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Biological Characterization (biological + characterization)
Selected AbstractsSynthesis and Biological Characterization of [3H]BBL454, a New CCK2 Selective Radiolabeled Agonist Displaying Original Pharmacological Properties.CHEMINFORM, Issue 16 2004Bruno Bellier No abstract is available for this article. [source] Synthesis and Biological Characterization of Argyrin,FCHEMMEDCHEM, Issue 6 2010Leila Bülow No abstract is available for this article. [source] Synthesis and Biological Characterization of Argyrin,FCHEMMEDCHEM, Issue 6 2010Leila Bülow Argyrin,F unfolds its promising antitumor activity twice: First through stabilization of the tumor suppressor protein p27 and second by vascular damage. [source] Virtual Screening and Biological Characterization of Novel Histone Arginine Methyltransferase PRMT1 InhibitorsCHEMMEDCHEM, Issue 1 2009Ralf Heinke Abstract Lysine and arginine methyltransferases participate in the posttranslational modification of histones and regulate key cellular functions. Protein arginine methyltransferase,1 (PRMT1) has been identified as an essential component of mixed lineage leukemia (MLL) oncogenic complexes, revealing its potential as a novel therapeutic target in human cancer. The first potent arginine methyltransferase inhibitors were recently discovered by random- and target-based screening approaches. Herein we report virtual and biological screening for novel inhibitors of PRMT1. Structure-based virtual screening (VS) of the Chembridge database composed of 328,000 molecules was performed with a combination of ligand- and target-based in,silico approaches. Nine inhibitors were identified from the top-scored docking solutions; these were experimentally tested using human PRMT1 and an antibody-based assay with a time-resolved fluorescence readout. Among several aromatic amines, an aliphatic amine and an amide were also found to be active in the micromolar range. [source] Biological characterization of glutaraldehyde-modified Parietaria judaica pollen extractsCLINICAL & EXPERIMENTAL ALLERGY, Issue 2 2004I. Ibarrola Summary Background Allergoids are widely used in specific immunotherapy (SIT) for the treatment of IgE-mediated allergic diseases, but all techniques for standardization of conventional allergic extracts may not be appropriate for standardization of a glutaraldehyde (GA)-modified extract because of the unique characteristics of these extracts. Objective To assess an accurate methodology for standardization of chemically modified extracts. Methods GA-modified extracts from Parietaria judaica pollen were purified by diafiltration. Biochemical properties were investigated by determination of amino groups, chromatography, and SDS-PAGE. The IgE-binding activity was determined by skin prick test, enzyme allergosorbent test inhibition, basophil activation, and histamine release tests. Peripheral blood mononuclear cells (PBMCs) from P. judaica pollen-allergic subjects were stimulated with either native or allergoid extracts, and proliferation was measured. Results Biochemical data indicated a high degree of allergen polymerization resulting in extract components higher than 100 kDa. IgE-binding activity, both in vivo and in vitro, was reduced by more than 99.8%. Both allergen and allergoid induced PBMC proliferation and synthesis of blocking IgG antibodies at similar rates. Moreover, no evidence of introduction of new determinants by chemical modification was found. Conclusions The preparation of GA-modified extracts by diafiltration is faster and more reliable than previous chromatographic methods. These modified extracts have drastically reduced their allergenicity while maintaining their immunogenicity, and therefore they can be used in safer and shortened schedules of SIT. [source] Determination of the toxic potential of Bacillus cereus isolates by quantitative enterotoxin analysesFEMS MICROBIOLOGY LETTERS, Issue 2 2006Maximilian Moravek Abstract Haemolysin BL (HBL) and nonhaemolytic enterotoxin (Nhe), each consisting of three components, represent the major enterotoxins produced by Bacillus cereus. To evaluate the expression of these toxins, a set of 100 B. cereus strains was examined. Molecular biological characterization showed that 42% of the strains harboured the genes for HBL and 99% for Nhe. The production of all Nhe and HBL components were analyzed using specific antibodies and, in culture supernatants, detectable levels of HBL and Nhe were found for 100% of hbl- positive and 96% of nhe -positive strains. The concentrations of the HBL,L2 and NheB component ranged from 0.02 to 5.6 ,g mL,1 and from 0.03 to 14.2 ,g mL,1, respectively. Comparison of the amount of NheB produced by food poisoning and food/environmental strains revealed that the median value for all food poisoning strains was significantly higher than for the food/environmental isolates. The data presented in this study provide evidence that specific and quantitative determination of the enterotoxins is necessary to evaluate the toxic potential of B. cereus. In particular, the level of Nhe seems to explain most of the cytotoxic activity of B. cereus isolates and may indicate a highly diarrheic potential. [source] Novel bioactive scaffolds with fibronectin recognition nanosites based on molecular imprinting technologyJOURNAL OF APPLIED POLYMER SCIENCE, Issue 6 2010Elisabetta Rosellini Abstract Biomimetic materials for application in the field of tissue engineering are usually obtained through covalent bonding between the polymer backbone and the bioactive molecules. A totally new approach, proposed for the first time by our research group, for the creation of advanced synthetic support structures for cell adhesion and proliferation is represented by molecular imprinting (MI) technology. In this article, we describe the synthesis and characterization of molecularly imprinted polymers with recognition properties toward a fibronectin peptide sequence and their application as functionalization structures. Polymers, in the form of densely fused microgel particles, were obtained by precipitation polymerization. The imprinted particles showed good performance in terms of recognition capacity and quantitative rebinding; moreover, the epitope effect was observed, with the particles able to recognize and rebind not only the specific peptide sequence but also a larger fibronectin fragment. The cytotoxicity tests showed normal vitality in C2C12 myoblasts cultured in a medium that was put in contact with the imprinted particles. Therefore, imprinted particles were used to functionalize synthetic polymeric films by deposition on their surface. The deposition of the imprinted particles did not alter their specific recognition and rebinding behavior. The most remarkable result was obtained by the biological characterization: in fact, the functionalized materials appeared able to promote cell adhesion and proliferation. These results are very promising and suggest that MI can be used as an innovative functionalization technique to prepare bioactive scaffolds with an effective capacity for improving tissue regeneration. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010 [source] Isolation and biological characterization of HIV-1 BG intersubtype recombinants and other genetic forms circulating in Galicia, SpainJOURNAL OF MEDICAL VIROLOGY, Issue 12 2006Lucía Pérez-Alvarez Abstract The biological characteristics of HIV-1 primary isolates of different recombinant forms (RFs) and non-B subtypes from Galicia, Spain, were investigated and the relationships between biological phenotype and evolution of infection were determined. Peripheral blood mononuclear cells (PBMCs) were obtained during the follow-up of 32 patients infected with HIV-1 non-subtype B genetic forms, characterized in partial sequences of pol (protease-reverse transcriptase) and env V3 region: 12 (37.5%) circulating RFs (CRFs), 9 (28.1%) unique RFs (URFs), and 11(34.4%) non-B subtypes. Primary isolates were obtained by coculture with donor PBMCs. Syncytium-inducing (SI) phenotype was examined in MT2 cell line and coreceptor use in GHOST and U87.CD4 cells. Fifty percent of tissue culture infective dose (TCID50) and viral phenotype based on V3 net charge and Geno2phenocoreceptor bioinformatic method were determined. Fifty-four HIV-1 primary isolates were obtained. CRF14_BG and BG URFs represented the largest group, being all SI/X4, independently of the CD4+ cell count, viral load, or the duration of infection. By contrast, 10 of 11 CRF02_AG viruses were NSI/R5. The prediction of co-receptor use was concordant with biological characterization in all NSI/R5 and in 23 of 26 SI/X4 isolates. The presence of SI/X4 or SI/X4,R5 isolates at early stages of the infection in addition to a decrease in CD4+ counts below 500 cells/µl between 2 and 6 years since diagnosis was observed in all patients infected with CRF14_BG and BG URFs. These data contrast with the usual progression in B subtype infections, in which SI/X4 viruses rarely predominate in the early years of HIV-1 infection. J. Med. Virol. 78:1520,1528, 2006. © 2006 Wiley-Liss, Inc. [source] Intracellular and cell-free (infectious) HIV-1 in rectal mucosaJOURNAL OF MEDICAL VIROLOGY, Issue 4 2001Mariantonietta Di Stefano Abstract The intestinal mucosa contains most of the total lymphocyte pool and plays an important role in viral transmission, but only slight attention has been given to the immunological and virological aspects of human immunodeficiency virus-1 (HIV-1) infection at this site. In this study, before initiating or changing antiretroviral therapy, paired blood samples and rectal biopsies (RB) were obtained from 26 consecutive HIV-infected subjects. HIV-1 isolation and biological characterization, DNA, and HIV-1 RNA titration were assessed, as were in vitro tumor necrosis factor-alpha (TNF-,) and interleukin-, (IL-1,) spontaneous production. The rate of HIV-1 isolation from peripheral blood mononuclear cells (PBMCs) and RBs was 75% and 58%, respectively. All RB-derived isolates were nonsyncytium inducing (NSI), independent of the phenotype of blood-derived isolates. Proviral DNA and detectable HIV-1 RNA levels were measured in 100% and 77% of RBs, respectively. A statistical correlation was observed between HIV-1 DNA and HIV-1 RNA levels in rectal mucosa (P,=,0.0075), whereas no correlation was found between these levels in blood samples (P,>,0.05). Antiretroviral treatment did not seem to influence HIV-1 detection in RBs. Higher levels of in vitro proinflammmatory cytokine production were found in the RBs of most infected patients when compared with healthy controls. Therefore, the rectal mucosa is an important HIV-1 reservoir that demonstrates a discordant viral evolution with respect to blood. Both the virus type and the mucosa pathway of immunoactive substances might have important implications for therapeutic decision-making and monitoring and could influence the bidirectional transmission of HIV-1 in mucosal surfaces. J. Med. Virol. 65:637,643, 2001. © 2001 Wiley-Liss, Inc. [source] Synthesis and biological characterization of human monocyte chemoattractant protein 1 (MCP-1) and its analogsJOURNAL OF PEPTIDE SCIENCE, Issue 1 2006Marian Kruszynski Abstract Novel analogs of human monocyte chemoattractant protein 1 (MCP-1) were designed, synthesized and characterized to be used as tools to generate monoclonal antibodies as potential human therapeutics. MCP-1 and three analogs were synthesized by step-wise Fmoc solid phase synthesis. After oxidation to form the two-disulfide bonds, affinity chromatography using an immobilized mouse anti-human MCP-1 monoclonal antibody (mAb) was utilized for a simple and highly effective purification procedure for the proteins. The final products were extensively characterized and compared with recombinant human MCP-1 (rhMCP-1). All proteins showed identical binding with mouse anti-human MCP-1 mAbs as measured by surface plasmon resonance. Synthetic MCP-1 and the analogs were comparable to recombinant MCP-1 in competition radio-ligand binding to CCR2 receptors on THP-1 cells, and MCP-1-induced, calcium mobilization and chemotaxis assays. Copyright © 2005 European Peptide Society and John Wiley & Sons, Ltd. [source] Solid emulsion gel as a vehicle for delivery of polyunsaturated fatty acids: implications for tissue repair, dermal angiogenesis and wound healingJOURNAL OF TISSUE ENGINEERING AND REGENERATIVE MEDICINE, Issue 7 2008Kirill I. Shingel Abstract The paper describes preparation and biological characterization of the solid hybrid biomaterial that was designed for cell-targeted lipid delivery in healing tissues. The material referred to as ,solid emulsion gel' combines a protein-stabilized lipid emulsion and a hydrogel structure in a single compartment. The potential of the omega-3 (n-3)-fatty acids rich solid emulsion gel for tissue repair applications was investigated at the macro-, micro-, molecular and gene expression levels, using human fibroblasts and endothelial cells and a porcine model of full-thickness wounds. Being non-cytotoxic in vitro and in vivo, the biomaterial was found to affect cell metabolism, modulate expression of certain genes, stimulate early angiogenesis and promote wound repair in vivo. The neovascular response in vivo was correlated with upregulated expression of the genes involved in lipid transport (e.g. adipophilin), anti-apoptosis (e.g. heat shock proteins, haem oxygenase 1) and angiogenesis (vascular endothelial growth factor, placental growth factor). Collectively, the results of this study provide first evidence that the angiogenic response provided by solid emulsion gel-mediated delivery of n-3 fatty acids is an alternative to the topical administration of exogenous growth factors or gene therapy, and can be advantageously used for the stimulation of tissue repair in complex wounds. Copyright © 2008 John Wiley & Sons, Ltd. [source] Sediment dynamics and pollutant mobility in rivers: An interdisciplinary approachLAKES & RESERVOIRS: RESEARCH AND MANAGEMENT, Issue 1 2004Ulrich Förstner Abstract Characteristic dynamic features of sediment-related processes in rivers include dramatic effects of stormwater events on particle transport, rapid and far-reaching effects of sulphide oxidation during resuspension, and biological accumulation and potential release of toxic chemicals. Pollutant mobility is the net result of the stabilizing and mobilizing effects in both hydraulic and chemical fields. In practice, emphasis has to be given to fine-grained sediments and suspended matter as these materials exhibit large surface areas and high sorption capacities. Organic materials are highly reactive. Degradation of organic matter will induce oxygen depletion and might enhance formation of flocs and biofilms. Study of variations of sediment and water chemistry should predominantly include changes of pH and redox conditions, competition of dissolved ions and processes such as complexation by organic substances. Major questions relate to the potential reduction of sorption sites on minerals and degradation of organic carrier materials. All these processes will influence solution/solid equilibrium conditions and have to be studied prior to modelling the overall effects of pollutants on the water body and aquatic ecosystems. With respect to handling and remediation of contaminated river sediments, either in-place or excavated, a chemical and biological characterization of the material, of the (disposal) site and of the long-term processes is crucial. Passive techniques (e.g. in situ stabilization, subaqueous capping) provide economic advantages as there are no operation costs following their installation. However, the success of these ecological and geochemical engineering approaches is mainly based on an in-depth knowledge of the underlying processes. [source] The influence of species and growing conditions on the 18-O enrichment of leaf water and its impact on ,effective path length'NEW PHYTOLOGIST, Issue 3 2009Ansgar Kahmen Summary ,,The stable oxygen isotope ratio (,18O) of plant material has been shown to contain essential information on water and carbon fluxes at the plant and ecosystem scales. However, the effective path length (Lm), a parameter introduced to leaf-water models still requires a comprehensive biological characterization to allow interpretation of ,18O values in plant material with confidence. ,,Here, we tested the variability of Lm across and within three species that developed leaves in environments with different relative humidity. We also tested whether the Lm of fully developed leaves is affected by short-term fluctuations in relative humidity. ,,We determined that significant differences in Lm exist among Phaseolus vulgaris, Rizinus communis and Helianthus annuus. Within a given species, however, Lm values did not differ significantly among individuals. ,,These findings indicate that Lm is species specific and a relatively constant parameter and that Lm will not obscure the interpretation of ,18O values in plant material of a given species. We urge caution, however, because values for Lm are derived from fitting leaf-water models to measured values of ,18O, so care must be taken in assigning a ,cause' to values of Lm as they likely capture a combination of different biological leaf properties [source] Synthesis and characterization of synthetic analogs of cinnacidin, a novel phytotoxin from Nectria sp.,PEST MANAGEMENT SCIENCE (FORMERLY: PESTICIDE SCIENCE), Issue 9 2008Nicholas M Irvine Abstract BACKGROUND: The novel natural product cinnacidin was isolated from a fungal fermentation extract of Nectria sp. DA060097. The compound was found to contain a cyclopentalenone ring system with an isoleucine subunit linked through an amide bond. Initial biological characterization of cinnacidin suggested promising herbicidal activity. RESULTS: Two synthetic analogs, (2S,3S)-2-[(3RS,3aSR,6aRS)-3-methoxy-4-oxo-3,3a,4,5,6,6a-hexahydropentalen-1-ylcarbamoyl]-3-methylvaleric acid and benzyl (2S,3S)-2-[(3RS,3aSR,6aRS)-3-methoxy-4-oxo-3,3a,4, 5,6,6a-hexahydropentalen-1-ylcarbamoyl]-3-methylvalerate, were prepared for further characterization, and their herbicidal activities were compared with that of cinnacidin. CONCLUSIONS: The synthetic compounds were highly phytotoxic on a range of weeds. Based on the symptoms in treated plants, the mode of action of these compounds is suggested to be similar to that of coronatine and jasmonic acid. Coronatine was more active against warm-season grasses, while the cinnacidin benzyl ester analog was more effective on cool-season grasses. In a seedling growth bioassay conducted on bentgrass, the cinnacidin analog was equivalent in activity to coronatine. Copyright © 2008 Society of Chemical Industry [source] Characterization of Passionfruit severe leaf distortion virus, a novel begomovirus infecting passionfruit in Brazil, reveals a close relationship with tomato-infecting begomovirusesPLANT PATHOLOGY, Issue 2 2010S. S. Ferreira Molecular and biological characterization of the begomovirus isolate BR:LNS2:Pas:01, obtained from yellow passionfruit plants in Livramento de Nossa Senhora, Bahia state, Brazil, was carried out. Sequence analysis demonstrated that the BR:LNS2:Pas:01 DNA-A had highest nucleotide sequence identity with Tomato chlorotic mottle virus (77%) and had five ORFs corresponding to the genes cp, rep, trap, ren and ac4. The DNA-B had highest nucleotide sequence identity with Tomato yellow spot virus (74%) and two ORFs corresponding to the genes mp and nsp. These identity values indicate that this isolate represents a new begomovirus species, for which the name Passionfruit severe leaf distortion virus (PSLDV), is proposed. Phylogenetic analysis clustered the PSLDV DNA-A and -B in a monophyletic branch with Brazilian tomato-infecting begomoviruses. The isolate's host range was restricted to species from the Passifloraceae and Solanaceae. PSLDV-[BR:LNS2:Pas:01] was capable of forming pseudorecombinants with tomato-infecting begomoviruses, reinforcing its close relationship with these viruses and suggesting a possible common origin. However, the virus was not capable of infecting tomato. [source] Molecular and biological characterization of Macroptilium yellow mosaic virus from JamaicaPLANT PATHOLOGY, Issue 3 2008I. I. Amarakoon The molecular and biological characterization of a begomovirus infecting the common weed Macroptilium lathyroides from Jamaica are reported. The virus showed 92% sequence identity to an isolate of Macroptilium yellow mosaic virus (MaYMV) from Cuba, but was distinct from the two other begomoviruses isolated from M. lathyroides, namely Macroptilium yellow mosaic Florida virus (80% identity) and Macroptilium mosaic Puerto Rico virus (68% identity). Hence, the Jamaican begomovirus was considered an isolate of MaYMV and called Macroptilium yellow mosaic virus -[Jamaica] (MaYMV-[JM]). In infectivity studies using cloned DNA-A and DNA-B genomic components, MaYMV-[JM] infected red kidney bean (Phaseolus vulgaris) and produced mild symptoms in Scotch Bonnet pepper (Capsicum chinense), but did not infect cabbage (Brassica oleracea). This information has implications for the development of strategies to control begomovirus diseases in Jamaica and elsewhere. [source] | ||||||||||||||||