attractive target for anti-colorectal-cancer therapy. We rationally designed a series of peptidomimetics that act as potent inhibitors of the APC interface. Crystal structures and biochemical and cellular assays showed that the peptidomimetics in the APC pocket inhibited the migration of colorectal cells by disrupting APC-Asef interaction. By using the peptidomimetic inhibitor as a chemical probe, we found that CDC42 was the downstream GTPase involved in APC-stimulated Asef activation in colorectal cancer cells. Our work demonstrates the feasibility of exploiting APC-Asef interaction to regulate the migration of colorectal cancer cells, and provides what to our knowledge is the first class of protein-protein interaction inhibitors available for the development of cancer therapeutics targeting APC-Asef signaling.

  8. Eco-Friendly Insecticide Discovery via Peptidomimetics: Design, Synthesis, and Aphicidal Activity of Novel Insect Kinin Analogues.

    Science.gov (United States)

    Zhang, Chuanliang; Qu, Yanyan; Wu, Xiaoqing; Song, Dunlun; Ling, Yun; Yang, Xinling

    2015-05-13

    Insect kinin neuropeptides are pleiotropic peptides that are involved in the regulation of hindgut contraction, diuresis, and digestive enzyme release. They share a common C-terminal pentapeptide sequence of Phe(1)-Xaa(2)-Yaa(3)-Trp(4)-Gly(5)-NH2 (where Xaa(2) = His, Asn, Phe, Ser, or Tyr; Yaa(3) = Pro, Ser, or Ala). Recently, the aphicidal activity of insect kinin analogues has attracted the attention of researchers. Our previous work demonstrated that the sequence-simplified insect kinin pentapeptide analogue Phe-Phe-[Aib]-Trp-Gly-NH2 could retain good aphicidal activity and be the lead compound for the further discovery of eco-friendly insecticides which encompassed a broad array of biochemicals derived from micro-organisms and other natural sources. Using the peptidomimetics strategy, we chose Phe-Phe-[Aib]-Trp-Gly-NH2 as the lead compound, and we designed and synthesized three series, including 31 novel insect kinin analogues. The aphicidal activity of the new analogues against soybean aphid was determined. The results showed that all of the analogues exhibited aphicidal activity. Of particular interest was the analogue II-1, which exhibited improved aphicidal activity with an LC50 of 0.019 mmol/L compared with the lead compound (LC50 = 0.045 mmol/L) or the commercial insecticide pymetrozine (LC50 = 0.034 mmol/L). This suggests that the analogue II-1 could be used as a new lead for the discovery of potential eco-friendly insecticides.

  9. Design, Synthesis, and Biological Evaluation of Peptidomimetic N-Substituted Cbz-4-Hyp-Hpa-Amides as Novel Inhibitors of Plasmodium falciparum.

    Science.gov (United States)

    Bacherikov, Valeriy A; Chittiboyina, Amar G; Avery, Mitchell A

    2017-08-01

    A new series of peptidomimetic N-substituted Cbz-4-Hyp-Hpa-amides were designed, synthesized, and evaluated for inhibition of the Plasmodium falciparum. Substituents on the N-atom of the amide group were selected alkyl-, allyl-, aryl-, 2-hydroxyethyl-, 2-cyanoethyl-, cyanomethyl-, 2-hydroxyethyl-, 2,2-diethoxyethyl-, or 2-ethoxy-2-oxoethylamino groups, and about of 40 new compounds were synthesized and evaluated for antiplasmodial activity in vitro. Antimalarial activity has been investigated as for the final peptide mimetics, and their immediate predecessors, carrying TBDMS or TBDPS protecting groups on 4-hydroxyproline residue and 18 derivatives exhibited toxicity against P. falciparum. Of these agents, compound 23e was shown to have potent antimalarial activity with IC 50 528 ng/ml. © 2017 Wiley-VHCA AG, Zurich, Switzerland.

  10. Membrane adsorption and binding, cellular uptake and cytotoxicity of cell-penetrating peptidomimetics with α-peptide/β-peptoid backbone

    DEFF Research Database (Denmark)

    Jing, Xiaona; Yang, Mingjun; Kasimova, Marina Robertovna

    2012-01-01

    to evaluate the effect of α-chirality in the β-peptoid residues and the presence of guanidinium groups in the α-amino acid residues on membrane interaction. The molecular properties of the peptidomimetics in solution (surface and intramolecular hydrogen bonding, aqueous diffusion rate and molecular size) were...... studied along with their adsorption to lipid bilayers, cellular uptake, and toxicity. The surface hydrogen bonding ability of the peptidomimetics reflected their adsorbed amounts onto lipid bilayers as well as with their cellular uptake, indicating the importance of hydrogen bonding for their membrane...

  11. Guanidino groups greatly enhance the action of antimicrobial peptidomimetics against bacterial cytoplasmic membranes

    DEFF Research Database (Denmark)

    Andreev, Konstantin; Bianchi, Christopher; Laursen, Jonas Striegler

    2014-01-01

    Antimicrobial peptides or their synthetic mimics are a promising class of potential new antibiotics. Herein we assess the effect of the type of cationic side chain (i.e., guanidino vs. amino groups) on the membrane perturbing mechanism of antimicrobial α-peptide-β-peptoid chimeras. Langmuir...... of the measurements using an array of techniques, including high-resolution synchrotron surface X-ray scattering, epifluorescence microscopy, and in vitro antimicrobial activity to study the molecular mechanisms of peptidomimetic interaction with bacterial membranes. We found guanidino group-containing chimeras...

  12. Supramolecular Properties of Triazole-containing Two Armed Peptidomimetics: From Organogelators to Nucleotide-binding Tweezers

    Science.gov (United States)

    Chui, Tin Ki

    This thesis described the development of a new type of branched peptidomimetics using a class of previously reported triazole-containing peptidomimetics as the structural motif. The propensity of these new branched peptiomimetics in being an organogelator, forming supramolecular assemblies and recognizing anions and biomolecules was investigated. The quest began with the preparation of two different series of branched peptidomimetics, namely 69-K-aa3 (aa = V or L) and 70-B-aa3. The former series made use of the flexible L-lysine (K) as the branching unit while the latter series was composed of the relatively rigid 3,5-diminobenzoate (B). In each series, the peptidomimetic arms were composed of solely valine (V) or leucine (L). The effects of the identity of the amino acids and the branching units on the gelation and self-assembling properties of these branched bis(tripeptidomimetic)s were investigated. The 69-K-aa3 series was found to exhibit poor solubility in common organic solvents yet it was able to form strong and stable gels in aromatic solvents. The 70-B-aa3 series, on the other hand, was a poor organogelator despite its excellent solubility. Morphological studies using scanning electron microscopy (SEM) and transmission electron microscopy (TEM) revealed the ability of the former to form a hyperbranched 3D network whereas the latter was only capable of forming isolated spherical lumps. Nevertheless, the latter displayed the ability in forming supramolecular polymers as shown from viscometric studies. Solution-to-gel transition temperature measurement of the gels formed by the 69-K-aa3 series and association constants determination by 1H NMR titration experiments for the supramolecular polymerization of the 70-B-aa3 series both suggested that peptidomimetic arms comprised of valine performed better than those made up of leucine in terms of association strength, and such a difference was attributed to the bulkier nature of the leucine side chain. In order to

  13. An antimicrobial peptidomimetic induces Mucorales cell death through mitochondria-mediated apoptosis.

    Directory of Open Access Journals (Sweden)

    E Magda Barbu

    Full Text Available The incidence of mucormycosis has dramatically increased in immunocompromised patients. Moreover, the array of cellular targets whose inhibition results in fungal cell death is rather limited. Mitochondria have been mechanistically identified as central regulators of detoxification and virulence in fungi. Our group has previously designed and developed a proteolytically-resistant peptidomimetic motif D(KLAKLAK2 with pleiotropic action ranging from targeted (i.e., ligand-directed activity against cancer and obesity to non-targeted activity against antibiotic resistant gram-negative rods. Here we evaluated whether this non-targeted peptidomimetic motif is active against Mucorales. We show that D(KLAKLAK2 has marked fungicidal action, inhibits germination, and reduces hyphal viability. We have also observed cellular changes characteristic of apoptosis in D(KLAKLAK2-treated Mucorales cells. Moreover, the fungicidal activity was directly correlated with vacuolar injury, mitochondrial swelling and mitochondrial membrane depolarization, intracellular reactive oxygen species accumulation (ROS, and increased caspase-like enzymatic activity. Finally, these apoptotic features were prevented by the addition of the ROS scavenger N-acetyl-cysteine indicating mechanistic pathway specificity. Together, these findings indicate that D(KLAKLAK2 makes Mucorales exquisitely susceptible via mitochondrial injury-induced apoptosis. This prototype may serve as a candidate drug for the development of translational applications against mucormycosis and perhaps other fungal infections.

  14. An antimicrobial peptidomimetic induces Mucorales cell death through mitochondria-mediated apoptosis.

    Science.gov (United States)

    Barbu, E Magda; Shirazi, Fazal; McGrath, Danielle M; Albert, Nathaniel; Sidman, Richard L; Pasqualini, Renata; Arap, Wadih; Kontoyiannis, Dimitrios P

    2013-01-01

    The incidence of mucormycosis has dramatically increased in immunocompromised patients. Moreover, the array of cellular targets whose inhibition results in fungal cell death is rather limited. Mitochondria have been mechanistically identified as central regulators of detoxification and virulence in fungi. Our group has previously designed and developed a proteolytically-resistant peptidomimetic motif D(KLAKLAK)2 with pleiotropic action ranging from targeted (i.e., ligand-directed) activity against cancer and obesity to non-targeted activity against antibiotic resistant gram-negative rods. Here we evaluated whether this non-targeted peptidomimetic motif is active against Mucorales. We show that D(KLAKLAK)2 has marked fungicidal action, inhibits germination, and reduces hyphal viability. We have also observed cellular changes characteristic of apoptosis in D(KLAKLAK)2-treated Mucorales cells. Moreover, the fungicidal activity was directly correlated with vacuolar injury, mitochondrial swelling and mitochondrial membrane depolarization, intracellular reactive oxygen species accumulation (ROS), and increased caspase-like enzymatic activity. Finally, these apoptotic features were prevented by the addition of the ROS scavenger N-acetyl-cysteine indicating mechanistic pathway specificity. Together, these findings indicate that D(KLAKLAK)2 makes Mucorales exquisitely susceptible via mitochondrial injury-induced apoptosis. This prototype may serve as a candidate drug for the development of translational applications against mucormycosis and perhaps other fungal infections.

  15. Olefin Metathesis in Peptidomimetics, Dynamic Combinatorial Chemistry, and Molecular Imprinting

    Science.gov (United States)

    2006-08-01

    organic, and biochemistry, lectured in chemistry of weapons, and researched on ionic liquids and nucleic acid derivatives. She discovered her joy of...Products from oligomerization of the dimer scaffold or olefin isomerization are excluded from these projected numbers.97,98 The number of...Figure 3-8). This is excluding any olefin isomerization products or oligomerization of the cyclic scaffold. If stereoisomers are considered, then

  16. Tailoring Peptidomimetics Antifreeze Protein from Exotic Antarctic Marine

    International Nuclear Information System (INIS)

    Mohd Basyaruddin Abdul Rahman; Azren Aida Asmawi; Emilia Abdulmalek

    2016-01-01

    Antifreeze proteins (AFPs) are synthesized by various cold-adapted organisms to enable them to survive in subzero environment. The unique role of AFPs recently attracted enormous interest to develop them as commercial products. In this work, we have studied the antifreeze activity of short helical protein fragments (peptides) instead of the entire antifreeze protein of Antarctic yeast Glaciozyma antarctica. Several short peptide segments were designed according to amino acid sequence of helical region of AFP-1 G.antarctica, which are assumed to be involved in its antifreeze activity. We have demonstrated that short peptide segments derived from yeast AFP possess antifreeze activity and result in modification of the ice crystals growth rates and habits. This strategy has enabled the preparation of short AFP with high antifreeze activity in large amount of quantities at a low cost further opens the chance of developing the commercial potentials of AFPs.(author)

  17. Small cationic antimicrobial peptidomimetics: emerging candidate for the development of potential anti-infective agents.

    Science.gov (United States)

    Lohan, Sandeep; Bisht, Gopal Singh

    2013-01-01

    Rapid increase in the emergence and spread of microbes resistant to conventionally used antibiotics has become a major threat to global health care. Antimicrobial peptides (AMPs) are considered as a potential source of novel antibiotics because of their numerous advantages such as broad-spectrum activity, lower tendency to induce resistance, immunomodulatory response and unique mode of action. However, AMPs have several drawbacks such as; susceptibility to protease degradation, toxicity and high costs of manufacturing. Therefore, extensive research efforts are underway to explore the therapeutic potential of these fascinating natural compounds. This review highlights the potential of small cationic antimicrobial peptidomimetics (SCAMPs; M.W. ≅ 700 Da) as new generation antibiotics. In particular, we focused on recently identified small active pharmacophore from bulky templates of native AMPs, β-peptides, and lipopeptides. In addition, various design strategies recently undertaken to improve the physicochemical properties (proteolytic stability & plasma protein binding) of small cationic peptides have also been discussed.

  18. Crystallization and preliminary X-ray characterization of Epstein–Barr virus BHRF1 in complex with a benzoylurea peptidomimetic

    International Nuclear Information System (INIS)

    Caria, Sofia; Chugh, Srishti; Nhu, Duong; Lessene, Guillaume; Kvansakul, Marc

    2012-01-01

    The expression and purification of Epstein–Barr virus BHRF1 as well as its co-crystallization with a peptidomimetic are described. BHRF1 is a pro-survival Bcl-2 homologue encoded by Epstein–Barr virus (EBV) that plays a key role in preventing premature host cell death during viral infection and may contribute to the development of malignancies associated with chronic EBV infections. The anti-apoptotic action of BHRF1 is based on its ability to sequester pro-apoptotic Bcl-2 family proteins, in particular Bim and Bak. These interactions have been previously studied in three dimensions by determining crystal structures of BHRF1 in complex with both Bim and Bak BH3 domains. Screening of a library of peptidomimetic compounds based on the benzoylurea scaffold that mimics critical Bim BH3 domain side chains against BHRF1 led to the identification of an inhibitor of BHRF1 that displays micromolar affinity. Single crystals were obtained from the co-crystallization of recombinant BHRF1 protein with this peptidomimetic compound. The crystals belonged to the orthorhombic space group P2 1 2 1 2 1 , with unit-cell parameters a = 66.8, b = 91.1, c = 151.9 Å. Diffraction data were collected to 2.11 Å resolution on the MX2 beamline at the Australian Synchrotron

  19. Water-structuring technology with the molecular chaperone proteins: indicated application of the α-crystallin domains and imidazole-containing peptidomimetics in cosmetic skin care systems or dermatological therapeutic drug carrier formulations.

    Science.gov (United States)

    Babizhayev, Mark A; Nikolayev, Gennady M; Nikolayeva, Juliana G; Yegorov, Yegor E

    2011-01-01

    Changes in structural proteins and hydration during aging are responsible for altered skin morphologic and mechanical properties manifested as wrinkling, sagging, loss of elasticity, and apparent dryness. Impairment in protein hydration may add to the ultrastructural, mechanical, and biochemical changes in structural proteins in the aged skin. At Innovative Vision Products, Inc., we have pioneered a molecular chaperone protein-activated therapeutic or cosmetic platform to enable simultaneous analysis of water-binding and structuring characteristics for biology-related or skin aging and skin disease-related pathways. This cutting-edge technology has changed the hydration of proteins in photoaged skin which so that they are more compact and interact with water to limited degree. The mechanisms of skin diseases, aging, and cellular and signaling pathways mediated by targeting with molecular chaperone protein(s) are considered. Skin lesions that are growing, spreading, or pigmented, and those that occur on exposed areas of skin are likely to be treated by these emerging pharmacological chaperones that could have cosmetic or dermatological benefits. Examples of such chaperones are anti-/trans-glycation-imidazole-containing peptidomimetic(s) (natural L-carnosine derivatives and mimetics) combined with the molecular chaperone protein α-crystallin derived from a natural source, brine shrimp (Artemia franciscana) cysts, or with recombinant human αA-crystallin. This patented biotechnology represents an efficient tool with which to mitigate the consequences of free radical-induced skin damage. The article is organized to provide in one place all of the relevant technical information, such as high-performance nuclear magnetic resonance and electron spin resonance application tools, and to describe the entire process from sample preparation to data analysis, which is moving from biological studies to biotechnology batches of the product. The proposed biotechnology results in

  20. A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys.

    Science.gov (United States)

    Barnhart, Kirstin F; Christianson, Dawn R; Hanley, Patrick W; Driessen, Wouter H P; Bernacky, Bruce J; Baze, Wallace B; Wen, Sijin; Tian, Mei; Ma, Jingfei; Kolonin, Mikhail G; Saha, Pradip K; Do, Kim-Anh; Hulvat, James F; Gelovani, Juri G; Chan, Lawrence; Arap, Wadih; Pasqualini, Renata

    2011-11-09

    Obesity, defined as body mass index greater than 30, is a leading cause of morbidity and mortality and a financial burden worldwide. Despite significant efforts in the past decade, very few drugs have been successfully developed for the treatment of obese patients. Biological differences between rodents and primates are a major hurdle for translation of anti-obesity strategies either discovered or developed in rodents into effective human therapeutics. Here, we evaluate the ligand-directed peptidomimetic CKGGRAKDC-GG-(D)(KLAKLAK)(2) (henceforth termed adipotide) in obese Old World monkeys. Treatment with adipotide induced targeted apoptosis within blood vessels of white adipose tissue and resulted in rapid weight loss and improved insulin resistance in obese monkeys. Magnetic resonance imaging and dual-energy x-ray absorptiometry confirmed a marked reduction in white adipose tissue. At experimentally determined optimal doses, monkeys from three different species displayed predictable and reversible changes in renal proximal tubule function. Together, these data in primates establish adipotide as a prototype in a new class of candidate drugs that may be useful for treating obesity in humans.

  1. The peptidomimetic Lau-(Lys-βNSpe)6-NH2 antagonizes formyl peptide receptor 2 expressed in mouse neutrophils

    DEFF Research Database (Denmark)

    Skovbakke, Sarah Line; Winther, Malene; Gabl, Michael

    2016-01-01

    /differences between the human and murine FPR family members is required. Compared to FPR1 and FPR2 expressed by human neutrophils, very little is known about agonist/antagonist recognition patterns for their murine orthologues, but now we have identified two potent and selective formylated peptide agonists (f...... to be devoid of effect on their murine orthologues as determined by their inability to inhibit superoxide release from murine neutrophils upon stimulation with receptor-specific agonists. The Boc-FLFLF peptide was found to be a selective antagonist for Fpr1, whereas the lipidated peptidomimetic Lau...

  2. Structure and conformational behaviour of peptoid peptidomimetics . Towards an understanding of the mechanism of action of substance P and NK1 antagonists

    NARCIS (Netherlands)

    Boks, Gerrit Jan

    1997-01-01

    Developing peptoid peptidomimetics is part of a strategy to come to a more rational development of ligands for therapeutically interesting macromolecular targets for which peptide-protein or protein-protein interactions play a role. While maintaining the functionalities and relative side-chain

  3. Structure-activity studies of peptidomimetics based on kinase-inhibitory region of suppressors of cytokine signaling 1.

    Science.gov (United States)

    La Manna, Sara; Lopez-Sanz, Laura; Leone, Marilisa; Brandi, Paola; Scognamiglio, Pasqualina Liana; Morelli, Giancarlo; Novellino, Ettore; Gomez-Guerrero, Carmen; Marasco, Daniela

    2017-11-20

    Suppressors of Cytokine Signaling (SOCS) proteins are negative regulators of JAK proteins that are receptor-associated tyrosine kinases, which play key roles in the phosphorylation and subsequent activation of several transcription factors named STATs. Unlike the other SOCS proteins, SOCS1 and 3 show, in the N-terminal portion, a small kinase inhibitory region (KIR) involved in the inhibition of JAK kinases. Drug discovery processes of compounds based on KIR sequence demonstrated promising in functional in vitro and in inflammatory animal models and we recently developed a peptidomimetic called PS5, as lead compound. Here, we investigated the cellular ability of PS5 to mimic SOCS1 biological functions in vascular smooth muscle cells and simultaneously we set up a new binding assay for the screening and identification of JAK2 binders based on a SPR experiment that revealed more robust with respect to previous ELISAs. On this basis, we designed several peptidomimetics bearing new structural constraints that were analyzed in both affinities toward JAK2 and conformational features through Circular Dichroism and NMR spectroscopies. Introduced chemical modifications provided an enhancement of serum stabilities of new sequences that could aid the design of future mimetic molecules of SOCS1 as novel anti-inflammatory compounds. © 2017 Wiley Periodicals, Inc.

  4. Efficacy of a synthetic antimicrobial peptidomimetic versus vancomycin in a Staphylococcus epidermidis device-related murine peritonitis model

    DEFF Research Database (Denmark)

    Cavanagh, Jorunn Pauline; Granslo, Hildegunn Norbakken; Fredheim, Elizabeth Aarag

    2013-01-01

    Objectives Biofilm-forming Staphylococcus epidermidis is a prevalent cause of peritonitis during peritoneal dialysis. We compared the efficacy of a synthetic antimicrobial peptidomimetic (Ltx21) versus vancomycin in a murine model mimicking a device-related peritonitis. Methods Silicone implants......, pre-colonized with an S. epidermidis biofilm, were inserted into the peritoneal cavity of BALB/c mice. Three groups (36 mice in each) with pre-colonized implants received intraperitoneal treatment with Ltx21, vancomycin or placebo. Mice were euthanized on day 3 (n = 12), day 6 (n = 12) or day 8 (n...... = 12) post-implantation. Controls were mice with sterile implants (n = 18) and mice without surgery (n = 6). Bacterial reductions in cfu were analysed from implants and peritoneal fluid (PF). Inflammatory responses in serum and PF were measured. Results Vancomycin resulted in a stronger reduction...

  5. Peptidomimetics with beta-peptoid resudies as carriers for intracellular delivery of small interfering RNA (siRNA)

    DEFF Research Database (Denmark)

    Foged, Camilla

    cytometry. We conclude that simple complex formation via electrostatic interactions between siRNA and the cationic peptidomimetics is not sufficient for the delivery of siRNA to the RNA interference (RNAi) pathway in the cytoplasm. We are currently testing chemical conjugates of si...... prepared by mixing and characterized with respect to size and surface charge. At ratios of peptide nitrogen to siRNA phosphate (N/P) of 1 and below, particles with narrow size distributions (poly dispersity indexes lower than 0.11) ranging from approximately 100 to 350 nm were formed, and they showed...... a negative zeta potential (-24 to -31 mV). At higher N/P ratios, larger aggregates with zeta potential close to neutral were formed. However, the complexes were not able to silence the expression of enhanced green fluorescent protein (EGFP) in HeLa-cells stably expressing EGFP, which was measured by flow...

  6. Structure-based drug design of novel peptidomimetic cellulose derivatives as HCV-NS3 protease inhibitors.

    Science.gov (United States)

    Saleh, Noha A; Elshemey, Wael M

    2017-10-15

    Hepatitis C Virus (HCV) represents a global health threat not only due to the large number of reported worldwide HCV infections, but also due to the absence of a reliable vaccine for its prevention. HCV NS3 protease is one of the most important targets for drug design aiming at the deactivation of HCV. In the present work, molecular docking simulations are carried out for suggested novel NS3 protease inhibitors applied to the Egyptian genotype 4. These inhibitors are modifications of dimer cellulose by adding a hexa-peptide to the cellulose at one of the positions 2, 3, 6, 2', 3' or 6'. Results show that the inhibitor compound with the hexa-peptide at position 6 shows significantly higher simulation docking score with HCV NS3 protease active site. This is supported by low total energy value of docking system, formation of two H-bonds with HCV NS3 protease active site residues, high binding affinity and increased stability in the interaction system. Copyright © 2017 Elsevier Inc. All rights reserved.

  7. Asymmetric Ugi 3CR on isatin-derived ketimine: synthesis of chiral 3,3-disubstituted 3-aminooxindole derivatives

    Directory of Open Access Journals (Sweden)

    Giordano Lesma

    2014-06-01

    Full Text Available An efficient Ugi three-component reaction of a preformed chiral ketimine derived from isatin with various isonitrile and acid components has been developed. The reactions proceeded smoothly and in a stereocontrolled manner with regard to the new center of the Ugi products due to the stereoinduction of the amine chiral residue. A wide variety of novel chiral 3,3-disubstituted 3-aminooxindoles were obtained, a selection of which were subjected to post-Ugi transformations, paving the way to application as peptidomimetics.

  8. Peptidomimetic hydroxamate metalloproteinase inhibitors abrogate local and systemic toxicity induced by Echis ocellatus (saw-scaled) snake venom.

    Science.gov (United States)

    Arias, Ana Silvia; Rucavado, Alexandra; Gutiérrez, José María

    2017-06-15

    The ability of two peptidomimetic hydroxamate metalloproteinase inhibitors, Batimastat and Marimastat, to abrogate toxic and proteinase activities of the venom of Echis ocellatus from Cameroon and Ghana was assessed. Since this venom largely relies for its toxicity on the action of zinc-dependent metalloproteinases (SVMPs), the hypothesis was raised that toxicity could be largely eliminated by using SVMP inhibitors. Both hydroxamate molecules inhibited local and pulmonary hemorrhagic, in vitro coagulant, defibrinogenating, and proteinase activities of the venoms in conditions in which venom and inhibitors were incubated prior to the test. In addition, the inhibitors prolonged the time of death of mice receiving 4 LD 50 s of venom by the intravenous route. Lower values of IC 50 were observed for in vitro and local hemorrhagic activities than for systemic effects. When experiments were performed in conditions that simulated the actual circumstances of snakebite, i.e. by administering the inhibitor after envenoming, Batimastat completely abrogated local hemorrhage if injected immediately after venom. Moreover, it was also effective at inhibiting lethality and defibrinogenation when venom and inhibitor were injected by the intraperitoneal route. Results suggest that these, and possibly other, metalloproteinase inhibitors may become an effective adjunct therapy in envenomings by E. ocellatus when administered at the anatomic site of venom injection rapidly after the bite. Copyright © 2017 Elsevier Ltd. All rights reserved.

  9. Light Activation of a Cysteine Protease Inhibitor: Caging of a Peptidomimetic Nitrile with RuII(bpy)2

    Science.gov (United States)

    Respondek, Tomasz; Garner, Robert N.; Herroon, Mackenzie K.; Podgorski, Izabela; Turro, Claudia; Kodanko, Jeremy J.

    2013-01-01

    A novel method for caging protease inhibitors is described. The complex [RuII(bpy)2(1)2](PF6)2 (2) was prepared from the nitrile-based peptidomimetic inhibitor Ac-Phe-NHCH2CN (1). 1H NMR, UV-vis and IR spectroscopic and mass spectrometric data confirm that two equiv of inhibitor 1 bind to RuII through the nitrile functional group. Complex 2 shows excellent stability in aqueous solution in the dark and fast release of 1 upon irradiation with visible light. Due to binding to the RuII center, the nitriles of complex 2 are caged, and 2 does not act as a potent enzyme inhibitor. However, when 2 is irradiated, it releases 1 that inhibits the cysteine proteases papain and cathepsins B, K and L, up to two times more potently than 1 alone. Ratios for IC50 values for 2 range from 6:1 to 33:1 under dark vs. light conditions, against isolated enzymes and in human cell lysates, confirming a high level of photoinduced enzyme inhibition is obtained with this method. PMID:21973207

  10. Evaluation of efficacy, pharmacokinetics and tolerability of peptidomimetic aspartic proteinase inhibitors as cream formulation in experimental vaginal candidiasis.

    Science.gov (United States)

    De Bernardis, Flavia; Arancia, Silvia; Tringali, Giuseppe; Greco, Maria Cristina; Ragazzoni, Enzo; Calugi, Chiara; Trabocchi, Andrea; Sandini, Silvia; Graziani, Sofia; Cauda, Roberto; Cassone, Antonio; Guarna, Antonio; Navarra, Pierluigi

    2014-08-01

    It has been previously shown that the treatment with the two protease inhibitors APG12 and APG19 confers protection in a rat model of mucosal candidiasis; in this study, we examined whether these peptidomimetic inhibitors are also effective as a cream formulation in reducing Candida albicans vaginal infection. These efficacy studies were performed in a rat model of estrogen-dependent rat vaginitis by C. albicans on both azole-susceptible and azole-resistant C. albicans, and on both caspofungin-susceptible and caspofungin-resistant C. albicans strains. In vivo studies were also conducted in female albino rats and rabbits to obtain information about the safety, local tolerability and principal pharmacokinetics parameters of the two compounds. Both hit compounds showed remarkable results within the 48-h range as effective inhibitors of the infection, particularly causing rapid decay of vaginal C. albicans burden. Importantly, the two compounds showed marked acceleration of fungus clearance in the rats challenged with the fluconazole-resistant as well as with the capsofungin-resistant strain of C. albicans. Both compounds showed fast elimination rates when given by the intravenous route, and poor systemic absorption after intravaginal cream administration. Test drugs were also well tolerated in 7-day local tolerability experiments in the rabbit. © 2014 Royal Pharmaceutical Society.

  11. Crystal and NMR Structures of a Peptidomimetic β-Turn That Provides Facile Synthesis of 13-Membered Cyclic Tetrapeptides.

    Science.gov (United States)

    Cameron, Alan J; Squire, Christopher J; Edwards, Patrick J B; Harjes, Elena; Sarojini, Vijayalekshmi

    2017-12-14

    Herein we report the unique conformations adopted by linear and cyclic tetrapeptides (CTPs) containing 2-aminobenzoic acid (2-Abz) in solution and as single crystals. The crystal structure of the linear tetrapeptide H 2 N-d-Leu-d-Phe-2-Abz-d-Ala-COOH (1) reveals a novel planar peptidomimetic β-turn stabilized by three hydrogen bonds and is in agreement with its NMR structure in solution. While CTPs are often synthetically inaccessible or cyclize in poor yield, both 1 and its N-Me-d-Phe analogue (2) adopt pseudo-cyclic frameworks enabling near quantitative conversion to the corresponding CTPs 3 and 4. The crystal structure of the N-methylated peptide (4) is the first reported for a CTP containing 2-Abz and reveals a distinctly planar 13-membered ring, which is also evident in solution. The N-methylation of d-Phe results in a peptide bond inversion compared to the conformation of 3 in solution. © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

  12. Surface coating of siRNA-peptidomimetic nano-self-assemblies with anionic lipid bilayers: enhanced gene silencing and reduced adverse effects in vitro

    Science.gov (United States)

    Zeng, Xianghui; de Groot, Anne Marit; Sijts, Alice J. A. M.; Broere, Femke; Oude Blenke, Erik; Colombo, Stefano; van Eden, Willem; Franzyk, Henrik; Nielsen, Hanne Mørck; Foged, Camilla

    2015-11-01

    Cationic vectors have demonstrated the potential to facilitate intracellular delivery of therapeutic oligonucleotides. However, enhanced transfection efficiency is usually associated with adverse effects, which also proves to be a challenge for vectors based on cationic peptides. In this study a series of proteolytically stable palmitoylated α-peptide/β-peptoid peptidomimetics with a systematically varied number of repeating lysine and homoarginine residues was shown to self-assemble with small interfering RNA (siRNA). The resulting well-defined nanocomplexes were coated with anionic lipids giving rise to net anionic liposomes. These complexes and the corresponding liposomes were optimized towards efficient gene silencing and low adverse effects. The optimal anionic liposomes mediated a high silencing effect, which was comparable to that of the control (cationic Lipofectamine 2000), and did not display any noticeable cytotoxicity and immunogenicity in vitro. In contrast, the corresponding nanocomplexes mediated a reduced silencing effect with a more narrow safety window. The surface coating with anionic lipid bilayers led to partial decomplexation of the siRNA-peptidomimetic nanocomplex core of the liposomes, which facilitated siRNA release. Additionally, the optimal anionic liposomes showed efficient intracellular uptake and endosomal escape. Therefore, these findings suggest that a more efficacious and safe formulation can be achieved by surface coating of the siRNA-peptidomimetic nano-self-assemblies with anionic lipid bilayers.Cationic vectors have demonstrated the potential to facilitate intracellular delivery of therapeutic oligonucleotides. However, enhanced transfection efficiency is usually associated with adverse effects, which also proves to be a challenge for vectors based on cationic peptides. In this study a series of proteolytically stable palmitoylated α-peptide/β-peptoid peptidomimetics with a systematically varied number of repeating lysine

  13. Biological activities of the natural imidazole-containing peptidomimetics n-acetylcarnosine, carcinine and L-carnosine in ophthalmic and skin care products.

    Science.gov (United States)

    Babizhayev, Mark A

    2006-04-11

    Apart from genetically programmed cell aging, different external aggressors related to oxidative stress and lipid peroxidation (LPO) can accelerate the skin aging phenomenon. Oxidative stress associated with the formation of lipid peroxides is suggested to contribute to pathological processes in aging and systemic diseases known as the risk factors for cataract. Despite the fact that L-carnosine-related peptidomimetics N-acetylcarnosine (N-acetyl-beta-alanyl-L-histidine) (NAC) and carcinine (beta-alanylhistamine) are metabolically related to L-carnosine and have been demonstrated to occur in tissues of many vertebrates, including humans, these compounds were shown resistant toward enzymatic hydrolysis. A series of related biocompatible imidazole-containing peptidomimetics were synthesized in order to confer resistance to enzymatic hydrolysis and ex vivo improvement of protective antioxidative properties related to L-carnosine. The included findings revealed a greater role of N-acetylcarnosine (NAC) and carcinine ex vivo in the prolongation and potentiation of physiological responses to the therapeutical and cosmetics treatments with L-carnosine as antioxidant. 3-D molecular conformation studies proposed the antioxidant activity of peptidomimetics (carcinine, L-prolylhistamine, N-acetylcarnosine, L-carnosine) for metal ion binding, quenching of a number free radicals, and binding of hydroperoxide or aldehyde (including dialdehyde LPO products) in an imidazole-peroxide adducts. NAC can act as a time release (carrier) stable version of L-carnosine during application in ophthalmic pharmaceutical and cosmetics formulations which include lubricants. Carcinine, L-prolylhistamine show efficient deactivation of lipid hydroperoxides monitored by HPLC and protection of membrane phospholipids and water soluble proteins from the lipid peroxides-induced damages. This activity is superior over the lipophilic antioxidant vitamin E. The biologically significant applications of

  14. Design, synthesis and crystallographic analysis of nitrile-based broad-spectrum peptidomimetic inhibitors for coronavirus 3C-like proteases.

    Science.gov (United States)

    Chuck, Chi-Pang; Chen, Chao; Ke, Zhihai; Wan, David Chi-Cheong; Chow, Hak-Fun; Wong, Kam-Bo

    2013-01-01

    Coronaviral infection is associated with up to 5% of respiratory tract diseases. The 3C-like protease (3CL(pro)) of coronaviruses is required for proteolytic processing of polyproteins and viral replication, and is a promising target for the development of drugs against coronaviral infection. We designed and synthesized four nitrile-based peptidomimetic inhibitors with different N-terminal protective groups and different peptide length, and examined their inhibitory effect on the in-vitro enzymatic activity of 3CL(pro) of severe-acute-respiratory-syndrome-coronavirus. The IC(50) values of the inhibitors were in the range of 4.6-49 μM, demonstrating that the nitrile warhead can effectively inactivate the 3CL(pro) autocleavage process. The best inhibitor, Cbz-AVLQ-CN with an N-terminal carbobenzyloxy group, was ~10x more potent than the other inhibitors tested. Crystal structures of the enzyme-inhibitor complexes showed that the nitrile warhead inhibits 3CL(pro) by forming a covalent bond with the catalytic Cys145 residue, while the AVLQ peptide forms a number of favourable interactions with the S1-S4 substrate-binding pockets. We have further showed that the peptidomimetic inhibitor, Cbz-AVLQ-CN, has broad-spectrum inhibition against 3CL(pro) from human coronavirus strains 229E, NL63, OC43, HKU1, and infectious bronchitis virus, with IC(50) values ranging from 1.3 to 3.7 μM, but no detectable inhibition against caspase-3. In summary, we have shown that the nitrile-based peptidomimetic inhibitors are effective against 3CL(pro), and they inhibit 3CL(pro) from a broad range of coronaviruses. Our results provide further insights into the future design of drugs that could serve as a first line defence against coronaviral infection. Copyright © 2012 Elsevier Masson SAS. All rights reserved.

  15. Improved in vitro evaluation of novel antimicrobials: potential synergy between human plasma and antibacterial peptidomimetics, AMPs and antibiotics against human pathogenic bacteria

    DEFF Research Database (Denmark)

    Citterio, Linda; Franzyk, Henrik; Palarasah, Yaseelan

    2016-01-01

    was affected by conditions mimicking in vivo settings. Their activity was enhanced to an unexpected degree in the presence of human blood plasma for thirteen pathogenic Gram-positive and Gram-negative bacteria. MIC values typically decreased 2- to 16-fold in the presence of a human plasma concentration...... that alone did not damage the cell membrane. Hence, MIC and MBC data collected in these settings appear to represent a more appropriate basis for in vivo experiments preceding clinical trials. In fact, concentrations of peptidomimetics and peptide antibiotics (e.g. polymyxin B) required for in vivo...

  16. Solid-Phase Synthesis of Smac Peptidomimetics Incorporating Triazoloprolines and Biarylalanines

    DEFF Research Database (Denmark)

    Le Quement, Sebastian T.; Ishoey, Mette; Petersen, Mette T.

    2011-01-01

    by deactivating proteolytic caspases. The Smac protein has an antagonistic effect on IAPs, thus providing structural clues for the synthesis of new pro-apoptotic compounds. Herein, we report a solid-phase approach for the synthesis of Smac-derived tetrapeptide libraries. On the basis of a common (N......-Me)AVPF sequence, peptides incorporating triazoloprolines and biarylalanines were synthesized by means of Cu(I)-catalyzed azide–alkyne cycloaddition and Pd-catalyzed Suzuki cross-coupling reactions. Solid-phase procedures were optimized to high efficiency, thus accessing all products in excellent crude purities...... and yields (both typically above 90%). The peptides were subjected to biological evaluation in a live/dead cellular assay which revealed that structural decorations on the AVPF sequence indeed are highly important for cytotoxicity toward HeLa cells....

  17. MicroPET/CT imaging of {alpha}{sub v}{beta}{sub 3} integrin via a novel {sup 68}Ga-NOTA-RGD peptidomimetic conjugate in rat myocardial infarction

    Energy Technology Data Exchange (ETDEWEB)

    Menichetti, Luca; Kusmic, Claudia; Panetta, Daniele; Petroni, Debora; Salvadori, Piero A. [CNR-Institute of Clinical Physiology (IFC), Pisa (Italy); Arosio, Daniela; Manzoni, Leonardo [CNR-Institute of Molecular Science and Technologies (ISTM), Milan (Italy); Matteucci, Marco [Scuola Superiore Sant' Anna, Pisa (Italy); Casagrande, Cesare [University of Milan, Department of Chemistry, Milan (Italy); L' Abbate, Antonio [CNR-Institute of Clinical Physiology (IFC), Pisa (Italy); Scuola Superiore Sant' Anna, Pisa (Italy)

    2013-08-15

    The {alpha}{sub v}{beta}{sub 3} integrin is expressed in angiogenic vessels and is a potential target for molecular imaging of evolving pathological processes. Its expression is upregulated in cancer lesions and metastases as well as in acute myocardial infarction (MI) as part of the infarct healing process. The purpose of our study was to determine the feasibility of a new imaging approach with a novel {sup 68}Ga-2,2',2''-(1,4,7-triazonane-1,4,7-triyl)triacetic acid (NOTA)-arginine-glycine-aspartic acid (RGD) construct to assess integrin expression in the evolving MI. A straightforward labelling chemistry to attach the radionuclide {sup 68}Ga to a NOTA-based chelating agent conjugated with a cyclic RGD peptidomimetic is described. Affinity for {alpha}{sub v}{beta}{sub 3} integrin was assessed by in vitro receptor binding assay. The proof-of-concept in vivo studies combined the {sup 68}Ga-NOTA-RGD with the flow tracer {sup 13}N-NH{sub 3} imaging in order to obtain positron emission tomography (PET)/CT imaging of both integrin expression and perfusion defect at 4 weeks after infarction. Hearts were then processed for immunostaining of integrin {beta}{sub 3}. NOTA-RGD conjugate displayed a binding affinity for {alpha}{sub v}{beta}{sub 3} integrin of 27.9 {+-} 6.8 nM. {sup 68}Ga-NOTA-RGD showed stability without detectable degradation or formation of by-products in urine up to 2 h following injection in the rat. MI hearts exhibited {sup 68}Ga-NOTA-RGD uptake in correspondence to infarcted and border zone regions. The tracer signal drew a parallel with vascular remodelling due to ischaemia-induced angiogenesis as assessed by immunohistochemistry. As compared to similar imaging approaches using the {sup 18}F-galacto-derivative, we documented for the first time with microPET/CT imaging the {sup 68}Ga-NOTA-RGD derivative that appears eligible for PET imaging in animal models of vascular remodelling during evolving MI. The simple chemistry employed to

  18. Tc-labeling of Peptidomimetic Antagonist to Selectively Target alpha(v)beta(3) Receptor-Positive Tumor: Comparison of PDA and EDDA as co-Ligands.

    Science.gov (United States)

    Shin, In Soo; Maeng, Jin Soo; Jang, Beom-Su; You, Eric; Cheng, Kenneth; Li, King C P; Wood, Bradford; Carrasquillo, Jorge A; Danthi, S Narasimhan; Paik, Chang H

    2010-01-01

    OBJECTIVES: The aim of this research was to synthesize radiolabeled peptidomimetic integrin alpha(v)beta(3) antagonist with (99m)Tc for rapid targeting of integrin alpha(v)beta(3) receptors in tumor to produce a high tumor to background ratio. METHODS: The amino terminus of 4-[2-(3,4,5,6-tetra-hydropyrimidin-2-ylamino)-ethyloxy]benzoyl-2-(S)-[N-(3-amino-neopenta-1-carbamyl)]-aminoethylsulfonyl-amino-beta-alanine hydrochloride (IAC) was conjugated with N-hydroxysuccinimide ester of HYNIC and labeled with (99m)Tc using tricine with either 1,5-pyridinedicarboxylic acid (PDA) or ethylenediamine-N,N'-diacetic acid (EDDA) as the co-ligand. The products, (99m)Tc EDDA(2)/HYNIC-IAC (P1) and (99m)Tc PDA (tricin)/HYNIC-IAC (P2) were subjected to in vitro serum stability, receptor-binding, biodistribution and imaging studies. RESULTS: P1 and P2 were synthesized with an overall yield of >80%. P1 was slightly more stable than P2 when incubated in serum at 37 degrees C for 18 hrs (84 vs 77% intact). The In vitro receptor-binding of P1 was higher than that of P2 (78.02 +/- 13.48 vs 51.05 +/- 14.05%) when incubated with alpha(v)beta(3) at a molar excess (0.8 muM). This receptor binding was completely blocked by a molar excess of an unlabeled peptidomimetic antagonist. Their differences shown in serum stability and the receptor-binding appeared to be related to their biological behaviors in tumor uptake and retention; the 1 h tumor uptakes of P1 and P2 were 3.17+/-0.52 and 2.13+/-0.17 % ID/g, respectively. P1 was retained in the tumor longer than P2. P1 was excreted primarily through the renal system whereas P2 complex was excreted equally via both renal and hepatobiliary systems. Thus, P1 was retained in the whole-body with 27.25 +/- 3.67% ID at 4 h whereas 54.04 +/- 3.57% ID of P2 remained in the whole-body at 4 h. This higher whole-body retention of P2 appeared to be resulted from a higher amount of radioactivity retained in liver and intestine. These findings were supported by

  19. The Proteolytically Stable Peptidomimetic Pam-(Lys-ßNSpe)6-NH2 Selectively Inhibits Human Neutrophil Activation via Formyl Peptide Receptor 2

    DEFF Research Database (Denmark)

    Skovbakke, Sarah Line; Heegaard, Peter M. H.; Larsen, Camilla J.

    2015-01-01

    of proteolytically stable HDP mimics consisting of lipidated α-peptide/β-peptoid oligomers was investigated for their effect on neutrophil function. The most promising compound, Pam-(Lys-βNSpe)6-NH2, was shown to inhibit formyl peptide receptor 2 (FPR2) agonist-induced neutrophil granule mobilization and release...... of reactive oxygen species. The potency of Pam-(Lys-βNSpe)6-NH2 was comparable to that of PBP10, the most potent FPR2-selective inhibitor known. The immunomodulatory effects of structural analogues of Pam-(Lys-βNSpe)6-NH2 emphasized the importance of both the lipid and peptidomimetic parts. By using imaging...... flow cytometry in primary neutrophils and FPR-transfected cell lines we found that a fluorescently labelled analogue of Pam-(Lys-βNSpe)6-NH2 interacted selectively with FPR2. Furthermore the interaction between Pam-(Lys-βNSpe)6-NH2 and FPR2 was found to prevent binding of the FPR2-specific activating...

  20. The proteolytically stable peptidomimetic Pam-(Lys-βNSpe)6-NH2 selectively inhibits human neutrophil activation via formyl peptide receptor 2.

    Science.gov (United States)

    Skovbakke, Sarah Line; Heegaard, Peter M H; Larsen, Camilla J; Franzyk, Henrik; Forsman, Huamei; Dahlgren, Claes

    2015-01-15

    Immunomodulatory host defense peptides (HDPs) are considered to be lead compounds for novel anti-sepsis and anti-inflammatory agents. However, development of drugs based on HDPs has been hampered by problems with toxicity and low bioavailability due to in vivo proteolysis. Here, a subclass of proteolytically stable HDP mimics consisting of lipidated α-peptide/β-peptoid oligomers was investigated for their effect on neutrophil function. The most promising compound, Pam-(Lys-βNSpe)6-NH2, was shown to inhibit formyl peptide receptor 2 (FPR2) agonist-induced neutrophil granule mobilization and release of reactive oxygen species. The potency of Pam-(Lys-βNSpe)6-NH2 was comparable to that of PBP10, the most potent FPR2-selective inhibitor known. The immunomodulatory effects of structural analogs of Pam-(Lys-βNSpe)6-NH2 emphasized the importance of both the lipid and peptidomimetic parts. By using imaging flow cytometry in primary neutrophils and FPR-transfected cell lines, we found that a fluorescently labeled analog of Pam-(Lys-βNSpe)6-NH2 interacted selectively with FPR2. Furthermore, the interaction between Pam-(Lys-βNSpe)6-NH2 and FPR2 was found to prevent binding of the FPR2-specific activating peptide agonist Cy5-WKYMWM, while the binding of an FPR1-selective agonist was not inhibited. To our knowledge, Pam-(Lys-βNSpe)6-NH2 is the first HDP mimic found to inhibit activation of human neutrophils via direct interaction with FPR2. Hence, we consider Pam-(Lys-βNSpe)6-NH2 to be a convenient tool in the further dissection of the role of FPR2 in inflammation and homeostasis as well as for investigation of the importance of neutrophil stimulation in anti-infective therapy involving HDPs. Copyright © 2014 Elsevier Inc. All rights reserved.

  1. Rationally Designed Peptides and Peptidomimetics as Inhibitors of Amyloid-β (Aβ) Aggregation: Potential Therapeutics of Alzheimer's Disease.

    Science.gov (United States)

    Goyal, Deepti; Shuaib, Suniba; Mann, Sukhmani; Goyal, Bhupesh

    2017-02-13

    Alzheimer's disease (AD) is a progressive neurodegenerative disease with no clinically accepted treatment to cure or halt its progression. The worldwide effort to develop peptide-based inhibitors of amyloid-β (Aβ) aggregation can be considered an unplanned combinatorial experiment. An understanding of what has been done and achieved may advance our understanding of AD pathology and the discovery of effective therapeutic agents. We review here the history of such peptide-based inhibitors, including those based on the Aβ sequence and those not derived from that sequence, containing both natural and unnatural amino acid building blocks. Peptide-based aggregation inhibitors hold significant promise for future AD therapy owing to their high selectivity, effectiveness, low toxicity, good tolerance, low accumulation in tissues, high chemical and biological diversity, possibility of rational design, and highly developed methods for analyzing their mode of action, proteolytic stability (modified peptides), and blood-brain barrier (BBB) permeability.

  2. Comparison of two cross-bridged macrocyclic chelators for the evaluation of 64Cu-labeled-LLP2A, a peptidomimetic ligand targeting VLA-4-positive tumors

    International Nuclear Information System (INIS)

    Jiang, Majiong; Ferdani, Riccardo; Shokeen, Monica; Anderson, Carolyn J.

    2013-01-01

    Integrin α 4 β 1 (also called very late antigen-4 or VLA-4) plays an important role in tumor growth, angiogenesis and metastasis, and there has been increasing interest in targeting this receptor for cancer imaging and therapy. In this study, we conjugated a peptidomimetic ligand known to have good binding affinity for α 4 β 1 integrin to a cross-bridged macrocyclic chelator with a methane phosphonic acid pendant arm, CB-TE1A1P. CB-TE1A1P-LLP2A was labeled with 64 Cu under mild conditions in high specific activity, in contrast to conjugates based on the “gold standard” di-acid cross-bridged chelator, CB-TE2A, which require high temperatures for efficient radiolabeling. Saturation binding assays demonstrated that 64 Cu-CB-TE1A1P-LLP2A had comparable binding affinity (1.2 nM vs 1.6 nM) but more binding sites (B max = 471 fmol/mg) in B16F10 melanoma tumor cells than 64 Cu-CB-TE2A-LLP2A (B max = 304 fmol/mg, p 64 Cu-CB-TE1A1P-LLP2A had less renal retention but higher uptake in tumor (11.4 ± 2.3 %ID/g versus 3.1 ± 0.6 %ID/g, p 64 Cu-CB-TE2A-LLP2A. At 2 h post-injection, 64 Cu-CB-TE1A1P-LLP2A also had significantly higher tumor:blood and tumor:muscle ratios than 64 Cu-CB-TE2A-LLP2A (CB-TE1A1P = 19.5 ± 3.0 and 13.0 ± 1.4, respectively, CB-TE2A = 4.2 ± 1.4 and 5.5 ± 0.9, respectively, p 64 Cu-CB-TE1A1P-LLP2A is an excellent PET radiopharmaceutical for the imaging of α 4 β 1 positive tumors and also has potential for imaging other α 4 β 1 positive cells such as those of the pre-metastatic niche

  3. De novo design and synthesis of ultra-short peptidomimetic antibiotics having dual antimicrobial and anti-inflammatory activities.

    Science.gov (United States)

    Murugan, Ravichandran N; Jacob, Binu; Ahn, Mija; Hwang, Eunha; Sohn, Hoik; Park, Hyo-Nam; Lee, Eunjung; Seo, Ji-Hyung; Cheong, Chaejoon; Nam, Ky-Youb; Hyun, Jae-Kyung; Jeong, Ki-Woong; Kim, Yangmee; Shin, Song Yub; Bang, Jeong Kyu

    2013-01-01

    Much attention has been focused on the design and synthesis of potent, cationic antimicrobial peptides (AMPs) that possess both antimicrobial and anti-inflammatory activities. However, their development into therapeutic agents has been limited mainly due to their large size (12 to 50 residues in length) and poor protease stability. In an attempt to overcome the issues described above, a set of ultra-short, His-derived antimicrobial peptides (HDAMPs) has been developed for the first time. Through systematic tuning of pendant hydrophobic alkyl tails at the N(π)- and N(τ)-positions on His, and the positive charge of Arg, much higher prokaryotic selectivity was achieved, compared to human AMP LL-37. Additionally, the most potent HDAMPs showed promising dual antimicrobial and anti-inflammatory activities, as well as anti-methicillin-resistant Staphylococcus aureus (MRSA) activity and proteolytic resistance. Our results from transmission electron microscopy, membrane depolarization, confocal laser-scanning microscopy, and calcein-dye leakage experiments propose that HDAMP-1 kills microbial cells via dissipation of the membrane potential by forming pore/ion channels on bacterial cell membranes. The combination of the ultra-short size, high-prokaryotic selectivity, potent anti-MRSA activity, anti-inflammatory activity, and proteolytic resistance of the designed HDAMP-1, -3, -5, and -6 makes these molecules promising candidates for future antimicrobial therapeutics.

  4. Data on human neutrophil activation induced by pepducins with amino acid sequences derived from β2AR and CXCR4

    Directory of Open Access Journals (Sweden)

    André Holdfeldt

    2016-09-01

    Full Text Available The data described here is related to the research article titled (Gabl et al., 2016 [1]. Pepducins with peptide sequence derived from one of the intracellular domains of a given G-protein coupled receptor (GPCR can either activate or inhibit cell functions. Here we include data on human neutrophil function induced by pepducins derived from β2AR (ICL3-8 and CXCR4 (ATI-2341, respectively. ICL3-8 exerts neither direct activating effect on the NADPH-oxidase as measured by superoxide release nor inhibitory effect on FPR signaling. ATI-2341 dose-dependently triggers neutrophil activation and these cells were subsequently desensitized in their response to FPR2 specific agonists F2Pal10 and WKYMVM. Moreover, the ATI-2341 response is inhibited by PBP10 and the peptidomimetic Pam-(Lys-betaNSpe6-NH2 (both are FPR2 specific inhibitors, but not to the FPR1 specific inhibitor cyclosporine H.

  5. Pharmacokinetics and biodistribution of a radioiodine labeled peptidomimetic ligand for high-affinity nerve growth factor receptors

    Energy Technology Data Exchange (ETDEWEB)

    Jung, K. H.; Kim, D. H.; Paik, J. Y.; Koh, B. H.; Bae, J. S.; Choe, Y. S.; Lee, K. H.; Kim, B. T. [Samsung Medical Center, Seoul (Korea, Republic of)

    2005-07-01

    Some of the obstacles for the clinical application of whole nerve growth factor (NGF) may be overcome by utilizing small molecule mimetics. We thus investigated the in vivo pharmacokinetics and biodistribution of a small cyclic peptide derived from NGF-[C(92-96)] with high receptor binding affinity. I-125 C(92-96) was labeled with the Bolton-Hunter method, and binding to TrkA/IgG chimeric protein was confirmed on a polyacrylamide gel after cross-linking. Pharmacokinetic analysis was performed in normal ICR mice intravenously injected with 0.5 MBq I-125 C(92-96) containing varying doses of C(92-96). Biodistribution studies were done at 6 h after injection. Cross-linkage analysis confirmed binding of I-125 C(92-96) to the high affinity NGF receptor, TrkA. Intravenously injected I-125 C(92-96) was cleared from the blood in a biexponential manner with an early T1/2{alpha} of 5.2 min and late T1/2{beta} of 121.3 min. Log blood-concentration decreased over time with a k-slope of 0.0025, clearance of 11.8{+-}0.5 ml/min, T1/2 of 4.1{+-}0.4 hr, and volume of distribution of 69.7{+-}4.6 ml. The pattern of elimination from the blood remained essentially unchanged regardless of the dose of added C(92-96), with dose-proportionate increases in AUCs and peak concentrations consistent with linear pharmacokinetics. Biodistribution studies demonstrated high kidney activity suggesting renal excretion of I-125 C(92-96). There were moderate levels of accumulation in the spleen, lungs and liver, followed by the myocardium and skeletal muscle, whereas brain uptake was low (< 0.2 %ID/gm). Intravenously administered C(92-96) follows linear pharmacokinetics, and is cleared from the circulation at a rate comparable to whole NGF despite its substantially smaller size. Although intravenous C(92-96) does not adequately reach brain tissue, clinically relevant doses can achieve major organ accumulation levels that may be sufficient to elicit biologic responses through NGF receptors.

  6. Pharmacokinetics and biodistribution of a radioiodine labeled peptidomimetic ligand for high-affinity nerve growth factor receptors

    International Nuclear Information System (INIS)

    Jung, K. H.; Kim, D. H.; Paik, J. Y.; Koh, B. H.; Bae, J. S.; Choe, Y. S.; Lee, K. H.; Kim, B. T.

    2005-01-01

    Some of the obstacles for the clinical application of whole nerve growth factor (NGF) may be overcome by utilizing small molecule mimetics. We thus investigated the in vivo pharmacokinetics and biodistribution of a small cyclic peptide derived from NGF-[C(92-96)] with high receptor binding affinity. I-125 C(92-96) was labeled with the Bolton-Hunter method, and binding to TrkA/IgG chimeric protein was confirmed on a polyacrylamide gel after cross-linking. Pharmacokinetic analysis was performed in normal ICR mice intravenously injected with 0.5 MBq I-125 C(92-96) containing varying doses of C(92-96). Biodistribution studies were done at 6 h after injection. Cross-linkage analysis confirmed binding of I-125 C(92-96) to the high affinity NGF receptor, TrkA. Intravenously injected I-125 C(92-96) was cleared from the blood in a biexponential manner with an early T1/2α of 5.2 min and late T1/2β of 121.3 min. Log blood-concentration decreased over time with a k-slope of 0.0025, clearance of 11.8±0.5 ml/min, T1/2 of 4.1±0.4 hr, and volume of distribution of 69.7±4.6 ml. The pattern of elimination from the blood remained essentially unchanged regardless of the dose of added C(92-96), with dose-proportionate increases in AUCs and peak concentrations consistent with linear pharmacokinetics. Biodistribution studies demonstrated high kidney activity suggesting renal excretion of I-125 C(92-96). There were moderate levels of accumulation in the spleen, lungs and liver, followed by the myocardium and skeletal muscle, whereas brain uptake was low (< 0.2 %ID/gm). Intravenously administered C(92-96) follows linear pharmacokinetics, and is cleared from the circulation at a rate comparable to whole NGF despite its substantially smaller size. Although intravenous C(92-96) does not adequately reach brain tissue, clinically relevant doses can achieve major organ accumulation levels that may be sufficient to elicit biologic responses through NGF receptors

  7. In vivo biokinetic and metabolic characterization of the {sup 68}Ga-labelled α5β1-selective peptidomimetic FR366

    Energy Technology Data Exchange (ETDEWEB)

    D' Alessandria, Calogero; Pohle, Karolin; Schwaiger, Markus [Technische Universitaet Muenchen, Nuklearmedizinische Klinik und Poliklinik, Klinikum rechts der Isar, Muenchen (Germany); Rechenmacher, Florian; Neubauer, Stefanie; Kessler, Horst [Technische Universitaet Muenchen, Institute for Advanced Study (IAS) and Center of Integrated Protein Science (CIPSM), Department Chemie, Garching (Germany); Notni, Johannes; Wester, Hans-Juergen [Technische Universitaet Muenchen, Lehrstuhl fuer Pharmazeutische Radiochemie, Garching (Germany); Beer, Ambros J. [Technische Universitaet Muenchen, Nuklearmedizinische Klinik und Poliklinik, Klinikum rechts der Isar, Muenchen (Germany); Ulm University, Department of Nuclear Medicine, Ulm (Germany)

    2016-05-15

    Integrins are transmembrane receptors responsible for cell-cell adhesion and cell-extracellular matrix binding and play an important role in angiogenesis and tumour metastasis. For this reason, integrins are increasingly used as targets for molecular imaging. Up to now interest has mostly been focused on the integrin subtype αvβ3. However, targeting of other subtypes such as the integrin α5β1 is also of high interest due to its central role in colonization of metastatic cells, resistance of tumour cells to chemotherapy and ionizing radiation, and tumour aggressiveness. Recently, a highly active antagonist ligand (2,2'-(7-(1-carboxy-4-((6-((3-(4-(((S)-1-carboxy-2-(2- (3-guanidinobenzamido)acet amido)ethyl)carbamoyl)-3,5-dimethylphenoxy) propyl)amino)-6-oxohexyl)amino)-4-oxo butyl)-1,4,7-triazonane-1,4-diyl)diacetic acid, FR366) for the integrin subtype α5β1 with high selectivity versus αvβ3, has been developed and tested successfully in preliminary in vitro and in vivo experiments. Here, we present our results of an investigation of the use of {sup 68}Ga-labelled α5β1 ligand in PET imaging. The free α5β1 peptidomimetic ligand was functionalized with a spacer (6-aminohexanoic acid) and the bifunctional chelator 1-((1,3-dicarboxy)propyl) -4,7-(carboxymethyl)-1,4,7-triazacyclononane (NODAGA) to yield FR366 and labelled with {sup 68}Ga. To confirm selective in vivo targeting of α5β1, female BALB/c nude mice xenografted with α5β1-expressing RKO cells in the right shoulder and α5β1/αvβ3-expressing M21 cells in the left shoulder were subjected to PET/CT scans and biodistribution experiments. Specificity of tracer uptake was proven by blocking studies. Metabolic stability of the injected tracer was measured in urine and in plasma. MicroPET/CT scans with radiolabelled FR366 showed a good tumour-to-normal tissue ratio with low uptake in the liver (0.32 ± 0.14 %ID/g) and good retention of {sup 68}Ga-NODAGA-FR366 in the tumour (0.71 ± 0.20 %ID/g and 0

  8. 99mTc-labeling of Peptidomimetic Antagonist to Selectively Target αvβ3 Receptor-Positive Tumor: Comparison of PDA and EDDA as co-Ligands

    Science.gov (United States)

    Shin, In Soo; Maeng, Jin Soo; Jang, Beom-Su; You, Eric; Cheng, Kenneth; Li, King C.P; Wood, Bradford; Carrasquillo, Jorge A.; Danthi, S. Narasimhan; Paik, Chang H.

    2010-01-01

    Objectives The aim of this research was to synthesize radiolabeled peptidomimetic integrin αvβ3 antagonist with 99mTc for rapid targeting of integrin αvβ3 receptors in tumor to produce a high tumor to background ratio. Methods The amino terminus of 4-[2-(3,4,5,6-tetra-hydropyrimidin-2-ylamino)-ethyloxy]benzoyl-2-(S)-[N-(3-amino-neopenta-1-carbamyl)]-aminoethylsulfonyl-amino-β-alanine hydrochloride (IAC) was conjugated with N-hydroxysuccinimide ester of HYNIC and labeled with 99mTc using tricine with either 1,5-pyridinedicarboxylic acid (PDA) or ethylenediamine-N,N′-diacetic acid (EDDA) as the co-ligand. The products, 99mTc EDDA2/HYNIC-IAC (P1) and 99mTc PDA (tricin)/HYNIC-IAC (P2) were subjected to in vitro serum stability, receptor-binding, biodistribution and imaging studies. Results P1 and P2 were synthesized with an overall yield of >80%. P1 was slightly more stable than P2 when incubated in serum at 37 °C for 18 hrs (84 vs 77% intact). The In vitro receptor-binding of P1 was higher than that of P2 (78.02 ± 13.48 vs 51.05 ± 14.05%) when incubated with αvβ3 at a molar excess (0.8 μM). This receptor binding was completely blocked by a molar excess of an unlabeled peptidomimetic antagonist. Their differences shown in serum stability and the receptor-binding appeared to be related to their biological behaviors in tumor uptake and retention; the 1 h tumor uptakes of P1 and P2 were 3.17±0.52 and 2.13±0.17 % ID/g, respectively. P1 was retained in the tumor longer than P2. P1 was excreted primarily through the renal system whereas P2 complex was excreted equally via both renal and hepatobiliary systems. Thus, P1 was retained in the whole-body with 27.25 ± 3.67% ID at 4 h whereas 54.04 ± 3.57% ID of P2 remained in the whole-body at 4 h. This higher whole-body retention of P2 appeared to be resulted from a higher amount of radioactivity retained in liver and intestine. These findings were supported by imaging studies showing higher tumor

  9. Application of PhSCF2CF2SiMe3 as a Tandem Anion and Radical Tetrafluoroethylene Equivalent: Fluoride-Catalyzed Addition to N-Substituted Cyclic Imides Followed by Radical Cyclization

    Czech Academy of Sciences Publication Activity Database

    Chernykh, Yana; Opekar, Stanislav; Klepetářová, Blanka; Beier, Petr

    2012-01-01

    Roč. 23, č. 8 (2012), s. 1187-1190 ISSN 0936-5214 R&D Projects: GA ČR GAP207/11/0421 Institutional research plan: CEZ:AV0Z40550506 Keywords : nucleophilic addition * radical reaction * fluorine * heterocycles * imides Subject RIV: CC - Organic Chemistry Impact factor: 2.655, year: 2012

  10. In vitro activities of novel 4-HPR derivatives on a panel of rhabdoid and other tumor cell lines

    Directory of Open Access Journals (Sweden)

    Das Bhaskar C

    2011-09-01

    Full Text Available Abstract Background Rhabdoid tumors (RTs are aggressive pediatric malignancies with poor prognosis. N-(4-hydroxy phenyl retinamide (4-HPR or fenretinide is a potential chemotherapeutic for RTs with activity correlated to its ability to down-modulate Cyclin D1. Previously, we synthesized novel halogen-substituted and peptidomimetic-derivatives of 4-HPR that retained activity in MON RT cells. Here we analyzed the effect of 4-HPR in inhibiting the growth of several RT, glioma, and breast cancer cell lines and tested their effect on cell cycle, apoptosis and Cyclin D1 expression. Methods Effect of compounds on RT cell cycle profiles, and cell death were assessed by MTS cell survival assays and FACS analysis. The effects of treatment on Cyclin D1 expression were determined by immunoblotting. The efficacy of these compounds on glioma and breast cancer cell lines was also determined using MTS assays. Results Low micromolar concentrations of 4-HPR derivatives inhibited cell survival of all RT cells tested. The 4-HPR derivatives altered RT cell cycle profiles and induced high levels of cell death that was correlated with their potency. ATRA exhibited high IC50 values in all cell lines tested and did not cause cell death. In MON RT cells, the iodo-substituted compounds were more active than 4-HPR in inducing cell cycle arrest and apoptosis. Additionally, the activity of the compounds correlated with their ability to down-modulate Cyclin D1: while active compounds reduced Cyclin D1 levels, inactive ATRA did not. In glioma and breast cancer cell lines, 4-HPR and 4-HPR derivatives showed variable efficacy. Conclusions Here we demonstrate, for the first time, that the inhibitory activities of novel halogen-substituted and peptidomimetic derivatives of 4-HPR are correlated to their ability to induce cell death and down-modulate Cyclin D1. These 4-HPR derivatives showed varied potencies in breast cancer and glioma cell lines. These data indicate that further

  11. Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)–Mixed Lineage Leukemia (MLL) Protein–Protein Interaction

    Energy Technology Data Exchange (ETDEWEB)

    Karatas, Hacer; Li, Yangbing; Liu, Liu; Ji, Jiao; Lee, Shirley; Chen, Yong; Yang, Jiuling; Huang, Liyue; Bernard, Denzil; Xu, Jing; Townsend, Elizabeth C.; Cao, Fang; Ran, Xu; Li, Xiaoqin; Wen, Bo; Sun, Duxin; Stuckey, Jeanne A; Lei, Ming; Dou, Yali; Wang, Shaomeng (Michigan)

    2017-06-06

    We report herein the design, synthesis, and evaluation of macrocyclic peptidomimetics that bind to WD repeat domain 5 (WDR5) and block the WDR5–mixed lineage leukemia (MLL) protein–protein interaction. Compound 18 (MM-589) binds to WDR5 with an IC50 value of 0.90 nM (Ki value <1 nM) and inhibits the MLL H3K4 methyltransferase (HMT) activity with an IC50 value of 12.7 nM. Compound 18 potently and selectively inhibits cell growth in human leukemia cell lines harboring MLL translocations and is >40 times better than the previously reported compound MM-401. Cocrystal structures of 16 and 18 complexed with WDR5 provide structural basis for their high affinity binding to WDR5. Additionally, we have developed and optimized a new AlphaLISA-based MLL HMT functional assay to facilitate the functional evaluation of these designed compounds. Compound 18 represents the most potent inhibitor of the WDR5–MLL interaction reported to date, and further optimization of 18 may yield a new therapy for acute leukemia.

  12. Global Derivatives

    DEFF Research Database (Denmark)

    Andersen, Torben Juul

    approaches to dealing in the global business environment." - Sharon Brown-Hruska, Commissioner, Commodity Futures Trading Commission, USA. "This comprehensive survey of modern risk management using derivative securities is a fine demonstration of the practical relevance of modern derivatives theory to risk......" provides comprehensive coverage of different types of derivatives, including exchange traded contracts and over-the-counter instruments as well as real options. There is an equal emphasis on the practical application of derivatives and their actual uses in business transactions and corporate risk...... management situations. Its key features include: derivatives are introduced in a global market perspective; describes major derivative pricing models for practical use, extending these principles to valuation of real options; practical applications of derivative instruments are richly illustrated...

  13. Financial Derivatives

    DEFF Research Database (Denmark)

    Wigan, Duncan

    2013-01-01

    Contemporary derivatives mark the development of capital and constitute a novel form of ownership. By reconfiguring the temporal, spatial and legal character of ownership derivatives present a substantive challenge to the tax collecting state. While fiscal systems are nationally bounded...... and inherently static, capital itself is unprecedentedly mobile, fluid and fungible. As such derivatives raise the specter of ‘financial weapons of mass destruction’....

  14. Financial Derivatives

    OpenAIRE

    Janečková, Alena

    2011-01-01

    1 Abstract/ Financial derivatives The purpose of this thesis is to provide an introduction to financial derivatives which has been, from the legal perspective, described in a not satisfactory manner as quite little literature that can be found about this topic. The main objectives of this thesis are to define the term "financial derivatives" and its particular types and to analyse legal nature of these financial instruments. The last objective is to try to draft future law regulation of finan...

  15. Derivative chameleons

    International Nuclear Information System (INIS)

    Noller, Johannes

    2012-01-01

    We consider generalized chameleon models where the conformal coupling between matter and gravitational geometries is not only a function of the chameleon field φ, but also of its derivatives via higher order co-ordinate invariants (such as ∂ μ φ∂ μ φ,□φ,...). Specifically we consider the first such non-trivial conformal factor A(φ,∂ μ φ∂ μ φ). The associated phenomenology is investigated and we show that such theories have a new generic mass-altering mechanism, potentially assisting the generation of a sufficiently large chameleon mass in dense environments. The most general effective potential is derived for such derivative chameleon setups and explicit examples are given. Interestingly this points us to the existence of a purely derivative chameleon protected by a shift symmetry for φ → φ+c. We also discuss potential ghost-like instabilities associated with mass-lifting mechanisms and find another, mass-lowering and instability-free, branch of solutions. This suggests that, barring fine-tuning, stable derivative models are in fact typically anti-chameleons that suppress the field's mass in dense environments. Furthermore we investigate modifications to the thin-shell regime and prove a no-go theorem for chameleon effects in non-conformal geometries of the disformal type

  16. Derivative chameleons

    Energy Technology Data Exchange (ETDEWEB)

    Noller, Johannes, E-mail: johannes.noller08@imperial.ac.uk [Theoretical Physics, Blackett Laboratory, Imperial College London, Prince Consort Road, London, SW7 2BZ (United Kingdom)

    2012-07-01

    We consider generalized chameleon models where the conformal coupling between matter and gravitational geometries is not only a function of the chameleon field φ, but also of its derivatives via higher order co-ordinate invariants (such as ∂{sub μ}φ∂{sup μ}φ,□φ,...). Specifically we consider the first such non-trivial conformal factor A(φ,∂{sub μ}φ∂{sup μ}φ). The associated phenomenology is investigated and we show that such theories have a new generic mass-altering mechanism, potentially assisting the generation of a sufficiently large chameleon mass in dense environments. The most general effective potential is derived for such derivative chameleon setups and explicit examples are given. Interestingly this points us to the existence of a purely derivative chameleon protected by a shift symmetry for φ → φ+c. We also discuss potential ghost-like instabilities associated with mass-lifting mechanisms and find another, mass-lowering and instability-free, branch of solutions. This suggests that, barring fine-tuning, stable derivative models are in fact typically anti-chameleons that suppress the field's mass in dense environments. Furthermore we investigate modifications to the thin-shell regime and prove a no-go theorem for chameleon effects in non-conformal geometries of the disformal type.

  17. Electricity derivatives

    CERN Document Server

    Aïd, René

    2015-01-01

    Offering a concise but complete survey of the common features of the microstructure of electricity markets, this book describes the state of the art in the different proposed electricity price models for pricing derivatives and in the numerical methods used to price and hedge the most prominent derivatives in electricity markets, namely power plants and swings. The mathematical content of the book has intentionally been made light in order to concentrate on the main subject matter, avoiding fastidious computations. Wherever possible, the models are illustrated by diagrams. The book should allow prospective researchers in the field of electricity derivatives to focus on the actual difficulties associated with the subject. It should also offer a brief but exhaustive overview of the latest techniques used by financial engineers in energy utilities and energy trading desks.

  18. β-Amyloid-derived pentapeptide RIIGLa inhibits Aβ1-42 aggregation and toxicity

    International Nuclear Information System (INIS)

    Fueloep, Livia; Zarandi, Marta; Datki, Zsolt; Soos, Katalin; Penke, Botond

    2004-01-01

    Pr-IIGL a , a derivative of the tetrapeptide β-amyloid 31-34 (Aβ 31-34 ), exerts controversial effects: it is toxic in a neuroblastoma culture, but it protects glial cells from the cytotoxic action of Aβ 1-42 . For an understanding of this phenomenon, a new pentapeptide, RIIGL a was synthetized, and both compounds were studied by different physicochemical and biological methods. Transmission electron microscopic (TEM) studies revealed that Pr-IIGL a forms fibrillar aggregates, whereas RIIGL a does not form fibrils. Congo red binding studies furnished the same results. Aggregated Pr-IIGL a acts as a cytotoxic agent in neuroblastoma cultures, but RIIGL a does not display inherent toxicity. RIIGL a co-incubated with Aβ 1-42 inhibits the formation of mature amyloid fibres (TEM studies) and reduces the cytotoxic effect of fibrillar Aβ 1-42 . These results indicate that RIIGL a is an effective inhibitor of both the aggregation and the toxic effects of Aβ 1-42 and can serve as a lead compound for the design of novel neuroprotective peptidomimetics

  19. Spectrum and activity of novel antimicrobial peptidomimetics

    DEFF Research Database (Denmark)

    Hein-Kristensen, Line

    of leaked ATP and subsequent loss of viability. A series of three peptides differing only in length all caused ATP leakage but only the longest of the three caused complete depletion of intracellular ATP, which correlated with a substantial loss in the number of viable cells. In a continuous selection...... is becoming increasingly limited. In the search for alternatives therapies, antimicrobial peptides (AMPs) have received considerable attention since they target the bacterial Achilles’ heel i.e. their distinct membrane structure. These host defence molecules are ubiquitous in nature by forming part......D protein. This protein functions in the reorganization of the peptidoglycan layer, and we consider it likely that a change in this protein is the cause of resistance, since the SNP was found exclusively in isolates with high levels of resistance. Conversely, these resistant isolates displayed increased...

  20. Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.

    Science.gov (United States)

    Galibert, Matthieu; Wartenberg, Mylène; Lecaille, Fabien; Saidi, Ahlame; Mavel, Sylvie; Joulin-Giet, Alix; Korkmaz, Brice; Brömme, Dieter; Aucagne, Vincent; Delmas, Agnès F; Lalmanach, Gilles

    2018-01-20

    Cathepsin (Cat) K is a critical bone-resorbing protease and is a relevant target for the treatment of osteoporosis and bone metastasis, while CatS is an attractive target for drugs in autoimmune diseases (e.g. rheumatoid arthritis), emphysema or neuropathic pain. Despite major achievements, current pharmacological inhibitors are still lacking in safety and may have damaging side effects. A promising strategy for developing safer reversible and competitive inhibitors as new lead compounds could be to insert non-cleavable bonds at the scissile P1-P1' position of selective substrates of CatS and CatK. Accordingly, we introduced a 1,4-disubstituted 1,2,3-triazole heterocycle that mimics most of the features of a trans-amide bond, or we incorporated a semicarbazide bond (azaGly residue) by replacing the α-carbon of the glycyl residue at P1 by a nitrogen atom. AzaGly-containing peptidomimetics inhibited powerfully their respective target proteases in the nM range, while triazolopeptides were weaker inhibitors (Ki in the μM range). The selectivity of the azaGly CatS inhibitor (1b) was confirmed by using spleen lysates from wild-type vs CatS-deficient mice. Alternatively, the azaGly bradykinin-derived CatK inhibitor (2b) potently inhibited CatK (Ki = 9 nM) and impaired its kininase activity in vitro. Molecular modeling studies support that the semicarbazide bond of 2b is more favorable than the 1,2,3-triazole linkage of the bradykinin-derived pseudopeptide 2a to preserve an effective affinity towards CatK, its protease target. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  1. Targeting interleukin-11 receptor in leukemia and lymphoma: A functional ligand-directed study and hematopathology analysis of patient-derived specimens

    Science.gov (United States)

    Karjalainen, Katja; Jaalouk, Diana E.; Bueso-Ramos, Carlos; Bover, Laura; Sun, Yan; Kuniyasu, Akihiko; Driessen, Wouter H. P.; Cardó-Vila, Marina; Rietz, Cecilia; Zurita, Amado J.; O’Brien, Susan; Kantarjian, Hagop M.; Cortes, Jorge E.; Calin, George A.; Koivunen, Erkki; Arap, Wadih; Pasqualini, Renata

    2015-01-01

    Purpose The interleukin-11 receptor (IL-11R) is an established molecular target in primary tumors of bone, such as osteosarcoma, and in secondary bone metastases from solid tumors such as prostate cancer. However, its potential role in management of hematopoietic malignancies has not yet been determined. Here we evaluated the IL-11R as a candidate therapeutic target in human leukemia and lymphoma. Experimental Design and Results First, we show that the IL-11R protein is expressed in a variety of human leukemia- and lymphoma derived cell lines and in a large panel of bone marrow samples from leukemia and lymphoma patients, while expression is absent from non-malignant control bone marrow. Moreover, a targeted peptidomimetic prototype (termed BMTP-11) specifically bound to leukemia and lymphoma cell membranes, induced ligand-receptor internalization mediated by the IL-11R, and resulted in a specific dose-dependent cell death induction in these cells. Finally, a pilot drug lead-optimization program yielded a new myristoylated BMTP-11 analog with an apparent improved anti-leukemia cell profile. Conclusion These results indicate (i) that the IL-11R is a suitable cell surface target for ligand-directed applications in human leukemia and lymphoma and (ii) that BMTP-11 and its derivatives have translational potential against this group of malignant diseases. PMID:25779950

  2. Targeting IL11 Receptor in Leukemia and Lymphoma: A Functional Ligand-Directed Study and Hematopathology Analysis of Patient-Derived Specimens.

    Science.gov (United States)

    Karjalainen, Katja; Jaalouk, Diana E; Bueso-Ramos, Carlos; Bover, Laura; Sun, Yan; Kuniyasu, Akihiko; Driessen, Wouter H P; Cardó-Vila, Marina; Rietz, Cecilia; Zurita, Amado J; O'Brien, Susan; Kantarjian, Hagop M; Cortes, Jorge E; Calin, George A; Koivunen, Erkki; Arap, Wadih; Pasqualini, Renata

    2015-07-01

    The IL11 receptor (IL11R) is an established molecular target in primary tumors of bone, such as osteosarcoma, and in secondary bone metastases from solid tumors, such as prostate cancer. However, its potential role in management of hematopoietic malignancies has not yet been determined. Here, we evaluated the IL11R as a candidate therapeutic target in human leukemia and lymphoma. First, we show that the IL11R protein is expressed in a variety of human leukemia- and lymphoma-derived cell lines and in a large panel of bone marrow samples from leukemia and lymphoma patients, whereas expression is absent from nonmalignant control bone marrow. Moreover, a targeted peptidomimetic prototype (termed BMTP-11), specifically bound to leukemia and lymphoma cell membranes, induced ligand-receptor internalization mediated by the IL11R, and resulted in a specific dose-dependent cell death induction in these cells. Finally, a pilot drug lead-optimization program yielded a new myristoylated BMTP-11 analogue with an apparent improved antileukemia cell profile. These results indicate (i) that the IL11R is a suitable cell surface target for ligand-directed applications in human leukemia and lymphoma and (ii) that BMTP-11 and its derivatives have translational potential against this group of malignant diseases. ©2015 American Association for Cancer Research.

  3. δ-Peptides from RuAAC-Derived 1,5-Disubstituted Triazole Units

    KAUST Repository

    Johansson, Johan R.

    2014-02-14

    Non-natural peptides with structures and functions similar to natural peptides have emerged lately in biomedical as well as nanotechnological contexts. They are interesting for pharmaceutical applications since they can adopt structures with new targeting potentials and because they are generally not prone to degradation by proteases. We report here a new set of peptidomimetics derived from δ-peptides, consisting of n units of a 1,5-disubstituted 1,2,3-triazole amino acid (5Tzl). The monomer was prepared using ruthenium-catalyzed azide-alkyne cycloaddition (RuAAC) chemistry using [RuCl2Cp]x as the catalyst, allowing for simpler purification and resulting in excellent yields. This achiral monomer was used to prepare peptide oligomers that are water soluble independent of peptide chain length. Conformational analysis and structural investigations of the oligomers were performed by 2D NOESY NMR experiments, and by quantum chemical calculations using the ωB97X-D functional. These data indicate that several conformations may co-exist with slight energetic differences. Together with their increased hydrophilicity, this feature of homo-5Tzl may prove essential for mimicking natural peptides composed of α-amino acids, where the various secondary structures are achieved by side chain effects and not by the rigidity of the peptide backbone. The improved synthetic method allows for facile variation of the 5Tzl amino acid side chains, further increasing the versatility of these compounds. A new set of non-natural peptides composed of 1,5-disubstituted 1,2,3-triazole amino acids is presented. These peptides benefit from: a) modular synthesis of the monomers, allowing variation of the side chains; b) increased solubility of the oligomers in water, irrespective of peptide length; c) flexibility of the backbone allowing these foldamers to adopt several conformations. Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  4. Interest rate derivatives

    DEFF Research Database (Denmark)

    Svenstrup, Mikkel

    This Ph.D. thesis consists of four self-contained essays on valuation of interest rate derivatives. In particular derivatives related to management of interest rate risk care are considered.......This Ph.D. thesis consists of four self-contained essays on valuation of interest rate derivatives. In particular derivatives related to management of interest rate risk care are considered....

  5. Preparation and study of dialkyl nitroxide radicals; Preparation et etude de radicaux nitroxydes diacyles

    Energy Technology Data Exchange (ETDEWEB)

    Chenavas, P. [Commissariat a l' Energie Atomique, Grenoble (France). Centre d' Etudes Nucleaires

    1969-07-01

    These radicals are obtained by oxidation of N-hydroxy-imides with lead tetracetate or p-nitro-perbenzoic acid. These imides are prepared by heating dicarboxylic acids anhydrides with benzyloxy-amine followed by catalytic hydrogenation of N-benzyloxy-imides so obtained. Two series of radicals have mainly been studied, the first concerning five-membered cyclic imides, the second six-membered cyclic imides, these molecules having methyls substituents or no on the carbon ring. N. M. R. spectra of some O-benzyl-imides have been analysed. These different results have made it possible to study the conformation and stereochemistry of these imides. (author) [French] Ces radicaux sont obtenus par oxydation d'imides N-hydroxyles par le tetracetate de plomb ou l'acide p-nitroperbenzoique; ces imides sont prepares par chauffage d'anhydrides de diacides en presence de benzyloxyamine suivie d'une hydrogenation catalytique des N-benzyloxyimides ainsi obtenus. Deux series de radicaux ont principalement ete etudies: la premiere relative a des imides cycliques a cinq chainons, la seconde a des imides cycliques a six chainons, ces molecules ayant des substituants methyles ou non sur la chaine carbonee. Les derives O-benzyles de quelques-uns de ces imides ont ete analyses en R. M. N. Ces differents resultats ont permis une etude de la conformation et de la stereochimie de ces imides. (auteur)

  6. Preparation and study of dialkyl nitroxide radicals; Preparation et etude de radicaux nitroxydes diacyles

    Energy Technology Data Exchange (ETDEWEB)

    Chenavas, P [Commissariat a l' Energie Atomique, Grenoble (France). Centre d' Etudes Nucleaires

    1969-07-01

    These radicals are obtained by oxidation of N-hydroxy-imides with lead tetracetate or p-nitro-perbenzoic acid. These imides are prepared by heating dicarboxylic acids anhydrides with benzyloxy-amine followed by catalytic hydrogenation of N-benzyloxy-imides so obtained. Two series of radicals have mainly been studied, the first concerning five-membered cyclic imides, the second six-membered cyclic imides, these molecules having methyls substituents or no on the carbon ring. N. M. R. spectra of some O-benzyl-imides have been analysed. These different results have made it possible to study the conformation and stereochemistry of these imides. (author) [French] Ces radicaux sont obtenus par oxydation d'imides N-hydroxyles par le tetracetate de plomb ou l'acide p-nitroperbenzoique; ces imides sont prepares par chauffage d'anhydrides de diacides en presence de benzyloxyamine suivie d'une hydrogenation catalytique des N-benzyloxyimides ainsi obtenus. Deux series de radicaux ont principalement ete etudies: la premiere relative a des imides cycliques a cinq chainons, la seconde a des imides cycliques a six chainons, ces molecules ayant des substituants methyles ou non sur la chaine carbonee. Les derives O-benzyles de quelques-uns de ces imides ont ete analyses en R. M. N. Ces differents resultats ont permis une etude de la conformation et de la stereochimie de ces imides. (auteur)

  7. Derivatives in emerging markets

    OpenAIRE

    Dubravko Mihaljek; Frank Packer

    2010-01-01

    Turnover of derivatives has grown more rapidly in emerging markets than in developed countries. Foreign exchange derivatives are the most commonly traded of all risk categories, with increasingly frequent turnover in emerging market currencies and a growing share of cross-border transactions. As the global reach of the financial centres in emerging Asia has expanded, the offshore trading of many emerging market currency derivatives has risen as well. Growth in derivatives turnover is positive...

  8. Global Derivatives Market

    Directory of Open Access Journals (Sweden)

    Stankovska Aleksandra

    2017-06-01

    Full Text Available Globalization of financial markets led to the enormous growth of volume and diversification of financial transactions. Financial derivatives were the basic elements of this growth. Derivatives play a useful and important role in hedging and risk management, but they also pose several dangers to the stability of financial markets and thereby the overall economy. Derivatives are used to hedge and speculate the risk associated with commerce and finance.

  9. Risk and Derivative Price

    OpenAIRE

    Yusuke Osaki

    2007-01-01

    We consider an asset market traded three types of assets: the risk–free asset, the market portfolio and derivatives written on the market portfolio return. We determine a sufficient condition to guarantee that noise risk monotonically changes their derivatives. The condition is that Arrow–Pratt absolute risk aversion is decreasing and convex.

  10. Financial Derivatives in China

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    Francis Repka sees bright prospects for the future development of the financial derivatives market in China. Repka,Vice President of the Asian Bond Finance Department of Societe Generale, says the situation in France just after the birth of derivatives was very similar to the situation in China today.

  11. Vitamin D derivatives

    International Nuclear Information System (INIS)

    Deluca, H.F.; Schnoes, H.K.; Napoli, J.L.; Fivizzani, M.A.

    1982-01-01

    The chemical preparation of 26,27-isotopically labelled vitamin D 3 derivatives of high specific activity is described. These labelled vitamin D derivatives are useful in the determination of vitamin D metabolite levels in the blood and tissues of man and animals. (U.K.)

  12. Taxation of Derivatives

    DEFF Research Database (Denmark)

    Dyppel, Katja Joo

    2013-01-01

    The main objective for this thesis is to analyse and systematise the Danish legislation on taxation of derivatives. According to financial terminology, a derivative is a financial instrument. Its value is derived from changes in the value of one or more underlying assets.The most common derivatives...... in the Danish tax legislation. However, contracts known as forwards (terminskontrakter) and options (aftaler om køberetter og salgsretter) are generally included in the term financials contracts covered by the Danish Act on Taxation of Gains and Losses on Claims and Debt. The main part of the analysis deals...... with the scope of sections 29-33 of the Danish Act on Taxation of Gains and Losses on Claims and Debt and the tax consequences for the covered financial contracts. In the analysis of taxation of derivatives, the fundamental issues of qualification and tax treatment of the instruments are dealt with....

  13. Superstability of Generalized Derivations

    Directory of Open Access Journals (Sweden)

    Ansari-Piri Esmaeil

    2010-01-01

    Full Text Available We investigate the superstability of the functional equation , where and are the mappings on Banach algebra . We have also proved the superstability of generalized derivations associated to the linear functional equation , where .

  14. Amphetamine derivative related deaths.

    Science.gov (United States)

    Lora-Tamayo, C; Tena, T; Rodríguez, A

    1997-02-28

    Amphetamine its methylendioxy (methylendioxyamphetamine methylenedioxymethylamphetamine, methylenedioxyethylamphetamine) and methoxy derivatives (p-methoxyamphetamine and p-methoxymethylamphetamine) are widely abused in Spanish society. We present here the results of a systematic study of all cases of deaths brought to the attention of the Madrid department of the Instituto Nacional de Toxicologia from 1993 to 1995 in which some of these drugs have been found in the cadaveric blood. The cases were divided into three categories: amphetamine and derivatives, amphetamines and alcohol, amphetamines and other drugs. Data on age, sex, clinical symptoms, morphological findings, circumstances of death, when known, and concentration of amphetamine derivatives, alcohol and other drugs in blood are given for each group. The information provided here may prove to be useful for the forensic interpretation of deaths which are directly or indirectly related to abuse of amphetamine derivatives.

  15. Investigation - Derived Waste Program

    International Nuclear Information System (INIS)

    Beardsley, C.; Anderson, R.

    1998-06-01

    The Investigation-Derived Waste Program is a software application that was developed to identify the groundwater monitoring wells at the Savannah River Site that require containerization and treatment for purge water generated during sampling

  16. Development of Derivatives Reporting

    OpenAIRE

    Pejčochová, Kristina

    2012-01-01

    This thesis aims to summarise the theoretical principles, concepts and considerations pertaining to accounting for and reporting of derivatives and to describe and analyse the development of major accounting standards dealing with related issues. Sections 1 and 2 provide a basic overview of derivative instruments'categorisation, mechanics, valuation and uses. Section 3 studies the principles that ensure the provision of useful financial information, with specific focus on financial instrument...

  17. On higher derivative gravity

    International Nuclear Information System (INIS)

    Accioly, A.J.

    1987-01-01

    A possible classical route conducting towards a general relativity theory with higher-derivatives starting, in a sense, from first principles, is analysed. A completely causal vacuum solution with the symmetries of the Goedel universe is obtained in the framework of this higher-derivative gravity. This very peculiar and rare result is the first known vcuum solution of the fourth-order gravity theory that is not a solution of the corresponding Einstein's equations.(Author) [pt

  18. Brain derived neurotrophic factor

    DEFF Research Database (Denmark)

    Mitchelmore, Cathy; Gede, Lene

    2014-01-01

    Brain Derived Neurotrophic Factor (BDNF) is a neurotrophin with important functions in neuronal development and neuroplasticity. Accumulating evidence suggests that alterations in BDNF expression levels underlie a variety of psychiatric and neurological disorders. Indeed, BDNF therapies are curre......Brain Derived Neurotrophic Factor (BDNF) is a neurotrophin with important functions in neuronal development and neuroplasticity. Accumulating evidence suggests that alterations in BDNF expression levels underlie a variety of psychiatric and neurological disorders. Indeed, BDNF therapies...

  19. Gorenstein derived functions

    DEFF Research Database (Denmark)

    Holm, Henrik Granau

    2004-01-01

    Over any associative ring R it is standard to derive HomR(􀀀;􀀀) using projective resolutions in the rst variable, or injective resolutions in the second variable, and doing this, one obtains Extn R(􀀀;􀀀) in both cases. We examine the situation where projective...... and injective modules are replaced by Gorenstein projective and Gorenstein injective ones, respectively. Furthermore, we derive the tensor product 􀀀 R 􀀀 using Gorenstein at modules....

  20. NMR structures of anti-HIV D-peptides derived from the N-terminus of viral chemokine vMIP-II

    International Nuclear Information System (INIS)

    Mori, Mayuko; Liu Dongxiang; Kumar, Santosh; Huang Ziwei

    2005-01-01

    The viral macrophage inflammatory protein-II (vMIP-II) encoded by Kaposi's sarcoma-associated herpesvirus has unique biological activities in that it blocks the cell entry by several different human immunodeficiency virus type 1 (HIV-1) strains via chemokine receptors including CXCR4 and CCR5. In this paper, we report the solution structure of all-D-amino acid peptides derived from the N-terminus of vMIP-II, which have been shown to have strong CXCR4 binding activity and potently inhibit HIV-1 entry via CXCR4, by using long mixing time two-dimensional nuclear Overhauser enhancement spectroscopy experiments. Both of all-D-peptides vMIP-II (1-10) and vMIP-II (1-21), which are designated as DV3 and DV1, respectively, have higher CXCR4 binding ability than their L-peptide counterparts. They are partially structured in aqueous solution, displaying a turn-like structure over residues 5-8. The small temperature coefficients of His-6 amide proton for both peptides also suggest the formation of a small hydrophobic pocket centered on His-6. The structural features of DV3 are very similar to the reported solution structure of all-L-peptide vMIP-II (1-10) [M.P. Crump, E. Elisseeva, J. Gong, I. Clark-Lewis, B.D. Sykes, Structure/function of human herpesvirus-8 MIP-II (1-71) and the antagonist N-terminal segment (1-10), FEBS Lett. 489 (2001) 171], which is consistent with the notion that D- and L-enantiomeric peptides can adopt mirror image conformations. The NMR structures of the D-peptides provide a structural basis to understand their mechanism of action and design new peptidomimetic analogs to further explore the structure-activity relationship of D-peptide ligand binding to CXCR4

  1. Virosome-formulated Plasmodium falciparum AMA-1 & CSP derived peptides as malaria vaccine: randomized phase 1b trial in semi-immune adults & children.

    Directory of Open Access Journals (Sweden)

    Patrick Georges Cech

    Full Text Available This trial was conducted to evaluate the safety and immunogenicity of two virosome formulated malaria peptidomimetics derived from Plasmodium falciparum AMA-1 and CSP in malaria semi-immune adults and children.The design was a prospective randomized, double-blind, controlled, age-deescalating study with two immunizations. 10 adults and 40 children (aged 5-9 years living in a malaria endemic area were immunized with PEV3B or virosomal influenza vaccine Inflexal®V on day 0 and 90.No serious or severe adverse events (AEs related to the vaccines were observed. The only local solicited AE reported was pain at injection site, which affected more children in the Inflexal®V group compared to the PEV3B group (p = 0.014. In the PEV3B group, IgG ELISA endpoint titers specific for the AMA-1 and CSP peptide antigens were significantly higher for most time points compared to the Inflexal®V control group. Across all time points after first immunization the average ratio of endpoint titers to baseline values in PEV3B subjects ranged from 4 to 15 in adults and from 4 to 66 in children. As an exploratory outcome, we found that the incidence rate of clinical malaria episodes in children vaccinees was half the rate of the control children between study days 30 and 365 (0.0035 episodes per day at risk for PEV3B vs. 0.0069 for Inflexal®V; RR  = 0.50 [95%-CI: 0.29-0.88], p = 0.02.These findings provide a strong basis for the further development of multivalent virosomal malaria peptide vaccines.ClinicalTrials.gov NCT00513669.

  2. Asia Pacific energy derivatives

    International Nuclear Information System (INIS)

    Fusaro, P.C.

    1997-09-01

    Asia Pacific Energy Derivatives, from FT Energy, is the first report of its kind to examine the growth of energy derivatives within Asia Pacific and their increasing importance within this region. It provides a comprehensive overview of the subject, including analysis of: deregulation as a market driver; the impact of privatisation; the future for energy risk management tools; the unique characteristics of the Asia Pacific energy market; the role of futures exchanges in Asia; existing indexes and their performance; the differences between the Asia Pacific markets and their more mature counterparts in London and New York; non-oil derivatives, project finance and cross commodity arbitrage; the thriving Pacific Rim Over the Counter (OTC) markets. (author)

  3. 4-Aminoquinoline derivatives

    DEFF Research Database (Denmark)

    Singh, Shailja; Agarwal, Drishti; Sharma, Kumkum

    2016-01-01

    and found them to be effective against Plasmodium falciparum under in vitro conditions. Further, we selected four most active derivatives 1m, 1o, 2c and 2j and evaluated their antimalarial potential against Plasmodium berghei in vivo. These 4-aminoquinolines cured BALB/c mice infected with P. berghei......Synthetic quinoline derivatives continue to be considered as candidates for new drug discovery if they act against CQ-resistant strains of malaria even after the widespread emergence of resistance to CQ. In this study, we explored the activities of two series of new 4-aminoquinoline derivatives...... for structure activity relationship to find lead molecules for treating multidrug-resistant Plasmodium falciparum and Plasmodium vivax....

  4. Essays on Derivatives Pricing

    DEFF Research Database (Denmark)

    Kokholm, Thomas

    . With the existence of a liquid market for derivatives with variance as underlying, such as VIX options, VIX futures and a well-developed over-the-counter market for options on variance swaps, it is important to consider models that are able to fit these markets while consistently pricing vanilla options...... financial models, and most importantly, to be aware of their limitations. Following that belief, this thesis consists of three independent and self-contained papers, all dealing with topics in derivatives pricing. The first paper considers the pricing of traffic light options, which are appropriate...... the market for multivariate credit instruments, we take a step back and focus on single-name default modeling and introduce two new model classes for modeling of the default time of a company. Finally, in the third paper we propose a consistent pricing model for index and volatility derivatives...

  5. The combinatorial derivation

    Directory of Open Access Journals (Sweden)

    Igor V. Protasov

    2013-09-01

    $\\Delta(A=\\{g\\in G:|gA\\cap A|=\\infty\\}$. The mapping $\\Delta:\\mathcal{P}_G\\rightarrow\\mathcal{P}_G$, $A\\mapsto\\Delta(A$, is called a combinatorial derivation and can be considered as an analogue of the topological derivation $d:\\mathcal{P}_X\\rightarrow\\mathcal{P}_X$, $A\\mapsto A^d$, where $X$ is a topological space and $A^d$ is the set of all limit points of $A$. Content: elementary properties, thin and almost thin subsets, partitions, inverse construction and $\\Delta$-trajectories,  $\\Delta$ and $d$.

  6. Quinazolin-4-one derivatives

    DEFF Research Database (Denmark)

    Mosley, Cara A; Acker, Timothy M; Hansen, Kasper Bø

    2010-01-01

    We describe a new class of subunit-selective antagonists of N-methyl D-aspartate (NMDA)-selective ionotropic glutamate receptors that contain the (E)-3-phenyl-2-styrylquinazolin-4(3H)-one backbone. The inhibition of recombinant NMDA receptor function induced by these quinazolin-4-one derivatives...

  7. Metal borohydrides and derivatives

    DEFF Research Database (Denmark)

    Paskevicius, Mark; Haarh Jepsen, Lars; Schouwink, Pascal

    2017-01-01

    major classes of metal borohydride derivatives have also been discovered: anion-substituted compounds where the complex borohydride anion, BH4 -, is replaced by another anion, i.e. a halide or amide ion; and metal borohydrides modified with neutral molecules, such as NH3, NH3BH3, N2H4, etc. Here, we...

  8. 78 FR 32191 - Derivatives

    Science.gov (United States)

    2013-05-29

    ... rate risk. This proposed rule applies to federal credit unions and any federally insured, state... risk to the National Credit Union Share Insurance Fund (NCUSIF). \\1\\ A derivative is an instrument... degrees of risk to a credit union. Accordingly, this risk calls for a more robust asset/ liability...

  9. Superstability of Generalized Derivations

    Directory of Open Access Journals (Sweden)

    Esmaeil Ansari-Piri

    2010-01-01

    Full Text Available We investigate the superstability of the functional equation f(xy=xf(y+g(xy, where f and g are the mappings on Banach algebra A. We have also proved the superstability of generalized derivations associated to the linear functional equation f(γx+βy=γf(x+βf(y, where γ,β∈ℂ.

  10. Approximate *-derivations and approximate quadratic *-derivations on C*-algebras

    Directory of Open Access Journals (Sweden)

    Park Choonkil

    2011-01-01

    Full Text Available Abstract In this paper, we prove the stability of *-derivations and of quadratic *-derivations on Banach *-algebras. We moreover prove the superstability of *-derivations and of quadratic *-derivations on C*-algebras. 2000 Mathematics Subject Classification: 39B52; 47B47; 46L05; 39B72.

  11. Derived enriched uranium market

    International Nuclear Information System (INIS)

    Rutkowski, E.

    1996-01-01

    The potential impact on the uranium market of highly enriched uranium from nuclear weapons dismantling in the Russian Federation and the USA is analyzed. Uranium supply, conversion, and enrichment factors are outlined for each country; inventories are also listed. The enrichment component and conversion components are expected to cause little disruption to uranium markets. The uranium component of Russian derived enriched uranium hexafluoride is unresolved; US legislation places constraints on its introduction into the US market

  12. Computation of Mie derivatives.

    Science.gov (United States)

    Li, Yang; Bowler, Nicola

    2013-07-10

    Analytical expressions are obtained for the derivatives of Mie scattering coefficients with respect to the electrical radius of the spherical scattering particle, and to the relative permittivity and permeability of both the particle and the surrounding medium. Their corresponding approximate expressions are developed to avoid numerical overflow based on the logarithmic derivative of Riccati-Bessel functions. The analytical expressions have been verified by comparing their results with those calculated by analytical expressions developed by Mathematica. Compared with the numerical derivative, the analytical expressions and approximate expressions show a higher accuracy and are 2.0 and 2.8 times, respectively, faster in the case of a single magnetodielectric sphere. Generally, for spheres with an electrical radius in a large range, the approximate expressions can yield acceptable accuracy and computation time up to a high order. This work can be used in the design of nonmetallic metamaterials, and in the retrieval of aerosol properties from remote sensing data. An example calculation is given for the design of an optical, all-dielectric, mu-negative metamaterial consisting of a simple cubic array of tellurium nanoparticles.

  13. Carnitine derivatives: clinical usefulness.

    Science.gov (United States)

    Malaguarnera, Mariano

    2012-03-01

    Carnitine and its derivatives are natural substances involved in both carbohydrate and lipid metabolism. This review summarizes the recent progress in the field in relation to the molecular mechanisms. The pool of different carnitine derivatives is formed by acetyl-L-carnitine (ALC), propionyl-L-carnitine (PLC), and isovaleryl-carnitine. ALC may have a preferential effect on the brain tissue. ALC represents a compound of great interest for its wide clinical application in various neurological disorders: it may be of benefit in treating Alzheimer's dementia, depression in the elderly, HIV infection, chronic fatigue syndrome, peripheral neuropathies, ischemia and reperfusion of the brain, and cognitive impairment associated with various conditions. PLC has been demonstrated to replenish the intermediates of the tricarboxylic acid cycle by the propionyl-CoA moiety, a greater affinity for the sarcolemmal carrier, peripheral vasodilator activity, a greater positive inotropism, and more rapid entry into myocytes. Most studies of the therapeutic use of PLC are focused on the prevention and treatment of ischemic heart disease, congestive heart failure, hypertrophic heart disease, and peripheral arterial disease. ALC and PLC are considered well tolerated without significant side-effects. A number of therapeutic effects possibly come from the interaction of carnitine and its derivatives with the elements of cellular membranes.

  14. Multifunctional Cinnamic Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Aikaterini Peperidou

    2017-07-01

    Full Text Available Our research to discover potential new multitarget agents led to the synthesis of 10 novel derivatives of cinnamic acids and propranolol, atenolol, 1-adamantanol, naphth-1-ol, and (benzylamino ethan-1-ol. The synthesized molecules were evaluated as trypsin, lipoxygenase and lipid peroxidation inhibitors and for their cytotoxicity. Compound 2b derived from phenoxyphenyl cinnamic acid and propranolol showed the highest lipoxygenase (LOX inhibition (IC50 = 6 μΜ and antiproteolytic activity (IC50 = 0.425 μΜ. The conjugate 1a of simple cinnamic acid with propranolol showed the higher antiproteolytic activity (IC50 = 0.315 μΜ and good LOX inhibitory activity (IC50 = 66 μΜ. Compounds 3a and 3b, derived from methoxylated caffeic acid present a promising combination of in vitro inhibitory and antioxidative activities. The S isomer of 2b also presented an interesting multitarget biological profile in vitro. Molecular docking studies point to the fact that the theoretical results for LOX-inhibitor binding are identical to those from preliminary in vitro study.

  15. Credit derivatives and risk management

    OpenAIRE

    Michael S. Gibson

    2007-01-01

    The striking growth of credit derivatives suggests that market participants find them to be useful tools for risk management. I illustrate the value of credit derivatives with three examples. A commercial bank can use credit derivatives to manage the risk of its loan portfolio. An investment bank can use credit derivatives to manage the risks it incurs when underwriting securities. An investor, such as an insurance company, asset manager, or hedge fund, can use credit derivatives to align its...

  16. Credit derivatives in emerging markets

    OpenAIRE

    Romain Rancière

    2002-01-01

    Credit Derivatives are securities that offer protection against credit or default risk of bonds or loans. The credit derivatives emerging market has grown rapidly and credit derivatives are widely used. This paper describes the emerging credit derivatives market structure. The current market activity is analyzed through elementary pricing dynamics and the study of the term structure of default risk. Focusing on the performance of credit derivatives in stress situation, including legal and mar...

  17. Bacterial resistance and susceptibility to antimicrobial peptides and peptidomimetics

    DEFF Research Database (Denmark)

    Citterio, Linda

    Bacterial resistance to conventional antibiotics has become a global challenge and there is urgent need for new and alternative compounds. Antimicrobial peptides (AMPs) are under investigation as novel antibiotics. These are part of the immune defense of all living organisms; hence, they represen...... be a threat to our immunity may be overestimated. In conclusion, this PhD project supports the belief that bacteria hold the potential to develop resistance to each novel antibacterial agent. Nevertheless, strategies to circumvent resistance exist and must be pursued....

  18. Antimicrobial activity of peptidomimetics against multidrug-resistant Escherichia coli

    DEFF Research Database (Denmark)

    Jahnsen, Rasmus D; Frimodt-Møller, Niels; Franzyk, Henrik

    2012-01-01

    Novel remedies in the battle against multidrug-resistant bacterial strains are urgently needed, and one obvious approach involves antimicrobial peptides and mimics hereof. The impact of a- and ß-peptoid as well as ß(3)-amino acid modifications on the activity profile against ß-lactamase-producing...

  19. Anti-inflammatory Properties of Antimicrobial Peptides and Peptidomimetics

    DEFF Research Database (Denmark)

    Skovbakke, Sarah Line; Franzyk, Henrik

    2017-01-01

    Lipopolysaccharide (LPS) and lipoteichoic acid (LTA) neutralization constitute potential non-antibiotic treatment strategies for sepsis - a systemic infection-induced inflammatory response. Studies on LPS- and LTA-neutralizing compounds are abundant in literature, and a number of peptides...

  20. In defense of derivations

    Science.gov (United States)

    Mungan, Carl E.

    2016-05-01

    At the 2015 AAPT Summer Meeting, I presented four derivations of the formula for motional emf. Such physics derivations involve the construction of explanatory frameworks involving diagrams and mathematical models. Although textbooks devote considerable space to such explanations, many teachers and students spend their time on worksheets, end-of-chapter problems, and the like. The book is reduced to a bank of solved (i.e., example) and unsolved (i.e., homework) questions, along with equations in colored boxes that presumably are to be used to answer those questions. Such an approach encourages fragmentation of knowledge, the view that there is only one right answer to a problem with the goal of physics being to find that answer (neatly boxed of course), and the inability to reason about even a slightly different (much less a novel) situation. If we are to develop scientific literacy, significant course time must be devoted to explaining the structure of and support for the models and equations we use.

  1. 6-Bromocholesterol derivatives

    International Nuclear Information System (INIS)

    Flanagan, R.J.

    1984-01-01

    Novel 6-bromo derivatives of cholesterol have the formula 3-(R-O-),6-BR,17-((H3C-)2-HC-H2C-H2C-H2C-HC(-CH3)-)-ESTR-5-ENE Such compounds are prepared from the known 6-iodocholesterol by treatment with cuprous bromide. These compounds, labelled with radioisotopes of Br-82 or Br-77, are localized in the adrenal, mammary and ovary tissue of female mammals and in the adrenal or prostate tissue of males when administered to such individuals. This provides a method for imaging adrenal, ovary or prostate tissue which is superior to use of the prior art 6-iodo-cholesterol

  2. Algae Derived Biofuel

    Energy Technology Data Exchange (ETDEWEB)

    Jahan, Kauser [Rowan Univ., Glassboro, NJ (United States)

    2015-03-31

    One of the most promising fuel alternatives is algae biodiesel. Algae reproduce quickly, produce oils more efficiently than crop plants, and require relatively few nutrients for growth. These nutrients can potentially be derived from inexpensive waste sources such as flue gas and wastewater, providing a mutual benefit of helping to mitigate carbon dioxide waste. Algae can also be grown on land unsuitable for agricultural purposes, eliminating competition with food sources. This project focused on cultivating select algae species under various environmental conditions to optimize oil yield. Membrane studies were also conducted to transfer carbon di-oxide more efficiently. An LCA study was also conducted to investigate the energy intensive steps in algae cultivation.

  3. SEMANTIC DERIVATION OF BORROWINGS

    Directory of Open Access Journals (Sweden)

    Shigapova, F.F.

    2017-09-01

    Full Text Available The author carried out the contrastive analysis of the word спикер borrowed into Russian from English and the English word speaker. The findings of the analysis include confirm (1 different derivational abilities and functions of the borrowed word and the native word; (2 distinctive features in the definitions, i.e. semantic structures, registered in monolingual non-abridged dictionaries; (3 heterogeneous parameters of frequencies recorded in the National Corpus of the Russian language and the British National Corpus; (4 absence of bilingual equivalent collocations with words спикер and speaker. The collocations with words studied revealed new lexical and connotative senses in the meaning of the word. Relevance of the study conducted is justified by the new facts revealed about the semantic adaptation of the borrowed word in the system of the Russian language and its paradigmatic and syntagmatic connections in the system of the recipient language.

  4. Original and Derived Judgment

    DEFF Research Database (Denmark)

    Foss, Kirsten; Foss, Nicolai Juul; Klein, Peter G.

    2007-01-01

    Recent work links entrepreneurship to the economic theory of the firm, using the concept of entrepreneurship as judgment introduced by Frank Knight. When judgment is complementary to other assets, it makes sense for entrepreneurs to hire labour and to own assets. The entrepreneur's role, then...... to subordinates, who exercise derived judgment. We call these employees `proxy-entrepreneurs', and ask how the firm's organizational structure - its formal and informal systems of rewards and punishments, rules for settling disputes and renegotiating agreements, means of evaluating performance and so on - can...... be designed to encourage forms of proxy entrepreneurship that increase firm value while discouraging actions that destroy value. Building on key ideas from the entrepreneurship literature, Austrian economics and the economic theory of the firm, we develop a framework for analysing the trade-off between...

  5. Piroxicam derivatives THz classification

    Science.gov (United States)

    Sterczewski, Lukasz A.; Grzelczak, Michal P.; Nowak, Kacper; Szlachetko, Bogusław; Plinska, Stanislawa; Szczesniak-Siega, Berenika; Malinka, Wieslaw; Plinski, Edward F.

    2016-02-01

    In this paper we report a new approach to linking the terahertz spectral shapes of drug candidates having a similar molecular structure to their chemical and physical parameters. We examined 27 newly-synthesized derivatives of a well-known nonsteroidal anti-inflammatory drug Piroxicam used for treatment of inflammatory arthritis and chemoprevention of colon cancer. The testing was carried out by means of terahertz pulsed spectroscopy (TPS). Using chemometric techniques we evaluated their spectral similarity in the terahertz range and attempted to link the position on the principal component analysis (PCA) score map to the similarity of molecular descriptors. A simplified spectral model preserved 75% and 85.1% of the variance in 2 and 3 dimensions respectively, compared to the input 1137. We have found that in 85% of the investigated samples a similarity of the physical and chemical parameters corresponds to a similarity in the terahertz spectra. The effects of data preprocessing on the generated maps are also discussed. The technique presented can support the choice of the most promising drug candidates for clinical trials in pharmacological research.

  6. Experts' understanding of partial derivatives using the Partial Derivative Machine

    OpenAIRE

    Roundy, David; Dorko, Allison; Dray, Tevian; Manogue, Corinne A.; Weber, Eric

    2014-01-01

    Partial derivatives are used in a variety of different ways within physics. Most notably, thermodynamics uses partial derivatives in ways that students often find confusing. As part of a collaboration with mathematics faculty, we are at the beginning of a study of the teaching of partial derivatives, a goal of better aligning the teaching of multivariable calculus with the needs of students in STEM disciplines. As a part of this project, we have performed a pilot study of expert understanding...

  7. Derivative spectrophotometry of cobalt alloys

    International Nuclear Information System (INIS)

    Spitsyn, P.K.

    1985-01-01

    The method of derivative spectrophotometry is briefly described, and derivative absorption spectra are presented for samarium, cobalt, and commercial Sm-Co alloys. It is shown that the use of derivative spectrophotometry not only improves the accuracy and selectivity of element determinations but also simplifies the analysis of alloys. Results of a statistical evaluation of the metrological characteristics of the analytical procedure described here are presented. 8 references

  8. Central Clearing of OTC Derivatives

    DEFF Research Database (Denmark)

    Cont, Rama; Kokholm, Thomas

    2014-01-01

    netting agreements. When a CCP exists for interest rate derivatives, adding a CCP for credit derivatives is shown to decrease overall exposures. These findings are shown to be robust to the statistical assumptions of the model as well as the choice of risk measure used to quantify exposures....

  9. Chemistry of aliphatic sulfurpentafluoride derivatives

    International Nuclear Information System (INIS)

    Bissell, E.R.

    1975-01-01

    This report summarizes the literature through 1974 on aliphatic sulfurpentafluoride compounds. Methods of preparation and methods of transforming one pentafluorothio compound into another are briefly discussed. The physical properties of all known derivatives are tabulated

  10. Higher derivatives in gauge transformations

    International Nuclear Information System (INIS)

    Gogilidze, S.A.; Sanadze, V.V.; Tkebuchava, F.G.

    1992-01-01

    The mechanism of appearance of highher derivatives of coordinates in the symmetry transformation law of the second Noether's theorem is established. It is shown that the corresponding transformations are canonical in the extended phase space. 15 refs

  11. Push-outs of derivations

    Indian Academy of Sciences (India)

    extension as a limit of operators b ↦→ D(ba) − b.D(a), a ∈ A in an appropriate operator topology, the main point in the proof being to show that the limit map is in fact a derivation. In this paper we make clear which part of this approach is analytic and which algebraic by presenting an algebraic scheme that gives derivations ...

  12. Elementary derivation of Kepler's laws

    International Nuclear Information System (INIS)

    Vogt, E.

    1995-02-01

    A simple derivation of all three so-called Kepler Laws is presented in which the orbits, bound and unbound, follow directly and immediately from conservation of energy and angular momentum. The intent is to make this crowning achievement of Newtonian Mechanics easily accessible to students in introductory physics courses. The method is also extended to simplify the derivation of the Rutherford Scattering Law. (author). 4 refs., 3 figs

  13. Derivatives Trading and Negative Voting

    OpenAIRE

    Spamann, Holger

    2012-01-01

    This paper exposits a model of parallel trading of corporate securities (shares, bonds) and derivatives in which a large trader can sometimes profitably acquire securities with their corporate control rights for the sole purpose of reducing the corporations value and gaining on a net short position created through off-setting derivatives. At other times, the large trader profitably takes a net long position. The large trader requires no private information beyond its own trades. The problem i...

  14. Quinazoline derivatives: synthesis and bioactivities

    OpenAIRE

    Wang, Dan; Gao, Feng

    2013-01-01

    Owing to the significant biological activities, quinazoline derivatives have drawn more and more attention in the synthesis and bioactivities research. This review summarizes the recent advances in the synthesis and biological activities investigations of quinazoline derivatives. According to the main method the authors adopted in their research design, those synthetic methods were divided into five main classifications, including Aza-reaction, Microwave-assisted reaction, Metal-mediated reac...

  15. Anisotropic inflation with derivative couplings

    Science.gov (United States)

    Holland, Jonathan; Kanno, Sugumi; Zavala, Ivonne

    2018-05-01

    We study anisotropic power-law inflationary solutions when the inflaton and its derivative couple to a vector field. This type of coupling is motivated by D-brane inflationary models, in which the inflaton, and a vector field living on the D-brane, couple disformally (derivatively). We start by studying a phenomenological model where we show the existence of anisotropic solutions and demonstrate their stability via a dynamical system analysis. Compared to the case without a derivative coupling, the anisotropy is reduced and thus can be made consistent with current limits, while the value of the slow-roll parameter remains almost unchanged. We also discuss solutions for more general cases, including D-brane-like couplings.

  16. Sol-gel derived sorbents

    Science.gov (United States)

    Sigman, Michael E.; Dindal, Amy B.

    2003-11-11

    Described is a method for producing copolymerized sol-gel derived sorbent particles for the production of copolymerized sol-gel derived sorbent material. The method for producing copolymerized sol-gel derived sorbent particles comprises adding a basic solution to an aqueous metal alkoxide mixture for a pH.ltoreq.8 to hydrolyze the metal alkoxides. Then, allowing the mixture to react at room temperature for a precalculated period of time for the mixture to undergo an increased in viscosity to obtain a desired pore size and surface area. The copolymerized mixture is then added to an immiscible, nonpolar solvent that has been heated to a sufficient temperature wherein the copolymerized mixture forms a solid upon the addition. The solid is recovered from the mixture, and is ready for use in an active sampling trap or activated for use in a passive sampling trap.

  17. Synthesis of 2-phosphaadamantane derivatives

    International Nuclear Information System (INIS)

    Zemlyanoi, V.N.; Aleksandrov, A.M.; Kukhar', V.P.

    1986-01-01

    The authors describe the synthesis and properties of 2-phosphadamantane derivatives. For the synthesis of 2-phosphaadamantane derivatives they decided to use the methodology of the synthesis of 2-thiaadamantane. The IR spectra were determined on CHCl 3 solutions with a Specord 711R spectrometer, the PMR spectra were determined on Tesla BS-467 (60 MHz) and Bruker WP-200 (200 MHz) spectrometers, external standard hexamethyldisiloxane, the 31 P NMR spectra were determined on Tesla BS-487 C (30 MHz) and Bruker WP-200 (81 MHz) spectrometers, external standard 85% phosphoric acid, and the mass spectra were determined on an MS-1302 spectrometer

  18. Bounded Densities and Their Derivatives

    DEFF Research Database (Denmark)

    Kozine, Igor; Krymsky, V.

    2009-01-01

    This paper describes how one can compute interval-valued statistical measures given limited information about the underlying distribution. The particular focus is on a bounded derivative of a probability density function and its combination with other available statistical evidence for computing ...... quantities of interest. To be able to utilise the evidence about the derivative it is suggested to adapt the ‘conventional’ problem statement to variational calculus and the way to do so is demonstrated. A number of examples are given throughout the paper....

  19. Risk Factors in Derivatives Markets

    Directory of Open Access Journals (Sweden)

    Raimonda Martinkutė-Kaulienė

    2015-02-01

    Full Text Available The objective of the article is to analyse and present the classification of risks actual to derivative securities. The analysis is based on classical and modern literature findings and analysis of newest statistical data. The analysis led to the conclusion, that the main risks typical for derivatives contracts and their traders are market risk, liquidity risk, credit and counterparty risk, legal risk and transactions risk. Pricing risk and systemic risk is also quite important. The analysis showed that market risk is the most important kind of risk that in many situations influences the level of remaining risks.

  20. Analytical application of derivative spectrophotometry

    Directory of Open Access Journals (Sweden)

    VIOLETA M. STEFANOVIC

    2000-07-01

    Full Text Available 1. Introduction 2. Basic characteristics of derivative spectrophotometry 2.1. Increase of spectra resolution 2.2. Elimination of the influence of baseline shift and matrix interferences 2.3. Enhancement of the detectability of minor spectral features 2.4. Precise determination of the positions of absorption maxima 2.5. Signal-to-noise ratio (SNR 2.6. Quantitative analysis 3. Analytical applications 3.1. Inorganic analysis 3.2. Organic and pharmaceutical analysis 3.3. Analysis of food and water 3.4. Application of derivative spectrophotometry for the determination of equilibrium constants

  1. Derived equivalences for group rings

    CERN Document Server

    König, Steffen

    1998-01-01

    A self-contained introduction is given to J. Rickard's Morita theory for derived module categories and its recent applications in representation theory of finite groups. In particular, Broué's conjecture is discussed, giving a structural explanation for relations between the p-modular character table of a finite group and that of its "p-local structure". The book is addressed to researchers or graduate students and can serve as material for a seminar. It surveys the current state of the field, and it also provides a "user's guide" to derived equivalences and tilting complexes. Results and proofs are presented in the generality needed for group theoretic applications.

  2. derivatives: Synthesis and antimicrobial evaluation

    Indian Academy of Sciences (India)

    cal activity study revealed that all compounds showed promising activities and bis-(1H-2-benzopyran-1-one) derivatives (5) ...... A and Galvez J 2004 Planta Med. 70 315. 6. ... Ante N, Erik De C, Jan B and Mladen M 2011 Molecules. 16 6023.

  3. Second derivative spectrophotometric determination of ...

    African Journals Online (AJOL)

    A new, simple, rapid, wide applicable range and reliable second derivative spectrophotometric method has been developed for determination of cyclophosphamide (CP) in bulk and pharmaceutical dosage forms. Calibration graph is linear in the concentration range of 25 - 200 μg/ml of CP with 10 μg/ml of detection limit and ...

  4. Hypoxanthine Derivatives in Experimental Infections

    Directory of Open Access Journals (Sweden)

    Claudio De Simone

    1992-01-01

    ability of ST 789 to increase interleukin-6 production, suggest that monocyte/macrophages are likely to be the main cellular target of the immunomodulating activity of ST 789. Finally, in the presentln vivo study, hypoxanthine derivatives did not enhance the mean survival time of tumour-bearing immunosuppressed mice.

  5. Radiological protection optimization using derivatives

    International Nuclear Information System (INIS)

    Freitas Acosta Perez, C. de; Sordi, G.M.A.A.

    2006-01-01

    The aim of this paper is to provide a different approach related to the integral cost-benefit and extended cost-benefit analysis used in the decision-aiding techniques. In the ICRP publication 55 the annual protection cost is envisaged as a set of points, each of them representing an option, linked by a straight line. The detriment cost function is considered a linear function whose angular coefficient is determined by the alpha value. In this paper the uranium mine example considered in the ICRP publication 55 was used. But the potential curve was introduced both in the integral cost benefit analysis and in the extended cost-benefit analysis, which the individual dose distribution attribute is added. The result was obtained using derivatives. The detriment cost, Y, is not necessary because the alpha value is known. The Y derivative dS/dY is the alpha value itself and so, the attention is directed to the derivative -dX/dS on the points that, along with the alpha value, present the optimum option. The results makes clear that the prevailing factor in the optimum option selection is the alpha value imputed, and those a single alpha value, as suggested now, probably as little efficiency on the optimization process. Obtaining a curve for the alpha value and using the derivative technique introduced in this paper, the analytical solution is more convenient and reliable compared to the one used now. (authors)

  6. Alchemical derivatives of reaction energetics

    Science.gov (United States)

    Sheppard, Daniel; Henkelman, Graeme; von Lilienfeld, O. Anatole

    2010-08-01

    Based on molecular grand canonical ensemble density functional theory, we present a theoretical description of how reaction barriers and enthalpies change as atoms in the system are subjected to alchemical transformations, from one element into another. The change in the energy barrier for the umbrella inversion of ammonia is calculated along an alchemical path in which the molecule is transformed into water, and the change in the enthalpy of protonation for methane is calculated as the molecule is transformed into a neon atom via ammonia, water, and hydrogen fluoride. Alchemical derivatives are calculated analytically from the electrostatic potential in the unperturbed system, and compared to numerical derivatives calculated with finite difference interpolation of the pseudopotentials for the atoms being transformed. Good agreement is found between the analytical and numerical derivatives. Alchemical derivatives are also shown to be predictive for integer changes in atomic numbers for oxygen binding to a 79 atom palladium nanoparticle, illustrating their potential use in gradient-based optimization algorithms for the rational design of catalysts.

  7. Radiolabeled derivatives of folic acid

    International Nuclear Information System (INIS)

    1980-01-01

    Derivatives of folic acid are described, in which the α-carboxyl group is substituted with an amino compound having an aromatic or heterocyclic ring substituent which is capable of being radiolabelled. Particularly mentioned as a radiolabel is 125 I. (author)

  8. Second derivative spectrophotometric determination of ...

    African Journals Online (AJOL)

    Hemn

    2013-11-13

    Nov 13, 2013 ... olanzapine in pharmaceutical formulation.Int.J.ChemTech. Res.2(1):756-761. Stanisz B, Paszun S, Lesniak M (2009). Validation of UV derivative spectrophotometric method for determination of benazepril hydrochloride in tablets and evaluation of its stability.ActaPoloniaePharmaceutica-Drug Research.

  9. Novel bisstyryl derivatives of bakuchiol

    DEFF Research Database (Denmark)

    Reddy, Mallepally V; Thota, Niranjan; Sangwan, Payare L

    2010-01-01

    Novel bisstyryl derivatives of bakuchiol using Heck coupling reaction as the key step were synthesized and screened against a panel of six oral cavity pathogens for their antimicrobial activity. Four compounds (9-12) showed two to fourfold and four to eightfold better activity (MIC 0.25-16 microg...

  10. Push-outs of derivations

    DEFF Research Database (Denmark)

    Grønbæk, Niels

    2008-01-01

    Let A be a Banach algebra and let X be a Banach A-bimodule. In studying H¹(A,X) it is often useful to extend a given derivation D: A->X to a Banach algebra B containing A as an ideal, thereby exploiting (or establishing) hereditary properties. This is usually done using (bounded/unbounded) approx...

  11. Asymptotic aspect of derivations in Banach algebras

    Directory of Open Access Journals (Sweden)

    Jaiok Roh

    2017-02-01

    Full Text Available Abstract We prove that every approximate linear left derivation on a semisimple Banach algebra is continuous. Also, we consider linear derivations on Banach algebras and we first study the conditions for a linear derivation on a Banach algebra. Then we examine the functional inequalities related to a linear derivation and their stability. We finally take central linear derivations with radical ranges on semiprime Banach algebras and a continuous linear generalized left derivation on a semisimple Banach algebra.

  12. Higher-derivative generalization of conformal mechanics

    Science.gov (United States)

    Baranovsky, Oleg

    2017-08-01

    Higher-derivative analogs of multidimensional conformal particle and many-body conformal mechanics are constructed. Their Newton-Hooke counterparts are derived by applying appropriate coordinate transformations.

  13. Derivatives in energy project finance

    International Nuclear Information System (INIS)

    Spencer, Lloyd

    1999-01-01

    This chapter focuses on risk management of merchant power generation projects and describes project finance as balancing risk and reward over time. The historical background to risk management is traced, and the case for derivatives in energy project finance is put forward with the hedging of forward output, and forwards and power purchase agreements discussed. Current and prospective usage, and the implementation issues of market liquidity, margin calls, letters of credit, derivative counterparty credit risk, and accounting policy are considered. A detailed example of a gas-fired plant in the US is presented with details given of the distribution of project earnings before tax. Oil field operating cashflows are examined, with reserved flow models, leverage effects, and price hedging addressed

  14. Diagnostic radio labelled polysaccharide derivatives

    International Nuclear Information System (INIS)

    Milbrath, D.S.; Ferber, R.H.; Barnett, W.E.

    1982-01-01

    A radiopharmaceutical compound for diagnosing blood clots is claimed. It is the reaction product of a compound characterized by a water-soluble polysaccharide moiety having an average of at least 0.25 anionic group per monosaccharide unit, and at least one chelating group derived from the group consisting of amino acids, substituted cyclic acid anhydrides, and carbon disulfide; and a radioactive tracer metal compound selected from In-111, Tc-99m, Cr-51, Ga-68, and a reduced pertechnetate compound

  15. Derivation of Hamiltonians for accelerators

    Energy Technology Data Exchange (ETDEWEB)

    Symon, K.R.

    1997-09-12

    In this report various forms of the Hamiltonian for particle motion in an accelerator will be derived. Except where noted, the treatment will apply generally to linear and circular accelerators, storage rings, and beamlines. The generic term accelerator will be used to refer to any of these devices. The author will use the usual accelerator coordinate system, which will be introduced first, along with a list of handy formulas. He then starts from the general Hamiltonian for a particle in an electromagnetic field, using the accelerator coordinate system, with time t as independent variable. He switches to a form more convenient for most purposes using the distance s along the reference orbit as independent variable. In section 2, formulas will be derived for the vector potentials that describe the various lattice components. In sections 3, 4, and 5, special forms of the Hamiltonian will be derived for transverse horizontal and vertical motion, for longitudinal motion, and for synchrobetatron coupling of horizontal and longitudinal motions. Hamiltonians will be expanded to fourth order in the variables.

  16. Financial Derivatives (Based on Two Supports Evaluation

    Directory of Open Access Journals (Sweden)

    Tiberiu Socaciu

    2016-07-01

    Full Text Available In this paper we build a PDE like Black-Scholes equation in hypothesis of a financial derivative that is dependent on two supports (usual is dependent only on one support, like amoption based on gold, when national currency has a great float.Keywords: Financial derivatives, derivatives evaluation, derivatives based on two supports, extended Itō like lemma.

  17. 12 CFR 403.4 - Derivative classification.

    Science.gov (United States)

    2010-01-01

    ... SAFEGUARDING OF NATIONAL SECURITY INFORMATION § 403.4 Derivative classification. (a) Use of derivative classification. (1) Unlike original classification which is an initial determination, derivative classification... 12 Banks and Banking 4 2010-01-01 2010-01-01 false Derivative classification. 403.4 Section 403.4...

  18. Clearing and settlement of exchange traded derivatives

    OpenAIRE

    John McPartland

    2009-01-01

    Derivatives are a class of financial instruments that derive their value from some underlying commodity, security, index, or other asset. Futures and options are common forms of derivatives. This article explains how clearing and settlement systems for exchange traded derivatives work.

  19. Development trends of the international derivatives market

    OpenAIRE

    Motorniuk, U.; Terebukh, M.; Kharchuk, V.

    2016-01-01

    The factors forming international derivatives market trends are researched in this article. The history of the formation of the global derivatives market was analyzed, in particular, events which have led to the growth of the derivatives market. Global derivatives market has revealed major changes in its trends and witnessed the gradual transformation of its structure, observed in recent years. Global derivatives market has revealed major changes in its trends and witnessed the gradual transf...

  20. Iron and iron derived radicals

    International Nuclear Information System (INIS)

    Borg, D.C.; Schaich, K.M.

    1987-04-01

    We have discussed some reactions of iron and iron-derived oxygen radicals that may be important in the production or treatment of tissue injury. Our conclusions challenge, to some extent, the usual lines of thought in this field of research. Insofar as they are born out by subsequent developments, the lessons they teach are two: Think fast! Think small! In other words, think of the many fast reactions that can rapidly alter the production and fate of highly reactive intermediates, and when considering the impact of competitive reactions on such species, think how they affect the microenvironment (on the molecular scale) ''seen'' by each reactive molecule. 21 refs., 3 figs., 1 tab

  1. Resorcinol derivatives from Ardisia maculosa.

    Science.gov (United States)

    Zheng, Ying; Wu, Feng-E

    2007-01-01

    Besides a series of known sterols and triterpenoids, a new resorcinol (1) and a known resorcinol (2) have been isolated from ethanol extract of Ardisia maculosa for the first time. The structures of these resorcinol derivatives were elucidated as 2-methyl-5-(Z-heptadec-8-enyl) resorcinol and 5-Z-heptadec-8-enyl) resorcinol by HRESI-MS, NMR ((1)H, (13)C, HSQC, HMBC) experiments. In our in vitro assay, compounds 1 and 2 showed no antimicrobial activities, however, compound 2 exhibited cytotoxity activity against human cancer cell line with GI(50) value of 2.14 x 10(- 4) mmol/ml.

  2. Topological Derivatives in Shape Optimization

    CERN Document Server

    Novotny, Antonio André

    2013-01-01

    The topological derivative is defined as the first term (correction) of the asymptotic expansion of a given shape functional with respect to a small parameter that measures the size of singular domain perturbations, such as holes, inclusions, defects, source-terms and cracks. Over the last decade, topological asymptotic analysis has become a broad, rich and fascinating research area from both theoretical and numerical standpoints. It has applications in many different fields such as shape and topology optimization, inverse problems, imaging processing and mechanical modeling including synthesis and/or optimal design of microstructures, sensitivity analysis in fracture mechanics and damage evolution modeling. Since there is no monograph on the subject at present, the authors provide here the first account of the theory which combines classical sensitivity analysis in shape optimization with asymptotic analysis by means of compound asymptotic expansions for elliptic boundary value problems. This book is intende...

  3. Antioxidant capacity of eugenol derivatives

    Directory of Open Access Journals (Sweden)

    María E. Hidalgo

    2009-01-01

    Full Text Available Toxicity and antioxidant capacity of eugenol derivatives (E2 = 2-Methoxy-4-[1-propenylphenyl]acetate, E3 = 4-Allyl-2-methoxyphenylacetate, E4 = 4-Allyl-2-methoxy-4-nitrophenol, E5 = 5-Allyl-3-nitrobenzene-1,2-diol, E6 = 4-Allyl-2-methoxy-5-nitrophenyl acetate were evaluated in order to determine the influence of the sustituents. E2-E6 were synthesized from eugenol (E1. E1 was extracted from cloves oil, and E2-E6 were obtained through acetylation and nitration reactions. Antioxidant capacity evaluated by DPPH (1, 1-Diphenyl-2-picrylhydrazil and ORAC fluorescein demonstrated that E1 and E5 have a higher capacity and the minor toxicity evaluated by red blood cells haemolysis and the Artemia saline test. In accordance with our results, the compound's (E1-E5 use in the pharmaceutical, cosmetic and or food industries could be suggested.

  4. Cytotoxicity study of pyrazole derivatives

    Directory of Open Access Journals (Sweden)

    Nusrat Binta Ahasan

    2007-06-01

    Full Text Available Pyrazolone heterocyclic compound, 3-methyl-1-phenyl-2-pyrazoline-5-one 2(a was synthesized by condensation reaction between ethyl acetoacetate and phenyl hydrazine and was converted into their corresponding heterocyclic derivatives 2(b to 2(f2 . Their cytotoxicity effects were measured by brine shrimp lethality bioassay. Among them the compounds 2(b , 2(f1 , and 2(f2 were highly active according to IC50 values 19.50, 19.50 and 20 ppm respectively. The rest of compounds 2(a , 2(c , 2(d1 , and 2(d2 having IC50 values 38, 33.50, 37.50, 36, 37.50 and 36 ppm in that order, were moderately active.

  5. Cytotoxicity study of pyrazole derivatives

    Directory of Open Access Journals (Sweden)

    Nusrat Binta Ahasan and Md. Rabiul Islam

    2007-12-01

    Full Text Available Pyrazolone heterocyclic compound, 3-methyl-1-phenyl-2-pyrazoline-5-one 2(a was synthesized by condensation reaction between ethyl acetoacetate and phenyl hydrazine and was converted into their corresponding heterocyclic derivatives 2(b to 2(f2. Their cytotoxicity effects were measured by brine shrimp lethality bioassay. Among them the compounds 2(b, 2(f1, and 2(f2 were highly active according to IC50 values 19.50, 19.50 and 20 ppm respectively. The rest of compounds 2(a, 2(c, 2(d1, and 2(d2 having IC50 values 38, 33.50, 37.50, 36, 37.50 and 36 ppm in that order, were moderately active.

  6. Silsesquioxane-derived ceramic fibres

    Science.gov (United States)

    Hurwitz, F. I.; Farmer, S. C.; Terepka, F. M.; Leonhardt, T. A.

    1991-01-01

    Fibers formed from blends of silsesquioxane polymers were characterized to study the pyrolytic conversion of these precursors to ceramics. The morphology of fibers pyrolyzed to 1400 C revealed primarily amorphous glasses whose conversion to beta-SiC is a function of both blend composition and pyrolysis conditions. Formation of beta-SiC crystallites within the glassy phase is favored by higher than stoichiometric C/Si ratios, while carbothermal reduction of Si-O bonds to form SiC with loss of SiO and CO occurs at higher methyl/phenylpropyl silsesquioxane (lower C/Si) ratios. As the carbothermal reduction is assumed to be diffusion controlled, the fibers can serve as model systems to gain understanding of the silsesquioxane pyrolysis behavior, and therefore are useful in the development of polysilsesquioxane-derived ceramic matrices and coatings as well.

  7. Radiation processing of polysaccharide derivatives

    International Nuclear Information System (INIS)

    Yoshii, Fumio

    2004-01-01

    Carboxymethylcellulose (CMC), carboxymethylstarch (CMS), carboxymethylchitin (CM-chitin) and carboxymethylchitosan (CM-chitosan) form gels when irradiated at paste-like condition. Bedsore prevention mat filled up CMC hydrogel crosslinked by irradiation at paste-like condition was practical applied as a health care products. It was found that CM-chitosan hydrogels have anti-microbial activity and effective as absorbents to remove metal ions. When crosslinked gel sheets of CM-chitin and CM-chitosan were immersed in copper (II) aqueous solution, absorption of Cu (II) were 161 mg/g and 172 mg/g, respectively. Radiation crosslinking of cellulose derivative such as hydroxypropyl methylcellulose phthalate, (HPMCP) kneaded with aqueous alkali solution and methanol was achieved with EB-irradiation at paste-like condition. The HPMCP gel absorbed organic solvents such as chloroform and pyridine. (author)

  8. Derived limits for surface contamination

    CERN Document Server

    Wrixon, A D; Linsley, G S; White, D F

    1979-01-01

    Derived limits (DLs) for surface contamination were first established for use in the nuclear energy industry where a wide variety of radionuclides is encountered. They were later used in factories, hospitals, and universities, where the radionuclides used are normally fewer in number, either known or readily identifiable, and often of low toxicity. In these situations the current limits are frequently over-restrictive. This report describes a reassessment of the values in the light of more recent information on the possible pathways of exposure and the dose equivalent limits given in ICRP Publication 26. The reassessment is prompted also by the introduction of SI units. The results of the reassessment are used to produce a classification of DLs for all radionuclides for active and inactive area surfaces and for skin.

  9. Derivation of the dipole map

    International Nuclear Information System (INIS)

    Ali, Halima; Punjabi, Alkesh; Boozer, Allen

    2004-01-01

    In our method of maps [Punjabi et al., Phy. Rev. Lett. 69, 3322 (1992), and Punjabi et al., J. Plasma Phys. 52, 91 (1994)], symplectic maps are used to calculate the trajectories of magnetic field lines in divertor tokamaks. Effects of the magnetic perturbations are calculated using the low MN map [Ali et al., Phys. Plasmas 11, 1908 (2004)] and the dipole map [Punjabi et al., Phys. Plasmas 10, 3992 (2003)]. The dipole map is used to calculate the effects of externally located current carrying coils on the trajectories of the field lines, the stochastic layer, the magnetic footprint, and the heat load distribution on the collector plates in divertor tokamaks [Punjabi et al., Phys. Plasmas 10, 3992 (2003)]. Symplectic maps are general, efficient, and preserve and respect the Hamiltonian nature of the dynamics. In this brief communication, a rigorous mathematical derivation of the dipole map is given

  10. Landslide in claystone derived soil

    Energy Technology Data Exchange (ETDEWEB)

    Richardson, A M

    1979-07-01

    This article describes a landslide that occured in the Pittsburgh area in a soil deposit derived from the Pittsburgh Redbed Claystone when a cut was made at the toe. (The Pittsburgh Redbed Claystone is the parent of much of the soil material involved in the Pittsburgh area and occurs about mid way between the base of Pittsburgh Coal and the top of the Upper Freepost Coal). The topography before the slide was known and the geometry of the slide mass was established. Slope stability analysis indicated that the landslide could have been predicted using effective stress-shear-strength parameters of s of 12 to 13 and c is 0, where s is angle of shearing resistance and c is cohesion intercept in terms of effective stresses.

  11. THE SPECIFICITY OF KERATEINE DERIVATIVES.

    Science.gov (United States)

    Pillemer, L; Ecker, E E; Martiensen, E W

    1939-09-30

    Carboxymethyl, alpha-carboxyethyl-, alpha-carboxy-n-propyl-, alpha-carboxyisopropyl-, alpha-carboxy-n-butyl, alpha-carboxyisobutyl, alpha-carboxyamyl-, benzyl-, and beta-phenylethylkeratemes were prepared from the parent protein, reduced keratin or kerateine. Chemical analysis disclosed that the various compounds differed in their isoelectric points and solubilities depending on the nature of the substituent group introduced. In general, it was found that in so far as could be determined, nearly all of the available sulfhydryl groups were substituted, while no detectable substitution of the free amino groups of the proteins occurred. The results of the serologic studies revealed that the kerateine derivatives acquired a new immunologie character dependent on the nature of the introduced determinant group. Inhibition tests confirmed the results obtained. Evidence was also produced to show that the grouping See PDF for structure may play a rôle in some of the reactions observed.

  12. Penetratin and derivatives acting as antifungal agents

    NARCIS (Netherlands)

    Masman, Marcelo F.; Rodriguez, Ana M.; Raimondi, Marcela; Zacchino, Susana A.; Luiten, Paul G. M.; Somlai, Csaba; Kortvelyesi, Tamas; Penke, Botond; Enriz, Ricardo D.

    The synthesis, in vitro evaluation, and conformational study of RQIKTWFQNRRMKWKK-NH(2) (penetratin) and related derivatives acting as antifungal agents are reported. Penetratin and some of its derivatives displayed antifungal activity against the human opportunistic pathogenic standardized ATCC

  13. Nature of the basic financial derivatives

    OpenAIRE

    Kats, Svetlana

    2014-01-01

    The article reveals the essence of basic derivatives. Studied by various authors approaches to defining derivatives and their definitions in the legislation and proposed his own definition of the most appropriate for use in accounting practice.

  14. fq-Derivations of G-Algebra

    Directory of Open Access Journals (Sweden)

    Deena Al-Kadi

    2016-01-01

    Full Text Available We introduce the notion of fq-derivation as a new derivation of G-algebra. For an endomorphism map f of any G-algebra X, we show that at least one fq-derivation of X exists. Moreover, for such a map, we show that a self-map dqf of X is fq-derivation of X if X is an associative medial G-algebra. For a medial G-algebra X, dqf is fq-derivation of X if dqf is an outside fq-derivation of X. Finally, we show that if f is the identity endomorphism of X then the composition of two fq-derivations of X is a fq-derivation. Moreover, we give a condition to get a commutative composition.

  15. Polymer-Derived Ceramic Fibers

    Science.gov (United States)

    Ichikawa, Hiroshi

    2016-07-01

    SiC-based ceramic fibers are derived from polycarbosilane or polymetallocarbosilane precursors and are classified into three groups according to their chemical composition, oxygen content, and C/Si atomic ratio. The first-generation fibers are Si-C-O (Nicalon) fibers and Si-Ti-C-O (Tyranno Lox M) fibers. Both fibers contain more than 10-wt% oxygen owing to oxidation during curing and lead to degradation in strength at temperatures exceeding 1,300°C. The maximum use temperature is 1,100°C. The second-generation fibers are SiC (Hi-Nicalon) fibers and Si-Zr-C-O (Tyranno ZMI) fibers. The oxygen content of these fibers is reduced to less than 1 wt% by electron beam irradiation curing in He. The thermal stability of these fibers is improved (they are stable up to 1,500°C), but their creep resistance is limited to a maximum of 1,150°C because their C/Si atomic ratio results in excess carbon. The third-generation fibers are stoichiometric SiC fibers, i.e., Hi-Nicalon Type S (hereafter Type S), Tyranno SA, and Sylramic™ fibers. They exhibit improved thermal stability and creep resistance up to 1,400°C. Stoichiometric SiC fibers meet many of the requirements for the use of ceramic matrix composites for high-temperature structural application. SiBN3C fibers derived from polyborosilazane also show promise for structural applications, remain in the amorphous state up to 1,800°C, and have good high-temperature creep resistance.

  16. 40 CFR 721.1820 - Bisphenol derivative.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Bisphenol derivative. 721.1820 Section... Substances § 721.1820 Bisphenol derivative. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as bisphenol derivative (PMN No. P-92-509) is...

  17. 45 CFR 601.5 - Derivative classification.

    Science.gov (United States)

    2010-10-01

    ... CLASSIFICATION AND DECLASSIFICATION OF NATIONAL SECURITY INFORMATION § 601.5 Derivative classification. Distinct... 45 Public Welfare 3 2010-10-01 2010-10-01 false Derivative classification. 601.5 Section 601.5... classification guide, need not possess original classification authority. (a) If a person who applies derivative...

  18. 5 CFR 1312.7 - Derivative classification.

    Science.gov (United States)

    2010-01-01

    ..., DOWNGRADING, DECLASSIFICATION AND SAFEGUARDING OF NATIONAL SECURITY INFORMATION Classification and Declassification of National Security Information § 1312.7 Derivative classification. A derivative classification... 5 Administrative Personnel 3 2010-01-01 2010-01-01 false Derivative classification. 1312.7 Section...

  19. 6 CFR 7.26 - Derivative classification.

    Science.gov (United States)

    2010-01-01

    ... 6 Domestic Security 1 2010-01-01 2010-01-01 false Derivative classification. 7.26 Section 7.26 Domestic Security DEPARTMENT OF HOMELAND SECURITY, OFFICE OF THE SECRETARY CLASSIFIED NATIONAL SECURITY INFORMATION Classified Information § 7.26 Derivative classification. (a) Derivative classification is defined...

  20. 22 CFR 9.6 - Derivative classification.

    Science.gov (United States)

    2010-04-01

    ... 22 Foreign Relations 1 2010-04-01 2010-04-01 false Derivative classification. 9.6 Section 9.6 Foreign Relations DEPARTMENT OF STATE GENERAL SECURITY INFORMATION REGULATIONS § 9.6 Derivative classification. (a) Definition. Derivative classification is the incorporating, paraphrasing, restating or...

  1. Quantum derivatives and the Schroedinger equation

    International Nuclear Information System (INIS)

    Ben Adda, Faycal; Cresson, Jacky

    2004-01-01

    We define a scale derivative for non-differentiable functions. It is constructed via quantum derivatives which take into account non-differentiability and the existence of a minimal resolution for mean representation. This justify heuristic computations made by Nottale in scale-relativity. In particular, the Schroedinger equation is derived via the scale-relativity principle and Newton's fundamental equation of dynamics

  2. 12 CFR 563.172 - Financial derivatives.

    Science.gov (United States)

    2010-01-01

    ... underlying assets, indices, or reference rates. The most common types of financial derivatives are futures, forward commitments, options, and swaps. A mortgage derivative security, such as a collateralized mortgage... 12 Banks and Banking 5 2010-01-01 2010-01-01 false Financial derivatives. 563.172 Section 563.172...

  3. Deriving the bond pricing equation

    Directory of Open Access Journals (Sweden)

    Kožul Nataša

    2014-01-01

    Full Text Available Given the recent focus on Eurozone debt crisis and the credit rating downgrade not only of US debt, but that of other countries and many UK major banking institutions, this paper aims to explain the concept of bond yield, its different measures and bond pricing equation. Yields on capital market instruments are rarely quoted on the same basis, which makes direct comparison between different as investment choices impossible. Some debt instruments are quoted on discount basis, whilst coupon-bearing ones accrue interest differently, offer different compounding opportunities, have different coupon payment frequencies, and manage non-business day maturity dates differently. Moreover, rules governing debt vary across countries, markets and currencies, making yield calculation and comparison a rather complex issue. Thus, some fundamental concepts applicable to debt instrument yield measurement, with focus on bond equation, are presented here. In addition, bond equation expressed in annuity form and used to apply Newton-Raphson algorithm to derive true bond yield is also shown.

  4. Classical gravity with higher derivatives

    International Nuclear Information System (INIS)

    Stelle, K.S.

    1978-01-01

    Inclusion of the four-derivative terms ∫Rsub(μν) Rsup(μν)(-g)sup(1/2) and ∫R 2 (-g)sup(1/2) into the gravitational action gives a class of effectively multimass models of gravity. In addition to the usual massless excitations of the field, there are now, for general amounts of the two new terms, massive spin-two and massive scalar excitations, with a total of eight degrees of freedom. The massive spin-two part of the field has negative energy. Specific ration of the two new terms give models with either the massive tensor or the massive scalar missing, with correspondingly fewer degrees of freedom. The static, linearized solutions of the field equations are combinations of Newtonian and Yukawa potentials. Owing to the Yukawa form of the corrections, observational evidence sets only very weak restrictions on the new masses. The acceptable static metric solutions in the full nonlinear theory are regular at the origin. The dynamical content of the linearized field is analyzed by reducing the fourth-order field equations to separated second-order equations, related by coupling to external sources in a fixed ratio. This analysis is carried out into the various helicity components using the transverse-traceless decomposition of the metric. (author)

  5. The estimation of derived limits

    International Nuclear Information System (INIS)

    Harrison, N.T.; Bryant, P.M.; Clarke, R.H.; Morley, F.

    1979-08-01

    In practical radiation protection, it is often necessary to calculate limits of intake of radionuclides associated with various quantities; such limits are needed, for example, to assess the adequacy of the control of environmental contamination. In publication 26 of the International Commission on Radiological Protection (ICRP), these limits, when related to the basic limits of dose-equivalent by a defined model, are referred to as Derived Limits (DLs). In the present report the principles to be adopted by the Board in calculating DLs to be recommended for general application within the United Kingdom are outlined. DLs will be recommended for a wide range of radionuclides and for circumstances relevant to the workplace, and, more frequently, the general environment. The latter will include DLs in foodstuffs and associated environmental materials, such as soil and grass, and DLs for discharges from stacks. DLs will be related to dose equivalents for workers or members of the public for stochastic or non-stochastic effects as appropriate. Consideration will be given to relevant data on radiosensitivity, metabolism and dosimetry for children and to the physicochemical forms of radionuclides. (author)

  6. Option Derivatives in Electricity Hedging

    Directory of Open Access Journals (Sweden)

    P. Pavlátka

    2010-01-01

    Full Text Available Despite the high volatility of electricity prices, there is still little demand for electricity power options, and the liquidity on the power exchanges of these power derivatives is quite low. One of the reasons is the uncertainty about how to evaluate these electricity options and about finding the right fair value of this product. Hedging of electricity is associated mainly with products such as futures and forwards. However, due to new trends in electricity trading and hedging, it is also useful to think more about options and the principles for working with them in hedging various portfolio positions and counterparties. We can quite often encounter a situation when we need to have a perfect hedge for our customer’s (end user consuming electricity portfolio, or we have to evaluate the volumetric risk (inability of a customer to predict consumption, which is very similar to selling options. Now comes the moment to compare the effects of using options or futures to hedge these open positions. From a practical viewpoint, the Black-Scholes prices appear to be the best available and the simplest method for evaluating option premiums, but there are some limitations that we have to consider.

  7. 21 CFR 184.1685 - Rennet (animal-derived) and chymosin preparation (fermentation-derived).

    Science.gov (United States)

    2010-04-01

    ... (fermentation-derived). 184.1685 Section 184.1685 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... (animal-derived) and chymosin preparation (fermentation-derived). (a)(1) Rennet and bovine rennet are... clear solution containing the active enzyme chymosin (E.C. 3.4.23.4). It is derived, via fermentation...

  8. Drug Nanoparticle Formulation Using Ascorbic Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Kunikazu Moribe

    2011-01-01

    Full Text Available Drug nanoparticle formulation using ascorbic acid derivatives and its therapeutic uses have recently been introduced. Hydrophilic ascorbic acid derivatives such as ascorbyl glycoside have been used not only as antioxidants but also as food and pharmaceutical excipients. In addition to drug solubilization, drug nanoparticle formation was observed using ascorbyl glycoside. Hydrophobic ascorbic acid derivatives such as ascorbyl mono- and di-n-alkyl fatty acid derivatives are used either as drugs or carrier components. Ascorbyl n-alkyl fatty acid derivatives have been formulated as antioxidants or anticancer drugs for nanoparticle formulations such as micelles, microemulsions, and liposomes. ASC-P vesicles called aspasomes are submicron-sized particles that can encapsulate hydrophilic drugs. Several transdermal and injectable formulations of ascorbyl n-alkyl fatty acid derivatives were used, including ascorbyl palmitate.

  9. Perturbative reduction of derivative order in EFT

    Science.gov (United States)

    Glavan, Dražen

    2018-02-01

    Higher derivative corrections are ubiquitous in effective field theories, which seemingly introduces new degrees of freedom at successive orders. This is actually an artefact of the implicit local derivative expansion defining effective field theories. We argue that higher derivative corrections that introduce additional degrees of freedom should be removed and their effects captured either by lower derivative corrections, or special combinations of higher derivative corrections not propagating extra degrees of freedom. Three methods adapted for this task are examined and field redefinitions are found to be most appropriate. First order higher derivative corrections in a scalar tensor theory are removed by field redefinition and it is found that their effects are captured by a subset of Horndeski theories. A case is made for restricting the effective field theory expansions in principle to only terms not introducing additional degrees of freedom.

  10. Weather Derivatives – Origin, Types and Application

    Directory of Open Access Journals (Sweden)

    Piotr Binkowski

    2008-01-01

    Full Text Available The number of companies that are exposed to the revenues loss risk caused by weather variability is still increasing. The businesses that are mostly exposed to weather risk are following: energy, agriculture, constructions and transport. That situation has initiated dynamic growth of weather derivatives markets as well as the awareness of the weather risk among the market participants. Presently, the weather derivatives markets evaluate rapidly in all the mature economies: USA, Asia and Europe. Constructing weather derivatives relies on qu- antifying climate factors in the form of indexes, what is quite simple task, more difficultly can be gathering precise historical data of required climate factors. Taking into consideration so far development of derivatives especially the financial derivatives based on different types of indexes financial market has at disposal wide range of different types of proved derivatives (futures, forward, options, swaps, which can be successfully utilised on the weather-driven markets both for hedging weather risk and speculating.

  11. Derivative pricing based on local utility maximization

    OpenAIRE

    Jan Kallsen

    2002-01-01

    This paper discusses a new approach to contingent claim valuation in general incomplete market models. We determine the neutral derivative price which occurs if investors maximize their local utility and if derivative demand and supply are balanced. We also introduce the sensitivity process of a contingent claim. This process quantifies the reliability of the neutral derivative price and it can be used to construct price bounds. Moreover, it allows to calibrate market models in order to be co...

  12. Chromatic Derivatives, Chromatic Expansions and Associated Spaces

    OpenAIRE

    Ignjatovic, Aleksandar

    2009-01-01

    This paper presents the basic properties of chromatic derivatives and chromatic expansions and provides an appropriate motivation for introducing these notions. Chromatic derivatives are special, numerically robust linear differential operators which correspond to certain families of orthogonal polynomials. Chromatic expansions are series of the corresponding special functions, which possess the best features of both the Taylor and the Shannon expansions. This makes chromatic derivatives and ...

  13. Quantile driven identification of structural derivatives

    OpenAIRE

    Andrew Chesher

    2001-01-01

    Conditions are derived under which there is local nonparametric identification of derivatives of structural equations in nonlinear triangular simultaneous equations systems. The attack on this problem is via conditional quantile functions and exploits local quantile independence conditions. The identification conditions include local analogues of the order and rank conditions familiar in the analysis of linear simultaneous equations models. The objects whose identification is sought are deriv...

  14. Isotope-labelled folic acid derivatives

    International Nuclear Information System (INIS)

    Lewin, N.; Wong, E.T.

    1976-01-01

    The suggestion deals with the production of folic acid derivatives suitable as indicators or tracers for analyses of serum folates. These folic acid derivatives contain folic acid which is bound by one or both carboxyl groups to the amino nitrogen of compounds such as, e.g., tyramine, glycyl tyrosine, tyrosine, or the methyl ester of tyrosine. The derivative obtained can be substituted by a gamma emitter, e.g. the iodine isotope I 125. The radioactive derivative is used in the method for the competitive protein bonding to determine endogenic folates in the serum. (UWI) [de

  15. Superstability for Generalized Module Left Derivations and Generalized Module Derivations on a Banach Module (I

    Directory of Open Access Journals (Sweden)

    Rassias JM

    2009-01-01

    Full Text Available We discuss the superstability of generalized module left derivations and generalized module derivations on a Banach module. Let be a Banach algebra and a Banach -module, and . The mappings , and are defined and it is proved that if (resp., is dominated by then is a generalized (resp., linear module- left derivation and is a (resp., linear module- left derivation. It is also shown that if (resp., is dominated by then is a generalized (resp., linear module- derivation and is a (resp., linear module- derivation.

  16. Derivative analyticity relations and asymptotic energies

    International Nuclear Information System (INIS)

    Fischer, J.

    1976-01-01

    On the basis of general principles of the S-matrix theory theorems are derived showing that derivative analyticity relations analogous to those of Bronzen, Kane and Sukhatme hold at asymptotic energies if the high-energy limits of certain physical quantities exist

  17. 28 CFR 17.26 - Derivative classification.

    Science.gov (United States)

    2010-07-01

    ... 28 Judicial Administration 1 2010-07-01 2010-07-01 false Derivative classification. 17.26 Section 17.26 Judicial Administration DEPARTMENT OF JUSTICE CLASSIFIED NATIONAL SECURITY INFORMATION AND ACCESS TO CLASSIFIED INFORMATION Classified Information § 17.26 Derivative classification. (a) Persons...

  18. 5 CFR 2500.5 - Derivative classification.

    Science.gov (United States)

    2010-01-01

    ... 5 Administrative Personnel 3 2010-01-01 2010-01-01 false Derivative classification. 2500.5 Section 2500.5 Administrative Personnel OFFICE OF ADMINISTRATION, EXECUTIVE OFFICE OF THE PRESIDENT INFORMATION SECURITY REGULATION § 2500.5 Derivative classification. The Office of Administration serves only as the...

  19. Derivative Securities and Financial Crisis in Romania

    OpenAIRE

    Gogoncea Ramona

    2012-01-01

    This paper aims to investigate the impact of the global financial crisis on the young Romanian market of derivative securities. It also describes the recent developments within Romanian capital market, in general, with focus on innovation in the field of derivative products.

  20. 46 CFR 503.55 - Derivative classification.

    Science.gov (United States)

    2010-10-01

    ... Security Program § 503.55 Derivative classification. (a) In accordance with Part 2 of Executive Order 12958 and directives of the Information Security Oversight Office, the incorporation, paraphrasing... 46 Shipping 9 2010-10-01 2010-10-01 false Derivative classification. 503.55 Section 503.55...

  1. Synthesis and Cytotoxicity of Novel Hexahydrothienocycloheptapyridazinone Derivatives

    Directory of Open Access Journals (Sweden)

    Irene Marchesi

    2009-09-01

    Full Text Available Designed as a new group of tricyclic molecules containing the thienocycloheptapyridazinone ring system, a number of 2N-substituted-hexahydrothienocycloheptapyridazinone derivatives were synthesized and their biological activity evaluated. Among the synthesized compounds, derivatives 7d and 7h were found to possess cytotoxic activity against non-small cell lung cancer and central nervous system cancer cell lines, respectively.

  2. "Nonmorphological Derivations" and the Four Main English ...

    African Journals Online (AJOL)

    This article addresses the problem of "nonmorphological derivations" in English and its consequences for pedagogical lexicography, i.e. learner's dictionaries. The term "nonmorphological derivation" refers to cases such as sun — solar, moon — lunar, cat — feline, and in general to all cases where instead of, or in addition ...

  3. Mesogenic benzothiazole derivatives with methoxy substituents

    Indian Academy of Sciences (India)

    Unknown

    2003-10-11

    Oct 11, 2003 ... literature. Barbera et al14 have synthesized 2-pyr- azoline derivatives and also studied the optical,. NLO and mesogenic properties of such materials. Highly polar thiophene-based liquid crystals have also been reported15 in the literature. However, fused ring heterocyclic derivatives which are two conden-.

  4. Deriving force field parameters for coordination complexes

    DEFF Research Database (Denmark)

    Norrby, Per-Ola; Brandt, Peter

    2001-01-01

    The process of deriving molecular mechanics force fields for coordination complexes is outlined. Force field basics are introduced with an emphasis on special requirements for metal complexes. The review is then focused on how to set up the initial model, define the target, refine the parameters......, and validate the final force field, Alternatives to force field derivation are discussed briefly....

  5. Weyl and Marchaud Derivatives: A Forgotten History

    Directory of Open Access Journals (Sweden)

    Fausto Ferrari

    2018-01-01

    Full Text Available In this paper, we recall the contribution given by Hermann Weyl and André Marchaud to the notion of fractional derivative. In addition, we discuss some relationships between the fractional Laplace operator and Marchaud derivative in the perspective to generalize these objects to different fields of the mathematics.

  6. Weyl and Marchaud derivatives: a forgotten history

    OpenAIRE

    Ferrari, Fausto

    2017-01-01

    In this paper, we recall the contribution given by Hermann Weyl and André Marchaud to the notion of fractional derivative. In addition, we discuss some relationships between the fractional Laplace operator and Marchaud derivative in the perspective to generalize these objects to different fields of the mathematics.

  7. New uracil derivatives and their biological activity

    International Nuclear Information System (INIS)

    Hudecova, D.; Striganova, J.; Chovanec, P.; Uher, M.

    1998-01-01

    Present study is concentrated to the research of antimicrobial activity of some derivatives of the uracil and 1,3-dimethyluracyl. The antimicrobial effects of these compounds have been tested on various strains of bacteria, yeasts, and filamentous fungi. The highest antimicrobial effects were found with dithiocarbamato-derivatives, which were effective against pathogenic and non-pathogenic bacteria (IC 50 = 7-25 μg cm -3 ), yeasts (IC 50 = 9-60 μg cm -3 ) and filamentous fungi.The most sensitive fungus to dithiocarbamato-derivatives was Botritis cinerea. It seems to be apparent that the presence of the -NH-C(S)-S- group in molecules of derivatives of uracil and and 1,3-dimethyluracyl influencing the incorporation rate [ 14 ]-adenine and 14 ]-leucine into the biomolecules and also markedly inhibits oxygen consumption (IC 50 = 58 μg cm -3 ). The same derivative demonstrated no mutagenic activity. (authors)

  8. Generalized Fractional Derivative Anisotropic Viscoelastic Characterization

    Directory of Open Access Journals (Sweden)

    Harry H. Hilton

    2012-01-01

    Full Text Available Isotropic linear and nonlinear fractional derivative constitutive relations are formulated and examined in terms of many parameter generalized Kelvin models and are analytically extended to cover general anisotropic homogeneous or non-homogeneous as well as functionally graded viscoelastic material behavior. Equivalent integral constitutive relations, which are computationally more powerful, are derived from fractional differential ones and the associated anisotropic temperature-moisture-degree-of-cure shift functions and reduced times are established. Approximate Fourier transform inversions for fractional derivative relations are formulated and their accuracy is evaluated. The efficacy of integer and fractional derivative constitutive relations is compared and the preferential use of either characterization in analyzing isotropic and anisotropic real materials must be examined on a case-by-case basis. Approximate protocols for curve fitting analytical fractional derivative results to experimental data are formulated and evaluated.

  9. Combinatorial assembly of small molecules into bivalent antagonists of TrkC or TrkA receptors.

    Directory of Open Access Journals (Sweden)

    Fouad Brahimi

    Full Text Available A library of peptidomimetics was assembled combinatorially into dimers on a triazine-based core. The pharmacophore corresponds to β-turns of the neurotrophin polypeptides neurotrophin-3 (NT-3, nerve growth factor (NGF, or brain-derived neurotrophic factor (BDNF. These are the natural ligands for TrkC, TrkA, and TrkB receptors, respectively. The linker length and the side-chain orientation of each monomer within the bivalent mimics were systematically altered, and the impact of these changes on the function of each ligand was evaluated. While the monovalent peptidomimetics had no detectable binding or bioactivity, four bivalent peptidomimetics (2c, 2d, 2e, 3f are selective TrkC ligands with antagonistic activity, and two bivalent peptidomimetics (1a, 1b are TrkC and TrkA ligands with antagonistic activity. All these bivalent compounds block ligand-dependent receptor activation and cell survival, without affecting neuritogenic differentiation. This work adds to our understanding of how the neurotrophins function through Trk receptors, and demonstrates that peptidomimetics can be designed to selectively disturb specific biological signals, and may be used as pharmacological probes or as therapeutic leads. The concept of altering side-chain, linker length, and sequence orientation of a subunit within a pharmacophore provides an easy modular approach to generate larger libraries with diversified bioactivity.

  10. Risk management, derivatives and shariah compliance

    Science.gov (United States)

    Bacha, Obiyathulla Ismath

    2013-04-01

    Despite the impressive growth of Islamic Banking and Finance (IBF), a number of weaknesses remain. The most important of this is perhaps the lack of shariah compliant risk management tools. While the risk sharing philosophy of Islamic Finance requires the acceptance of risk to justify returns, the shariah also requires adherents to avoid unnecessary risk-maysir. The requirement to avoid maysir is in essence a call for the prudent management of risk. Contemporary risk management revolves around financial engineering, the building blocks of which are financial derivatives. Despite the proven efficacy of derivatives in the management of risk in the conventional space, shariah scholars appear to be suspicious and uneasy with their use in IBF. Some have imposed outright prohibition of their use. This paper re-examines the issue of contemporary derivative instruments and shariah compliance. The shariah compatibility of derivatives is shown in a number of ways. First, by way of qualitative evaluation of whether derivatives can be made to comply with the key prohibitions of the sharia. Second, by way of comparing the payoff profiles of derivatives with risk sharing finance and Bai Salam contracts. Finally, the equivalence between shariah compliant derivatives like the IPRS and Islamic FX Currency Forwards with conventional ones is presented.

  11. On derived groups of division rings II

    International Nuclear Information System (INIS)

    Mahdavi Hezavehi, M.; Akbari Feyzaabaadi, S.; Mehraabaadi, M.; Hajie Abolhassan, H.

    1995-05-01

    Let D be a division ring with centre F and denote by D' the derived group (commutator subgroup) of D * = D - {0}. It is shown that if each element of D' is algebraic over F, then D is algebraic over F. It is also proved that each finite separable extension of F in D is of the form F(c) for some element c in the derived group D'. Using these results, it is shown that if each element of the derived group D' is of bounded degree over F, then D is finite dimensional over F. (author). 5 refs

  12. Derivation of GFDM Based on OFDM Principles

    Energy Technology Data Exchange (ETDEWEB)

    Hussein Moradi; Behrouz Farhang-Boroujeny

    2015-06-01

    This paper starts with discussing the principle based on which the celebrated orthogonal frequency division multiplexing (OFDM) signals are constructed. It then extends the same principle to construct the newly introduced generalized frequency division multiplexing (GFDM) signals. This novel derivation sheds light on some interesting properties of GFDM. In particular, our derivation seamlessly leads to an implementation of GFDM transmitter which has significantly lower complexity than what has been reported so far. Our derivation also facilitates a trivial understanding of how GFDM (similar to OFDM) can be applied in MIMO channels.

  13. Mechanism of Platinum Derivatives Induced Kidney Injury

    Directory of Open Access Journals (Sweden)

    Feifei YAN

    2015-09-01

    Full Text Available Platinum derivatives are the most widely used chemotherapeutic agents to treat solid tumors including ovarian, head and neck, and testicular germ cell tumors, lung cancer, and colorectal cancer. Two major problems exist, however, in the clinic use of platinum derivatives. One is the development of tumor resistance to the drug during therapy, leading to treatment failure. The other is the drug’s toxicity such as the cisplatin’s nephrotoxicity, which limits the dose that can be administered. This paper describes the mechanism of platinum derivatives induced kidney injury.

  14. MANGROVE-DERIVED NUTRIENTS AND CORAL REEFS

    Science.gov (United States)

    Understanding the consequences of the declining global cover of mangroves due to anthropogenic disturbance necessitates consideration of how mangrove-derived nutrients contribute to threatened coral reef systems. We sampled potential sources of organic matter and a suite of sessi...

  15. Preparation of 7-substituted ginkgolide derivatives

    DEFF Research Database (Denmark)

    Vogensen, Stine Byskov; Strømgaard, Kristian; Shindou, Hideo

    2003-01-01

    alpha-fluoro ginkgolide B was equipotent to ginkgolide B underlining the critical importance of the 7-position of ginkgolides for PAF receptor activity. Herein we describe the synthesis of a series of ginkgolide B derivatives with modifications at the 7-position and the pharmacological evaluation...... of these derivatives as assayed by cloned PAF receptors. In two cases nucleophilic attack on a 7beta-O-triflate ginkgolide B did not lead to the expected products, but gave rise to two unprecedented ginkgolide derivatives, one with a novel rearranged skeleton. Furthermore, standard reduction of 7alpha-azido ginkgolide......-chloro ginkgolide B, the most potent nonaromatic ginkgolide derivative described to date with a K(i) value of 110 nM....

  16. Patient-Derived Antibody Targets Tumor Cells

    Science.gov (United States)

    An NCI Cancer Currents blog on an antibody derived from patients that killed tumor cells in cell lines of several cancer types and slowed tumor growth in mouse models of brain and lung cancer without evidence of side effects.

  17. Overtone spectroscopy of some benzaldehyde derivatives

    Indian Academy of Sciences (India)

    internuclear distances for the aryl CH bond in the different molecules. The small variation observed in these distances is ..... [6] D N Singh, Vibrational spectra and force fields for some benzaldehyde derivatives, Ph.D. Thesis. (Banaras Hindu ...

  18. SYNTHESIS OF SUBSTITUTED FLAVONE DERIVATIVES AS ...

    African Journals Online (AJOL)

    Preferred Customer

    Flavone (2-phenylchromone) derivatives are naturally occurring heterocyclic compound belongs to the flavanoid group. It showed significant role in pharmaceutical effects [1] including leishmanicidal activity, oviposter stimulant phytoalexins, anti-HIV, vasodilator, antiviral, anti- oxidants, bactericidal, DNA cleavage, ...

  19. Synthesis of Lipophilic Guanine N-9 Derivatives

    DEFF Research Database (Denmark)

    Wamberg, Michael C; Pedersen, Pernille L; Löffler, Philipp M G

    2017-01-01

    the synthesis of five new guanine-N9 derivatives bearing alkyl chains with different attachment chemistries, exploiting a synthesis pathway that allows a flexible choice of hydrophobic anchor moiety. In this study, these guanine derivatives were functionalized with C10 chains for insertion into decanoic acid...... bilayer structures, in which both alkyl chain length and attachment chemistry determined their interaction with the membrane. Incubation of these guanine conjugates, as solids, with a decanoic acid vesicle suspension, showed that ether- and triazole-linked C10 anchors yielded an increased partitioning...... of the guanine derivative into the membranous phase compared to directly N-9-linked saturated alkyl anchors. Decanoic acid vesicle membranes could be loaded with up to 5.5 mol % guanine derivative, a 6-fold increase over previous limits. Thus, anchor chemistries exhibiting favorable interactions with a bilayer...

  20. Particle production in higher derivative theory

    Indian Academy of Sciences (India)

    Lemaitre–Robertson–Walker cosmological model during the early stages of the universe is analysed in the framework of higher derivative theory. The universe has been considered as an open thermodynamic system where particle production ...

  1. Langmuir-Blodgett Films of Graphene Derivatives

    DEFF Research Database (Denmark)

    Petersen, Søren Vermehren

    The work presented in this PhD thesis can be divided into two main categories: 1) Syn-thesis and Langmuir-Blodgett assembly of graphene derivatives and 2) Application and characterization of graphene derivatives as an interface material in molecular electron-ics. While the first category could...... be divided further, the synthesis and Langmuir-Blodgett results are intertwined in such a way that it would be more confusing to pre-sent them separately. The Langmuir-Blodgett deposition also played a crucial, but more isolated, part in the investigation of graphene derivatives as interface material....... Solution processable graphene in the form of chemically derived graphene has been synthesized through the modified Hummers method with subsequent reduction into reduced graphene oxide with hydrazine. The completeness of oxidation, the effect of the refinement steps and the reduction of the graphene oxide...

  2. 76 FR 4751 - Position Limits for Derivatives

    Science.gov (United States)

    2011-01-26

    ... saleable by long traders at its market value in normal cash marketing channels at the derivative contract's... Association, Futures Industry Association, GDF Suez Energy, Morgan Stanley, and NextEra Energy Power Marketing...

  3. Second derivative parallel block backward differentiation type ...

    African Journals Online (AJOL)

    Second derivative parallel block backward differentiation type formulas for Stiff ODEs. ... Log in or Register to get access to full text downloads. ... and the methods are inherently parallel and can be distributed over parallel processors. They are ...

  4. Novel hydroquinone derivatives alleviate algesia, inflammation and ...

    African Journals Online (AJOL)

    derivatives were synthesized and their structures were confirmed by .... to water. The baseline rectal temperature of all mice was noted by inserting a lubricated digital thermometer ... (PDB) and the binding site residues of the receptors were ...

  5. Plant-derived nanostructures: types and applications

    Science.gov (United States)

    Plant-derived nanostructures and nanoparticles (NPs) have functional applications in numerous disciplines such as health care, food and feed, cosmetics, biomedical science, energy science, drug-gene delivery, environmental health, and so on. Consequently, it is imperative for res...

  6. Anodic selective functionalization of cyclic amine derivatives

    OpenAIRE

    Onomura, Osamu

    2012-01-01

    Anodic reactions are desirable methods from the viewpoint of Green Chemistry, since no toxic oxidants are necessary for the oxidation of organic molecules. This review introduces usefulness of anodic oxidation and successive reaction for selective functionalization of cyclic amine derivatives.

  7. Regional Ecological Corridors - MLCCS derived 2008

    Data.gov (United States)

    Minnesota Department of Natural Resources — Identification of potential ecological corridors between the MLCCS derived ecological patches (ear_eco08py3). This was generated using cost / distance analysis,...

  8. MEAN OF MEDIAN ABSOLUTE DERIVATION TECHNIQUE MEAN ...

    African Journals Online (AJOL)

    eobe

    development of mean of median absolute derivation technique based on the based on the based on .... of noise mean to estimate the speckle noise variance. Noise mean property ..... Foraging Optimization,” International Journal of. Advanced ...

  9. An alternative to the flutter derivatives

    DEFF Research Database (Denmark)

    Andersen, Michael Styrk; Brandt, Anders

    A new simplified framework to study flutter and assess the full scale flutter wind speed is suggested. The flutter instability problem is reduced from a problem involving 8 flutter derivatives to only 4 coefficients. With this method it is possible to estimate the self-excited forces with increased...... precision by using stability diagrams. Furthermore, the physical transparency of the aerodynamic damping and stiffness terms is increased because the development in vertical and torsional damping and stiffness is analysed instead of flutter derivatives....

  10. Higher-derivative Lee-Wick unification

    International Nuclear Information System (INIS)

    Carone, Christopher D.

    2009-01-01

    We consider gauge coupling unification in Lee-Wick extensions of the Standard Model that include higher-derivative quadratic terms beyond the minimally required set. We determine how the beta functions are modified when some Standard Model particles have two Lee-Wick partners. We show that gauge coupling unification can be achieved in such models without requiring the introduction of additional fields in the higher-derivative theory and we comment on possible ultraviolet completions.

  11. Financial derivatives in power marketing: The basics

    International Nuclear Information System (INIS)

    Ramesh, V.C.; Ghosh, K.

    1996-01-01

    With the ongoing changes in the power industry worldwide, electricity is beginning to be traded like other commodities. The use of financial derivative instruments in power markets is on the rise. The purpose of this paper is to explain the role of these derivatives in risk management which is vital for survival in the increasingly competitive industry. Starting with the familiar cash markets, the paper discusses the basics of futures, options, and swap markets as applied to electric energy trading

  12. Higher derivative regularization and chiral anomaly

    International Nuclear Information System (INIS)

    Nagahama, Yoshinori.

    1985-02-01

    A higher derivative regularization which automatically leads to the consistent chiral anomaly is analyzed in detail. It explicitly breaks all the local gauge symmetry but preserves global chiral symmetry and leads to the chirally symmetric consistent anomaly. This regularization thus clarifies the physics content contained in the consistent anomaly. We also briefly comment on the application of this higher derivative regularization to massless QED. (author)

  13. Complexes of salicylic acid and its derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Tel' zhenskaya, P N; Shvarts, E M [AN Latvijskoj SSR, Riga. Inst. Neorganicheskoj Khimii

    1977-01-01

    A generalization and systematization have been made of literature data on complexing of various elements, including beryllium, cadmium, boron, indium, rare-earth elements, actinides, and transition elements with salicylic acid and it derivatives (amino-, nitro- and halosalicylic acids). The effect of the position and nature of the substitute, in the case of salicylic acid derivatives, on the complexing process is discussed. Certain physicochemical properties of the complexes under consideration are described along with data indicative of their stability.

  14. On computing Laplace's coefficients and their derivatives.

    Science.gov (United States)

    Gerasimov, I. A.; Vinnikov, E. L.

    The algorithm of computing Laplace's coefficients and their derivatives is proposed with application of recurrent relations. The A.G.M.-method is used for the calculation of values L0(0), L0(1). The FORTRAN-program corresponding to the algorithm is given. The precision control was provided with numerical integrating by Simpsons method. The behavior of Laplace's coefficients and their third derivatives whith varying indices K, n for fixed values of the α-parameter is presented graphically.

  15. Weather Derivatives – Origin, Types and Application

    OpenAIRE

    Piotr Binkowski

    2008-01-01

    The number of companies that are exposed to the revenues loss risk caused by weather variability is still increasing. The businesses that are mostly exposed to weather risk are following: energy, agriculture, constructions and transport. That situation has initiated dynamic growth of weather derivatives markets as well as the awareness of the weather risk among the market participants. Presently, the weather derivatives markets evaluate rapidly in all the mature economies: USA, Asia and Europ...

  16. A note on derivations in semiprime rings

    Directory of Open Access Journals (Sweden)

    Joso Vukman

    2005-01-01

    Full Text Available We prove in this note the following result. Let n>1 be an integer and let R be an n!-torsion-free semiprime ring with identity element. Suppose that there exists an additive mapping D:R→R such that D(xn=∑j=1nxn−jD(xxj−1 is fulfilled for all x∈R. In this case, D is a derivation. This research is motivated by the work of Bridges and Bergen (1984. Throughout, R will represent an associative ring with center Z(R. Given an integer n>1, a ring R is said to be n-torsion-free if for x∈R, nx=0 implies that x=0. Recall that a ring R is prime if for a,b∈R, aRb=(0 implies that either a=0 or b=0, and is semiprime in case aRa=(0 implies that a=0. An additive mapping D:R→R is called a derivation if D(xy=D(xy+xD(y holds for all pairs x,y∈R and is called a Jordan derivation in case D(x2=D(xx+xD(x is fulfilled for all x∈R. Every derivation is a Jordan derivation. The converse is in general not true. A classical result of Herstein (1957 asserts that any Jordan derivation on a prime ring with characteristic different from two is a derivation. A brief proof of Herstein's result can be found in 1988 by Brešar and Vukman. Cusack (1975 generalized Herstein's result to 2-torsion-free semiprime rings (see also Brešar (1988 for an alternative proof. For some other results concerning derivations on prime and semiprime rings, we refer to Brešar (1989, Vukman (2005, Vukman and Kosi-Ulbl (2005.

  17. Introduction of Credit Derivatives and Valuation of Credit Default Swap

    OpenAIRE

    Han, Lu

    2006-01-01

    The credit derivative market was established at the beginning of the 1990s since the emergence of credit derivatives fits the rapid development of the whole derivatives market. However, compare to other derivative market, this market is still small and incomplete. As with other derivatives, credit derivatives can be used to either take more risk or hedge it, hence various credit derivatives instruments are accepted and widely used by market participants such as banks, insurance companies, etc...

  18. Multiscale analysis of the CMB temperature derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Marcos-Caballero, A.; Martínez-González, E.; Vielva, P., E-mail: marcos@ifca.unican.es, E-mail: martinez@ifca.unican.es, E-mail: vielva@ifca.unican.es [Instituto de Física de Cantabria, CSIC-Universidad de Cantabria, Avda. de los Castros s/n, 39005 Santander, Spain. (Spain)

    2017-02-01

    We study the Planck CMB temperature at different scales through its derivatives up to second order, which allows one to characterize the local shape and isotropy of the field. The problem of having an incomplete sky in the calculation and statistical characterization of the derivatives is addressed in the paper. The analysis confirms the existence of a low variance in the CMB at large scales, which is also noticeable in the derivatives. Moreover, deviations from the standard model in the gradient, curvature and the eccentricity tensor are studied in terms of extreme values on the data. As it is expected, the Cold Spot is detected as one of the most prominent peaks in terms of curvature, but additionally, when the information of the temperature and its Laplacian are combined, another feature with similar probability at the scale of 10{sup o} is also observed. However, the p -value of these two deviations increase above the 6% when they are referred to the variance calculated from the theoretical fiducial model, indicating that these deviations can be associated to the low variance anomaly. Finally, an estimator of the directional anisotropy for spinorial quantities is introduced, which is applied to the spinors derived from the field derivatives. An anisotropic direction whose probability is <1% is detected in the eccentricity tensor.

  19. Structure Activity Relationship of Brevenal Hydrazide Derivatives

    Directory of Open Access Journals (Sweden)

    Allan Goodman

    2014-03-01

    Full Text Available Brevenal is a ladder frame polyether produced by the dinoflagellate Karenia brevis. This organism is also responsible for the production of the neurotoxic compounds known as brevetoxins. Ingestion or inhalation of the brevetoxins leads to adverse effects such as gastrointestinal maladies and bronchoconstriction. Brevenal shows antagonistic behavior to the brevetoxins and shows beneficial attributes when administered alone. For example, in an asthmatic sheep model, brevenal has been shown to increase tracheal mucosal velocity, an attribute which has led to its development as a potential treatment for Cystic Fibrosis. The mechanism of action of brevenal is poorly understood and the exact binding site has not been elucidated. In an attempt to further understand the mechanism of action of brevenal and potentially develop a second generation drug candidate, a series of brevenal derivatives were prepared through modification of the aldehyde moiety. These derivatives include aliphatic, aromatic and heteroaromatic hydrazide derivatives. The brevenal derivatives were tested using in vitro synaptosome binding assays to determine the ability of the compounds to displace brevetoxin and brevenal from their native receptors. A sheep inhalation model was used to determine if instillation of the brevenal derivatives resulted in bronchoconstriction. Only small modifications were tolerated, with larger moieties leading to loss of affinity for the brevenal receptor and bronchoconstriction in the sheep model.

  20. PROCEDURES FOR THE DERIVATION OF EQUILIBRIUM ...

    Science.gov (United States)

    This equilibrium partitioning sediment benchmark (ESB) document describes procedures to derive concentrations for 32 nonionic organic chemicals in sediment which are protective of the presence of freshwater and marine benthic organisms. The equilibrium partitioning (EqP) approach was chosen because it accounts for the varying biological availability of chemicals in different sediments and allows for the incorporation of the appropriate biological effects concentration. This provides for the derivation of benchmarks that are causally linked to the specific chemical, applicable across sediments, and appropriately protective of benthic organisms. EqP can be used to calculate ESBs for any toxicity endpoint for which there are water-only toxicity data; it is not limited to any single effect endpoint. For the purposes of this document, ESBs for 32 nonionic organic chemicals, including several low molecular weight aliphatic and aromatic compounds, pesticides, and phthalates, were derived using Final Chronic Values (FCV) from Water Quality Criteria (WQC) or Secondary Chronic Values (SCV) derived from existing toxicological data using the Great Lakes Water Quality Initiative (GLI) or narcosis theory approaches. These values are intended to be the concentration of each chemical in water that is protective of the presence of aquatic life. For nonionic organic chemicals demonstrating a narcotic mode of action, ESBs derived using the GLI approach specifically for fres

  1. Studies on Synthesis of Some Novel Heterocyclic Azlactone Derivatives and Imidazolinone Derivatives and their Antimicrobial Activity

    Directory of Open Access Journals (Sweden)

    Rakesh N. Mistry

    2005-01-01

    Full Text Available p - Methyl benzoic acid on reaction with phosphorus pentachloride gives p - methyl benzoyl chloride derivative which on condensation with glycine gives p - methyl benzoyl glycine derivative. Now, this p - methyl benzoyl glycine derivative on condensation with various substituted aldehydes gives corresponding substituted 4 - [aryl methylidine] - 2 - [p - methyl phenyl] - oxazole - 5 - one derivatives [1(a-j]. Further, these derivatives [1(a-j] on condensation with 4 , 4’ - diamino diphenyl sulphone gives corresponding substituted imidazolinone - dibenzsulphone derivatives [2(a-j], on condensation with 4 , 4’ - diamino diphenyl methane gives corresponding substituted imidazolinone - dibenzmethane derivatives [3(a-j], on condensation with 4,4’- diamino benzanilide gives corresponding substituted imidazolinone - benzanilide derivatives [4(a-j] and on condensation with 2 - amino pyridine gives corresponding substituted imidazolinone - pyridine derivatives [5(a-j] respectively. Structure elucidation of synthesised compounds has been made on the basis of elemental analysis, I.R. spectral studies and 1H N.M.R. spectral studies. The antimicrobial activity of the synthesised compounds has been studied against the cultures “Staphylococcus aureus”, “Escherichia coli” and “Candela albicans”.

  2. Adaptive synchronization of the complex dynamical network with non-derivative and derivative coupling

    Energy Technology Data Exchange (ETDEWEB)

    Xu Yuhua, E-mail: yuhuaxu2004@163.co [College of Information Science and Technology, Donghua University, Shanghai 201620 (China) and Department of Maths, Yunyang Teachers' College, Hubei 442000 (China); Zhou Wuneng, E-mail: wnzhou@163.co [College of Information Science and Technology, Donghua University, Shanghai 201620 (China); Fang Jian' an [College of Information Science and Technology, Donghua University, Shanghai 201620 (China); Sun Wen [School of Mathematics and Information, Yangtze University, Hubei Jingzhou 434023 (China)

    2010-04-05

    This Letter investigates the synchronization of a general complex dynamical network with non-derivative and derivative coupling. Based on LaSalle's invariance principle, adaptive synchronization criteria are obtained. Analytical result shows that under the designed adaptive controllers, a general complex dynamical network with non-derivative and derivative coupling can asymptotically synchronize to a given trajectory, and several useful criteria for synchronization are given. What is more, the coupling matrix is not assumed to be symmetric or irreducible. Finally, simulations results show the method is effective.

  3. 32 CFR 2400.14 - Use of derivative classification.

    Science.gov (United States)

    2010-07-01

    ... SECURITY PROGRAM Derivative Classification § 2400.14 Use of derivative classification. (a) Derivative... 32 National Defense 6 2010-07-01 2010-07-01 false Use of derivative classification. 2400.14... person who applies derivative classification markings believes that the paraphrasing, restating, or...

  4. Contact allergy to isoeugenol and its derivatives

    DEFF Research Database (Denmark)

    Tanaka, Susumu; Royds, C; Buckley, Christopher D

    2004-01-01

    A total of 2261 (808 male, 1453 female) consecutive patients attending contact dermatitis clinics were patch tested to isoeugenol and its derivatives listed in the EU Inventory of Fragrance Ingredients. Positive reactions were found to isoeugenol in 40, transisoeugenol in 40, isoeugenyl acetate...... and 15/16 of those to isoeugenyl phenylacetate but in none of those 6 positive to isoeugenyl methyl ether and in neither of those 2 positive to benzyl isoeugenyl ether. Concomitant contact allergy between isoeugenol and its derivatives may occur through chemical cross-reactivity or local skin metabolism...... of the derivatives. It is more commonly observed with the esters rather than the ethers. Isoeugenyl acetate has been proposed as an alternative to isoeugenol, but there is a high degree of concomitant reactivity with isoeugenol....

  5. Funding climate adaptation strategies with climate derivatives

    Directory of Open Access Journals (Sweden)

    L. Richard Little

    2015-01-01

    Full Text Available Climate adaptation requires large capital investments that could be provided not only by traditional sources like governments and banks, but also by derivatives markets. Such markets would allow two parties with different tolerances and expectations about climate risks to transact for their mutual benefit and, in so doing, finance climate adaptation. Here we calculate the price of a derivative called a European put option, based on future sea surface temperature (SST in Tasmania, Australia, with an 18 °C strike threshold. This price represents a quantifiable indicator of climate risk, and forms the basis for aquaculture industries exposed to the risk of higher SST to finance adaptation strategies through the sale of derivative contracts. Such contracts provide a real incentive to parties with different climate outlooks, or risk exposure to take a market assessment of climate change.

  6. Structure-activity relationships of bumetanide derivatives

    DEFF Research Database (Denmark)

    Pedersen, Kasper Lykke; Töllner, Kathrin; Römermann, Kerstin

    2015-01-01

    of diuretics such as bumetanide. Bumetanide was discovered by screening ∼5000 3-amino-5-sulfamoylbenzoic acid derivatives, long before NKCC2 was identified in the kidney. Therefore, structure-activity studies on effects of bumetanide derivatives on NKCC2 are not available. EXPERIMENTAL APPROACH: In this study......, the effect of a series of diuretically active bumetanide derivatives was investigated on human NKCC2 variant A (hNKCC2A) expressed in Xenopus laevis oocytes. KEY RESULTS: Bumetanide blocked hNKCC2A transport with an IC50 of 4 μM. There was good correlation between the diuretic potency of bumetanide and its...... of the structural requirements that determine relative potency of loop diuretics on human NKCC2 splice variants, and may lead to the discovery of novel high-ceiling diuretics....

  7. FINANCIAL DERIVATIVES - MEANINGS BEYOND SUBPRIME CRISIS STIGMA

    Directory of Open Access Journals (Sweden)

    FELICIA RAMONA BIRĂU

    2012-12-01

    Full Text Available Derivatives are designed as complex financial instruments and their main aim is to manage the risk associated with the underlying asset, in order to ensure against fluctuations in value, or to profit from periods of inactivity, instability or decline. In recent years financial derivatives have experienced a fulminant development and also they have been perceived as an effective lever of the modern economy. The subprime crisis was triggered by a quite significant financial infrastructure glitch, which coalesced around certain factors influence, such as : highly permissive regulation of financial markets, speculative bubbles, underperforming risk management, liquidity injections and structural imbalances. Despite the fact that is a innovative segment and quite difficult affordable as understanding level of the operation mechanisms, financial derivatives were only the tool triggering this global dimension crisis.

  8. Deriving Trading Rules Using Gene Expression Programming

    Directory of Open Access Journals (Sweden)

    Adrian VISOIU

    2011-01-01

    Full Text Available This paper presents how buy and sell trading rules are generated using gene expression programming with special setup. Market concepts are presented and market analysis is discussed with emphasis on technical analysis and quantitative methods. The use of genetic algorithms in deriving trading rules is presented. Gene expression programming is applied in a form where multiple types of operators and operands are used. This gives birth to multiple gene contexts and references between genes in order to keep the linear structure of the gene expression programming chromosome. The setup of multiple gene contexts is presented. The case study shows how to use the proposed gene setup to derive trading rules encoded by Boolean expressions, using a dataset with the reference exchange rates between the Euro and the Romanian leu. The conclusions highlight the positive results obtained in deriving useful trading rules.

  9. Additive derivations on algebras of measurable operators

    International Nuclear Information System (INIS)

    Ayupov, Sh.A.; Kudaybergenov, K.K.

    2009-08-01

    Given a von Neumann algebra M we introduce the so-called central extension mix(M) of M. We show that mix(M) is a *-subalgebra in the algebra LS(M) of all locally measurable operators with respect to M, and this algebra coincides with LS(M) if and only if M does not admit type II direct summands. We prove that if M is a properly infinite von Neumann algebra then every additive derivation on the algebra mix(M) is inner. This implies that on the algebra LS(M), where M is a type I ∞ or a type III von Neumann algebra, all additive derivations are inner derivations. (author)

  10. 5-Nitroimidazole Derivatives and their Antimicrobial Activity

    International Nuclear Information System (INIS)

    Khan, K.M.; Salar, U.; Yousuf, S.; Naz, F.

    2016-01-01

    5-Nitroimidazole derivatives 2-8 were synthesized from secnidazole. The syntheses were accomplished in two steps which start from the oxidation of secnidazole to the secnidazolone 1. Secnidazolone 1 was converted into its hydrazone derivative 2-8 by treating with different substituted acid hydrazide. Compounds 2-8 were evaluated for their antimicrobial activity against Gram-positive and Gram-negative bacteria, compounds 3 and 4 showed the significant activity against Staphylococcus epidermidis, however, compound 2 showed good inhibitions against Corynebacterium diphtheria when compared with the standard. Compound 3 showed good inhibitory potential against tested Gram-negative bacterial strains i.e. Enterobacter aerogene, Escherichia coli, Salmonella typhi, Salmonella paratyphi A, Shigella flexeneri and Vibrio choleriae. All synthetic derivatives were also tested against eight fungal stains, however, they were weekly active against Aspergillus flavus and Candida albican. The synthesized compounds were characterized by different spectroscopy techniques. (author)

  11. Multivalent Peptidomimetic Conjugates as Inhibitors of Androgen Receptor Function in Therapy-Resistant Prostate Cancer

    Science.gov (United States)

    2017-10-01

    response, including the time for reviewing instructions, searching existing data sources, gathering and maintaining the data needed, and completing and...hormones that play a critical role in stimulating prostate cancer growth. Androgens activate a protein called the androgen receptor (AR), which...treat patients with prostate cancer, over time the tumors become resistant to the drugs, leaving few treatment options. The goal of this proposal is to

  12. The role of formyl peptide receptors for immunomodulatory activities of antimicrobial peptides and peptidomimetics

    DEFF Research Database (Denmark)

    Skovbakke, Sarah Line; Holdfeldt, André; Forsman, Huamei

    2018-01-01

    In recent years, the therapeutic potential of antimicrobial peptides (AMPs) as immunomodulators has become generally accepted. Nevertheless, only very few AMP-based compounds have progressed into clinical trials. This paradox may be explained by the fact, that some of the intrinsic properties...... displaying analogous immunomodulatory activity profiles. Neutrophils play key roles in host defense as major effector cells in clearance of pathogens by phagocytosis and by regulating other processes of innate immunity as well as promotion of resolution of inflammation. Several aspects of these effects...... are correlated to their expression of formyl peptide receptors (FPRs) that have been shown to be targets of both natural and synthetic antimicrobial peptides. In the present review recent findings highlighting the role of FPRs in mediating immunomodulatory activities of natural and synthetic AMPs as well...

  13. Interferon gamma peptidomimetic targeted to hepatic stellate cells ameliorates acute and chronic liver fibrosis in vivo

    NARCIS (Netherlands)

    Bansal, Ruchi; Prakash, Jai; De Ruiter, Marieke; Poelstra, Klaas

    2014-01-01

    Hepatic stellate cells play a crucial role in the pathogenesis of hepatic fibrosis. Thus, pharmacological inhibition of pro-fibrotic activities of these cells might lead to an effective therapy for this disease. Among the potent antifibrotics, interferon gamma (IFN gamma), a proinflammatory

  14. Interferon gamma peptidomimetic targeted to hepatic stellate cells ameliorates acute and chronic liver fibrosis in vivo

    NARCIS (Netherlands)

    Bansal, Ruchi; Prakash, Jai; de Ruiter, Marieke; Poelstra, Klaas

    2014-01-01

    Hepatic stellate cells play a crucial role in the pathogenesis of hepatic fibrosis. Thus, pharmacological inhibition of pro-fibrotic activities of these cells might lead to an effective therapy for this disease. Among the potent anti-fibrotics, interferon gamma (IFNγ), a proinflammatory cytokine, is

  15. Interferon gamma peptidomimetic targeted to interstitial myofibroblasts attenuates renal fibrosis after unilateral ureteral obstruction in mice

    NARCIS (Netherlands)

    Poosti, Fariba; Bansal, Ruchi; Yazdani, Saleh; Prakash, Jai; Beljaars, Leonie; van den Born, Jacob; de Borst, Martin H.; van Goor, Harry; Hillebrands, Jan-Luuk; Poelstra, Klaas

    2016-01-01

    Renal fibrosis cannot be adequately treated since anti-fibrotic treatment is lacking. Interferon-gamma is a pro-inflammatory cytokine with anti-fibrotic properties. Clinical use of interferon-gamma is hampered due to inflammation-mediated systemic side effects. We used an interferon-gamma

  16. Topological side-chain classification of beta-turns: ideal motifs for peptidomimetic development.

    Science.gov (United States)

    Tran, Tran Trung; McKie, Jim; Meutermans, Wim D F; Bourne, Gregory T; Andrews, Peter R; Smythe, Mark L

    2005-08-01

    Beta-turns are important topological motifs for biological recognition of proteins and peptides. Organic molecules that sample the side chain positions of beta-turns have shown broad binding capacity to multiple different receptors, for example benzodiazepines. Beta-turns have traditionally been classified into various types based on the backbone dihedral angles (phi2, psi2, phi3 and psi3). Indeed, 57-68% of beta-turns are currently classified into 8 different backbone families (Type I, Type II, Type I', Type II', Type VIII, Type VIa1, Type VIa2 and Type VIb and Type IV which represents unclassified beta-turns). Although this classification of beta-turns has been useful, the resulting beta-turn types are not ideal for the design of beta-turn mimetics as they do not reflect topological features of the recognition elements, the side chains. To overcome this, we have extracted beta-turns from a data set of non-homologous and high-resolution protein crystal structures. The side chain positions, as defined by C(alpha)-C(beta) vectors, of these turns have been clustered using the kth nearest neighbor clustering and filtered nearest centroid sorting algorithms. Nine clusters were obtained that cluster 90% of the data, and the average intra-cluster RMSD of the four C(alpha)-C(beta) vectors is 0.36. The nine clusters therefore represent the topology of the side chain scaffold architecture of the vast majority of beta-turns. The mean structures of the nine clusters are useful for the development of beta-turn mimetics and as biological descriptors for focusing combinatorial chemistry towards biologically relevant topological space.

  17. Peptidomimetic ligands for the tandem SH2 domain of Syk kinase

    NARCIS (Netherlands)

    Kuil, J.

    2009-01-01

    The Spleen tyrosine kinase (Syk) protein functions as a switch in a number of receptor signaling cascades. One of these cascades is the high affinity IgE receptor (Fc?RI) signaling pathway. Fc?RI consists of an ?-, ?- and two ?-chains. The ?- and ?-chains have intracellular an Immunoreceptor

  18. Conformationally Constrained Peptidomimetics as Inhibitors of the Protein Arginine Methyl Transferases

    DEFF Research Database (Denmark)

    Knuhtsen, Astrid; Legrand, Baptiste; Van der Poorten, Olivier

    2016-01-01

    Protein arginine N-methyl transferases (PRMTs) belong to a family of enzymes that modulate the epigenetic code through modifications of histones. In the present study, peptides emerging from a phage display screening were modified in the search for PRMT inhibitors through substitution with non-pr...

  19. Guanidino Groups Greatly Enhance the Action of Antimicrobial Peptidomimetics Against Bacterial Cytoplasmic Membranes

    Science.gov (United States)

    2014-05-28

    permeated is not completely understood, and several models have been proposed based on studies conducted with various peptidic structures [1]. Moreover...approach has been successfully used in conjunction with liquid surface X-ray scattering to study bacterial membrane lysis by human antimicrobial peptide...diluted in MHB pH 7.4 to a final concentration of approx. 5 × 105 CFU/mL in each well. Polypropylene plates (Nunc 442587) were used to minimize peptide

  20. Multivalent Peptidomimetic Conjugates as Inhibitors of Androgen Receptor Function in Therapy Resistant Prostate Cancer

    Science.gov (United States)

    2016-10-01

    Haugbro M, Imberg-Kazdan K, Logan SK, Kirshenbaum K, Garabedian MJ. Multivalent Peptoid Conjugates Which Overcome Enzalutamide Resistance in Prostate...attached documents Wang Y, Dehigaspitiya DC, Levine PM, Profit AA, Haugbro M, Imberg-Kazdan K, Logan SK, Kirshenbaum K, Garabedian MJ. Multivalent...Enzalutamide Resistance in Prostate Cancer Cells Yu Wang1, Dilani C. Dehigaspitiya2, Paul M. Levine2, Adam A. Profit3, Michael Haugbro2, Keren Imberg

  1. Multivalent Peptidomimetic Conjugates as Inhibitors of Androgen Receptor Function in Therapy-Resistant Prostate Cancer

    Science.gov (United States)

    2016-10-01

    K, Logan SK, Kirshenbaum K, Garabedian MJ. Multivalent Peptoid Conjugates Which Overcome Enzalutamide Resistance in Prostate Cancer Cells. Cancer...Wang Y, Dehigaspitiya DC, Levine PM, Profit AA, Haugbro M, Imberg-Kazdan K, Logan SK, Kirshenbaum K, Garabedian MJ. Multivalent Peptoid Conjugates...Prostate Cancer Cells Yu Wang1, Dilani C. Dehigaspitiya2, Paul M. Levine2, Adam A. Profit3, Michael Haugbro2, Keren Imberg-Kazdan4, Susan K. Logan1,5

  2. Unorthodox Inhibitors of HIV Protease: Looking Beyond Active-site-directed Peptidomimetics

    Czech Academy of Sciences Publication Activity Database

    Schimer, Jiří; Konvalinka, Jan

    2014-01-01

    Roč. 20, č. 21 (2014), s. 3389-3397 ISSN 1381-6128 R&D Projects: GA ČR GAP207/11/1798 Institutional support: RVO:61388963 Keywords : proteinase * proteolytic processing * virostatic * rational drug design * resistance development Subject RIV: CE - Biochemistry Impact factor: 3.452, year: 2014

  3. Design and Synthesis of New Peptidomimetics as Potential Inhibitors of MurE.

    Science.gov (United States)

    Zivec, Matej; Turk, Samo; Blanot, Didier; Gobec, Stanislav

    2011-03-01

    With the continuing emergence and spread of multidrug-resistant bacteria, there is an urgent need for the development of new antimicrobial agents. One possible source of new antibacterial targets is the biosynthesis of the bacterial cell-wall peptidoglycan. The assembly of the peptide stem is carried out by four essential enzymes, known as the Mur ligases (MurC, D, E and F). We have designed and synthesised a focused library of compounds as potential inhibitors of UDP-N-acetylmuramoyl-L-alanyl-D-glutamate:L-lysine ligase (MurE) from Staphylococcus aureus. This was achieved using two approaches: (i) synthesis of transition-state analogues based on the methyleneamino core; and (ii) synthesis of MurE reaction product analogues. Two methyleneamino-based compounds are identified as initial hits for inhibitors of MurE.

  4. Multivalent Peptidomimetic Conjugates as Inhibitors of Androgen Receptor Function in Therapy-Resistant Prostate Cancer

    Science.gov (United States)

    2017-10-01

    androgen), with more or less intervening monomers in between the ethisterone ligands diminishing compound activities. We are now creating a set of MPC6...disseminated to communities of interest ? We published a paper on this topic in Cancer Research Cancer Res. 2016 Sep 1;76(17):5124- 32. doi: 10.1158/0008...We will test all of the MPC6 variants in the in vitro and cell based assays. We are waiting to test all of the compounds simultaneously to minimize

  5. Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1

    DEFF Research Database (Denmark)

    Brodin, Birger; Nielsen, Carsten Uhd; Steffansen, Bente

    2002-01-01

    The apical membrane of small intestinal enterocytes possess an uptake system for di- and tripeptides. The physiological function of the system is to transport small peptides resulting from digestion of dietary protein. Moreover, due to the broad substrate specificity of the system, it is also cap...

  6. A Peptidomimetic Antibiotic Targets Outer Membrane Proteins and Disrupts Selectively the Outer Membrane in Escherichia coli.

    Science.gov (United States)

    Urfer, Matthias; Bogdanovic, Jasmina; Lo Monte, Fabio; Moehle, Kerstin; Zerbe, Katja; Omasits, Ulrich; Ahrens, Christian H; Pessi, Gabriella; Eberl, Leo; Robinson, John A

    2016-01-22

    Increasing antibacterial resistance presents a major challenge in antibiotic discovery. One attractive target in Gram-negative bacteria is the unique asymmetric outer membrane (OM), which acts as a permeability barrier that protects the cell from external stresses, such as the presence of antibiotics. We describe a novel β-hairpin macrocyclic peptide JB-95 with potent antimicrobial activity against Escherichia coli. This peptide exhibits no cellular lytic activity, but electron microscopy and fluorescence studies reveal an ability to selectively disrupt the OM but not the inner membrane of E. coli. The selective targeting of the OM probably occurs through interactions of JB-95 with selected β-barrel OM proteins, including BamA and LptD as shown by photolabeling experiments. Membrane proteomic studies reveal rapid depletion of many β-barrel OM proteins from JB-95-treated E. coli, consistent with induction of a membrane stress response and/or direct inhibition of the Bam folding machine. The results suggest that lethal disruption of the OM by JB-95 occurs through a novel mechanism of action at key interaction sites within clusters of β-barrel proteins in the OM. These findings open new avenues for developing antibiotics that specifically target β-barrel proteins and the integrity of the Gram-negative OM. © 2016 by The American Society for Biochemistry and Molecular Biology, Inc.

  7. Linear peptidomimetics as potent antagonists of Staphylococcus aureus agr quorum sensing

    DEFF Research Database (Denmark)

    Karathanasi, Georgia; Bojer, Martin Saxtorph; Baldry, Mara

    2018-01-01

    Staphylococcus aureus is an important pathogen causing infections in humans and animals. Increasing problems with antimicrobial resistance has prompted the development of alternative treatment strategies, including antivirulence approaches targeting virulence regulation such as the agr quorum...

  8. Metal-Binding Ability of Leu-Enkephalin, Related Glycoconjugates and Peptidomimetics

    Directory of Open Access Journals (Sweden)

    Zsuzsa Majer

    2015-12-01

    Full Text Available Both the chemistry and consequences of the nonenzymatic reaction between reducing sugars and reactive amino groups of amino acids, peptides and proteins (known as the Maillard reaction, have received considerable attention in food and health science fields. This initial reaction results in Amadori and similar products formation, followed by degradation to advanced glycation end products (AGEs. It is well established that AGEs are associated with color and odor of thermally processed or stored food, as well as with pathogen products in a number of diseases. The model systems of early stage Maillard reaction products (MRP were prepared between endogenous opioid peptide leucine enkephalin (1 and D-glucose / D-glucuronic acid. The complexation ability of prepared MRP with metal ions (Ca2+, Zn2+, Al3+, Pb2+ and Cu2+ was investigated and compared to the complexation ability of parent peptide using ECD and FTIR spectroscopic measurements.

  9. Structural studies of 4-aminoantipyrine derivatives

    Science.gov (United States)

    Cunha, Silvio; Oliveira, Shana M.; Rodrigues, Manoel T.; Bastos, Rodrigo M.; Ferrari, Jailton; de Oliveira, Cecília M. A.; Kato, Lucília; Napolitano, Hamilton B.; Vencato, Ivo; Lariucci, Carlito

    2005-10-01

    Reaction of 4-aminoantipyrine with acetylacetone, ethyl acetoacetate, benzoyl isothiocyanate, phenyl isothiocyanate, maleic anhydride and methoxymethylene Meldrum's acid afforded a series of new antipyrine derivatives. The antibacterial activity of the synthesized compounds against Micrococcus luteus ATCC 9341, Staphilococcus aureus ATCC 29737, and Escherichia coli ATCC 8739 was evaluated and the minimal inhibitory concentration determined. Modest activity was found only to the maleamic acid obtained from the reaction of 4-aminoantipyrine and maleic anhydride. 1H NMR investigation of this maleamic acid showed that it is slowly converted to the corresponding toxic maleimide. The structures of three derivatives were determined by X-ray diffraction analysis.

  10. Ethanolamine derivatives of dysprosium and holmium

    International Nuclear Information System (INIS)

    Gharia, K.S.; Singh, M.; Mathur, S.; Sankhla, B.S.

    1981-01-01

    The preparation and properties of dysprosium and holmium derivatives of mono-, di- and tri-ethanolamine derivatives are described. Compounds of general formulae: Ln(OPrsup(i)) 2 (mea), Ln(OPrsup(i))(mea) 2 , Ln(mea) 3 , Ln(OPrsup(i))(dea), Ln 2 (dea) 3 , Ln(dea)(deaH) and Ln(tea) (where Ln = Dy or Ho and mea, dea and tea are the anions of respective ethanolamine) were obtained and characterized by elemental analysis and IR spectra. (author)

  11. Geometric derivation of the quantum speed limit

    International Nuclear Information System (INIS)

    Jones, Philip J.; Kok, Pieter

    2010-01-01

    The Mandelstam-Tamm and Margolus-Levitin inequalities play an important role in the study of quantum-mechanical processes in nature since they provide general limits on the speed of dynamical evolution. However, to date there has been only one derivation of the Margolus-Levitin inequality. In this paper, alternative geometric derivations for both inequalities are obtained from the statistical distance between quantum states. The inequalities are shown to hold for unitary evolution of pure and mixed states, and a counterexample to the inequalities is given for evolution described by completely positive trace-preserving maps. The counterexample shows that there is no quantum speed limit for nonunitary evolution.

  12. A 'simple' hybrid model for power derivatives

    International Nuclear Information System (INIS)

    Lyle, Matthew R.; Elliott, Robert J.

    2009-01-01

    This paper presents a method for valuing power derivatives using a supply-demand approach. Our method extends work in the field by incorporating randomness into the base load portion of the supply stack function and equating it with a noisy demand process. We obtain closed form solutions for European option prices written on average spot prices considering two different supply models: a mean-reverting model and a Markov chain model. The results are extensions of the classic Black-Scholes equation. The model provides a relatively simple approach to describe the complicated price behaviour observed in electricity spot markets and also allows for computationally efficient derivatives pricing. (author)

  13. Novel Aflatoxin Derivatives and Protein Conjugates

    Directory of Open Access Journals (Sweden)

    Reinhard Niessner

    2007-03-01

    Full Text Available Aflatoxins, a group of structurally related mycotoxins, are well known for their toxic and carcinogenic effects in humans and animals. Aflatoxin derivatives and protein conjugates are needed for diverse analytical applications. This work describes a reliable and fast synthesis of novel aflatoxin derivatives, purification by preparative HPLC and characterisation by ESI-MS and one- and two-dimensional NMR. Novel aflatoxin bovine serum albumin conjugates were prepared and characterised by UV absorption and MALDI-MS. These aflatoxin protein conjugates are potentially interesting as immunogens for the generation of aflatoxin selective antibodies with novel specificities.

  14. Derived limits and their practical applications

    International Nuclear Information System (INIS)

    Minarik, F.

    1982-01-01

    Attention is devoted to the approach and methodological procedure in determining derived limits for surface contamination with special regard to external exposure of hands, inhalation of resuspended activity, contamination of the skin and with regard to ingestion of radioactive material from the skin. In the practical part of the article, results are given of measuring contamination by radionuclides 134 Cs, 133 Cs and 60 Co, and the resulting annual equivalent dose rates and their comparison with derived air contamination in the sense of ICRP Publ. No. 30. (author)

  15. Development of chitosan derivatives with anhydride maleic

    International Nuclear Information System (INIS)

    Silva, Solranny C.C.C.; Braz, Elton Marks de A.; Brito, Carla Adriana R. de S.; Silva, Durcilene A. da; Junior, Luiz de S.S.; Silva Filho, Edson C. da

    2015-01-01

    Chitosan was chemically modified with maleic anhydride in ratios of 1/2, 1/5 and 1/10 in the absence of solvents. The obtained derivatives were characterized by elemental analysis, FTIR, thermal analysis (TGA / DTG) and XRD where it was possible to prove the chemical modification. Elemental analysis showed an increase of the relation C / N with the increasing of the proportion of anhydrides. The FTIR showed the incorporation of the anhydride in the biopolymer structure. The thermal stability of the derivatives was lower in comparison to the polysaccharide and by XRD the modified materials were less crystalline. (author)

  16. High ethanol producing derivatives of Thermoanaerobacter ethanolicus

    Science.gov (United States)

    Ljungdahl, L.G.; Carriera, L.H.

    1983-05-24

    Derivatives of the newly discovered microorganism Thermoanaerobacter ethanolicus which under anaerobic and thermophilic conditions continuously ferment substrates such as starch, cellobiose, glucose, xylose and other sugars to produce recoverable amounts of ethanol solving the problem of fermentations yielding low concentrations of ethanol using the parent strain of the microorganism Thermoanaerobacter ethanolicus are disclosed. These new derivatives are ethanol tolerant up to 10% (v/v) ethanol during fermentation. The process includes the use of an aqueous fermentation medium, containing the substrate at a substrate concentration greater than 1% (w/v).

  17. Derivation of Mayer Series from Canonical Ensemble

    International Nuclear Information System (INIS)

    Wang Xian-Zhi

    2016-01-01

    Mayer derived the Mayer series from both the canonical ensemble and the grand canonical ensemble by use of the cluster expansion method. In 2002, we conjectured a recursion formula of the canonical partition function of a fluid (X.Z. Wang, Phys. Rev. E 66 (2002) 056102). In this paper we give a proof for this formula by developing an appropriate expansion of the integrand of the canonical partition function. We further derive the Mayer series solely from the canonical ensemble by use of this recursion formula. (paper)

  18. Derivation of Mayer Series from Canonical Ensemble

    Science.gov (United States)

    Wang, Xian-Zhi

    2016-02-01

    Mayer derived the Mayer series from both the canonical ensemble and the grand canonical ensemble by use of the cluster expansion method. In 2002, we conjectured a recursion formula of the canonical partition function of a fluid (X.Z. Wang, Phys. Rev. E 66 (2002) 056102). In this paper we give a proof for this formula by developing an appropriate expansion of the integrand of the canonical partition function. We further derive the Mayer series solely from the canonical ensemble by use of this recursion formula.

  19. Special relativity derived from spacetime magma.

    Science.gov (United States)

    Greensite, Fred

    2014-01-01

    We present a derivation of relativistic spacetime largely untethered from specific physical considerations, in constrast to the many physically-based derivations that have appeared in the last few decades. The argument proceeds from the inherent magma (groupoid) existing on the union of spacetime frame components [Formula: see text] and Euclidean [Formula: see text] which is consistent with an "inversion symmetry" constraint from which the Minkowski norm results. In this context, the latter is also characterized as one member of a class of "inverse norms" which play major roles with respect to various unital [Formula: see text]-algebras more generally.

  20. Special relativity derived from spacetime magma.

    Directory of Open Access Journals (Sweden)

    Fred Greensite

    Full Text Available We present a derivation of relativistic spacetime largely untethered from specific physical considerations, in constrast to the many physically-based derivations that have appeared in the last few decades. The argument proceeds from the inherent magma (groupoid existing on the union of spacetime frame components [Formula: see text] and Euclidean [Formula: see text] which is consistent with an "inversion symmetry" constraint from which the Minkowski norm results. In this context, the latter is also characterized as one member of a class of "inverse norms" which play major roles with respect to various unital [Formula: see text]-algebras more generally.

  1. Scale up of proteoliposome derived Cochleate production.

    Science.gov (United States)

    Zayas, Caridad; Bracho, Gustavo; Lastre, Miriam; González, Domingo; Gil, Danay; Acevedo, Reinaldo; del Campo, Judith; Taboada, Carlos; Solís, Rosa L; Barberá, Ramón; Pérez, Oliver

    2006-04-12

    Cochleate are highly stable structures with promising immunological features. Cochleate structures are usually obtaining from commercial lipids. Proteoliposome derived Cochleate are derived from an outer membrane vesicles of Neisseria meningitidis B. Previously, we obtained Cochleates using dialysis procedures. In order to increase the production process, we used a crossflow system (CFS) that allows easy scale up to obtain large batches in an aseptic environment. The raw material and solutions used in the production process are already approved for human application. This work demonstrates that CFS is very efficient process to obtain Cochleate structures with a yield of more than 80% and the immunogenicity comparable to that obtained by dialysis membrane.

  2. Urinary Derivations: Radiological Anatomy and Complications

    International Nuclear Information System (INIS)

    Rodriguez, A.; Escartin, I.; Zapater, C.; Riazuelo, G.; Canon, R.; Solanas, S.; Garcia de Jalon, A.

    2003-01-01

    Cystectomy with urine derivation is a common procedure in the treatment of transition cell carcinoma of the bladder. We present radiological findings (ultrasound scan, computerized tomography (CT) and urography) from the surgical reconstruction techniques most often performed by the Urology staff of our hospital as well as some of the complications which occur. The above-mentioned techniques are basically divided into two types: incontinent derivations, of which we highlight the Bicker-Wallace technique and continent ones. The latter can either be ortho topic, with urethral anastomosis (Hauptmann's technique), or heterotopic, with urine excretion through the anus (Mains II technique) or employing a self-catheter (Mainz I technique). (Author) 7 refs

  3. Preparation and study of dialkyl nitroxide radicals

    International Nuclear Information System (INIS)

    Chenavas, P.

    1969-01-01

    These radicals are obtained by oxidation of N-hydroxy-imides with lead tetracetate or p-nitro-perbenzoic acid. These imides are prepared by heating dicarboxylic acids anhydrides with benzyloxy-amine followed by catalytic hydrogenation of N-benzyloxy-imides so obtained. Two series of radicals have mainly been studied, the first concerning five-membered cyclic imides, the second six-membered cyclic imides, these molecules having methyls substituents or no on the carbon ring. N. M. R. spectra of some O-benzyl-imides have been analysed. These different results have made it possible to study the conformation and stereochemistry of these imides. (author) [fr

  4. Derivation and characterization of a pig embryonic stem cell-derived exocrine pancreatic cell line

    Science.gov (United States)

    The establishment and initial characterization of a pig embryonic stem cell-derived pancreatic cell line, PICM-31, and a colony-cloned derivative cell line, PICM-31A, is described. The cell lines were propagated for several months at split ratios of 1:3 or 1:5 at each passage on STO feeder cells af...

  5. A class of constitutive relations with internal variable derivatives. Derivation from homogenization and initial value problem

    International Nuclear Information System (INIS)

    Andrieux, S.; Joussemet, M.; Lorentz, E.

    1996-01-01

    A general framework for deriving and using a class of constitutive laws incorporating spatial gradients of internal variables is presented. It uses two basic ingredients: a derivation of such models by homogenization techniques and a reformulation of the evolution equation at the scale of the whole structure. (orig.)

  6. 18 CFR 367.2440 - Account 244, Derivative instrument liabilities.

    Science.gov (United States)

    2010-04-01

    ..., Derivative instrument liabilities. This account must include the change in the fair value of all derivative instrument liabilities not designated as cash flow or fair value hedges. Account 426.5, Other deductions... the fair value of the derivative instrument. ...

  7. Optimal economic order quantity for buyer-distributor-vendor supply chain with backlogging derived without derivatives

    Science.gov (United States)

    Teng, Jinn-Tsair; Cárdenas-Barrón, Leopoldo Eduardo; Lou, Kuo-Ren; Wee, Hui Ming

    2013-05-01

    In this article, we first complement an inappropriate mathematical error on the total cost in the previously published paper by Chung and Wee [2007, 'Optimal the Economic Lot Size of a Three-stage Supply Chain With Backlogging Derived Without Derivatives', European Journal of Operational Research, 183, 933-943] related to buyer-distributor-vendor three-stage supply chain with backlogging derived without derivatives. Then, an arithmetic-geometric inequality method is proposed not only to simplify the algebraic method of completing prefect squares, but also to complement their shortcomings. In addition, we provide a closed-form solution to integral number of deliveries for the distributor and the vendor without using complex derivatives. Furthermore, our method can solve many cases in which their method cannot, because they did not consider that a squared root of a negative number does not exist. Finally, we use some numerical examples to show that our proposed optimal solution is cheaper to operate than theirs.

  8. Energy derivatives, experiences in derivative trading from the natural gas industry : back to basics

    International Nuclear Information System (INIS)

    Dittmer, G.; Coyle, T.

    1998-01-01

    Some basic facts regarding derivatives in the electric power industry were discussed based on experiences in the natural gas industry. Derivatives were described as financial instruments that have no value of their own but derive their value from other assets, such as commodities. Futures and Options are the two forms of derivatives. Electricity as a commodity was characterized, and a historical parallel was drawn between deregulation in the natural gas and electric power industry. Short term and long term factors impacting the market and market dynamics impacting derivatives were identified. The latter include: (1) volatility, (2) liquidity, (3) correlations, and (4) price discovery. In contrast to the natural gas market, the electricity market is considered as lacking liquidity and in need of moving farther along the maturity timeline. The question of natural gas/ electricity convergence was also addressed refs., tabs., figs

  9. Deriving simulators for hybrid Chi models

    NARCIS (Netherlands)

    Beek, van D.A.; Man, K.L.; Reniers, M.A.; Rooda, J.E.; Schiffelers, R.R.H.

    2006-01-01

    The hybrid Chi language is formalism for modeling, simulation and verification of hybrid systems. The formal semantics of hybrid Chi allows the definition of provably correct implementations for simulation, verification and realtime control. This paper discusses the principles of deriving an

  10. Unedoside derivatives in Nuxia and their biosynthesis

    DEFF Research Database (Denmark)

    Jensen, Søren Rosendal; Ravnkilde, Lene; Schripsema, Jan

    1998-01-01

    An investigation of two species of Nuxia showed that this genus is characterized by the presence of the eight-carbon iridoid glucoside unedoside and/or its derivatives. From N. floribunda unedoside, nuxioside (6-O-alpha-L-rhamnopyranosyl-unedoside) and 2 "-acetyl-3 "-cinnamoyl-nuxioside were...

  11. Significant exposures to isoeugenol derivatives in perfumes

    DEFF Research Database (Denmark)

    Rastogi, S.C.; Johansen, Jeanne Duus

    2008-01-01

    Background: Isoeugenol, an important fragrance allergen in consumers, has been restricted to 200 p.p.m. since 1998 according to guidelines issued by the fragrance industry. However, no decline in contact allergy to isoeugnol has been detected. It has been speculated that isoeugenol derivatives...

  12. Structural Studies of Some Binaphthyl Derivatives

    DEFF Research Database (Denmark)

    Thorup, Niels; Bjørnholm, T.; Bechgaard, K.

    1996-01-01

    Crystal structures of several 1,1'-binaphthyl derivatives have been determined. In particular compounds which at the 2,2' positions have either identical ethoxy groups or a closed bridged ether and furthermore have identical substitution at the 6,6' positions. The latter groups may be Br, CHO, CN...

  13. Generalized Jackknife Estimators of Weighted Average Derivatives

    DEFF Research Database (Denmark)

    Cattaneo, Matias D.; Crump, Richard K.; Jansson, Michael

    With the aim of improving the quality of asymptotic distributional approximations for nonlinear functionals of nonparametric estimators, this paper revisits the large-sample properties of an important member of that class, namely a kernel-based weighted average derivative estimator. Asymptotic...

  14. Synthesis and characterization of novel sulfonamides derivatives

    African Journals Online (AJOL)

    3Department of Chemistry, Comsat Institute of Information & Technology Riawind road. Lahore ... Newer sulfonamides and their derivatives has obtained great attention in pharmaceutical field in ... MS data was recorded on Finnigan MAT 112 mass ..... potent and orally active sulfonamide ETB selective antagonists. Bioorg.

  15. 17 CFR 200.506 - Derivative classification.

    Science.gov (United States)

    2010-04-01

    ... 17 Commodity and Securities Exchanges 2 2010-04-01 2010-04-01 false Derivative classification. 200.506 Section 200.506 Commodity and Securities Exchanges SECURITIES AND EXCHANGE COMMISSION ORGANIZATION; CONDUCT AND ETHICS; AND INFORMATION AND REQUESTS Classification and Declassification of National Security...

  16. Fundamentals of futures, options, basis and derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Jones, D. [TD Securities Inc., Toronto, ON (Canada)

    1997-08-01

    Characteristic features of futures and options contracts, basis differentials and derivatives were defined and explained. A futures contract refers to an exchange-traded supply contract between a buyer and a seller where the buyer is obligated to take delivery and the seller is obligated to provide delivery of a fixed amount of a commodity at a predetermined price at a specified location. In contrast, an option contract gives the purchaser the right, but not the obligation, to buy or sell the underlying commodity at a certain price on or before an agreed date. Basis differential refers to the discount between two distinct delivery points to reflect the relative value of a commodity, such as natural gas, at those points. Advantages and disadvantages of futures and options contacts, the factors affecting options pricing, and basis differentials, and the methods of calculating basis differentials were described. The nature and intricacies of derivatives, their benefits, in particular their use as a tool for the effective management of the volatilities associated with the oil and gas industry were explained. Their shortcomings such as the high liquidity risk, were also described. Examples of derivative transactions were provided to illustrate the interrelationships of futures/options/derivatives, and their role in financial risk management.

  17. 32 CFR 2001.22 - Derivative classification.

    Science.gov (United States)

    2010-07-01

    ... 32 National Defense 6 2010-07-01 2010-07-01 false Derivative classification. 2001.22 Section 2001.22 National Defense Other Regulations Relating to National Defense INFORMATION SECURITY OVERSIGHT OFFICE, NATIONAL ARCHIVES AND RECORDS ADMINISTRATION CLASSIFIED NATIONAL SECURITY INFORMATION...

  18. Interest Rate Derivative Pricing with Stochastic Volatility

    NARCIS (Netherlands)

    Chen, B.

    2012-01-01

    One purpose of exotic derivative pricing models is to enable financial institutions to quantify and manage their financial risk, arising from large books of portfolios. These portfolios consist of many non-standard exotic financial products. Risk is managed by means of the evaluation of sensitivity

  19. Microscopically derived free energy of dislocations

    NARCIS (Netherlands)

    Kooiman, M.; Hütter, M.; Geers, M.G.D.

    2015-01-01

    The dynamics of large amounts of dislocations is the governing mechanism in metal plasticity. The free energy of a continuous dislocation density profile plays a crucial role in the description of the dynamics of dislocations, as free energy derivatives act as the driving forces of dislocation

  20. Econometric Analysis of Financial Derivatives : An overview

    NARCIS (Netherlands)

    C-L. Chang (Chia-Lin); M.J. McAleer (Michael)

    2014-01-01

    markdownabstract__Abstract__ One of the fastest growing areas in empirical finance, and also one of the least rigorously analyzed, especially from a financial econometrics perspective, is the econometric analysis of financial derivatives, which are typically complicated and difficult to analyze.

  1. Econometric Analysis of Financial Derivatives: An Overview

    NARCIS (Netherlands)

    C-L. Chang (Chia-Lin); M.J. McAleer (Michael)

    2014-01-01

    markdownabstract__Abstract__ One of the fastest growing areas in empirical finance, and also one of the least rigorously analyzed, especially from a financial econometrics perspective, is the econometric analysis of financial derivatives, which are typically complicated and difficult to analyze.

  2. Nitration of Thiacalix[4]arene Derivatives

    Czech Academy of Sciences Publication Activity Database

    Lhoták, P.; Svoboda, J.; Stibor, I.; Sýkora, Jan

    2002-01-01

    Roč. 43, č. 41 (2002), s. 7413-7417 ISSN 0040-4039 R&D Projects: GA ČR GA104/00/1722 Keywords : derivatives * nitation of thiacalix[4]arene Subject RIV: CI - Industrial Chemistry, Chemical Engineering Impact factor: 2.357, year: 2002

  3. Deriving GENERIC from a generalized fluctuation symmetry

    NARCIS (Netherlands)

    Kraaij, R.; Lazarescu, A.; Maes, C.; Peletier, M.A.

    2018-01-01

    Much of the structure of macroscopic evolution equations for relaxation to equilibrium can be derived from symmetries in the dynamical fluctuations around the most typical trajectory. For example, detailed balance as expressed in terms of the Lagrangian for the path-space action leads to gradient

  4. Enabling quaternion derivatives: the generalized HR calculus

    Science.gov (United States)

    Xu, Dongpo; Jahanchahi, Cyrus; Took, Clive C.; Mandic, Danilo P.

    2015-01-01

    Quaternion derivatives exist only for a very restricted class of analytic (regular) functions; however, in many applications, functions of interest are real-valued and hence not analytic, a typical case being the standard real mean square error objective function. The recent HR calculus is a step forward and provides a way to calculate derivatives and gradients of both analytic and non-analytic functions of quaternion variables; however, the HR calculus can become cumbersome in complex optimization problems due to the lack of rigorous product and chain rules, a consequence of the non-commutativity of quaternion algebra. To address this issue, we introduce the generalized HR (GHR) derivatives which employ quaternion rotations in a general orthogonal system and provide the left- and right-hand versions of the quaternion derivative of general functions. The GHR calculus also solves the long-standing problems of product and chain rules, mean-value theorem and Taylor's theorem in the quaternion field. At the core of the proposed GHR calculus is quaternion rotation, which makes it possible to extend the principle to other functional calculi in non-commutative settings. Examples in statistical learning theory and adaptive signal processing support the analysis. PMID:26361555

  5. Initial value formulation of higher derivative gravity

    International Nuclear Information System (INIS)

    Noakes, D.R.

    1983-01-01

    The initial value problem is considered for the conformally coupled scalar field and higher derivative gravity, by expressing the equations of each theory in harmonic coordinates. For each theory it is shown that the (vacuum) equations can take the form of a diagonal hyperbolic system with constraints on the initial data. Consequently these theories possess well-posed initial value formulations

  6. Orchard navigation using derivative free Kalman filtering

    DEFF Research Database (Denmark)

    Hansen, Søren; Bayramoglu, Enis; Andersen, Jens Christian

    2011-01-01

    This paper describes the use of derivative free filters for mobile robot localization and navigation in an orchard. The localization algorithm fuses odometry and gyro measurements with line features representing the surrounding fruit trees of the orchard. The line features are created on basis of 2...

  7. Curcumin derivatives as HIV-1 protease inhibitors

    Energy Technology Data Exchange (ETDEWEB)

    Sui, Z.; Li, J.; Craik, C.S.; Ortiz de Montellano, P.R. [Univ. of California, San Francisco, CA (United States)

    1993-12-31

    Curcumin, a non-toxic natural compound from Curcuma longa, has been found to be an HIV-1 protease inhibitor. Some of its derivatives were synthesized and their inhibitory activity against the HIV-1 protease was tested. Curcumin analogues containing boron enhanced the inhibitory activity. At least of the the synthesized compounds irreversibly inhibits the HIV-1 protease.

  8. Genetic enrichment of cardiomyocytes derived from mouse ...

    African Journals Online (AJOL)

    Genetic enrichment of cardiomyocytes derived from mouse embryonic stem cells. WJ He, SC Li, LL Ye, H Liu, QW Wang, WD Han, XB Fu, ZL Chen. Abstract. Pluripotent embryonic stem cells (ESC) have the ability to differentiate into a variety of cell lineages in vitro, including cardiomyocytes. Successful applications of ...

  9. Cocktail : a tool for deriving correct programs

    NARCIS (Netherlands)

    Franssen, M.G.J.; Swart, de H.C.M.

    2004-01-01

    Cocktail is a tool for deriving correct programs from their specifications. The present version is powerful enough for educational purposes. The tool yields support for many sorted first order predicate logic, formulated in a pure type system with parametric constants (CPTS), as the specification

  10. A new pyrrolidone derivative from Pistacia chinensis

    Institute of Scientific and Technical Information of China (English)

    Jian Jun Liu; Chang An Geng; Xi Kui Liu

    2008-01-01

    A new N-phenyl-pyrrolidone derivative had been isolated from Pistacia chinesis Bunge. Its structure was elucidated as4-hydroxy-5-(2-oxo-1-pyrrolidinyl)-benzoic acid, named pistaciamide on the basis of the 1D-NMR, DEPT, HMQC and HMBCspectroscopic techniques.

  11. Particle production in higher derivative theory

    Indian Academy of Sciences (India)

    Cosmological models; particle production; higher derivative theory of gravitation. PACS No. 98.80. 1. ... is of singular models where the cosmic expansion is driven by the big-bang impulse; all ... According to Gibbs integrability condition, one cannot independently specify an equa- .... [3] B Hartle and S W Hawking Phys. Rev.

  12. morphological characteristics and classification of soils derived

    African Journals Online (AJOL)

    Prof. Ekwueme

    MORPHOLOGICAL CHARACTERISTICS AND CLASSIFICATION OF. SOILS DERIVED FROM DIVERSE PARENT MATERIALS IN CENTRAL. CROSS RIVER STATE, NIGERIA. 271. M. E. NSOR and I. J. IBANGA. (Received 5 October 2007; Revision Accepted 5 December 2007). ABSTRACT. Variation in soil characteristics ...

  13. Novel hydroquinone derivatives alleviate algesia, inflammation and ...

    African Journals Online (AJOL)

    The in silico studies predicted high binding affinity of the hydroquinone derivatives to the active site of the cyclooxygenase 2 (COX-2) enzyme. Conclusion: The synthesized hydroquinone compounds possess analgesic, antipyretic and antiinflammatory properties with low gastric-ulcerogenic potential. This may be credited to ...

  14. OPINION Is the repo a derivative?

    African Journals Online (AJOL)

    Introduction. The literature on the derivative markets and the spot (cash) financial markets ... value of R9 450 000, and the interest factor for the period of the repo is R35 000 ... mathematics is simple and in the case of bonds a little less simple.

  15. Characterization of sugar beet pulp derived oligosaccharides

    NARCIS (Netherlands)

    Leijdekkers, M.

    2015-01-01

    Abstract

    This thesis aimed at characterizing complex mixtures of sugar beet pulp derived oligosaccharides, in order to be able to monitor and optimize the enzymatic saccharification of sugar beet pulp.

    Hydrophilic interaction chromatography with on-line evaporative

  16. Nanomaterials derived from metal-organic frameworks

    Science.gov (United States)

    Dang, Song; Zhu, Qi-Long; Xu, Qiang

    2018-01-01

    The thermal transformation of metal-organic frameworks (MOFs) generates a variety of nanostructured materials, including carbon-based materials, metal oxides, metal chalcogenides, metal phosphides and metal carbides. These derivatives of MOFs have characteristics such as high surface areas, permanent porosities and controllable functionalities that enable their good performance in sensing, gas storage, catalysis and energy-related applications. Although progress has been made to tune the morphologies of MOF-derived structures at the nanometre scale, it remains crucial to further our knowledge of the relationship between morphology and performance. In this Review, we summarize the synthetic strategies and optimized methods that enable control over the size, morphology, composition and structure of the derived nanomaterials. In addition, we compare the performance of materials prepared by the MOF-templated strategy and other synthetic methods. Our aim is to reveal the relationship between the morphology and the physico-chemical properties of MOF-derived nanostructures to optimize their performance for applications such as sensing, catalysis, and energy storage and conversion.

  17. Actuarial risk measures for financial derivative pricing

    NARCIS (Netherlands)

    Goovaerts, M.J.; Laeven, R.J.A.

    2008-01-01

    We present an axiomatic characterization of price measures that are superadditive and comonotonic additive for normally distributed random variables. The price representation derived involves a probability measure transform that is closely related to the Esscher transform, and we call it the

  18. Immunochemical analysis of apamin and its derivatives

    International Nuclear Information System (INIS)

    Vasilenko, S.V.; Kolesnikova, I.N.; Miroshnikov, A.I.; Komissarenko, S.V.

    1981-01-01

    The radioimmunologic analysis of apamin (neurotoxin of the venom of Apis mellifica honey bee) is carried out using its derivatives which have modifications of various aminoacidic remnants and antibodies against apamin. The curves of 125 J apamin binding with antiserum against apamin and the curves of inhibition with various nonlabelled binding effectors of 125 J-apamin with antiserum are obtained

  19. Derivation of the Ideal Gas Law

    Science.gov (United States)

    Laugier, Alexander; Garai, Jozsef

    2007-01-01

    Undergraduate and graduate physics and chemistry books usually state that combining the gas laws results in the ideal gas law. Leaving the derivation to the students implies that this should be a simple task, most likely a substitution. Boyle's law, Charles's law, and the Avogadro's principle are given under certain conditions; therefore, direct…

  20. Cinnamic Acid Derivatives as Antidiabetics Agents

    Directory of Open Access Journals (Sweden)

    Teni Ernawati

    2017-04-01

    Full Text Available Diabetes mellitus is a metabolic disorder of carbohydrate metabolism. Treatment of type II diabetes is usually done by prescribing diet and exercise for the patient however it can also be treated with antidiabetic drugs. The purpose of this paper is to illustrate some cinnamic acid derivative compounds which are either isolated from natural materials or the results of the chemical synthesis. In addition, their biological activities as an agent of α-glucosidase inhibitors have also been evaluated. Chemically, cinnamic acid has three main functional groups:  first is the substitution on the phenyl group, second is the additive reaction into the α-β unsaturated, and third is the chemical reaction with carboxylic acid functional groups. Chemical aspects of cinnamic acid derivative compounds have received much attention in the research and development of drugs, especially modifications within three functional groups are very influential. In the last 10 years, a lot of research and development of cinnamic acid derivatives as inhibitors of the α-glucosidase enzyme has been done. One example of the research done in this field is the modification of para position in the structure of cinnamic acid and addition of alkyl groups in the carboxylic group which would increase the activity of the α-glucosidase enzyme therefore the level of inhibition is 100 times higher than that of cinnamic acid compound itself. The novelty of this review article is to focus on the antidiabetic activity of cinnamic acid derivatives.

  1. On pricing of interest rate derivatives

    OpenAIRE

    Di Matteo, T.; Airoldi, M.; Scalas, E.

    2004-01-01

    At present, there is an explosion of practical interest in the pricing of interest rate (IR) derivatives. Textbook pricing methods do not take into account the leptokurticity of the underlying IR process. In this paper, such a leptokurtic behaviour is illustrated using LIBOR data, and a possible martingale pricing scheme is discussed.

  2. Antimutagenic activity of dextran gammaphos derivatives

    International Nuclear Information System (INIS)

    Bakhitova, L.M.; Pashin, O.V.; Drobchenko, S.N.; Bondarev, G.I.

    1991-01-01

    In experiments with V-79 Chinese hamster cell culture the influence of dextran gammaphos derivatives on the mutagenic effects of γ-radiation was studied by the number of cells with micronuclei and fragmented nuclei. Products of interaction between gammaphos and dialdehyde dextran were shown to a higher antimutagenic activity than gammaphos

  3. Sol-Gel Derived Hafnia Coatings

    Science.gov (United States)

    Feldman, Jay D.; Stackpoole, Mairead; Blum, Yigal; Sacks, Michael; Ellerby, Don; Johnson, Sylvia M.; Venkatapathy, Ethiras (Technical Monitor)

    2002-01-01

    Sol-gel derived hafnia coatings are being developed to provide an oxidation protection layer on ultra-high temperature ceramics for potential use in turbine engines (ultra-efficient engine technology being developed by NASA). Coatings using hafnia sol hafnia filler particles will be discussed along with sol synthesis and characterization.

  4. Undesired Plant-Derived Components in Food

    NARCIS (Netherlands)

    Dusemund, Birgit; Rietjens, Ivonne M.C.M.; Abraham, Klaus; Cartus, Alexander; Schrenk, Dieter

    2017-01-01

    Among the various chemical compounds, the class of natural plant-derived substances in the modern food chain is generating increasing concern. Adverse effects encountered may be various and pose risks of acute, subchronic, or chronic toxicity. The underlying mechanisms of toxicity may be

  5. Knot invariants derived from quandles and racks

    OpenAIRE

    Kamada, Seiichi

    2002-01-01

    The homology and cohomology of quandles and racks are used in knot theory: given a finite quandle and a cocycle, we can construct a knot invariant. This is a quick introductory survey to the invariants of knots derived from quandles and racks.

  6. Supersymmetric higher derivative couplings and their applications

    NARCIS (Netherlands)

    Lodato, I.

    2014-01-01

    After an elementary introduction on black hole physics, supersymmetry and effective theories, which motivates the importance of higher derivative couplings in supergravity, we give an exhaustive treatment of the covariant phase space formalism with many examples explicitly worked out. This sets the

  7. Synthesis of hydroxy derivatives of limonene

    International Nuclear Information System (INIS)

    Ardashov, O V; Volcho, K P; Salakhutdinov, N F

    2014-01-01

    Synthetic routes to mono-, di- and trihydroxy derivatives of limonene are presented. Emphasis is given to the problems of regio- and stereoselectivity of transformations. Data on the isolation from natural sources and on the biological activities of the title compounds are given. The bibliography includes 107 references

  8. Approximate methods for derivation of covariance data

    International Nuclear Information System (INIS)

    Tagesen, S.

    1992-01-01

    Several approaches for the derivation of covariance information for evaluated nuclear data files (EFF2 and ENDF/B-VI) have been developed and used at IRK and ORNL respectively. Considerations, governing the choice of a distinct method depending on the quantity and quality of available data are presented, advantages/disadvantages are discussed and examples of results are given

  9. Waste-wood-derived fillers for plastics

    Science.gov (United States)

    Brent English; Craig M. Clemons; Nicole Stark; James P. Schneider

    1996-01-01

    Filled thermoplastic composites are stiffer, stronger, and more dimensionally stable than their unfilled counterparts. Such thermoplastics are usually provided to the end-user as a precompounded, pelletized feedstock. Typical reinforcing fillers are inorganic materials like talc or fiberglass, but materials derived from waste wood, such as wood flour and recycled paper...

  10. Deriving Process Congruences from Reaction Rules

    DEFF Research Database (Denmark)

    Sobocinski, Pawel

    This thesis is concerned with the development of a theory which, given a formalism with a reduction semantics, allows the derivation of a canonical labelled transition system on which bisimilarity as well as other other equiv� alences are congruences; provided that the contexts of the formalism f...

  11. Formula-derived prostate volume determination

    NARCIS (Netherlands)

    Aarnink, R. G.; de la Rosette, J. J.; Debruyne, F. M.; Wijkstra, H.

    1996-01-01

    OBJECTIVES: Despite disadvantages such as time-consuming and tedious to the user, planimetric volumetry is considered to be the most accurate method for prostate volume determination. This study investigates the possibilities of formula-derived volume determination and reveals the best alternative

  12. Surface tree languages and parallel derivation trees

    NARCIS (Netherlands)

    Engelfriet, Joost

    1976-01-01

    The surface tree languages obtained by top-down finite state transformation of monadic trees are exactly the frontier-preserving homomorphic images of sets of derivation trees of ETOL systems. The corresponding class of tree transformation languages is therefore equal to the class of ETOL languages.

  13. Higher-Derivative Supergravity and Moduli Stabilization

    International Nuclear Information System (INIS)

    Ciupke, David; Westphal, Alexander; Louis, Jan; Hamburg Univ.

    2015-05-01

    We review the ghost-free four-derivative terms for chiral superfields in N=1 supersymmetry and supergravity. These terms induce cubic polynomial equations of motion for the chiral auxiliary fields and correct the scalar potential. We discuss the different solutions and argue that only one of them is consistent with the principles of effective field theory. Special attention is paid to the corrections along flat directions which can be stabilized or destabilized by the higher-derivative terms. We then compute these higher-derivative terms explicitly for the type IIB string compactified on a Calabi-Yau orientifold with fluxes via Kaluza-Klein reducing the (α') 3 R 4 corrections in ten dimensions for the respective N=1 Kaehler moduli sector. We prove that together with flux and the known (α') 3 -corrections the higher-derivative term stabilizes all Calabi-Yau manifolds with positive Euler number, provided the sign of the new correction is negative.

  14. INVESTIGATION OF ANTIFUNGAL ACTIVITY OF QUINOLINIUM DERIVATIVES

    Directory of Open Access Journals (Sweden)

    G. A. Alexandrova

    2013-01-01

    Full Text Available Abstract. Antifungal activity (Candida albicans, Candida krusei of some substituted quinolinium derivatives has been investigated. It was established that the most perspective compound for detail investigation of antifungal activity by labeled biomarkers method was N-phenylbenzoquinaldinium tetrafluoroborate.

  15. Ineffective higher derivative black hole hair

    Science.gov (United States)

    Goldstein, Kevin; Mashiyane, James Junior

    2018-01-01

    Inspired by the possibility that the Schwarzschild black hole may not be the unique spherically symmetric vacuum solution to generalizations of general relativity, we consider black holes in pure fourth order higher derivative gravity treated as an effective theory. Such solutions may be of interest in addressing the issue of higher derivative hair or during the later stages of black hole evaporation. Non-Schwarzschild solutions have been studied but we have put earlier results on a firmer footing by finding a systematic asymptotic expansion for the black holes and matching them with known numerical solutions obtained by integrating out from the near-horizon region. These asymptotic expansions can be cast in the form of trans-series expansions which we conjecture will be a generic feature of non-Schwarzschild higher derivative black holes. Excitingly we find a new branch of solutions with lower free energy than the Schwarzschild solution, but as found in earlier work, solutions only seem to exist for black holes with large curvatures, meaning that one should not generically neglect even higher derivative corrections. This suggests that one effectively recovers the nonhair theorems in this context.

  16. Simulation of chemical reactions using fractional derivatives

    International Nuclear Information System (INIS)

    Zabadal, J.; Vilhena, M.; Livotto, P.

    2001-01-01

    In this work a new approach to solve time-dependant Schroedinger equation for molecular systems is proposed. The method employs functional derivatives to describe the time evolution of the wave functions in reactive systems, in order to establish the mechanisms and products of the reaction. A numerical simulation is reported

  17. Inequalities for a Polynomial and its Derivative

    Indian Academy of Sciences (India)

    Annual Meetings · Mid Year Meetings · Discussion Meetings · Public Lectures · Lecture Workshops · Refresher Courses · Symposia · Live Streaming. Home; Journals; Proceedings – Mathematical Sciences; Volume 110; Issue 2. Inequalities for a Polynomial and its Derivative. V K Jain. Volume 110 Issue 2 May 2000 pp 137- ...

  18. Derivation of the fine-structure constant

    International Nuclear Information System (INIS)

    Samec, A.

    1980-01-01

    The fine-structure constant is derived as a dynamical property of quantum electrodynamics. Single-particle solutions of the coupled Maxwell and Dirac equations have a physical charge spectrum. The solutions are used to construct lepton-and quark-like particles. The strong, weak, electromagnetic, and gravitational forces are described as the interactions of complex charges in multiple combinations

  19. Fundamentals of futures, options, basis and derivatives

    International Nuclear Information System (INIS)

    Jones, D.

    1997-01-01

    Characteristic features of futures and options contracts, basis differentials and derivatives were defined and explained. A futures contract refers to an exchange-traded supply contract between a buyer and a seller where the buyer is obligated to take delivery and the seller is obligated to provide delivery of a fixed amount of a commodity at a predetermined price at a specified location. In contrast, an option contract gives the purchaser the right, but not the obligation, to buy or sell the underlying commodity at a certain price on or before an agreed date. Basis differential refers to the discount between two distinct delivery points to reflect the relative value of a commodity, such as natural gas, at those points. Advantages and disadvantages of futures and options contacts, the factors affecting options pricing, and basis differentials, and the methods of calculating basis differentials were described. The nature and intricacies of derivatives, their benefits, in particular their use as a tool for the effective management of the volatilities associated with the oil and gas industry were explained. Their shortcomings such as the high liquidity risk, were also described. Examples of derivative transactions were provided to illustrate the interrelationships of futures/options/derivatives, and their role in financial risk management

  20. Risk Management and Financial Derivatives: An Overview

    NARCIS (Netherlands)

    S.M. Hammoudeh (Shawkat); M.J. McAleer (Michael)

    2012-01-01

    textabstractRisk management is crucial for optimal portfolio management. One of the fastest growing areas in empirical finance is the expansion of financial derivatives. The purpose of this special issue on “Risk Management and Financial Derivatives” is to highlight some areas in which novel

  1. WEATHER INDEX- THE BASIS OF WEATHER DERIVATIVES

    Directory of Open Access Journals (Sweden)

    Botos Horia Mircea

    2011-07-01

    Full Text Available This paper approaches the subject of Weather Derivatives, more exactly their basic element the weather index. The weather index has two forms, the Heating Degree Day (HDD and the Cooling Degree Day (CDD. We will try to explain their origin, use and the relationship between the two forms of the index. In our research we started from the analysis of the weather derivatives and what they are based on. After finding out about weather index, we were interested in understanding exactly how they work and how they influence the value of the contract. On the national level the research in the field is scares, but foreign materials available. The study for this paper was based firstly on reading about Weather Derivative, and then going in the meteorogical field and determining the way by which the indices were determined. After this, we went to the field with interest in the indices, such as the energy and gas industries, and figured out how they determined the weather index. For the examples we obtained data from the weather index database, and calculated the value for the period. The study is made on a period of five years, in 8 cities of the European Union. The result of this research is that we can now understand better the importance of the way the indices work and how they influence the value of the Weather Derivatives. This research has an implication on the field of insurance, because of the fact that weather derivative are at the convergence point of the stock markets and the insurance market. The originality of the paper comes from the personal touch given to the theoretical aspect and through the analysis of the HDD and CDD index in order to show their general behaviour and relationship.

  2. Derivative based sensitivity analysis of gamma index

    Directory of Open Access Journals (Sweden)

    Biplab Sarkar

    2015-01-01

    Full Text Available Originally developed as a tool for patient-specific quality assurance in advanced treatment delivery methods to compare between measured and calculated dose distributions, the gamma index (γ concept was later extended to compare between any two dose distributions. It takes into effect both the dose difference (DD and distance-to-agreement (DTA measurements in the comparison. Its strength lies in its capability to give a quantitative value for the analysis, unlike other methods. For every point on the reference curve, if there is at least one point in the evaluated curve that satisfies the pass criteria (e.g., δDD = 1%, δDTA = 1 mm, the point is included in the quantitative score as "pass." Gamma analysis does not account for the gradient of the evaluated curve - it looks at only the minimum gamma value, and if it is <1, then the point passes, no matter what the gradient of evaluated curve is. In this work, an attempt has been made to present a derivative-based method for the identification of dose gradient. A mathematically derived reference profile (RP representing the penumbral region of 6 MV 10 cm × 10 cm field was generated from an error function. A general test profile (GTP was created from this RP by introducing 1 mm distance error and 1% dose error at each point. This was considered as the first of the two evaluated curves. By its nature, this curve is a smooth curve and would satisfy the pass criteria for all points in it. The second evaluated profile was generated as a sawtooth test profile (STTP which again would satisfy the pass criteria for every point on the RP. However, being a sawtooth curve, it is not a smooth one and would be obviously poor when compared with the smooth profile. Considering the smooth GTP as an acceptable profile when it passed the gamma pass criteria (1% DD and 1 mm DTA against the RP, the first and second order derivatives of the DDs (δD', δD" between these two curves were derived and used as the

  3. A New Grünwald-Letnikov Derivative Derived from a Second-Order Scheme

    Directory of Open Access Journals (Sweden)

    B. A. Jacobs

    2015-01-01

    Full Text Available A novel derivation of a second-order accurate Grünwald-Letnikov-type approximation to the fractional derivative of a function is presented. This scheme is shown to be second-order accurate under certain modifications to account for poor accuracy in approximating the asymptotic behavior near the lower limit of differentiation. Some example functions are chosen and numerical results are presented to illustrate the efficacy of this new method over some other popular choices for discretizing fractional derivatives.

  4. Arbitrage-free valuation of energy derivatives

    International Nuclear Information System (INIS)

    Amin, K.; Ng, V.; Pirrong, C.

    1999-01-01

    This chapter focuses on techniques available for valuing energy-contingent claims and develops an arbitrage-free framework to value energy derivatives. The relationship between the spot, forward and futures prices is explained. Option valuation with deterministic convenience yields is discussed using an extension of the Black (1976) framework, and details of the risk-neutral valuation of European options, and valuation of American and European-style options are given. Option valuations with stochastic convenience yields, the evolution of the term structure of convenience yield, and a tree approach to valuing American and other options are discussed. Applications and limitations of the models for pricing energy derivative products are considered. The stochastic differential equation for the futures prices when the convenience yields are stochastic is presented in an appendix

  5. Fundamentals and advanced techniques in derivatives hedging

    CERN Document Server

    Bouchard, Bruno

    2016-01-01

    This book covers the theory of derivatives pricing and hedging as well as techniques used in mathematical finance. The authors use a top-down approach, starting with fundamentals before moving to applications, and present theoretical developments alongside various exercises, providing many examples of practical interest. A large spectrum of concepts and mathematical tools that are usually found in separate monographs are presented here. In addition to the no-arbitrage theory in full generality, this book also explores models and practical hedging and pricing issues. Fundamentals and Advanced Techniques in Derivatives Hedging further introduces advanced methods in probability and analysis, including Malliavin calculus and the theory of viscosity solutions, as well as the recent theory of stochastic targets and its use in risk management, making it the first textbook covering this topic. Graduate students in applied mathematics with an understanding of probability theory and stochastic calculus will find this b...

  6. Higher derivatives and renormalization in quantum cosmology

    International Nuclear Information System (INIS)

    Mazzitelli, F.D.

    1991-10-01

    In the framework of the canonical quantization of general relativity, quantum field theory on a fixed background formally arises in an expansion in powers of the Planck length. In order to renormalize the theory, quadratic terms in the curvature must be included in the gravitational action from the beginning. These terms contain higher derivatives which change the Hamiltonian structure of the theory completely, making the relation between the renormalized-theory and the original one not clear. We show that it is possible to avoid this problem. We replace the higher derivative theory by a second order one. The classical solutions of the latter are also solutions of the former. We quantize the theory, renormalize the infinities and show that there is a smooth limit between the classical and the renormalized theories. We work in a Robertson Walker minisuperspace with a quantum scalar field. (author). 32 refs

  7. Renminbi Derivatives: Recent Development and Issues

    Institute of Scientific and Technical Information of China (English)

    Wensheng Peng; Chang Shu; Raymond Yip

    2007-01-01

    This study reviews the developments in the onshore and offshore renminbi derivatives markets. The onshore market has seen a rapid build-up in the market infrastructure and price discovery mechanism in the past year, with empirical evidence suggesting that its pricing is increasingly determined by financial fundamentals, such as the covered interest rate parity. However, the growth of the market has been restrained by restrictions on the participant base, limited variations in the RMB/US$ exchange rate, market participants'lack of technical capacity and experience, and inadequate supporting financial market infrastructure. The non-deliverable forward (NDF) market, concentrated in Hong Kong and Singapore, is more developed, but has the drawback that its pricing is not tied to financial fundamentals. The comparison between onshore and offshore markets suggests that two issues are of particular importance for future derivatives market development in China: the balance between regulation and development, and the relationship between onshore and offshore markets.

  8. Electrochemical Behavior of Biologically Important Indole Derivatives

    Directory of Open Access Journals (Sweden)

    Cigdem Karaaslan

    2011-01-01

    Full Text Available Voltammetric techniques are most suitable to investigate the redox properties of a new drug. Use of electrochemistry is an important approach in drug discovery and research as well as quality control, drug stability, and determination of physiological activity. The indole nucleus is an essential element of a number of natural and synthetic products with significant biological activity. Indole derivatives are the well-known electroactive compounds that are readily oxidized at carbon-based electrodes, and thus analytical procedures, such as electrochemical detection and voltammetry, have been developed for the determination of biologically important indoles. This paper explains some of the relevant and recent achievements in the electrochemistry processes and parameters mainly related to biologically important indole derivatives in view of drug discovery and analysis.

  9. Algebraic theory of locally nilpotent derivations

    CERN Document Server

    Freudenburg, Gene

    2017-01-01

    This book explores the theory and application of locally nilpotent derivations, a subject motivated by questions in affine algebraic geometry and having fundamental connections to areas such as commutative algebra, representation theory, Lie algebras and differential equations. The author provides a unified treatment of the subject, beginning with 16 First Principles on which the theory is based. These are used to establish classical results, such as Rentschler's Theorem for the plane and the Cancellation Theorem for Curves. More recent results, such as Makar-Limanov's theorem for locally nilpotent derivations of polynomial rings, are also discussed. Topics of special interest include progress in classifying additive actions on three-dimensional affine space, finiteness questions (Hilbert's 14th Problem), algorithms, the Makar-Limanov invariant, and connections to the Cancellation Problem and the Embedding Problem. A lot of new material is included in this expanded second edition, such as canonical factoriza...

  10. Feynman graph derivation of Einstein quadrupole formula

    International Nuclear Information System (INIS)

    Dass, N.D.H.; Soni, V.

    1980-11-01

    The one graviton transition operator, and consequently, the classical energy loss formula for gravitational radiation are derived from the Feynman graphs of helicity +- 2 theories of gravitation. The calculations are done both for the case of electromagnetic and gravitational scattering. The departure of the in and out states from plane waves owing to the long range nature of gravitation is taken into account to improve the Born approximation calculations. This also includes a long range modification of the graviton wave function which is shown to be equivalent to the classical problem of the true light cones deviating logarithmically at large distances from the flat space light cones. The transition from the S-matrix elements calculated graphically to the graviton transition operator is done by using complimentarity of space-time and momentum descriptions. The energy loss formula derived originally by Einstein is shown to be correct. (Auth.)

  11. Biodegradation of polyurethane derived from castor oil

    Directory of Open Access Journals (Sweden)

    José M. Cangemi

    2008-09-01

    Full Text Available The aim of this research was to study the biodegradation of a polymer derived from castor oil, which is a renewable, natural material that is a practical alternative for the replacement of traditional polyurethane foams. Due to its molecular structure, which contains polyester segments derived from vegetable oil, the polymeric surface is susceptible to microorganism attack. This study tested the biological degrading agent that was in contact with the microorganisms resulting from microbiological grease degrading agents, when foam was inoculated. Solid-media agar-plate tests were conducted for their potential to evaluate the biodegradation of polymeric particles by specific strains of microorganisms during 216 hours. The growth rate was defined. This technique provides a way of distinguishing the degradation abilities of microorganisms from the degradability of materials.

  12. Phloroglucinol derivatives and flavones from Helichrysum paronychioides

    Directory of Open Access Journals (Sweden)

    J. Mutanyatta-Comar

    2006-06-01

    Full Text Available Investigation of Helichrysum paronychioides afforded a total of nine compounds: 4 phloroglucinol derivatives, 2 of which are novel natural products, and 5 flavone derivatives. Structures were established by various spectroscopic techniques (NMR, MS, UV, IR, CD and by comparison with literature data for the known compounds. The four phloroglucinols, trans-(2R,3R-5,7-dihydroxy-2,3-dimethyl-4-chromanone (1, 2-butanoyl-4-prenyl-1-methoxy phloroglucinol (2, 2-(2-methylpropanoyl-4-prenylphloroglucinol (3 and 2-(2-methyl- butanoyl-4-prenylphloroglucinol (4 were screened for antioxidant activity against Cu-induced LDL oxidation. Compound 4 was found to be the most active inhibiting LDL oxidation at all concentrations (0.5-10 μM while the other three showed moderate to no activity.

  13. Inconsistency of Minkowski higher-derivative theories

    Energy Technology Data Exchange (ETDEWEB)

    Aglietti, Ugo G. [Universita di Roma ' ' La Sapienza' ' , Dipartimento di Fisica, Rome (Italy); Anselmi, Damiano [Universita di Pisa, Dipartimento di Fisica ' ' Enrico Fermi' ' , Pisa (Italy); INFN, Sezione di Pisa, Pisa (Italy)

    2017-02-15

    We show that Minkowski higher-derivative quantum field theories are generically inconsistent, because they generate nonlocal, non-hermitian ultraviolet divergences, which cannot be removed by means of standard renormalization procedures. By ''Minkowski theories'' we mean theories that are defined directly in Minkowski spacetime. The problems occur when the propagators have complex poles, so that the correlation functions cannot be obtained as the analytic continuations of their Euclidean versions. The usual power counting rules fail and are replaced by much weaker ones. Self-energies generate complex divergences proportional to inverse powers of D'Alembertians. Three-point functions give more involved nonlocal divergences, which couple to infrared effects. We illustrate the violations of the locality and hermiticity of counterterms in scalar models and higher-derivative gravity. (orig.)

  14. Evaluation of antiproliferative activity of pyrazolothiazolopyrimidine derivatives

    Directory of Open Access Journals (Sweden)

    N. S. Finiuk

    2018-04-01

    Full Text Available The research aim was to test cytotoxic effects in vitro of seven novel pyrazolothiazolopyrimidine derivatives in targeting several lines of tumor and pseudo-normal mammalian cells. We demonstrated that cytotoxic effects of these derivatives depended on the tissue origin of targeted cells. Leukemia cells were found to be the most sensitive to the action of compounds 2 and 7. Compound 2 demonstrated approximately two times higher toxicity towards the multidrug-resistant sub-line of HL-60/ADR cells compared to the Doxorubicin effect. Antiproliferative action of compounds 2 and 7 dropped in the order: leukemia > melanoma > hepatocarcinoma > glioblastoma > colon carcinoma > breast and ovarian carcinoma cells. These compounds were less toxic than Doxorubicin towards the non-tumor cells. The novel pyrazolothiazolopyrimidine, compound 2, demonstrated high toxicity towards human leukemia and, of special importance, towards multidrug-resistant leukemia cells, and low toxicity towards pseudo-normal cells.

  15. A generalization of the Lie derivative

    International Nuclear Information System (INIS)

    Dolan, P.

    1984-01-01

    If X=xisup(i)deltasub(i) and Y=etasup(i)deltasub(i) are vector fields then it is well-known that the Lie derivative Poundsub(X)Y equivalent to [X,Y] (xisup(s)deltasub(s) etasup(s)deltasub(s)xisup(i))deltasub(i) is also a vector field under general coordinate transformations. A generalization of this result, due to previous workers, allows a definition of Poundsub(F)G, where F,G are arbitrary contravariant tensor fields. The formulae are linear in the first partial derivatives of F and G. An application to the theory of Killing-Yano tensor fields on Riemannian manifolds is given. (author)

  16. Folic acid derivatives for use in radioimmunoassay

    International Nuclear Information System (INIS)

    Ali, A.

    1981-01-01

    The chemical preparation of two folic acid derivatives, labelled with 125 I or 131 I, is described for use in radioimmunoassay of folic acid and its metabolites in biological fluids such as blood serum. Labelled compounds of the present invention more closely resemble folic acid in that they have glutamic acid in the terminal position. Examples of the use of these compounds in three different assays are given. (U.K.)

  17. Parallel Aircraft Trajectory Optimization with Analytic Derivatives

    Science.gov (United States)

    Falck, Robert D.; Gray, Justin S.; Naylor, Bret

    2016-01-01

    Trajectory optimization is an integral component for the design of aerospace vehicles, but emerging aircraft technologies have introduced new demands on trajectory analysis that current tools are not well suited to address. Designing aircraft with technologies such as hybrid electric propulsion and morphing wings requires consideration of the operational behavior as well as the physical design characteristics of the aircraft. The addition of operational variables can dramatically increase the number of design variables which motivates the use of gradient based optimization with analytic derivatives to solve the larger optimization problems. In this work we develop an aircraft trajectory analysis tool using a Legendre-Gauss-Lobatto based collocation scheme, providing analytic derivatives via the OpenMDAO multidisciplinary optimization framework. This collocation method uses an implicit time integration scheme that provides a high degree of sparsity and thus several potential options for parallelization. The performance of the new implementation was investigated via a series of single and multi-trajectory optimizations using a combination of parallel computing and constraint aggregation. The computational performance results show that in order to take full advantage of the sparsity in the problem it is vital to parallelize both the non-linear analysis evaluations and the derivative computations themselves. The constraint aggregation results showed a significant numerical challenge due to difficulty in achieving tight convergence tolerances. Overall, the results demonstrate the value of applying analytic derivatives to trajectory optimization problems and lay the foundation for future application of this collocation based method to the design of aircraft with where operational scheduling of technologies is key to achieving good performance.

  18. Cholestane derivatives as antitumor and antiangiogenic drugs

    Czech Academy of Sciences Publication Activity Database

    Hoffmannová, L.; Steigerová, J.; Oklešťková, J.; Kohout, Ladislav; Chodounská, Hana; Hniličková, Jaroslava; Kasal, Alexander; Černý, Ivan; Kolář, Z.; Strnad, M.

    2010-01-01

    Roč. 35, SA (2010), s. 205-205 ISSN 0377-8282. [EFMC-ISMC 2010. International Symposium on Medicinal Chemistry /21./. 05.09.2010-09.09.2010, Brussels] R&D Projects: GA MŠk(CZ) LC06077; GA AV ČR KAN200200651 Institutional research plan: CEZ:AV0Z40550506 Keywords : cholestane derivatives * anticancer drugs Subject RIV: CC - Organic Chemistry

  19. On the Feasibility of Decentralized Derivatives Markets

    OpenAIRE

    Eskandari, Shayan; Clark, Jeremy; Sundaresan, Vignesh; Adham, Moe

    2018-01-01

    In this paper, we present Velocity, a decentralized market deployed on Ethereum for trading a custom type of derivative option. To enable the smart contract to work, we also implement a price fetching tool called PriceGeth. We present this as a case study, noting challenges in development of the system that might be of independent interest to whose working on smart contract implementations. We also apply recent academic results on the security of the Solidity smart contract language in valida...

  20. The Brain Derived Neurotrophic Factor and Personality

    OpenAIRE

    Christian Montag

    2014-01-01

    The study of the biological basis of personality is a timely research endeavor, with the aim of deepening our understanding of human nature. In recent years, a growing body of research has investigated the role of the brain derived neurotrophic factor (BDNF) in the context of individual differences across human beings, with a focus on personality traits. A large number of different approaches have been chosen to illuminate the role of BDNF for personality, ranging from the measurement of BDNF...

  1. Alkylation of Zwitterionic Thiooxalic Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Manfred Michalik

    2001-05-01

    Full Text Available The new S-alkyl thiooxal-1-hydrazono-2-amidrazonium halides 2-4 were synthesized by reaction of the corresponding zwitterionic thiooxalic acid derivatives 1 with alkyl halides in methanol. The structures of compounds 4b and 4d were proven by X-ray structural analysis. Both compounds form an interesting intermolecular network of hydrogen bonds in the solid state.

  2. Coronary CT Angiography Derived Fractional Flow Reserve

    DEFF Research Database (Denmark)

    Nørgaard, Bjarne Linde; Jensen, Jesper Møller; Blanke, Philipp

    2017-01-01

    Purpose of Review: To summarize the scientific basis of CT derived fractional flow reserve (FFRCT) and present an updated review on the evidence from clinical trials and real-world observational data Recent Findings: In prospective multicenter studies of patients with stable coronary artery disea...... of patients with stable CAD. The optimal FFRCT testing interpretation strategy, as well as the relative cost-efficiency of FFRCT against standard noninvasive functional testing, need further investigation....

  3. Eisenhart lift for higher derivative systems

    Energy Technology Data Exchange (ETDEWEB)

    Galajinsky, Anton, E-mail: galajin@tpu.ru; Masterov, Ivan, E-mail: masterov@tpu.ru

    2017-02-10

    The Eisenhart lift provides an elegant geometric description of a dynamical system of second order in terms of null geodesics of the Brinkmann-type metric. In this work, we attempt to generalize the Eisenhart method so as to encompass higher derivative models. The analysis relies upon Ostrogradsky's Hamiltonian. A consistent geometric description seems feasible only for a particular class of potentials. The scheme is exemplified by the Pais–Uhlenbeck oscillator.

  4. Strong commutativity preserving generalized derivations on ...

    African Journals Online (AJOL)

    Let R be a non-commutative prime ring of characteristic different from 2, with right Utumi quotient ring U and extended centroid C and let F and G be generalized derivations of R such that F(x)G(y)-F(y)G(x) = [x; y], for all x; y ∈ S, where S is a subset of R. Here we will discuss the following cases: (a) S = [R;R];. b) S = L, where ...

  5. Covariant derivatives of the Berezin transform

    Czech Academy of Sciences Publication Activity Database

    Engliš, Miroslav; Otáhalová, R.

    2011-01-01

    Roč. 363, č. 10 (2011), s. 5111-5129 ISSN 0002-9947 R&D Projects: GA AV ČR IAA100190802 Keywords : Berezin transform * Berezin symbol * covariant derivative Subject RIV: BA - General Mathematics Impact factor: 1.093, year: 2011 http://www.ams.org/journals/tran/2011-363-10/S0002-9947-2011-05111-1/home.html

  6. Derivation of plutonium-239 materials disposition categories

    International Nuclear Information System (INIS)

    Brough, W.G.

    1995-01-01

    At this time, the Office of Fissile Materials Disposition within the DOE, is assessing alternatives for the disposition of excess fissile materials. To facilitate the assessment, the Plutonium-Bearing Materials Feed Report for the DOE Fissile Materials Disposition Program Alternatives report was written. The development of the material categories and the derivation of the inventory quantities associated with those categories is documented in this report

  7. On butterfly effect in higher derivative gravities

    Energy Technology Data Exchange (ETDEWEB)

    Alishahiha, Mohsen [School of Physics, Institute for Research in Fundamental Sciences (IPM),P.O. Box 19395-5531, Tehran (Iran, Islamic Republic of); Davody, Ali; Naseh, Ali; Taghavi, Seyed Farid [School of Particles and Accelerators, Institute for Research in Fundamental Sciences (IPM),P.O. Box 19395-5531, Tehran (Iran, Islamic Republic of)

    2016-11-07

    We study butterfly effect in D-dimensional gravitational theories containing terms quadratic in Ricci scalar and Ricci tensor. One observes that due to higher order derivatives in the corresponding equations of motion there are two butterfly velocities. The velocities are determined by the dimension of operators whose sources are provided by the metric. The three dimensional TMG model is also studied where we get two butterfly velocities at generic point of the moduli space of parameters. At critical point two velocities coincide.

  8. On butterfly effect in higher derivative gravities

    International Nuclear Information System (INIS)

    Alishahiha, Mohsen; Davody, Ali; Naseh, Ali; Taghavi, Seyed Farid

    2016-01-01

    We study butterfly effect in D-dimensional gravitational theories containing terms quadratic in Ricci scalar and Ricci tensor. One observes that due to higher order derivatives in the corresponding equations of motion there are two butterfly velocities. The velocities are determined by the dimension of operators whose sources are provided by the metric. The three dimensional TMG model is also studied where we get two butterfly velocities at generic point of the moduli space of parameters. At critical point two velocities coincide.

  9. Literature Review of Polymer Derived Ceramics

    Energy Technology Data Exchange (ETDEWEB)

    Peterson, Reuben James [Los Alamos National Lab. (LANL), Los Alamos, NM (United States)

    2016-05-25

    Polymer Derived Ceramics (PDCs), also known as preceramic polymers, are valuable coating agents that are used to produce surface barriers on substrates such as stainless steel. These barriers protect against a multitude of environmental threats, and have been used since their research and development in 19772. This paper seeks to review and demonstrate the remarkable properties and versatility that PDCs have to offer, while also giving a brief overview of the processing techniques used today.

  10. Photoinactivation of HIV by benzoporphyrin derivative

    International Nuclear Information System (INIS)

    North, J.; Levy, J.; Coombs, R.

    1992-01-01

    Using both the feline leukemia virus and human immunodeficiency virus it is shown that the photosensitizer benzoporphyrin derivative when activated by narrow band red light is effective in eliminating both free virus and virally infected leukocytes from spiked blood products and whole blood drawn from either virally infected animals or humans, under conditions which appear to spare red cell and uninfected leukocytes. (author). 14 refs., 7 figs

  11. Derivatives of the Incomplete Beta Function

    Directory of Open Access Journals (Sweden)

    Robert J. Boik

    1998-03-01

    Full Text Available The incomplete beta function is defined as where Beta(p, q is the beta function. Dutka (1981 gave a history of the development and numerical evaluation of this function. In this article, an algorithm for computing first and second derivatives of Ix,p,q with respect to p and q is described. The algorithm is useful, for example, when fitting parameters to a censored beta, truncated beta, or a truncated beta-binomial model.

  12. Detectability in a derivative Moessbauer spectroscopy

    International Nuclear Information System (INIS)

    Yoshimura, Takeaki; Miyamoto, Masashi; Wakabayashi, Nobuo

    1978-01-01

    In Moessbauer spectrometry, a criterion for detecting a faint peak under the condition that the peak is superimposed onto a tail of a large and broad peak is discussed. By adopting a derivative method, it is found that the criterion is improved in comparison with a usual method, and that the condition for determining the modulation amplitude W/2 is 1.5 GAMMA 1 1 where GAMMA 1 is the spectral linewidth of the faint peak. (auth.)

  13. Bio-Detergent oil derivative used frying

    Directory of Open Access Journals (Sweden)

    Alfonso Jesús Torres Ortega

    2011-04-01

    Full Text Available Currently, the global trend towards sustainable development for environmental friendly products such as biosurfactants shows an excellent performance. Anionic surface active agents can be produced from renewable natural raw materials such as vegetable oils mainly derived from palm oil. Methyl ester sulfonate is an active component of highly biodegradable detergents, one advantage compared with detergents derived from petrochemicals which generate a high pollutant load. This paper proposes the study of sulfonation with sulfur trioxide of esters derived from waste cooking oil which main component is palm oil. The falling film reactor allows determining the conditions of the process at pilot scale. The experimentation allowed an enhancement of empirical equations in the equipment implemented for this purpose and to determine some physicochemical properties. The comparison obtained for this same process with petrochemicals compounds indicates that the model could be applied to any film sulfonation but adjusting the parameters and specific conditions, such as the physicochemical properties of the compounds used, since the sulfonation process described in this work is one of the more complicated cases. The technological development presented here seeks to contribute with the industrial needs to promote green chemical industry for the production of biosurfactant from waste frying oil.

  14. 7-oxygenated Derivatives of Dehydroepiandrosterone and Obesity

    Directory of Open Access Journals (Sweden)

    B. Sedláčková

    2012-01-01

    Full Text Available 7-hydroxy/oxo derivatives of dehydroepiandrosterone are potential regulators of the local cortisol activity due to their competition in the cortisolcortisone balance mediated by 11β-hydroxysteroid dehydrogenase. 7-hydroxydehydroepiandrosterone is marketed as anti-obesity medication, though no clinical study aimed at the benefit of administering 7-oxygenated derivatives of dehydroepiandrosterone has appeared until now. We tried to show whether there exist differences in levels of circulating 7-hydroxy/oxo-dehydroepiandrosterone derivatives between lean and obese boys and girls. From a cohort of adolescents investigated within the frame of anti-obesity programme 10 obese boys and 10 obese girls were compared with age-matched lean boys and girls in their anthropometric data, and concentrations of both epimers of 7-hydroxydehydroepiandrosterone and 7-oxo-dehydroepiandrosterone were determined by the RIA method. The basal levels of 7α-hydroxy-dehydroepiandrosterone were significantly higher in obese boys than in lean boys but not in girls. The association was found for anthropometric parameters and 7α-hydroxy-dehydroepiandrosterone, however again only in boys and not in girls. Higher levels of 7α-hydroxydehydroepiandrosterone its positive association with anthropometric data in obese boys may serve as a sign that, at least in boys, 7-oxygenated 5-ene-steroids may take part in regulating the hormonal signal for fat formation or distribution.

  15. Metal complex derivatives of hydrogen uranyl phosphate

    International Nuclear Information System (INIS)

    Grohol, D.; Blinn, E.L.

    1994-01-01

    Derivatives of hydrogen uranyl phosphate were prepared by incorporating transition metal complexes into the uranyl phosphate matrix. The transition metal complexes employed include bis(ethylenediamine)copper(II), bis(1,3-propanediamine)copper(II) chloride, (triethylenetetramine)copper(II), (1,4,8,11-tetraazacyclotetradecane)copper(II), (1,4,8,12-tetraazacyclopentadecane)copper(II), (1,4,8,11-tetraazacyclotetradecane)nickel(II) chloride, (triethylenetetramine)nickel(II) and others. The chemical analyses of these derivatives indicated that the incorporation of the transition metal complexes into the uranyl phosphate matrix via ion exchange was not stoichiometric. The extent of ion exchange is dependent on the size and structure of the transition metal complex. All complexes were characterized by X-ray powder diffractometry, electronic and infrared spectra, thermal analyses and chemical analysis. An attempt was made to correlate the degree of quenching of the luminescence of the uranyl ion to the spacing between the uranyl phosphate layers in the derivatives

  16. Price models for oil derivates in Slovenia

    International Nuclear Information System (INIS)

    Nemac, F.; Saver, A.

    1995-01-01

    In Slovenia, a law is currently applied according to which any change in the price of oil derivatives is subject to the Governmental approval. Following the target of getting closer to the European Union, the necessity has arisen of finding ways for the introduction of liberalization or automated approach to price modifications depending on oscillations of oil derivative prices on the world market and the rate of exchange of the American dollar. It is for this reason that at the Agency for Energy Restructuring we made a study for the Ministry of Economic Affairs and Development regarding this issue. We analysed the possible models for the formation of oil derivative prices for Slovenia. Based on the assessment of experiences of primarily the west European countries, we proposed three models for the price formation for Slovenia. In future, it is expected that the Government of the Republic of Slovenia will make a selection of one of the proposed models to be followed by enforcement of price liberalization. The paper presents two representative models for price formation as used in Austria and Portugal. In the continuation the authors analyse the application of three models that they find suitable for the use in Slovenia. (author)

  17. Surface spectral emissivity derived from MODIS data

    Science.gov (United States)

    Chen, Yan; Sun-Mack, Sunny; Minnis, Patrick; Smith, William L.; Young, David F.

    2003-04-01

    Surface emissivity is essential for many remote sensing applications including the retrieval of the surface skin temperature from satellite-based infrared measurements, determining thresholds for cloud detection and for estimating the emission of longwave radiation from the surface, an important component of the energy budget of the surface-atmosphere interface. In this paper, data from the Terra MODIS (MODerate-resolution Imaging Spectroradiometer) taken at 3.7, 8.5, 10.8, 12.0 micron are used to simultaneously derive the skin temperature and the surface emissivities at the same wavelengths. The methodology uses separate measurements of the clear-sky temperatures that are determined by the CERES (Clouds and Earth's Radiant Energy System) scene classification in each channel during the daytime and at night. The relationships between the various channels at night are used during the day when solar reflectance affects the 3.7 micron data. A set of simultaneous equations is then solved to derive the emissivities. Global results are derived from MODIS. Numerical weather analyses are used to provide soundings for correcting the observed radiances for atmospheric absorption. These results are verified and will be available for remote sensing applications.

  18. Modeling of heat conduction via fractional derivatives

    Science.gov (United States)

    Fabrizio, Mauro; Giorgi, Claudio; Morro, Angelo

    2017-09-01

    The modeling of heat conduction is considered by letting the time derivative, in the Cattaneo-Maxwell equation, be replaced by a derivative of fractional order. The purpose of this new approach is to overcome some drawbacks of the Cattaneo-Maxwell equation, for instance possible fluctuations which violate the non-negativity of the absolute temperature. Consistency with thermodynamics is shown to hold for a suitable free energy potential, that is in fact a functional of the summed history of the heat flux, subject to a suitable restriction on the set of admissible histories. Compatibility with wave propagation at a finite speed is investigated in connection with temperature-rate waves. It follows that though, as expected, this is the case for the Cattaneo-Maxwell equation, the model involving the fractional derivative does not allow the propagation at a finite speed. Nevertheless, this new model provides a good description of wave-like profiles in thermal propagation phenomena, whereas Fourier's law does not.

  19. FOREST AREA DERIVATION FROM SENTINEL-1 DATA

    Directory of Open Access Journals (Sweden)

    A. Dostálová

    2016-06-01

    Full Text Available The recently launched Sentinel-1A provides the high resolution Synthetic Aperture Radar (SAR data with very high temporal coverage over large parts of European continent. Short revisit time and dual polarization availability supports its usability for forestry applications. The following study presents an analysis of the potential of the multi-temporal dual-polarization Sentinel-1A data for the forest area derivation using the standard methods based on Otsu thresholding and K-means clustering. Sentinel-1 data collected in winter season 2014-2015 over a test area in eastern Austria were used to derive forest area mask with spatial resolution of 10m and minimum mapping unit of 500 m2. The validation with reference forest mask derived from airborne full-waveform laser scanning data revealed overall accuracy of 92 % and kappa statistics of 0.81. Even better results can be achieved when using external mask for urban areas, which might be misclassified as forests when using the introduced approach based on SAR data only. The Sentinel-1 data and the described methods are well suited for forest change detection between consecutive years.

  20. P-Splines Using Derivative Information

    KAUST Repository

    Calderon, Christopher P.

    2010-01-01

    Time series associated with single-molecule experiments and/or simulations contain a wealth of multiscale information about complex biomolecular systems. We demonstrate how a collection of Penalized-splines (P-splines) can be useful in quantitatively summarizing such data. In this work, functions estimated using P-splines are associated with stochastic differential equations (SDEs). It is shown how quantities estimated in a single SDE summarize fast-scale phenomena, whereas variation between curves associated with different SDEs partially reflects noise induced by motion evolving on a slower time scale. P-splines assist in "semiparametrically" estimating nonlinear SDEs in situations where a time-dependent external force is applied to a single-molecule system. The P-splines introduced simultaneously use function and derivative scatterplot information to refine curve estimates. We refer to the approach as the PuDI (P-splines using Derivative Information) method. It is shown how generalized least squares ideas fit seamlessly into the PuDI method. Applications demonstrating how utilizing uncertainty information/approximations along with generalized least squares techniques improve PuDI fits are presented. Although the primary application here is in estimating nonlinear SDEs, the PuDI method is applicable to situations where both unbiased function and derivative estimates are available.

  1. Generalised derived limits for radioisotopes of iodine

    International Nuclear Information System (INIS)

    Hughes, J.S.; Haywood, S.M.; Simmonds, J.R.

    1984-04-01

    Generalised Derived Limits (GDLs) are evaluated for iodine-125,129,131,132,133,134,135 in selected materials from the terrestrial and aquatic environments and for discharge to atmosphere. They are intended for use as convenient reference levels against which the results of environmental monitoring can be compared and atmospheric discharges assessed. GDLs are intended for use when the environmental contamination or discharge to atmosphere is less than about 5% of the GDL. If the level of environmental contamination or discharge to the atmosphere exceeds this percentage of the GDL it does not necessarily mean that the dose equivalents to members of the public are approaching the dose equivalent limit. It is rather an indication that it may be appropriate to obtain a more specific derived limit for the particular situation by reviewing the values of the parameters involved in the calculation. GDL values are specified for iodine radionuclides in water, soil, grass, sediments and various foodstuffs derived from the terrestrial and aquatic environments. GDLs are also given for iodine radionuclides on terrestrial surfaces and for their discharge to atmosphere. (author)

  2. Naturally Occurring Cinnamic Acid Sugar Ester Derivatives

    Directory of Open Access Journals (Sweden)

    Yuxin Tian

    2016-10-01

    Full Text Available Cinnamic acid sugar ester derivatives (CASEDs are a class of natural product with one or several phenylacrylic moieties linked with the non-anomeric carbon of a glycosyl skeleton part through ester bonds. Their notable anti-depressant and brains protective activities have made them a topic of great interest over the past several decades. In particular the compound 3′,6-disinapoylsucrose, the index component of Yuanzhi (a well-known Traditional Chinese Medicine or TCM, presents antidepressant effects at a molecular level, and has become a hotspot of research on new lead drug compounds. Several other similar cinnamic acid sugar ester derivatives are reported in traditional medicine as compounds to calm the nerves and display anti-depression and neuroprotective activity. Interestingly, more than one third of CASEDs are distributed in the family Polygalaceae. This overview discusses the isolation of cinnamic acid sugar ester derivatives from plants, together with a systematic discussion of their distribution, chemical structures and properties and pharmacological activities, with the hope of providing references for natural product researchers and draw attention to these interesting compounds.

  3. 32 CFR 2400.16 - Derivative classification markings.

    Science.gov (United States)

    2010-07-01

    ... SECURITY PROGRAM Derivative Classification § 2400.16 Derivative classification markings. (a) Documents... 32 National Defense 6 2010-07-01 2010-07-01 false Derivative classification markings. 2400.16..., as described in § 2400.12 of this part, the information may not be used as a basis for derivative...

  4. 17 CFR 240.16a-4 - Derivative securities.

    Science.gov (United States)

    2010-04-01

    ... 17 Commodity and Securities Exchanges 3 2010-04-01 2010-04-01 false Derivative securities. 240.16a....16a-4 Derivative securities. (a) For purposes of section 16 of the Act, both derivative securities and... securities, except that the acquisition or disposition of any derivative security shall be separately...

  5. 14 CFR 1203.501 - Applying derivative classification markings.

    Science.gov (United States)

    2010-01-01

    ... INFORMATION SECURITY PROGRAM Derivative Classification § 1203.501 Applying derivative classification markings. Persons who apply derivative classification markings shall: (a) Observe and respect original... 14 Aeronautics and Space 5 2010-01-01 2010-01-01 false Applying derivative classification markings...

  6. On Functional Inequalities Originating from Module Jordan Left Derivations

    OpenAIRE

    Kang Sheon-Young; Chang Ick-Soon; Kim Hark-Mahn

    2008-01-01

    Abstract We first examine the generalized Hyers-Ulam stability of functional inequality associated with module Jordan left derivation (resp., module Jordan derivation). Secondly, we study the functional inequality with linear Jordan left derivation (resp., linear Jordan derivation) mapping into the Jacobson radical.

  7. On Functional Inequalities Originating from Module Jordan Left Derivations

    Directory of Open Access Journals (Sweden)

    Kang Sheon-Young

    2008-01-01

    Full Text Available Abstract We first examine the generalized Hyers-Ulam stability of functional inequality associated with module Jordan left derivation (resp., module Jordan derivation. Secondly, we study the functional inequality with linear Jordan left derivation (resp., linear Jordan derivation mapping into the Jacobson radical.

  8. Lie n-derivations on 7 -subspace lattice algebras

    Indian Academy of Sciences (India)

    all x ∈ K and all A ∈ Alg L. Based on this result, a complete characterization of linear n-Lie derivations on Alg L is obtained. Keywords. J -subspace lattice algebras; Lie derivations; Lie n-derivations; derivations. 2010 Mathematics Subject Classification. 47B47, 47L35. 1. Introduction. Let A be an algebra. Recall that a linear ...

  9. Haenamindole, an unusual diketopiperazine derivative from a marine-derived Penicillium sp. KCB12F005.

    Science.gov (United States)

    Kim, Jong Won; Ko, Sung-Kyun; Son, Sangkeun; Shin, Kee-Sun; Ryoo, In-Ja; Hong, Young-Soo; Oh, Hyuncheol; Hwang, Bang Yeon; Hirota, Hiroshi; Takahashi, Shunji; Kim, Bo Yeon; Osada, Hiroyuki; Jang, Jae-Hyuk; Ahn, Jong Seog

    2015-11-15

    During the chemical investigation of marine-derived fungus, an unusual diketopiperazine (DKP) alkaloid, haenamindole (1), was isolated from a culture of the marine-derived fungus Penicillium sp. KCB12F005. The structure of 1, which possesses benzyl-hydroxypiperazindione and phenyl-pyrimidoindole rings system in the molecule, was elucidated by analysis of NMR and MS data. The stereochemistry of 1 was determined by ROESY and advanced Marfey's method. Copyright © 2015 Elsevier Ltd. All rights reserved.

  10. Performance of small-scale aero-derivative industrial gas turbines derived from helicopter engines

    Directory of Open Access Journals (Sweden)

    Barinyima Nkoi

    2013-12-01

    Full Text Available This paper considers comparative assessment of simple and advanced cycle small-scale aero-derivative industrial gas turbines derived from helicopter engines. More particularly, investigation was made of technical performance of the small-scale aero-derivative engine cycles based on existing and projected cycles for applications in industrial power generation, combined heat and power concept, rotating equipment driving, and/or allied processes. The investigation was done by carrying out preliminary design and performance simulation of a simple cycle (baseline two-spool small-scale aero-derivative turboshaft engine model, and some advanced counterpart aero-derivative configurations. The advanced configurations consist of recuperated and intercooled/recuperated engine cycles of same nominal power rating of 1.567 MW. The baseline model was derived from the conversion of an existing helicopter engine model. In doing so, design point and off-design point performances of the engine models were established. In comparing their performances, it was observed that to a large extent, the advanced engine cycles showed superior performance in terms of thermal efficiency, and specific fuel consumption. In numerical terms, thermal efficiencies of recuperated engine cycle, and intercooled/recuperated engine cycles, over the simple cycle at DP increased by 13.5%, and 14.5% respectively, whereas specific fuel consumption of these cycles over simple cycle at DP decreased by 12.5%, and 13% respectively. This research relied on open access public literature for data.

  11. Superstability for Generalized Module Left Derivations and Generalized Module Derivations on a Banach Module (I

    Directory of Open Access Journals (Sweden)

    Huai-Xin Cao

    2009-01-01

    Full Text Available We discuss the superstability of generalized module left derivations and generalized module derivations on a Banach module. Let 𝒜 be a Banach algebra and X a Banach 𝒜-module, f:X→X and g:𝒜→𝒜. The mappings Δf,g1, Δf,g2, Δf,g3, and Δf,g4 are defined and it is proved that if ∥Δf,g1(x,y,z,w∥ (resp., ∥Δf,g3(x,y,z,w,α,β∥ is dominated by φ(x,y,z,w, then f is a generalized (resp., linear module-𝒜 left derivation and g is a (resp., linear module-X left derivation. It is also shown that if ∥Δf,g2(x,y,z,w∥ (resp., ∥Δf,g4(x,y,z,w,α,β∥ is dominated by φ(x,y,z,w, then f is a generalized (resp., linear module-𝒜 derivation and g is a (resp., linear module-X derivation.

  12. MODERN TRENDS OF DEVELOPMENT OF INTERNATIONAL DERIVATIVES MARKET

    Directory of Open Access Journals (Sweden)

    V. Shelydko

    2014-09-01

    Full Text Available Article is devoted to analysis of structure and peculiarities of development of the international derivatives market. The history of formation of the international derivatives market is investigated. The nature, functions and advantages of use of derivatives, and also their role in the modern international securities market are defined. Classification of financial derivatives is considered. Product lines of financial derivatives are analyzed. The regional structure of the international derivatives market and dynamics of its development are investigated. The comparative characteristic of volumes and structure of exchange and over-the-counter segments of international derivatives market are carried out. Dynamics and structure of international markets of interest-bearing derivatives and currency derivatives are analyzed. The fundamental trends of development of the modern international derivatives market are defined.

  13. ON THE DERIVATIVE OF SMOOTH MEANINGFUL FUNCTIONS

    Directory of Open Access Journals (Sweden)

    Sanjo Zlobec

    2011-02-01

    Full Text Available The derivative of a function f in n variables at a point x* is one of the most important tools in mathematical modelling. If this object exists, it is represented by the row n-tuple f(x* = [∂f/∂xi(x*] called the gradient of f at x*, abbreviated: “the gradient”. The evaluation of f(x* is usually done in two stages, first by calculating the n partials and then their values at x = x*. In this talk we give an alternative approach. We show that one can characterize the gradient without differentiation! The idea is to fix an arbitrary row n-tuple G and answer the following question: What is a necessary and sufficient condition such that G is the gradient of a given f at a given x*? The answer is given after adjusting the quadratic envelope property introduced in [3]. We work with smooth, i.e., continuously differentiable, functions with a Lipschitz derivative on a compact convex set with a non-empty interior. Working with this class of functions is not a serious restriction. In fact, loosely speaking, “almost all” smooth meaningful functions used in modelling of real life situations are expected to have a bounded “acceleration” hence they belong to this class. In particular, the class contains all twice differentiable functions [1]. An important property of the functions from this class is that every f can be represented as the difference of some convex function and a convex quadratic function. This decomposition was used in [3] to characterize the zero derivative points. There we obtained reformulations and augmentations of some well known classic results on optimality such as Fermats extreme value theorem (known from high school and the Lagrange multiplier theorem from calculus [2, 3]. In this talk we extend the results on zero derivative points to characterize the relation G = f(x*, where G is an arbitrary n-tuple. Some special cases: If G = O, we recover the results on zero derivative points. For functions of a single

  14. Usefulness Of Derivative Instruments In Emerging Markets: Turkish Experience

    OpenAIRE

    Cem Saatcioglu; Iskender Karagul; Ara G. Volkan

    2011-01-01

    This article presents an overview of derivative markets, definitions of derivative investment instruments, development of global derivative markets and the applicability of derivative markets in Turkey, given their economic value added to the Turkish economy. Readers will acquire insight into investing in various investment instruments and hedging against risk. Turkish derivative markets will be described, supportive statistical data will be presented, and readers will be introduced to the de...

  15. Biologic rhythms derived from Siberian mammoths' hairs.

    Directory of Open Access Journals (Sweden)

    Mike Spilde

    Full Text Available Hair is preserved for millennia in permafrost; it enshrines a record of biologic rhythms and offers a glimpse at chronobiology as it was in extinct animals. Here we compare biologic rhythms gleaned from mammoth's hairs with those of modern human hair. Four mammoths' hairs came from varying locations in Siberia 4600 km, four time zones, apart ranging in age between 18,000 and 20,000 years before present. We used two contemporaneous human hairs for comparison. Power spectra derived from hydrogen isotope ratios along the length of the hairs gave insight into biologic rhythms, which were different in the mammoths depending on location and differed from humans. Hair growth for mammoths was ∼31 cms/year and ∼16 cms/year for humans. Recurrent annual rhythms of slow and fast growth varying from 3.4 weeks/cycles to 8.7 weeks/cycles for slow periods and 1.2 weeks/cycles to 2.2 weeks/cycles for fast periods were identified in mammoth's hairs. The mineral content of mammoth's hairs was measured by electron microprobe analysis (k-ratios, which showed no differences in sulfur amongst the mammoth hairs but significantly more iron then in human hair. The fractal nature of the data derived from the hairs became evident in Mandelbrot sets derived from hydrogen isotope ratios, mineral content and geographic location. Confocal microscopy and scanning electron microscopy showed varied degrees of preservation of the cuticle largely independent of age but not location of the specimens. X-ray fluorescence microprobe and fluorescence computed micro-tomography analyses allowed evaluation of metal distribution and visualization of hollow tubes in the mammoth's hairs. Seasonal variations in iron and copper content combined with spectral analyses gave insights into variation in food intake of the animals. Biologic rhythms gleaned from power spectral plots obtained by modern methods revealed life style and behavior of extinct mega-fauna.

  16. Studies in higher-derivative gravitation

    International Nuclear Information System (INIS)

    Dutt, S.K.

    1987-01-01

    In this work two formulations of gravitation in which the action includes the second-derivatives of the metric in a non-trivial fashion are investigated. In the first part, the gauge theory of gravitation proposed by Yang in 1974 is investigated. The implications of coupling the pure space equations to matter sources via the action principle proposed by Yang is studied. It is shown that this action principle does not couple to matter sources in a satisfactory fashion. An earlier study by Fairchild along similar lines is critically examined. It is argued that Fairchild's action functional, and his objections to Yang's gauge approach to gravitation, arise from a not very meaningful analogy with the case of a general gauge field. Also, a conjecture originated in that work is refuted. A modification of Yang's action functional is provided which leads to both the Einstein and Yang field-equations. This system is shown to have non-trivial solutions in the presence of matter. An additional advantage is that the unphysical solutions of the pure space equations can be ruled out. It is shown that the joint system of Einstein and Yang field-equations leads to a physically viable cosmological model based on the Robertson-Walker metric, which satisfies both sets of field-equations. In the second part of this work, the Hamiltonian for pure gravity in Einstein's theory is obtained directly from the Hilbert Lagrangian. Since the Lagrangian depends upon the second-derivatives of the metric tensor, first the Hamiltonian formulation for a Lagrangian which may, in general depend upon the Nth-order time derivatives of the dynamical variables is developed

  17. Hydration of urea and alkylated urea derivatives

    Science.gov (United States)

    Kaatze, Udo

    2018-01-01

    Compressibility data and broadband dielectric spectra of aqueous solutions of urea and some of its alkylated derivatives have been evaluated to yield their numbers Nh of hydration water molecules per molecule of solute. Nh values in a broad range of solute concentrations are discussed and are compared to hydration numbers of other relevant molecules and organic ions. Consistent with previous results, it is found that urea differs from other solutes in its unusually small hydration number, corresponding to just one third of the estimated number of nearest neighbor molecules. This remarkable hydration behavior is explained by the large density φH of hydrogen bonding abilities offered by the urea molecule. In terms of currently discussed models of reorientational motions and allied dynamics in water and related associating liquids, the large density φH causes a relaxation time close to that of undisturbed water with most parts of water encircling the solute. Therefore only a small part of disturbed ("hydration") water is left around each urea molecule. Adding alkyl groups to the basic molecule leads to Nh values which, within the series of n-alkylurea derivatives, progressively increase with the number of methyl groups per solute. With n-butylurea, Nh from dielectric spectra, in conformity with many other organic solutes, slightly exceeds the number of nearest neighbors. Compared to such Nh values, hydration numbers from compressibility data are substantially smaller, disclosing incorrect assumptions in the formula commonly used to interpret the experimental compressibilities. Similar to other series of organic solutes, effects of isomerization have been found with alkylated urea derivatives, indicating that factors other than the predominating density φH of hydrogen bond abilities contribute also to the hydration properties.

  18. Warm Inflation with Nonminimal Derivative Coupling

    International Nuclear Information System (INIS)

    Rashidi, N.; Nozari, Kourosh; Shoukrani, M.

    2014-01-01

    We study the effects of the nonminimal derivative coupling on the dissipative dynamics of the warm inflation where the scalar field is nonminimally coupled to gravity via its kinetic term. We present a detailed calculation of the cosmological perturbations in this setup. We use the recent observational data from the joint data set of WMAP9 + BAO + H 0 and also the Planck satellite data to constrain our model parameters for natural and chaotic inflation potentials. We study also the levels of non-Gaussianity in this warm inflation model and we confront the result with recent observational data from the Planck satellite

  19. Nonextensive entropies derived from Gauss' principle

    International Nuclear Information System (INIS)

    Wada, Tatsuaki

    2011-01-01

    Gauss' principle in statistical mechanics is generalized for a q-exponential distribution in nonextensive statistical mechanics. It determines the associated stochastic and statistical nonextensive entropies which satisfy Greene-Callen principle concerning on the equivalence between microcanonical and canonical ensembles. - Highlights: → Nonextensive entropies are derived from Gauss' principle and ensemble equivalence. → Gauss' principle is generalized for a q-exponential distribution. → I have found the condition for satisfying Greene-Callen principle. → The associated statistical q-entropy is found to be normalized Tsallis entropy.

  20. Deriving GENERIC from a Generalized Fluctuation Symmetry

    Science.gov (United States)

    Kraaij, Richard; Lazarescu, Alexandre; Maes, Christian; Peletier, Mark

    2018-02-01

    Much of the structure of macroscopic evolution equations for relaxation to equilibrium can be derived from symmetries in the dynamical fluctuations around the most typical trajectory. For example, detailed balance as expressed in terms of the Lagrangian for the path-space action leads to gradient zero-cost flow. We expose a new such fluctuation symmetry that implies GENERIC, an extension of gradient flow where a Hamiltonian part is added to the dissipative term in such a way as to retain the free energy as Lyapunov function.

  1. Superspace higher derivative terms in two dimensions

    Energy Technology Data Exchange (ETDEWEB)

    Farakos, Fotis [Dipartimento di Fisica “Galileo Galilei”, Università di Padova,Via Marzolo 8, 35131 Padova (Italy); INFN, Sezione di Padova,Via Marzolo 8, 35131 Padova (Italy); Kočí, Pavel; Unge, Rikard von [Institute for Theoretical Physics, Masaryk University,611 37 Brno (Czech Republic)

    2017-04-03

    We study (2,2) and (4,4) supersymmetric theories with superspace higher derivatives in two dimensions. A characteristic feature of these models is that they have several different vacua, some of which break supersymmetry. Depending on the vacuum, the equations of motion describe different propagating degrees of freedom. Various examples are presented which illustrate their generic properties. As a by-product we see that these new vacua give a dynamical way of generating non-linear realizations. In particular, our 2D (4,4) example is the dimensional reduction of a 4D N=2 model, and gives a new way for the spontaneous breaking of extended supersymmetry.

  2. Derivation of Batho's correction factor for heterogeneities

    International Nuclear Information System (INIS)

    Lulu, B.A.; Bjaerngard, B.E.

    1982-01-01

    Batho's correction factor for dose in a heterogeneous, layered medium is derived from the tissue--air ratio method (TARM). The reason why the Batho factor is superior to the TARM factor at low energy is ascribed to the fact that it accounts for the distribution of the scatter-generating matter along the centerline. The poor behavior of the Batho factor at high energies is explained as a consequence of the lack of electron equilibrium at appreciable depth below the surface. Key words: Batho factor, heterogeneity, inhomogeneity, tissue--air ratio method

  3. Derivative expansion and renormalisation group flows

    CERN Document Server

    Litim, Daniel F

    2001-01-01

    We study the convergence of the derivative expansion for flow equations. The convergence strongly depends on the choice for the infrared regularisation. Based on the structure of the flow, we explain why optimised regulators lead to better physical predictions. This is applied to O(N)-symmetric real scalar field theories in 3d, where critical exponents are computed for all N. In comparison to the sharp cut-off regulator, an optimised flow improves the leading order result up to 10%. An analogous reasoning is employed for a proper time renormalisation group. We compare our results with those obtained by other methods.

  4. [A new eremophilane derivative from Senecio dianthus].

    Science.gov (United States)

    Han, He-Dong; Hu, Hai-Qing; Li, Yan; Wang, Xiao-Ling

    2013-10-01

    A new eremophilane derivative, 4,5,11-trimethyl-9( 10), 7 ( 11) -eremophiladien-8-keto-12-carboxylic acid-beta-D-glucopyranoside( which named dianthuside A) 1 and four known compounds, 5,7,4'-trihydroxy-flavonone-3-0-beta-D-glucoside (2), quercetin-3-0-beta-D-glucoside(3) ,hyperin(4) and rutin(5) have been isolated from the aerial part of Senecio dianthus. Their structures were elucidated by physicochemical properties and spectroscopic data analysis. Compounds 2, 4 and 5 were isolated from this plant for the first time.

  5. Black holes in higher derivative gravity.

    Science.gov (United States)

    Lü, H; Perkins, A; Pope, C N; Stelle, K S

    2015-05-01

    Extensions of Einstein gravity with higher-order derivative terms arise in string theory and other effective theories, as well as being of interest in their own right. In this Letter we study static black-hole solutions in the example of Einstein gravity with additional quadratic curvature terms. A Lichnerowicz-type theorem simplifies the analysis by establishing that they must have vanishing Ricci scalar curvature. By numerical methods we then demonstrate the existence of further black-hole solutions over and above the Schwarzschild solution. We discuss some of their thermodynamic properties, and show that they obey the first law of thermodynamics.

  6. A microscopic derivation of stochastic differential equations

    International Nuclear Information System (INIS)

    Arimitsu, Toshihico

    1996-01-01

    With the help of the formulation of Non-Equilibrium Thermo Field Dynamics, a unified canonical operator formalism is constructed for the quantum stochastic differential equations. In the course of its construction, it is found that there are at least two formulations, i.e. one is non-hermitian and the other is hermitian. Having settled which framework should be satisfied by the quantum stochastic differential equations, a microscopic derivation is performed for these stochastic differential equations by extending the projector methods. This investigation may open a new field for quantum systems in order to understand the deeper meaning of dissipation

  7. Derivation of an applied nonlinear Schroedinger equation

    Energy Technology Data Exchange (ETDEWEB)

    Pitts, Todd Alan [Sandia National Laboratories (SNL-NM), Albuquerque, NM (United States); Laine, Mark Richard [Sandia National Laboratories (SNL-NM), Albuquerque, NM (United States); Schwarz, Jens [Sandia National Laboratories (SNL-NM), Albuquerque, NM (United States); Rambo, Patrick K. [Sandia National Laboratories (SNL-NM), Albuquerque, NM (United States); Karelitz, David B. [Sandia National Laboratories (SNL-NM), Albuquerque, NM (United States)

    2015-01-01

    We derive from first principles a mathematical physics model useful for understanding nonlinear optical propagation (including filamentation). All assumptions necessary for the development are clearly explained. We include the Kerr effect, Raman scattering, and ionization (as well as linear and nonlinear shock, diffraction and dispersion). We explain the phenomenological sub-models and each assumption required to arrive at a complete and consistent theoretical description. The development includes the relationship between shock and ionization and demonstrates why inclusion of Drude model impedance effects alters the nature of the shock operator. Unclassified Unlimited Release

  8. Radioprotective properties of sulpholane amidoalkyl derivatives

    International Nuclear Information System (INIS)

    Izmozherov, N.N.; Girshik, G.V.

    A series of sulpholane derivatives has been studied from the viewpoint of their possible anti-radiation efficiency. The highest activity at experiments in vitro has been manifested by compounds with dimethylamide radicals in a molecule. The estimate of anti-radiation action was provided by testing with the analysis of cytogenetic damages in the cell culture of the Chinese hamster. The compounds studied were introduced into the medium 20-30 min before irradiation, with the dose of 600 rad at the intensity of 27 rad/min. The percentage of aberrant metaphases and the number of chromosomal aberrations of various types decreased more than 2 times

  9. Molecular Recognition Studies on Naphthyridine Derivatives

    Directory of Open Access Journals (Sweden)

    José Carlos Iglesias-Sánchez

    2010-03-01

    Full Text Available The association constants Kb of three hosts I–III designed to have both enhanced hydrogen bonding donor strength and conformational preorganization with biotin analogues 1–5 are reported. 1H-NMR titrations under two different concentration conditions have been employed to determine the association constants Kb. A statistical analysis using a presence absence matrix has been applied to calculate the different contributions. Hydrogen bond interactions make naphthyridine derivatives II and III potent binders and effective receptors for (+-biotin methyl ester (1, due to the complex stabilization by additional hydrogen bonds.

  10. Biochemical activity of fullerenes and related derivatives

    International Nuclear Information System (INIS)

    Huczko, A.; Lange, H.; Calko, E.

    1999-01-01

    An astonishing scientific interest, embodied in over 15000 research articles so far, has been encountered since 1985 when fullerenes were discovered. From new superconductors to a rich electrochemistry and reaction chemistry, fullerene nanostructures continue to excite the scientific world, and new findings continue at record pace. This review presents many examples of the biochemical activities of fullerenes and derivatives, e. g. cytotoxic activity, selective DNA cleavage and antiviral activity against HIV. We also present some results of our testing which show that, despite its chemical and biochemical activity, fullerene matter does not present any health hazard directly related to skin irritation and allergic risks. (author)

  11. Pharmacokinetics of thiamine derivatives especially of benfotiamine.

    Science.gov (United States)

    Loew, D

    1996-02-01

    Pharmacokinetic data of orally administered lipid-soluble thiamine analogues like benfotiamine are reviewed and assessed. It is quite clear that benfotiamine is absorbed much more better than water-soluble thiamine salts: maximum plasma levels of thiamine are about 5 times higher after benfotiamine, the bioavailability is at maximum about 3.6 times as high as that of thiamine hydrochloride and better than other lipophilic thiamine derivates. The physiological activity (alphaETK) increased only after benfotiamine was given. Due to its excellent pharmacokinetic profile benfotiamine should be preferred in treatment of relevant indications.

  12. Superspace higher derivative terms in two dimensions

    International Nuclear Information System (INIS)

    Farakos, Fotis; Kočí, Pavel; Unge, Rikard von

    2017-01-01

    We study (2,2) and (4,4) supersymmetric theories with superspace higher derivatives in two dimensions. A characteristic feature of these models is that they have several different vacua, some of which break supersymmetry. Depending on the vacuum, the equations of motion describe different propagating degrees of freedom. Various examples are presented which illustrate their generic properties. As a by-product we see that these new vacua give a dynamical way of generating non-linear realizations. In particular, our 2D (4,4) example is the dimensional reduction of a 4D N=2 model, and gives a new way for the spontaneous breaking of extended supersymmetry.

  13. Bootstrapping Density-Weighted Average Derivatives

    DEFF Research Database (Denmark)

    Cattaneo, Matias D.; Crump, Richard K.; Jansson, Michael

    Employing the "small bandwidth" asymptotic framework of Cattaneo, Crump, and Jansson (2009), this paper studies the properties of a variety of bootstrap-based inference procedures associated with the kernel-based density-weighted averaged derivative estimator proposed by Powell, Stock, and Stoker...... (1989). In many cases validity of bootstrap-based inference procedures is found to depend crucially on whether the bandwidth sequence satisfies a particular (asymptotic linearity) condition. An exception to this rule occurs for inference procedures involving a studentized estimator employing a "robust...

  14. Valence electronic properties of porphyrin derivatives.

    Science.gov (United States)

    Stenuit, G; Castellarin-Cudia, C; Plekan, O; Feyer, V; Prince, K C; Goldoni, A; Umari, P

    2010-09-28

    We present a combined experimental and theoretical investigation of the valence electronic structure of porphyrin-derived molecules. The valence photoemission spectra of the free-base tetraphenylporphyrin and of the octaethylporphyrin molecule were measured using synchrotron radiation and compared with theoretical spectra calculated using the GW method and the density-functional method within the generalized gradient approximation. Only the GW results could reproduce the experimental data. We found that the contribution to the orbital energies due to electronic correlations has the same linear behavior in both molecules, with larger deviations in the vicinity of the HOMO level. This shows the importance of adequate treatment of electronic correlations in these organic systems.

  15. Selective Oxidation of Biomass-Derived Chemicals

    DEFF Research Database (Denmark)

    Modvig, Amalie Elise

    . These processes should be able to compete with the established processes based on fossil resources. Glycolaldehyde is an often-observed by-product formed from degradation of larger sugars. Due to competing ecological and economical aspects of the well-established processes for extraction and conversion....... The objective of this dissertation was to develop new, alternative and sustainable methods for oxidative catalytic upgrading of biomass-derived compounds, with focus on oxidation of glycolaldehyde and simple alcohols as model substrates for larger sugars. Supported gold nanoparticle were studied...

  16. Boundary layer heights derived from velocity spectra

    Energy Technology Data Exchange (ETDEWEB)

    Hoejstrup, J.; Barthelmie, R.J. [Risoe National Lab., Roskilde (Denmark); Kaellstrand, B. [Univ. of Uppsala, Uppsala (Sweden)

    1997-10-01

    It is a well-known fact that the height of the mixed layer determines the size of the largest and most energetic eddies that can be observed in the unstable boundary layer, and consequently a peak can be observed in the power spectra of the along-wind velocity component at scales comparable to the mixed layer depth. We will now show how the mixed layer depth can be derived from the u-specta and the results will be compared with direct measurements using pibal and tethersonde measurements. (au)

  17. History of myeloid-derived suppressor cells.

    Science.gov (United States)

    Talmadge, James E; Gabrilovich, Dmitry I

    2013-10-01

    Tumour-induced granulocytic hyperplasia is associated with tumour vasculogenesis and escape from immunity via T cell suppression. Initially, these myeloid cells were identified as granulocytes or monocytes; however, recent studies have revealed that this hyperplasia is associated with populations of multipotent progenitor cells that have been identified as myeloid-derived suppressor cells (MDSCs). The study of MDSCs has provided a wealth of information regarding tumour pathobiology, has extended our understanding of neoplastic progression and has modified our approaches to immune adjuvant therapy. In this Timeline article, we discuss the history of MDSCs, their influence on tumour progression and metastasis, and the crosstalk between tumour cells, MDSCs and the host macroenvironment.

  18. Measurements of brain-derived neurotrophic factor

    DEFF Research Database (Denmark)

    Trajkovska, Viktorija; Klein, Anders Bue; Vinberg, Maj

    2007-01-01

    Although numerous studies have dealt with changes in blood brain-derived neurotrophic factor (BDNF), methodological issues about BDNF measurements have only been incompletely resolved. We validated BDNF ELISA with respect to accuracy, reproducibility and the effect of storage and repeated freezing...... (18.6+/-1.3 ng/ml versus 16.5+/-1.4 ng/ml), and showed a right-skewed BDNF concentration distribution. No association between whole blood BDNF concentrations and thrombocyte count, age, or BDNF genotype was found. In conclusion, the BDNF ELISA assay determines whole blood BDNF accurately and with high...

  19. Statistical Analysis of Asian WeatherDerivatives

    OpenAIRE

    Jiao, Yue

    2009-01-01

    Since last decade, weather derivatives have been traded by Chicago Mercantile Exchange(CME) to hedge the weather risk. In addition to HDD,CDD and CAT, which are index written on the temperature in U.S. and Europe, Pacific Rim Index is newly developed and actively traded nowadays. In terms of the great value of research on this new instrument, we study the temperature dynamics of 4 cities in Asia: Tokyo, Osaka, Taipei and Beijing by a continuous-time autoregressive process. We further inferred...

  20. Residues in food derived from animals

    International Nuclear Information System (INIS)

    Grossklaus, D.

    1989-01-01

    The first chapter presents a survey of fundamentals and methods of the detection and analysis of residues in food derived from animals, also referring to the resulting health hazards to man, and to the relevant legal provisions. The subsequent chapters have been written by experts of the Federal Health Office, each dealing with particular types of residues such as those of veterinary drugs, additives to animal feeds, pesticide residues, and with environmental pollutants and the contamination of animal products with radionuclides. (MG) With 35 figs., 61 tabs [de

  1. Quinoxaline derivatives: a patent review (2006--present).

    Science.gov (United States)

    González, Mercedes; Cerecetto, Hugo

    2012-11-01

    Quinoxaline scaffold is included in a large number of therapeutic agents because of its physicochemical properties that make the difference between them and the carbono analogue, naphthalene. This review of patented products presents the quinoxaline heterocycle as part of the structural patent claims from a medicinal chemistry perspective. We centred our discussion in the various drug patent applications of the quinoxaline and its derivatives. The applications are based firstly in the specific enzyme target with very low development in the disease treatment. Only for cancer and antimicrobial agents they were specifically determined but little is mentioned in order to insight in the last development activities.

  2. Survey on the Use of Derivatives in Indonesia

    Directory of Open Access Journals (Sweden)

    I Wayan Nuka Lantara

    2010-09-01

    Full Text Available This paper provides survey evidence on the use of derivatives among firms listed on the Indonesian Stock Exchange. The finding shows that the participation rate in the use of derivatives is 28.8 percent, much lower than those found in developed countries. For the derivatives non-users, insignificant risk exposure is reported as the most important rationale for not using derivatives. Consumer goods industry constitutes the largest proportion of firms using derivatives. The majority of respondents utilize derivatives to hedge against financial risks rather than to speculate. Foreign currency risk and interest rate risk are the most important types of risks faced with by respondents. Using the Chi-square and the Fisher’s exact tests, the result corroborates the size effect hypothesis, where the use of derivatives is more popular among large firms than small firms. A SURVEY ON THE USE OF DERIVATIVES IN INDONESIA Keywords: derivatives; hedging; risk management

  3. SYNTHESIS OF FLAVANONE-6-CARBOXYLIC ACID DERIVATIVES FROM SALICYLIC ACID DERIVATIVE

    Directory of Open Access Journals (Sweden)

    Muhammad Idham Darussalam Mardjan

    2012-02-01

    Full Text Available Synthesis of flavanone-6-carboxylic acid derivatives had been conducted via the route of chalcone. The synthesis was carried out from salicylic acid derivative, i.e. 4-hydroxybenzoic acid, via esterification, Fries rearrangement, Claisen-Schmidt condensation and 1,4-nucleophilic addition reactions. Structure elucidation of products was performed using FT-IR, 1H-NMR, GC-MS and UV-Vis spectrometers. Reaction of 4-hydroxybenzoic acid with methanol catalyzed with sulfuric acid produced methyl 4-hydroxybenzoate in 87% yield. The acid-catalyzed-acetylation of the product using acetic anhydride gave methyl 4-acetoxybenzoate in 75% yield. Furthermore, solvent-free Fries rearrangement of methyl 4-acetoxybenzoate in the presence of AlCl3 produced 3-acetyl-4-hydroxybenzoic acid as the acetophenone derivatives in 67% yield. Then, Claisen-Schmidt condensation of the acetophenone and benzaldehyde derivatives of p-anisaldehyde and veratraldehyde in basic condition gave 2'-hydroxychalcone-5'-carboxylic acid derivatives  in 81 and 71 % yield, respectively. Finally, the ring closure reaction of the chalcone yielded the corresponding flavanone-6-carboxylic acids in 67 and 59% yield, respectively.

  4. Deriving inflation forecasts from government bond prices

    Directory of Open Access Journals (Sweden)

    Kožul Nataša

    2014-01-01

    Full Text Available In financial research and practice, it is widely accepted that nominal interest rates derived from the prices of various financial products of different maturities comprise of corresponding real interest rates and inflation. While extensive research has been conducted on the relationship between these three variables, estimation of their levels is still largely based on the industry surveys and market data. As this information only indicates the current expectations of interest rate and inflation movements over time, a number of caveats should be noted when interpreting such measures. In the US and the UK, where the government bond markets are the largest and most active, a comparative analysis between conventional government bonds and those whose yield is linked to inflation provides a measure of inflation expectations. However, as such analyses implicitly assume that investment in government bonds is virtually risk free, it is questionable whether the derived estimates are of any value in current economic conditions. Moreover, this approach cannot be generalized to other countries, where number of traded products from which any relationship between interest rates and inflation can be determined is limited and different economic conditions prevail. Thus, this paper aims to present an overview of the methodologies used to forecast inflation rates from government bond prices, drawing attention to the key assumptions and limitations of these approaches. The goal is to ascertain their accuracy, and thus their value in determining the real yields of various interest rate-linked products.

  5. Derivative Securities on Romanian Capital Market

    Directory of Open Access Journals (Sweden)

    Ramona Maria GOGONCEA

    2011-12-01

    Full Text Available This study aimed to investigate whether the world wide agreed models of valuation of derivates may be properly applied to the Romanian capital market, obtaining reliable results for decision makers. The most common valuation models take into account market data such as, interest and exchange rates, volatilities and the price of the underlying instrument. The procedures for valuation must clearly define the nature of the market data to be taken into consideration (for example the zero-coupon curve for the valuation of swaps and the independent reference base to be used (Reuters at a given time, bid/offer or mid price, broker. In order to be able to obtain the results, I based my study on a self-developed software which can calculate the price and characteristics for different types of derivatives securities once the primary data are filled in. I compared the results obatined usig the valuation models with the actual prices on the Romanian capital market. I expected that the results obtained to be more accurate as the parameters used in the calculation models properly reflect market data as at that date being as widely as possible.. These assumptions were only supported for certain value orientations. In conclusion, explanations for these results are given and limitations for this study are discussed. Also, suggestions for future research are presented in the final part of the article.

  6. Primer on electricity futures and other derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Stoft, S.; Belden, T.; Goldman, C.; Pickle, S.

    1998-01-01

    Increased competition in bulk power and retail electricity markets is likely to lower electricity prices, but will also result in greater price volatility as the industry moves away from administratively determined, cost-based rates and encourages market-driven prices. Price volatility introduces new risks for generators, consumers, and marketers. Electricity futures and other derivatives can help each of these market participants manage, or hedge, price risks in a competitive electricity market. Futures contracts are legally binding and negotiable contracts that call for the future delivery of a commodity. In most cases, physical delivery does not take place, and the futures contract is closed by buying or selling a futures contract on or near the delivery date. Other electric rate derivatives include options, price swaps, basis swaps, and forward contracts. This report is intended as a primer for public utility commissioners and their staff on futures and other financial instruments used to manage price risks. The report also explores some of the difficult choices facing regulators as they attempt to develop policies in this area.

  7. Platelet-Derived Microvesicles in Cardiovascular Diseases

    Directory of Open Access Journals (Sweden)

    Maria T. K. Zaldivia

    2017-11-01

    Full Text Available Microvesicles (MVs circulating in the blood are small vesicles (100–1,000 nm in diameter derived from membrane blebs of cells such as activated platelets, endothelial cells, and leukocytes. A growing body of evidence now supports the concept that platelet-derived microvesicles (PMVs, the most abundant MVs in the circulation, are important regulators of hemostasis, inflammation, and angiogenesis. Compared with healthy individuals, a large increase of circulating PMVs has been observed, particularly in patients with cardiovascular diseases. As observed in MVs from other parent cells, PMVs exert their biological effects in multiple ways, such as triggering various intercellular signaling cascades and by participating in transcellular communication by the transfer of their “cargo” of cytoplasmic components and surface receptors to other cell types. This review describes our current understanding of the potential role of PMVs in mediating hemostasis, inflammation, and angiogenesis and their consequences on the pathogenesis of cardiovascular diseases, such as atherosclerosis, myocardial infarction, and venous thrombosis. Furthermore, new developments of the therapeutic potential of PMVs for the treatment of cardiovascular diseases will be discussed.

  8. Assessment of satellite derived diffuse attenuation coefficients ...

    Science.gov (United States)

    Optical data collected in coastal waters off South Florida and in the Caribbean Sea between January 2009 and December 2010 were used to evaluate products derived with three bio-optical inversion algorithms applied to MOIDS/Aqua, MODIS/Terra, and SeaWiFS satellite observations. The products included the diffuse attenuation coefficient at 490 nm (Kd_490) and for the visible range (Kd_PAR), and euphotic depth (Zeu, corresponding to 1% of the surface incident photosynthetically available radiation or PAR). Above-water hyperspectral reflectance data collected over optically shallow waters of the Florida Keys between June 1997 and August 2011 were used to help understand algorithm performance over optically shallow waters. The in situ data covered a variety of water types in South Florida and the Caribbean Sea, ranging from deep clear waters, turbid coastal waters, and optically shallow waters (Kd_490 range of ~0.03 – 1.29m-1). An algorithm based on Inherent Optical Properties (IOPs) showed the best performance (RMSD turbidity or shallow bottom contamination. Similar results were obtained when only in situ data were used to evaluate algorithm performance. The excellent agreement between satellite-derived remote sensing reflectance (Rrs) and in situ Rrs suggested that

  9. Waste derived bioeconomy in India: A perspective.

    Science.gov (United States)

    S, Venkata Mohan; P, Chiranjeevi; Dahiya, Shikha; A, Naresh Kumar

    2018-01-25

    Environmental and climatic change issues, population explosion, rapid urbanisation, depletion of fossil reserves, need for energy security, huge waste generation, etc. are some of the inherent issues associated with the fossil based linear economy which need greater attention. In this context, the world is gradually transforming from fossil-based economy to a sustainable circular bio-economy. The biogenic waste which is generated in enormous quanties in India can be considered as potential feedstock for structuring the bio-based economy. This communication depicts the need for developing waste derived bioeconomy in the Indian perspective. Waste is now being perceived as a resource with value and believed to supplement petroleum feedstock to a great extent if properly utilized. The necessity to introduce waste as the core element for the future economic models which also allows sustainable development is discussed. The review also establishes drivers for the bioeconomy and structures the waste derived bioeconomy in a sustainable format to address the futuristic needs, scope and opportunities envisaged in the business and economic realm. The enabling technologies/processes that can be applied for biogenic wastes valorisation are elaborated. Circularizing the economy in a waste biorefinery model for the production of biobased products including bioenergy is discussed. Copyright © 2017 Elsevier B.V. All rights reserved.

  10. Primer on electricity futures and other derivatives

    International Nuclear Information System (INIS)

    Stoft, S.; Belden, T.; Goldman, C.; Pickle, S.

    1998-01-01

    Increased competition in bulk power and retail electricity markets is likely to lower electricity prices, but will also result in greater price volatility as the industry moves away from administratively determined, cost-based rates and encourages market-driven prices. Price volatility introduces new risks for generators, consumers, and marketers. Electricity futures and other derivatives can help each of these market participants manage, or hedge, price risks in a competitive electricity market. Futures contracts are legally binding and negotiable contracts that call for the future delivery of a commodity. In most cases, physical delivery does not take place, and the futures contract is closed by buying or selling a futures contract on or near the delivery date. Other electric rate derivatives include options, price swaps, basis swaps, and forward contracts. This report is intended as a primer for public utility commissioners and their staff on futures and other financial instruments used to manage price risks. The report also explores some of the difficult choices facing regulators as they attempt to develop policies in this area

  11. Thermal electron heating rate: a derivation

    International Nuclear Information System (INIS)

    Hoegy, W.R.

    1983-11-01

    The thermal electron heating rate is an important heat source term in the ionospheric electron energy balance equation, representing heating by photoelectrons or by precipitating higher energy electrons. A formula for the thermal electron heating rate is derived from the kinetic equation using the electron-electron collision operator as given by the unified theory of Kihara and Aono. This collision operator includes collective interactions to produce a finite collision operator with an exact Coulomb logarithm term. The derived heating rate O(e) is the sum of three terms, O(e) O(p) + S + O(int), which are respectively: (1) primary electron production term giving the heating from newly created electrons that have not yet suffered collisions with the ambient electrons, (2) a heating term evaluated on the energy surface m(e)/2 E(T) at the transition between Maxwellian and tail electrons at E(T), and (3) the integral term representing heating of Maxwellian electrons by energetic tail electrons at energies ET. Published ionospheric electron temperature studies used only the integral term O(int) with differing lower integration limits. Use of the incomplete heating rate could lead to erroneous conclusions regarding electron heat balance, since O(e) is greater than O(int) by as much as a factor of two

  12. Sorption of uranium by cellulose derivatives

    International Nuclear Information System (INIS)

    Muroi, M.; Imai, S.; Hamaguchi, A.

    1985-01-01

    The sorption behaviour of uranium was investigated by batch and column methods using four cellulose derivatives, two having an amino group and two having an amino group plus a dithiocarboxylate group. All four derivatives showed maximum uranium sorption from pure water in the neutral region or from artificial sea water in the acidic region. In the batch method, quantitative removal of 100 μg of uranium from 50 ml of water at pH 5.0 was achieved by equilibration with 50 mg of any of the four sorbents. The percentage removal under these conditions decreased gradually with increasing concentration of uranium above 100 μg per 50 ml. A similar high percentage removal of uranium was achieved using artificial sea water. In the column method, quantitative removal of 5 μg of uranium from 1l of water at pH 6.7 was achieved with 200 mg of either of the two sorbents. Similar quantitative removal of uranium was achieved from 1l of artificial sea water at pH 5.4 with 500 mg of either of the two sorbents. (author)

  13. Fluoride removal performance of glass derived hydroxyapatite

    International Nuclear Information System (INIS)

    Liang, Wen; Zhan, Lei; Piao, Longhua; Russel, Christian

    2011-01-01

    Research highlights: → Novel sodium calcium borate glass derived hydroxyapatite (G-HAP) is prepared. → Micro-G-HAP adsorbs F - ions in solutions more effectively than commercial nano-HAP. → The adsorption kinetics and isotherms are well fitted by a second order kinetic model and Freundlich isotherm model. -- Abstract: A novel sodium calcium borate glass derived hydroxyapatite (G-HAP) with different ranges of particle size was prepared by immersion sodium calcium borate glass in 0.1 M K 2 HPO 4 solution by the ratio of 50 g L -1 for 7 days. The unique advantage of G-HAP for the adsorption of fluoride ions in solutions was studied. The effects of size and quantity of particles, pH value and adsorption time on adsorption performance were investigated. The maximum adsorption capacity was 17.34 mg g -1 if 5 g L -1 , - in solution more effectively than commercial nano-HAP, which makes potential application of the G-HAP in removing the fluoride ions from wastewater. The adsorption kinetics and isotherms for F - could be well fitted by a second order kinetic model and Freundlich isotherm model respectively, which could be used to describe the adsorption behavior. The mechanism of G-HAP in immobilizing F - from aqueous solutions was investigated by the X-ray diffraction (XRD), infrared spectra (IR) and scanning electron microscopy (SEM).

  14. Chromoionophoric Recognition of Alkylamines by Nitro Derivative

    International Nuclear Information System (INIS)

    Kim, Ju Hee; Hwang, Ah Ran; Choe, Jong In; Chang, Suk Kyu

    2004-01-01

    The molecular design of efficient and selective chromogenic and fluorogenic ionophore systems for the sensing of chemically and biologically important ionic guests has attracted much attention in the past decade. Many of the compounds are based on the well-known molecular framework of crown ethers, calixarenes, and other EDTA type efficient chelating compounds. Among them the calix[4]arenes are particularly attractive for their selective ionophoric properties toward many of interesting organic ammonium guests. Particularly, the calix[4]arene-crown ethers are known to have unique binding properties toward some of alkali, alkaline earth metal ions, and biogenic amines. Many of the chromogenic sensing materials are developed by conjugating molecular framework of calix[4]- arene-crown ethers with suitable signaling functions of azophenols, thiazoles, and indophenols. Quite unexpectedly, however, the ionophoric properties of simple nitro derivative of calix[4]arene-crown ethers were not reported, except for the closely related structure having ester-ether functions in crown moiety, in spite of their synthetically easy availability and expectedly efficient ionophoric properties toward organic amine guests. In this paper, we report the ionophoric properties of dinitro derivative of calix[4]arene-crown-5 ether 1 toward representative alkylammonium ions aiming for the development of efficient and selective chromogenic sensing material for the biologically important organic amine guests. The Ba 2+ -selective chromogenic behavior of 1 over the representative alkali and alkaline earth metal ions has been reported earlier.

  15. A One Line Derivation of EGARCH

    Directory of Open Access Journals (Sweden)

    Michael McAleer

    2014-06-01

    Full Text Available One of the most popular univariate asymmetric conditional volatility models is the exponential GARCH (or EGARCH specification. In addition to asymmetry, which captures the different effects on conditional volatility of positive and negative effects of equal magnitude, EGARCH can also accommodate leverage, which is the negative correlation between returns shocks and subsequent shocks to volatility. However, the statistical properties of the (quasi- maximum likelihood estimator of the EGARCH parameters are not available under general conditions, but rather only for special cases under highly restrictive and unverifiable conditions. It is often argued heuristically that the reason for the lack of general statistical properties arises from the presence in the model of an absolute value of a function of the parameters, which does not permit analytical derivatives, and hence does not permit (quasi- maximum likelihood estimation. It is shown in this paper for the non-leverage case that: (1 the EGARCH model can be derived from a random coefficient complex nonlinear moving average (RCCNMA process; and (2 the reason for the lack of statistical properties of the estimators of EGARCH under general conditions is that the stationarity and invertibility conditions for the RCCNMA process are not known.

  16. Automatic approach to deriving fuzzy slope positions

    Science.gov (United States)

    Zhu, Liang-Jun; Zhu, A.-Xing; Qin, Cheng-Zhi; Liu, Jun-Zhi

    2018-03-01

    Fuzzy characterization of slope positions is important for geographic modeling. Most of the existing fuzzy classification-based methods for fuzzy characterization require extensive user intervention in data preparation and parameter setting, which is tedious and time-consuming. This paper presents an automatic approach to overcoming these limitations in the prototype-based inference method for deriving fuzzy membership value (or similarity) to slope positions. The key contribution is a procedure for finding the typical locations and setting the fuzzy inference parameters for each slope position type. Instead of being determined totally by users in the prototype-based inference method, in the proposed approach the typical locations and fuzzy inference parameters for each slope position type are automatically determined by a rule set based on prior domain knowledge and the frequency distributions of topographic attributes. Furthermore, the preparation of topographic attributes (e.g., slope gradient, curvature, and relative position index) is automated, so the proposed automatic approach has only one necessary input, i.e., the gridded digital elevation model of the study area. All compute-intensive algorithms in the proposed approach were speeded up by parallel computing. Two study cases were provided to demonstrate that this approach can properly, conveniently and quickly derive the fuzzy slope positions.

  17. New arylsparteine derivatives as positive inotropic drugs.

    Science.gov (United States)

    Boido, Vito; Ercoli, Marcella; Tonelli, Michele; Novelli, Federica; Tasso, Bruno; Sparatore, Fabio; Cichero, Elena; Fossa, Paola; Dorigo, Paola; Froldi, Guglielmina

    2017-12-01

    Positive inotropic agents are fundamental in the treatment of heart failure; however, their arrhythmogenic liability and the increased myocardial oxygen demand strongly limit their therapeutic utility. Pursuing our study on cardiovascular activities of lupin alkaloid derivatives, several 2-(4-substituted-phenyl)-2-dehydrosparteines and 2-(4-substituted-phenyl)sparteines were prepared and tested for inotropic and chronotropic activities on isolated guinea pig atria. Four compounds (6b, 6e, 7b, and 7f) exhibited significant inotropism that, at the higher concentrations, was followed by negative inotropism or toxicity. Compound 7e (2-(4-tolyl)sparteine) exhibited a steep dose-depending inotropic activity up to the highest concentration tested (300 µM) with an E max of 116.5 ± 3.4% of basal force, proving less potent but much more active in comparison to the highest concentrations tested of digoxin and milrinone having E max of 87.5 ± 3.1% and 52.2 ± 1.1%, respectively. Finally, docking studies suggested that the relevant sparteine derivatives could target the sigma-1 receptor, whose involvement in cardiac activity is well documented.

  18. Derivative-free and blackbox optimization

    CERN Document Server

    Audet, Charles

    2017-01-01

    This book is designed as a textbook, suitable for self-learning or for teaching an upper-year university course on derivative-free and blackbox optimization.  The book is split into 5 parts and is designed to be modular; any individual part depends only on the material in Part I.  Part I of the book discusses what is meant by Derivative-Free and Blackbox Optimization, provides background material, and early basics while Part II focuses on heuristic methods (Genetic Algorithms and Nelder-Mead).  Part III presents direct search methods (Generalized Pattern Search and Mesh Adaptive Direct Search) and Part IV focuses on model-based methods (Simplex Gradient and Trust Region).  Part V discusses dealing with constraints, using surrogates, and bi-objective optimization. End of chapter exercises are included throughout as well as 15 end of chapter projects and over 40 figures.  Benchmarking techniques are also presented in the appendix.

  19. Antitumor Effect of Burchellin Derivatives Against Neuroblastoma.

    Science.gov (United States)

    Kurita, Masahiro; Takada, Tomomi; Wakabayashi, Noriko; Asami, Satoru; Ono, Shinichi; Uchiyama, Taketo; Suzuki, Takashi

    2018-02-01

    Neuroblastoma is one of the most commonly encountered malignant solid tumors in the pediatric age group. We examined the antitumor effects of five burchellin derivatives against human neuroblastoma cell lines. We evaluated cytotoxicity by the MTT assay for four human neuroblastoma and two normal cell lines. We also performed analysis of the apoptotic induction effect by flow cytometry, and examined the expression levels of apoptosis- and cell growth-related proteins by western blot analysis. We found that one of the burchellin derivatives (compound 4 ) exerted cytotoxicity against the neuroblastoma cell lines. Compound 4 induced caspase-dependent apoptosis via a mitochondrial pathway. The apoptosis mechanisms induced by compound 4 involved caspase-3, -7 and -9 activation and poly (ADP-ribose) polymerase cleavage. In addition, compound 4 induced cell death through inhibition of the cell growth pathway (via extracellular signal-regulated kinase 1 and 2, AKT8 virus oncogene cellular homolog, and signal transducer and activator of transcription 3). Compound 4 exerted cellular cytotoxicity against neuroblastoma cells via induction of caspase-dependent apoptosis, and may offer promise for further development as a useful drug for the treatment of advanced neuroblastoma. Copyright© 2018, International Institute of Anticancer Research (Dr. George J. Delinasios), All rights reserved.

  20. Simple derivation of magnetic space groups

    International Nuclear Information System (INIS)

    Bertaut, E.F.; CEA Centre d'Etudes Nucleaires de Grenoble, 38

    1975-01-01

    The magnetic translation lattices can be described by invariant wave vectors k. Advantages of the wave vector notation over the notations used by Belov et al. and Opechowski et al. are pointed out. In a one-dimensional real representation a space group element (α/tau(1)) has either the character +1 (symmetry element) or -1 (antisymmetry element). Thus the square of any space group operation must have the character +1 in a one-dimensional real representation. This simple ''square criterion'' is used to limit the admissible k-vectors and to derive the family of magnetic space groups, i.e. the set of all possible magnetic space groups, belonging to the same crystallographic space group. In the discussion some useful side results are obtained. Not only the real one-dimensional representations of point groups are connected to real one-dimensional representations of space groups, but a direct connection is shown to exist between one-dimensional complex representations of the point groups 3, 4 and 6 and one-dimensional real representations, belonging to P[001/2]=Psub(2c)(Psub(c))-lattices with screw axes 3 1 , 3 2 , 4 2 , 6 2 and 6 4 . Rules are derived for finding the Belov symbol when the Opechowski-Guccione symbol of the magnetic space group is known and this opportunity is used for correcting errors in the Opechowski-Guccione tables [fr

  1. Effects of titanium dioxide nanoparticles derived from ...

    Science.gov (United States)

    Increased manufacture of TiO2 nano-products has caused concern about the potential toxicity of these products to the environment and in public health. Identification and confirmation of the presence of TiO2 nanoparticles derived from consumer products as opposed to industrial TiO2 NPs warrants examination in exploring the significance of their release and resultant impacts on the environment. To this end we examined the significance of the release of these particles and their toxic effect on the marine diatom algae Thalassiosira pseudonana. Our results indicate that nano-TiO2 sunscreen and toothpaste exhibit more toxicity in comparison to industrial TiO2, and inhibited the growth of the marine diatom Thalassiosira pseudonana. This inhibition was proportional to the exposure time and concentrations of nano-TiO2. Our findings indicate a significant effect, and therefore further research is warranted in evaluation and assessment of the toxicity of modified nano-TiO2 derived from consumer products and their physicochemical properties. Submit to journal Environmental Science and Pollution Research.

  2. Kalman-predictive-proportional-integral-derivative (KPPID)

    International Nuclear Information System (INIS)

    Fluerasu, A.; Sutton, M.

    2004-01-01

    With third generation synchrotron X-ray sources, it is possible to acquire detailed structural information about the system under study with time resolution orders of magnitude faster than was possible a few years ago. These advances have generated many new challenges for changing and controlling the state of the system on very short time scales, in a uniform and controlled manner. For our particular X-ray experiments on crystallization or order-disorder phase transitions in metallic alloys, we need to change the sample temperature by hundreds of degrees as fast as possible while avoiding over or under shooting. To achieve this, we designed and implemented a computer-controlled temperature tracking system which combines standard Proportional-Integral-Derivative (PID) feedback, thermal modeling and finite difference thermal calculations (feedforward), and Kalman filtering of the temperature readings in order to reduce the noise. The resulting Kalman-Predictive-Proportional-Integral-Derivative (KPPID) algorithm allows us to obtain accurate control, to minimize the response time and to avoid over/under shooting, even in systems with inherently noisy temperature readings and time delays. The KPPID temperature controller was successfully implemented at the Advanced Photon Source at Argonne National Laboratories and was used to perform coherent and time-resolved X-ray diffraction experiments.

  3. Synthesis and anticancer evaluation of imidazolinone and benzoxazole derivatives

    Directory of Open Access Journals (Sweden)

    Heba A. El-Hady

    2017-05-01

    Full Text Available A series of imidazolinone and benzoxazole derivatives (3 and 5 have been synthesized by the condensation of oxazolinone derivatives (2a–c with aniline and 2-hydroxyaniline. Acetyl derivatives (4, 6 and 7 were prepared via acetylation of compounds 3 and 5 with acetic anhydride and chloroacetyl chloride. The results revealed that imidazolinone and benzoxazole derivatives are potent against the cancer cell lines MCF-7 and HePG2. In particular, benzoxazole derivatives are more potent than imidazolinone derivatives.

  4. Fractional derivatives. An introduction; Derivate frazionarie. Che cosa sono, a cosa servono

    Energy Technology Data Exchange (ETDEWEB)

    Dattoli, G. [ENEA, Div. Fisica Applicata, Centro Ricerche Frascati, Rome (Italy)

    2001-07-01

    In this item is presented a brief survey of fractional calculus and of the relevant applications. In the work are discussed different points of view of the operation of fractional derivative and present a unifying definition. The role played by fractional derivatives and integrals within the framework of integral transform is analyzed. [Italian] In questo articolo si traccia un profilo del cosidetto calcolo frazionario e delle relative applicazioni a problemi di matematica pura ed applicata. Si discutono varie definizioni dell'operazione di derivata frazionaria, non tutte coincidenti fra loro, e si mostra come sia possibile proporre una definizione univoca che inglobi tutte le altre. Si analizza infine il ruolo giocato dalle derivate e dagli integrali frazionari e, piu' in generale, quello degli operatori differenziali ad esponente frazionario, nell'ambito della teoria delle rappresentazioni integrali.

  5. Mass Spectrometric Characteristics of Prenylated Indole Derivatives from Marine-Derived Penicillium sp. NH-SL.

    Science.gov (United States)

    Ding, Hui; Ding, Wanjing; Ma, Zhongjun

    2017-03-22

    Two prenylated indole alkaloids were isolated from the ethyl acetate extracts of a marine-derived fungus Penicillium sp. NH-SL and one of them exhibited potent cytotoxic activity against mouse hepa 1c1c7 cells. In order to detect other bioactive analogs, we used liquid chromatogram tandem mass spectrometry (LC-MS/MS) to analyze the mass spectrometric characteristics of the isolated compounds as well as the crude extracts. As a result, three other analogs were detected, and their structures were deduced according to the similar fragmentation patterns. This is the first systematic report on the mass spectrometric characteristics of prenylated indole derivatives.

  6. Biologic Rhythms Derived from Siberian Mammoths Hairs

    Energy Technology Data Exchange (ETDEWEB)

    M Spilde; A Lanzirotti; C Qualls; G Phillips; A Ali; L Agenbroad; O Appenzeller

    2011-12-31

    Hair is preserved for millennia in permafrost; it enshrines a record of biologic rhythms and offers a glimpse at chronobiology as it was in extinct animals. Here we compare biologic rhythms gleaned from mammoth's hairs with those of modern human hair. Four mammoths' hairs came from varying locations in Siberia 4600 km, four time zones, apart ranging in age between 18,000 and 20,000 years before present. We used two contemporaneous human hairs for comparison. Power spectra derived from hydrogen isotope ratios along the length of the hairs gave insight into biologic rhythms, which were different in the mammoths depending on location and differed from humans. Hair growth for mammoths was {approx}31 cms/year and {approx}16 cms/year for humans. Recurrent annual rhythms of slow and fast growth varying from 3.4 weeks/cycles to 8.7 weeks/cycles for slow periods and 1.2 weeks/cycles to 2.2 weeks/cycles for fast periods were identified in mammoth's hairs. The mineral content of mammoth's hairs was measured by electron microprobe analysis (k-ratios), which showed no differences in sulfur amongst the mammoth hairs but significantly more iron then in human hair. The fractal nature of the data derived from the hairs became evident in Mandelbrot sets derived from hydrogen isotope ratios, mineral content and geographic location. Confocal microscopy and scanning electron microscopy showed varied degrees of preservation of the cuticle largely independent of age but not location of the specimens. X-ray fluorescence microprobe and fluorescence computed micro-tomography analyses allowed evaluation of metal distribution and visualization of hollow tubes in the mammoth's hairs. Seasonal variations in iron and copper content combined with spectral analyses gave insights into variation in food intake of the animals. Biologic rhythms gleaned from power spectral plots obtained by modern methods revealed life style and behavior of extinct mega-fauna.

  7. A conformational study of proline derivatives

    Directory of Open Access Journals (Sweden)

    M.E. Kamwaya

    2002-12-01

    Full Text Available From the study of the structures and molecular conformations of a number of proline derivatives, some conclusions were drawn. The widening effect of angle Cα-C'-N' is caused by steric repulsion between a hydrogen atom at Cα of the preceding prolyl residue with any other at either Cα or Cδ of the pyrrolidine ring cis to it. This effect is influenced by the distance between the said hydrogen atoms: the nearer this distance is, the greater is the steric repulsion and the wider is the angle of steric repulsion. The ratio of the angle of steric repulsion to the distance between Cα and the following Cα (or Cδ cis to it is approximately 40 and 41 for peptides with trans and cis configurations, respectively. The torsion angle ranges for χ1, χ3, χ 4, θ and φ in these derivatives are widened more than usual. The highest vibration, which more often takes place at either the Cβ or Cγ of the pyrrolidine ring, does so not necessarily at the one that is puckered. A Δ&psi -relationship is established, for the determination of α-helixity or collageneity, also in small peptides and amino acids that contain proline. The Δ&psi-relationship is versatile and gives about +180o and –180o for the two categories, respectively. The distance between the carbonyl and hydroxyl (or otherwise terminal end atoms is minimal (2.2 Å and constant, for all peptides. The ratios of the angles at the carbonyl carbons (O'-C'-N' or (O'-C'-O' to this distance is also constant: 56 and 57 for the cis and trans confirgurations, respectively; i.e. a proline O'-C'-N'- (or O'-C'-O'-test, hereinafter called the CT-test, has been established for the determination of cis and trans configurations. It is also established in these proline derivatives, that whereas puckering takes place at Cβ for the CS form, it does so at Cγ for the C2 form.

  8. Artemisinin derivatives for treating severe malaria.

    Science.gov (United States)

    McIntosh, H M; Olliaro, P

    2000-01-01

    Artemisinin derivatives may have advantages over quinoline drugs for treating severe malaria since they are fast acting and effective against quinine resistant malaria parasites. The objective of this review was to assess the effects of artemisinin drugs for severe and complicated falciparum malaria in adults and children. We searched the Cochrane Infectious Diseases Group trials register, Cochrane Controlled Trials Register, Medline, Embase, Science Citation Index, Lilacs, African Index Medicus, conference abstracts and reference lists of articles. We contacted organisations, researchers in the field and drug companies. Randomised and pseudo-randomised trials comparing artemisinin drugs (rectal, intramuscular or intravenous) with standard treatment, or comparisons between artemisinin derivatives in adults or children with severe or complicated falciparum malaria. Eligibility, trial quality assessment and data extraction were done independently by two reviewers. Study authors were contacted for additional information. Twenty three trials are included, allocation concealment was adequate in nine. Sixteen trials compared artemisinin drugs with quinine in 2653 patients. Artemisinin drugs were associated with better survival (mortality odds ratio 0.61, 95% confidence interval 0.46 to 0.82, random effects model). In trials where concealment of allocation was adequate (2261 patients), this was barely statistically significant (odds ratio 0.72, 95% CI 0.54 to 0.96, random effects model). In 1939 patients with cerebral malaria, mortality was also lower with artemisinin drugs overall (odds ratio 0.63, 95% CI 0.44 to 0.88, random effects model). The difference was not significant however when only trials reporting adequate concealment of allocation were analysed (odds ratio 0.78, 95% CI 0.55 to 1.10, random effects model) based on 1607 patients. No difference in neurological sequelae was shown. Compared with quinine, artemisinin drugs showed faster parasite clearance from

  9. Radon-Nikodym derivatives of quantum operations

    International Nuclear Information System (INIS)

    Raginsky, Maxim

    2003-01-01

    Given a completely positive (CP) map T, there is a theorem of the Radon-Nikodym type [W. B. Arveson, Acta Math. 123, 141 (1969); V. P. Belavkin and P. Staszewski, Rep. Math. Phys. 24, 49 (1986)] that completely characterizes all CP maps S such that T-S is also a CP map. This theorem is reviewed, and several alternative formulations are given along the way. We then use the Radon-Nikodym formalism to study the structure of order intervals of quantum operations, as well as a certain one-to-one correspondence between CP maps and positive operators, already fruitfully exploited in many quantum information-theoretic treatments. We also comment on how the Radon-Nikodym theorem can be used to derive norm estimates for differences of CP maps in general, and of quantum operations in particular

  10. Derivatives Trading, Climate Science and Human Rights

    DEFF Research Database (Denmark)

    Haigh, Matthew

    for capital flows associated with climate management. Media communications and decision making theories are used to interpret data drawn from participant observation and interviews with climate scientists, policy makers and institutional investors. Findings - The framework suggests a digital divide between...... the heaviest polluters as contributing to carbon-minimised investment portfolios. Assets owned by privately managed pension funds have remained materially exposed to risks posed by climate change. In public finance, a narrow range of financial instruments centred on derivatives trading has entrenched global...... between human rights, climate change, and the stability of private pensions provision. Originality/value - Provides policy sciences useful assessments of communication media and financial instruments used in climate management. Establishes bases for theoretical and applied communications research...

  11. A Shuttle Derived Vehicle launch system

    Science.gov (United States)

    Tewell, J. R.; Buell, D. N.; Ewing, E. S.

    1982-01-01

    This paper describes a Shuttle Derived Vehicle (SDV) launch system presently being studied for the NASA by Martin Marietta Aerospace which capitalizes on existing Shuttle hardware elements to provide increased accommodations for payload weight, payload volume, or both. The SDV configuration utilizes the existing solid rocket boosters, external tank and the Space Shuttle main engines but replaces the manned orbiter with an unmanned, remotely controlled cargo carrier. This cargo carrier substitution more than doubles the performance capability of the orbiter system and is realistically achievable for minimal cost. The advantages of the SDV are presented in terms of performance and economics. Based on these considerations, it is concluded that an unmanned SDV offers a most attractive complement to the present Space Transportation System.

  12. Chemical Sensors Based on Cyclodextrin Derivatives.

    Science.gov (United States)

    Ogoshi, Tomoki; Harada, Akira

    2008-08-25

    This review focuses on chemical sensors based on cyclodextrin (CD) derivatives. This has been a field of classical interest, and is now of current interest for numerous scientists. First, typical chemical sensors using chromophore appended CDs are mentioned. Various "turn-off" and "turn-on" fluorescent chemical sensors, in which fluorescence intensity was decreased or increased by complexation with guest molecules, respectively, were synthesized. Dye modified CDs and photoactive metal ion-ligand complex appended CDs, metallocyclodextrins, were also applied for chemical sensors. Furthermore, recent novel approaches to chemical sensing systems using supramolecular structures such as CD dimers, trimers and cooperative binding systems of CDs with the other macrocycle [2]rotaxane and supramolecular polymers consisting of CD units are mentioned. New chemical sensors using hybrids of CDs with p-conjugated polymers, peptides, DNA, nanocarbons and nanoparticles are also described in this review.

  13. Crown ether derivatives of EDTA: Pt. 6

    International Nuclear Information System (INIS)

    Liu Zhongqun; Qin Shengying; Chen Shaojin; Tan Lin

    1988-01-01

    EDTA-diaminodibenzo-18-crown-6 (cis- and trans-) condensation polymer is a new compound of crown ether derivatives of EDTA. In this paper the adsorption behaviors of U(IV) and U(VI) on this polymer from chloride solutions and effects of hydrochloric acid concentrations, salting-out agents and organic solvents on distribution coefficient (K d ) of uranium are investigated. Adsorption mechanism of uranyl ion (UO 2 2+ ) on this polymer was studied with IR spectra and by means of the adsorption behaviors of compounds of similar structure. Experimental results show that both polyether section and carboxyl groups in EDTA-diaminodibenzo-18-crown-6 take part in complexation with uranyl ion and synergistic effect appeared

  14. Autocrine Effects of Tumor-Derived Complement

    Directory of Open Access Journals (Sweden)

    Min Soon Cho

    2014-03-01

    Full Text Available We describe a role for the complement system in enhancing cancer growth. Cancer cells secrete complement proteins that stimulate tumor growth upon activation. Complement promotes tumor growth via a direct autocrine effect that is partially independent of tumor-infiltrating cytotoxic T cells. Activated C5aR and C3aR signal through the PI3K/AKT pathway in cancer cells, and silencing the PI3K or AKT gene in cancer cells eliminates the progrowth effects of C5aR and C3aR stimulation. In patients with ovarian or lung cancer, higher tumoral C3 or C5aR mRNA levels were associated with decreased overall survival. These data identify a role for tumor-derived complement proteins in promoting tumor growth, and they therefore have substantial clinical and therapeutic implications.

  15. Vowel quality alternation in Dinka verb derivation

    DEFF Research Database (Denmark)

    Andersen, Torben

    2017-01-01

    In Dinka, a predominantly monosyllabic and highly fusional Western Nilotic language, vowel quality alternation in the root plays a major and systematic role in the morphology of verbs, together with alternations in vowel length, voice quality, and tone. Earlier work has shown that in the inflecti...... modifications. These include a different distribution of the vowel grades and interaction with a shift in voice quality, to breathy voice.......In Dinka, a predominantly monosyllabic and highly fusional Western Nilotic language, vowel quality alternation in the root plays a major and systematic role in the morphology of verbs, together with alternations in vowel length, voice quality, and tone. Earlier work has shown that in the inflection...... of simple, i. e., underived, transitive verbs, the vowel quality alternation conforms to a vowel height gradation system with three vowel grades. The present article shows that this vowel gradation system is also operative in the morphology of derived verbs with a transitive root, but with certain...

  16. Reaction between chloromercurocobaltcarborane and undecaborate anion derivatives

    International Nuclear Information System (INIS)

    Lobanova, I.A.; Khitrova, O.M.; Petrovskij, P.V.; Bregadze, V.I.

    2004-01-01

    Interaction of Cs + C 2 B 9 H 12 - and exo-nido-5,6,10-[Cl(Ph 3 P) 2 RU]-5,6,10-(μ-H) 3 -10-H-7,8-C 2 B 9 H 8 with 9-chloromercurocobaltcarborane derivative - 3-(η 5 -Cp)-9-ClHg-3,1,2-CoC 2 B 9 H 10 (η 5 -Cp = cyclopentadiene) in mixed solvent tetrahydrofuran-water-ethanol at room temperature was studied using the methods of elementary analysis and 1 H, 31 P, 11 B NMR. Asymmetric metallocarborane cluster, in which exo-nido-ruthenacarborane and closo-cobalt- or dicarbo-nido-undecaborate fragments are bound via mercury atom, were prepared [ru

  17. A derivation of the beam equation

    International Nuclear Information System (INIS)

    Duque, Daniel

    2016-01-01

    The Euler–Bernoulli equation describing the deflection of a beam is a vital tool in structural and mechanical engineering. However, its derivation usually entails a number of intermediate steps that may confuse engineering or science students at the beginnig of their undergraduate studies. We explain how this equation may be deduced, beginning with an approximate expression for the energy, from which the forces and finally the equation itself may be obtained. The description is begun at the level of small ‘particles’, and the continuum level is taken later on. However, when a computational solution is sought, the description turns back to the discrete level again. We first consider the easier case of a string under tension, and then focus on the beam. Numerical solutions for several loads are obtained. (paper)

  18. A derivation of the beam equation

    Science.gov (United States)

    Duque, Daniel

    2016-01-01

    The Euler-Bernoulli equation describing the deflection of a beam is a vital tool in structural and mechanical engineering. However, its derivation usually entails a number of intermediate steps that may confuse engineering or science students at the beginnig of their undergraduate studies. We explain how this equation may be deduced, beginning with an approximate expression for the energy, from which the forces and finally the equation itself may be obtained. The description is begun at the level of small ‘particles’, and the continuum level is taken later on. However, when a computational solution is sought, the description turns back to the discrete level again. We first consider the easier case of a string under tension, and then focus on the beam. Numerical solutions for several loads are obtained.

  19. Isocorydine Derivatives and Their Anticancer Activities

    Directory of Open Access Journals (Sweden)

    Mei Zhong

    2014-08-01

    Full Text Available In order to improve the anticancer activity of isocorydine (ICD, ten isocorydine derivatives were prepared through chemical structure modifications, and their in vitro and in vivo activities were experimentally investigated. 8-Amino-isocorydine (8 and 6a,7-dihydrogen-isocorydione (10 could inhibit the growth of human lung (A549, gastric (SGC7901 and liver (HepG2 cancer cell lines in vitro. Isocorydione (2 could inhibit the tumor growth of murine sarcoma S180-bearing mice, and 8-acetamino-isocorydine (11, a pro-drug of 8-amino-isocorydine (8, which is instable in water solution at room temperature, had a good inhibitory effect on murine hepatoma H22-induced tumors. The results suggested that the isocorydine structural modifications at C-8 could significantly improve the biological activity of this alkaloid, indicating its suitability as a lead compound in the development of an effective anticancer agent.

  20. Proteoliposome derived cochleate as novel adjuvant.

    Science.gov (United States)

    Bracho, Gustavo; Lastre, Miriam; del Campo, Judith; Zayas, Caridad; González, Domingo; Gil, Danay; Acevedo, Reinaldo; Taboada, Carlos; Solís, Rosa L; Pérez, Oliver

    2006-04-12

    Cochleate structures (CS) consist in a highly stable lipid structures that have been reported to be a good antigen delivery system. The incorporation of pathogen associated molecular pattern (PAMP) from bacterial membranes into CS became in a promising approach to develop adjuvants, particularly mucosal adjuvants. Therefore, we prepare CS from proteoliposome (PL) obtained from Neisseria meningitidis B (PLCS) and evaluated it for its capability to stimulate the immune system as well as the adjuvant activity. The ability of PLCS to induce Thl polarization was also explored. The results and the easy capability for new antigen incorporation on CS support its use as adjuvant for immunization with a large variety of pathogen derived antigens and different routes of immunization.

  1. Current-induced forces: a simple derivation

    International Nuclear Information System (INIS)

    Todorov, Tchavdar N; Dundas, Daniel; Lü, Jing-Tao; Brandbyge, Mads; Hedegård, Per

    2014-01-01

    We revisit the problem of forces on atoms under current in nanoscale conductors. We derive and discuss the five principal kinds of force under steady-state conditions from a simple standpoint that—with the help of background literature—should be accessible to physics undergraduates. The discussion aims at combining methodology with an emphasis on the underlying physics through examples. We discuss and compare two forces present only under current—the non-conservative electron wind force and a Lorentz-like velocity-dependent force. It is shown that in metallic nanowires both display significant features at the wire surface, making it a candidate for the nucleation of current-driven structural transformations and failure. Finally we discuss the problem of force noise and the limitations of Ehrenfest dynamics. (paper)

  2. Higher derivative super Yang-Mills theories

    International Nuclear Information System (INIS)

    Bergshoeff, E.; Rakowski, M.; Sezgin, E.

    1986-11-01

    The most general higher derivative Yang-Mills actions of the type (F 2 +α2F 4 ) which are globally supersymmetric up to order α 2 in six and ten dimensional spacetimes are given. The F 4 -terms turn out to occur in the combination α 2 (tr F 4 - 1/4(tr F 2 ) 2 ), where the trace is over the Lorentz indices. This result agrees with the low energy limit of the open superstring in ten dimensions, where α is the string tension. Surprisingly, the transformation rules of the Yang-Mills multiplet receive order α 2 corrections even in the off-shell formulation. For the case of Abelian Yang-Mills group, the action is expressed in Born-Infeld form with a metric generically given by (1+α 2 F 2 +...). (author)

  3. Fluorescein Derivatives in Intravital Fluorescence Imaging

    Directory of Open Access Journals (Sweden)

    Michael S. Roberts

    2013-08-01

    Full Text Available Intravital fluorescence microscopy enables the direct imaging of fluorophores in vivo and advanced techniques such as fluorescence lifetime imaging (FLIM enable the simultaneous detection of multiple fluorophores. Consequently, it is now possible to record distribution and metabolism of a chemical in vivo and to optimise the delivery of fluorophores in vivo. Recent clinical applications with fluorescein and other intravital fluorescent stains have occurred in neurosurgery, dermatology [including photodynamic therapy (PDT] and endomicroscopy. Potential uses have been identified in periodontal disease, skin graft and cancer surgery. Animal studies have demonstrated that diseased tissue can be specifically stained with fluorophore conjugates. This review focuses on the fluorescein derived fluorophores in common clinical use and provides examples of novel applications from studies in tissue samples.

  4. Antimicrobial activity of chemically modified dextran derivatives.

    Science.gov (United States)

    Tuchilus, Cristina G; Nichifor, Marieta; Mocanu, Georgeta; Stanciu, Magdalena C

    2017-04-01

    Cationic amphiphilic dextran derivatives with a long alkyl group attached to the reductive end of the polysaccharide chain and quaternary ammonium groups attached as pendent groups to the main dextran backbone were synthesized and tested for their antimicrobial properties against several bacteria and fungi strains. Dependence of antimicrobial activity on both polymer chemical composition (dextran molar mass, length of end alkyl group and chemical structure of ammonium groups) and type of microbes was highlighted by disc-diffusion method (diameter of inhibition zone) and broth microdilution method (minimum inhibitory concentrations). Polymers had antimicrobial activity for all strains studied, except for Pseudomonas aeruginosa ATCC 27853. The best activity against Staphylococcus aureus (Minimun Inhibitory Concentration 60μg/mL) was provided by polymers obtained from dextran with lower molecular mass (Mn=4500), C 12 H 25 or C 18 H 37 end groups, and N,N-dimethyl-N-benzylammonium pendent groups. Copyright © 2017 Elsevier Ltd. All rights reserved.

  5. Determination of phosphorus using derivative neutron activation

    International Nuclear Information System (INIS)

    Scindia, Y.M.; Nair, A.G.C.; Reddy, A.V.R.; Manohar, S.B.

    2002-01-01

    For the determination of phosphorus in different matrices, the derivative neutron activation analysis is especially applicable to aqueous samples, since the conventional neutron activation analysis is not useful for the determination of phosphorus. Phosphorus when reacted with ammonium molybdate 4 hydrate and ammonium metavanadate forms molybdo vanado phosphoric acid. This complex is preconcentrated by extracting into methyl isobutyl ketone. The organic phase containing the molybdo vanado phosphoric acid is neutron activated and the phosphorus is determined through the activation product of 52 V. Preparation of this complex, its stoichiometry, application to trace level determination of phosphorus and improved detection limit are discussed. This method was applied for the analysis of industrial effluent samples. (author)

  6. On Derivations of Operator Algebras with Involution

    Directory of Open Access Journals (Sweden)

    Širovnik Nejc

    2014-12-01

    Full Text Available The purpose of this paper is to prove the following result. Let X be a complex Hilbert space, let L(X be an algebra of all bounded linear operators on X and let A(X ⊂ L(X be a standard operator algebra, which is closed under the adjoint operation. Suppose there exists a linear mapping D : A(X → L(X satisfying the relation 2D(AA*A = D(AA*A + AA*D(A + D(AA*A + AD(A*A for all A ∈ A(X. In this case, D is of the form D(A = [A,B] for all A ∈ A(X and some fixed B ∈ L(X, which means that D is a derivation.

  7. Derivation of the optical constants of anisotropic

    Science.gov (United States)

    Aronson, J. R.; Emslie, A. G.; Smith, E. M.; Strong, P. F.

    1985-07-01

    This report concerns the development of methods for obtaining the optical constants of anisotropic crystals of the triclinic and monoclinic systems. The principal method used, classical dispersion theory, is adapted to these crystal systems by extending the Lorentz line parameters to include the angles characterizing the individual resonances, and by replacing the dielectric constant by a dielectric tensor. The sample crystals are gypsium, orthoclase and chalcanthite. The derived optical constants are shown to be suitable for modeling the optical properties of particulate media in the infrared spectral region. For those materials where suitable size single crystals are not available, an extension of a previously used method is applied to alabaster, a polycrystalline material of the monoclinic crystal system.

  8. A topological derivative method for topology optimization

    DEFF Research Database (Denmark)

    Norato, J.; Bendsøe, Martin P.; Haber, RB

    2007-01-01

    resource constraint. A smooth and consistent projection of the region bounded by the level set onto the fictitious analysis domain simplifies the response analysis and enhances the convergence of the optimization algorithm. Moreover, the projection supports the reintroduction of solid material in void......We propose a fictitious domain method for topology optimization in which a level set of the topological derivative field for the cost function identifies the boundary of the optimal design. We describe a fixed-point iteration scheme that implements this optimality criterion subject to a volumetric...... regions, a critical requirement for robust topology optimization. We present several numerical examples that demonstrate compliance minimization of fixed-volume, linearly elastic structures....

  9. Cysteine sulfoxide derivatives in Petiveria alliacea.

    Science.gov (United States)

    Kubec, R; Musah, R A

    2001-11-01

    Two diastereomers of S-benzyl-L-cysteine sulfoxide have been isolated from fresh roots of Petiveria alliacea. Their structures and absolute configurations have been determined by NMR, MALDI-HRMS, IR and CD spectroscopy and confirmed by comparison with authentic compounds. Both the R(S) and S(S) diastereomers of the sulfoxide are present in all parts of the plant (root, stem, and leaves) with the latter diastereomer being predominant. Their total content greatly varied in different parts of the plant between 0.07 and 2.97 mg g(-1) fr. wt, being by far the highest in the root. S-Benzylcysteine has also been detected in trace amounts (<10 microg g(-1) fr. wt) in all parts of the plant. This represents the first report of the presence of S-benzylcysteine derivatives in nature.

  10. Covariant Derivatives and the Renormalization Group Equation

    Science.gov (United States)

    Dolan, Brian P.

    The renormalization group equation for N-point correlation functions can be interpreted in a geometrical manner as an equation for Lie transport of amplitudes in the space of couplings. The vector field generating the diffeomorphism has components given by the β functions of the theory. It is argued that this simple picture requires modification whenever any one of the points at which the amplitude is evaluated becomes close to any other. This modification necessitates the introduction of a connection on the space of couplings and new terms appear in the renormalization group equation involving covariant derivatives of the β function and the curvature associated with the connection. It is shown how the connection is related to the operator product expansion coefficients, but there remains an arbitrariness in its definition.

  11. Derivative markets, speculation and oil prices

    International Nuclear Information System (INIS)

    Babusiaux, D.; Lasserre, F.; Pierru, A.

    2010-01-01

    Recent movements in oil prices have been ascribed by a number of analysts and political leaders not to market fundamentals but to the speculative positions taken by financial investors in derivatives markets. Various economists including Nobel Prize Paul Krugman believe however that the constitution of stocks is a necessary element for speculation, a feature that was not very evident during the sudden price increase in 2008; but these points of view are not entirely incompatible. Various explanations can be put forward, among which the most important is demand inertia. On the very short run, demand price elasticity is significantly lower than that usually calculated for the short term, which can significantly reduce the impact - on stocks - of a temporary price increase provoked by financial investors' behavior. (authors)

  12. Beyond Lovelock gravity: Higher derivative metric theories

    Science.gov (United States)

    Crisostomi, M.; Noui, K.; Charmousis, C.; Langlois, D.

    2018-02-01

    We consider theories describing the dynamics of a four-dimensional metric, whose Lagrangian is diffeomorphism invariant and depends at most on second derivatives of the metric. Imposing degeneracy conditions we find a set of Lagrangians that, apart form the Einstein-Hilbert one, are either trivial or contain more than 2 degrees of freedom. Among the partially degenerate theories, we recover Chern-Simons gravity, endowed with constraints whose structure suggests the presence of instabilities. Then, we enlarge the class of parity violating theories of gravity by introducing new "chiral scalar-tensor theories." Although they all raise the same concern as Chern-Simons gravity, they can nevertheless make sense as low energy effective field theories or, by restricting them to the unitary gauge (where the scalar field is uniform), as Lorentz breaking theories with a parity violating sector.

  13. Commodity derivatives pricing with inventory effects

    DEFF Research Database (Denmark)

    Bach, Christian; Dziubinski, Matt P.

    We introduce tractable models for commodity derivatives pricing with inventory and volatility eects, and illustrate with applications to the oil market. We contribute to the existing literature in several respects. First, whereas the previous literature uses futures data for investigating...... the relationship between inventory and volatility, we use the information available in options traded on futures. Second, performance assessment in the previous literature has primarily evolved around explaining moments of data or forecasting prices of futures. Instead, we asses the performance of our model...... by considering both the ability of explaining prices in-sample and out-of-sample - assessing both the pricing-performance and the hedging-performance of the models. Third, we model the futures surface rather than the spot price process, and from the no-arbitrage relationship between spot and futures prices we...

  14. Selfinteraction force in a theory of gravitation with higher derivatives

    International Nuclear Information System (INIS)

    Jankiewicz, C.

    1981-01-01

    Approximate equations of motion are derived from gravitational field equations with higher derivatives. The approximation takes into account the selfinteraction force. The selfinteraction force coincides with the analogous force resulting from the Einstein field equations. (author)

  15. Deriving stellar parameters with the SME software package

    Science.gov (United States)

    Piskunov, N.

    2017-09-01

    Photometry and spectroscopy are complementary tools for deriving accurate stellar parameters. Here I present one of the popular packages for stellar spectroscopy called SME with the emphasis on the latest developments and error assessment for the derived parameters.

  16. Geochemical Constraints for Mercury's PCA-Derived Geochemical Terranes

    Science.gov (United States)

    Stockstill-Cahill, K. R.; Peplowski, P. N.

    2018-05-01

    PCA-derived geochemical terranes provide a robust, analytical means of defining these terranes using strictly geochemical inputs. Using the end members derived in this way, we are able to assess the geochemical implications for Mercury.

  17. Selenium- or tellurium- containing bile acids and derivatives thereof

    International Nuclear Information System (INIS)

    Monks, R.; Riley, A.L.M.

    1981-01-01

    This invention relates to the preparation of selenium and tellurium derivatives, particularly γ-emitting radioactive derivatives of bile acids and bile salts. Such compounds are valuable in the examination of body function, especially small bowel function. (author)

  18. Fractional derivative and its application in mathematics and physics

    International Nuclear Information System (INIS)

    Namsrai, K.

    2004-12-01

    We propose fractional derivatives and to study those mathematical and physical consequences. It is shown that fractional derivatives possess noncommutative and nonassociative properties and within which motion of a particle, differential and integral calculuses are investigated. (author)

  19. On an Inequality Concerning the Polar Derivative of a Polynomial

    Indian Academy of Sciences (India)

    Abstract. In this paper, we present a correct proof of an -inequality concerning the polar derivative of a polynomial with restricted zeros. We also extend Zygmund's inequality to the polar derivative of a polynomial.

  20. Vegetable milks and their fermented derivative products

    Directory of Open Access Journals (Sweden)

    Neus Bernat

    2014-04-01

    Full Text Available The so-called vegetable milks are in the spotlight thanks to their lactose-free, animal protein-free and cholesterol-free features which fit well with the current demand for healthy food products. Nevertheless, and with the exception of soya, little information is available about these types of milks and their derivatives. The aims of this review, therefore, are to: highlight the main nutritional benefits of the nut and cereal vegetable milks available on the market, fermented or not; describe the basic processing steps involved in their manufacturing process; and analyze the major problems affecting their overall quality, together with the current feasible solutions. On the basis of the information gathered, vegetable milks and their derivatives have excellent nutritional properties which provide them a high potential and positive market expectation. Nevertheless, optimal processing conditions for each raw material or the application of new technologies have to be researched in order to improve the quality of the products. Hence, further studies need to be developed to ensure the physical stability of the products throughout their whole shelf-life. These studies would also allow for a reduction in the amount of additives (hydrocolloids and/or emulsifiers and thus reduce the cost of the products. In the particular case of fermented products, the use of starters which are able to both improve the quality (by synthesizing enhanced flavors and providing optimal textures and exert health benefits for consumers (i.e. probiotics is the main challenge to be faced in future studies.

  1. Fluoride removal performance of glass derived hydroxyapatite

    Energy Technology Data Exchange (ETDEWEB)

    Liang, Wen, E-mail: wliang@ecust.edu.cn [Research Institute of Biomaterials, School of Materials Science and Engineering, East China University of Science and Technology (China); Zhan, Lei; Piao, Longhua [Research Institute of Biomaterials, School of Materials Science and Engineering, East China University of Science and Technology (China); Russel, Christian [Otto-Schott-Institut, Universitaet Jena, Jena (Germany)

    2011-02-15

    Research highlights: {yields} Novel sodium calcium borate glass derived hydroxyapatite (G-HAP) is prepared. {yields} Micro-G-HAP adsorbs F{sup -} ions in solutions more effectively than commercial nano-HAP. {yields} The adsorption kinetics and isotherms are well fitted by a second order kinetic model and Freundlich isotherm model. -- Abstract: A novel sodium calcium borate glass derived hydroxyapatite (G-HAP) with different ranges of particle size was prepared by immersion sodium calcium borate glass in 0.1 M K{sub 2}HPO{sub 4} solution by the ratio of 50 g L{sup -1} for 7 days. The unique advantage of G-HAP for the adsorption of fluoride ions in solutions was studied. The effects of size and quantity of particles, pH value and adsorption time on adsorption performance were investigated. The maximum adsorption capacity was 17.34 mg g{sup -1} if 5 g L{sup -1}, <100 {mu}m G-HAP was added to a solution with an initial pH value of 6.72 and the adsorption time was 12 h. The results showed that the micro-G-HAP could immobilize F{sup -} in solution more effectively than commercial nano-HAP, which makes potential application of the G-HAP in removing the fluoride ions from wastewater. The adsorption kinetics and isotherms for F{sup -} could be well fitted by a second order kinetic model and Freundlich isotherm model respectively, which could be used to describe the adsorption behavior. The mechanism of G-HAP in immobilizing F{sup -} from aqueous solutions was investigated by the X-ray diffraction (XRD), infrared spectra (IR) and scanning electron microscopy (SEM).

  2. Radiation Protection Using Carbon Nanotube Derivatives

    Science.gov (United States)

    Conyers, Jodie L., Jr.; Moore, Valerie C.; Casscells, S. Ward

    2010-01-01

    BHA and BHT are well-known food preservatives that are excellent radical scavengers. These compounds, attached to single-walled carbon nanotubes (SWNTs), could serve as excellent radical traps. The amino-BHT groups can be associated with SWNTs that have carbolyxic acid groups via acid-base association or via covalent association. The material can be used as a means of radiation protection or cellular stress mitigation via a sequence of quenching radical species using nano-engineered scaffolds of SWNTs and their derivatives. It works by reducing the number of free radicals within or nearby a cell, tissue, organ, or living organism. This reduces the risk of damage to DNA and other cellular components that can lead to chronic and/or acute pathologies, including (but not limited to) cancer, cardiovascular disease, immuno-suppression, and disorders of the central nervous system. These derivatives can show an unusually high scavenging ability, which could prove efficacious in protecting living systems from radical-induced decay. This technique could be used to protect healthy cells in a living biological system from the effects of radiation therapy. It could also be used as a prophylactic or antidote for radiation exposure due to accidental, terrorist, or wartime use of radiation- containing weapons; high-altitude or space travel (where radiation exposure is generally higher than desired); or in any scenario where exposure to radiation is expected or anticipated. This invention s ultimate use will be dependent on the utility in an overall biological system where many levels of toxicity have to be evaluated. This can only be assessed at a later stage. In vitro toxicity will first be assessed, followed by in vivo non-mammalian screening in zebra fish for toxicity and therapeutic efficacy.

  3. Jordan and left derivations on locally C*-algebras

    International Nuclear Information System (INIS)

    Shahzad, Naseer

    2002-07-01

    We show that left derivations as well as Jordan derivations on locally G*-algebras are always continuous. We also obtain some noncommutative extensions of the classical Singer-Wermer theorem for locally C*-algebras: (1) Every left derivation D on a locally (7*-algebra A is identically zero. (2) Every Jordan derivation D on a locally C*-algebra A which satisfies [D(x), x]D(x]=0 for all x in A, is identically zero. (author)

  4. Synthesis of Substituted α-Trifluoromethyl Piperidinic Derivatives

    Directory of Open Access Journals (Sweden)

    Sarah Rioton

    2017-03-01

    Full Text Available A comprehensive survey of pathways leading to the generation of α-trifluoromethyl monocyclic piperidinic derivatives is provided (65 references. These compounds have been synthesized either from 6-membered rings e.g., pipecolic acid or lactam derivatives by introduction a trifluoromethyl group, from pyridine or pyridinone derivatives by reduction, and from 5-membered rings e.g., prolinol derivatives by ring expansion, from linear amines by cyclization or from dienes/dienophiles by [4 + 2]-cycloaddition.

  5. Australian OTC Derivatives Markets: Insights from the BIS Semiannual Survey

    OpenAIRE

    Jason Ahn; Mihovil Matic; Christian Vallence

    2012-01-01

    The Reserve Bank of Australia recently commenced surveying participants in Australian over-the-counter (OTC) derivatives markets as part of the Bank for International Settlements’ (BIS) semiannual global OTC derivatives survey. Australia’s contribution to the survey complements regulatory efforts to improve the resilience and transparency of Australia’s OTC derivatives markets. It also facilitates a higher frequency comparison of the Australian and foreign OTC derivatives markets. The survey ...

  6. Options, Futures, and Other Derivatives in Russia: An Overview

    OpenAIRE

    Rotfuß, Waldemar

    2007-01-01

    This work provides a descriptive overview of Russian markets for financial derivatives. Available figures for the exchange-traded and over-the-counter-traded derivatives in Russia show that the Russian derivatives markets experienced enormous growth rates since the financial crisis in 1998. Starting from a very low level, turnover of exchange-traded derivatives in Russia rose from 2000 to 2006 on average 168 percent per year and reached a total turnover of EUR 102 billion in 2006. Among futur...

  7. INTEGRATION OF IMAGE-DERIVED AND POS-DERIVED FEATURES FOR IMAGE BLUR DETECTION

    Directory of Open Access Journals (Sweden)

    T.-A. Teo

    2016-06-01

    Full Text Available The image quality plays an important role for Unmanned Aerial Vehicle (UAV’s applications. The small fixed wings UAV is suffering from the image blur due to the crosswind and the turbulence. Position and Orientation System (POS, which provides the position and orientation information, is installed onto an UAV to enable acquisition of UAV trajectory. It can be used to calculate the positional and angular velocities when the camera shutter is open. This study proposes a POS-assisted method to detect the blur image. The major steps include feature extraction, blur image detection and verification. In feature extraction, this study extracts different features from images and POS. The image-derived features include mean and standard deviation of image gradient. For POS-derived features, we modify the traditional degree-of-linear-blur (blinear method to degree-of-motion-blur (bmotion based on the collinear condition equations and POS parameters. Besides, POS parameters such as positional and angular velocities are also adopted as POS-derived features. In blur detection, this study uses Support Vector Machines (SVM classifier and extracted features (i.e. image information, POS data, blinear and bmotion to separate blur and sharp UAV images. The experiment utilizes SenseFly eBee UAV system. The number of image is 129. In blur image detection, we use the proposed degree-of-motion-blur and other image features to classify the blur image and sharp images. The classification result shows that the overall accuracy using image features is only 56%. The integration of image-derived and POS-derived features have improved the overall accuracy from 56% to 76% in blur detection. Besides, this study indicates that the performance of the proposed degree-of-motion-blur is better than the traditional degree-of-linear-blur.

  8. 21 CFR 184.1317 - Garlic and its derivatives.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Garlic and its derivatives. 184.1317 Section 184... Listing of Specific Substances Affirmed as GRAS § 184.1317 Garlic and its derivatives. (a) Garlic is the... derivatives include essential oils, oleo-resins, and natural extractives obtained from garlic. (b) Garlic oil...

  9. Deriving a Bilingual Lexicon for Cross-Language Information Retrieval

    NARCIS (Netherlands)

    Hiemstra, Djoerd

    1997-01-01

    In this paper we describe a systematic approach to derive a bilingual lexicon automatically from parallel corpora. Following this approach, a lexicon was derived from the English and Dutch version of the Agenda 21 corpus. With the lexicon and a part of the corpus that was not used to derive the

  10. 17 CFR 240.16b-6 - Derivative securities.

    Science.gov (United States)

    2010-04-01

    ... 17 Commodity and Securities Exchanges 3 2010-04-01 2010-04-01 false Derivative securities. 240.16b... Exchange Act of 1934 Exemption of Certain Transactions from Section 16(b) § 240.16b-6 Derivative securities...). Note to paragraph (b): The exercise or conversion of a derivative security that does not satisfy the...

  11. 14 CFR 1203.500 - Use of derivative classification.

    Science.gov (United States)

    2010-01-01

    ... 14 Aeronautics and Space 5 2010-01-01 2010-01-01 false Use of derivative classification. 1203.500 Section 1203.500 Aeronautics and Space NATIONAL AERONAUTICS AND SPACE ADMINISTRATION INFORMATION SECURITY PROGRAM Derivative Classification § 1203.500 Use of derivative classification. The application of...

  12. Vulnerable Derivatives and Good Deal Bounds: A Structural Model

    DEFF Research Database (Denmark)

    Murgoci, Agatha

    2013-01-01

    We price vulnerable derivatives -- i.e. derivatives where the counterparty may default. These are basically the derivatives traded on the over-the-counter (OTC) markets. Default is modeled in a structural framework. The technique employed for pricing is good deal bounds (GDBs). The method imposes...

  13. 18 CFR 367.1750 - Account 175, Derivative instrument assets.

    Science.gov (United States)

    2010-04-01

    ... the corresponding amount of the change in the fair value of the derivative instrument. ... instrument assets. This account must include the amounts paid for derivative instruments, and the change in the fair value of all derivative instrument assets not designated as cash flow or fair value hedges...

  14. 45 CFR 1630.12 - Applicability to derivative income.

    Science.gov (United States)

    2010-10-01

    ..., regulations, guidelines, and instructions, the Accounting Guide for LSC recipients, the terms and conditions... 45 Public Welfare 4 2010-10-01 2010-10-01 false Applicability to derivative income. 1630.12... CORPORATION COST STANDARDS AND PROCEDURES § 1630.12 Applicability to derivative income. (a) Derivative income...

  15. Kinetic Theory Derivation of the Adiabatic Law for Ideal Gases.

    Science.gov (United States)

    Sobel, Michael I.

    1980-01-01

    Discusses how the adiabatic law for ideal gases can be derived from the assumption of a Maxwell-Boltzmann (or any other) distribution of velocities--in contrast to the usual derivations from thermodynamics alone, and the higher-order effect that leads to one-body viscosity. An elementary derivation of the adiabatic law is given. (Author/DS)

  16. Deriving Case, Agreement and Voice Phenomena in Syntax

    Science.gov (United States)

    Sigurdsson, Einar Freyr

    2017-01-01

    This dissertation places case, agreement and Voice phenomena in syntax. It argues that the derivation is driven by so-called derivational features, that is, structure-building features (Merge) and probe features (Agree) (Heck and Muller 2007 and Muller 2010; see also Chomsky 2000, 2001). Both types are essential in deriving case and agreement in…

  17. 21 CFR 172.275 - Synthetic paraffin and succinic derivatives.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Synthetic paraffin and succinic derivatives. 172... FOOD FOR HUMAN CONSUMPTION Coatings, Films and Related Substances § 172.275 Synthetic paraffin and succinic derivatives. Synthetic paraffin and succinic derivatives identified in this section may be safely...

  18. 76 FR 51878 - Modifications of Certain Derivative Contracts; Correction

    Science.gov (United States)

    2011-08-19

    ...) * * * (1) Both the party transferring or assigning its rights and obligations under the derivative contract... Modifications of Certain Derivative Contracts; Correction AGENCY: Internal Revenue Service (IRS), Treasury... temporary regulations (TD 9538) that address when a transfer or assignment of certain derivative contracts...

  19. Deamidation of asparagine and glutamine residues in proteins and peptides: structural determinants and analytical methodology

    NARCIS (Netherlands)

    Bischoff, Rainer; Kolbe, H.V.

    1994-01-01

    Non-enzymatic deamidation of asparagine and glutamine residues in proteins and peptides are reviewed by first outlining the well-described reaction mechanism involving cyclic imide intermediates, followed by a discussion of structural features which influence the reaction rate. The second and major

  20. Polymer compound

    NARCIS (Netherlands)

    1995-01-01

    A Polymer compound comprising a polymer (a) that contains cyclic imidesgroups and a polymer (b) that contains monomer groups with a 2,4-diamino-1,3,5-triazine side group. According to the formula (see formula) whereby themole percentage ratio of the cyclic imides groups in the polymer compoundwith