Search results for " concentration"
showing 10 items of 1684 documents
Discovery of 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles as potent firefly luciferase inhibitors.
2013
Luciferase reporter assays are commonly used in high-throughput screening methods. Here, we report new firefly luciferase (FLuc) inhibitors based on 5-benzyl-3-phenyl-4,5-dihydroisoxazoles and 5-benzyl-3-phenyl-1,4,2-dioxazoles, which showed up as "false positives" in a luciferase reporter gene-based assay for nuclear receptor antagonists. The inhibition was shown to be noncompetitive for both natural enzyme substrates (d-luciferin and ATP) and selective to FLuc and proven to arise from a direct interaction between the enzyme and the inhibitor. Of the 63 evaluated compounds, 28 showed significantly better inhibition potency than the well-known inhibitor resveratrol (IC(50) = 59 nM), with fi…
Bile acid–cysteamine conjugates: Structural properties, gelation, and toxicity evaluation
2011
Abstract Design, synthesis, and characterization of six novel bile acid–cysteamine conjugates together with investigation of their structural studies, gelation properties, and preliminary toxicity evaluation, are reported. Solid state properties of selected compounds were studied by means of X-ray diffraction and 13C CPMAS NMR spectroscopy. N-(2-thioethyl)-3α,7α,12α-trihydroxy-5β-cholan-24-amide was shown to exhibit (pseudo)polymorphism, and a single crystal structure of its non-stoichiometric hydrate is reported herein. Cholyl and dehydrocholyl derivatives bearing three functionalities in their steroidal backbone were shown to undergo self-assembly leading to gelation in certain organic so…
Enhancing the multiplication of nucleopolyhedrovirus in vitro by manipulation of the pH
2009
Insect nucleopolyhedroviruses (NPVs) are studied widely as agents for biological control, as expression vectors for the production of heterologous proteins, and as transduction vectors for gene therapy applications. Most of these applications rely on the existence of cell lines that allow in vitro multiplication of the virus. The influence of pH in the medium culture on the multiplication of SeMNPV, HearSNPV and AcMNPV in different cell culture lines was investigated. The study showed a strong influence of the medium pH on the virus multiplication with the best results at pH 6.5, about half pH unit above the pH of insect culture media used most commonly. Additional experiments using a recom…
Dynamics of particulate major and trace elements in the lower reaches of the Daugava River and adjacent area of the Gulf of Riga (Baltic Sea).
2004
Suspended particulate matter (SPM) was collected in the freshwater-seawater mixing zone in the lower reaches of the Daugava River (Latvia) and adjacent marine area, during five cruises in 1998-2001. The study focused on biogeochemical phase exchange processes. SPM in the freshwater was found to be mainly allochthonous with a high content of organic matter, Mn and sorbed phosphate. Property-salinity plots suggested flocculation of humic-Fe complexes across the salinity gradient. The variability of sorbed phosphate was related to particulate Fe, although no dependence on pH and ionic strength was observed. The Mn contents of SPM mainly follow conservative mixing, but there are also indication…
Influence of parent material and soil use on arsenic forms in soils A case study in the Amblés Valley (Castilla-León, Spain)
2014
Abstract The total, water soluble and extractable concentrations with EDTA of As from topsoils from the Ambles Valley (Avila, Spain) were determined. The geochemical baseline concentrations of total As were established, and the relationships between the concentration of the different As forms and soil properties were investigated. Total As content in soils was related with parent material, whereas anthropogenic activities affected its mobility. Iron, aluminium, clay content, soil organic matter and soil pH were the main controlling factors for As soil concentrations. The geochemical baseline concentrations obtained (mg kg − 1 ) were 7.3–35 in soils on granite parent material and 2.2–6.8 in …
Effects of dopamine infusion on plasma catecholamines in preterm and term newborn infants.
1991
Newborn infants (21 preterm and 13 term) received dopamine infusions at a low (2.5-3.4 micrograms/kg per min) and/or high (5-10 micrograms/kg per min) infusion rate and changes in plasma catecholamines were monitored. The mean baseline values for dopamine, noradrenaline and adrenaline were between 240 and 560, 125 and 144 and 62 and 82 pg/ml, respectively. During low-rate infusion of dopamine, there was a significant increase in plasma dopamine (20-100 fold), noradrenaline (three- to five-fold) and adrenaline (threefold). Administration of dopamine at the high rate resulted in an even larger increase in the plasma catecholamines (dopamine, 100-300 fold; noradrenaline, seven- to eightfold; a…
Influence of the pH on the synthesis of reduced graphene oxide under hydrothermal conditions
2012
Here we describe the important role played by the pH on the morphology and structure of the reduced graphite oxide (rGO) samples obtained by hydrothermal treatment of the previously prepared GO. The nature of the resulting samples has been studied on the basis of a complete battery of experimental techniques.
The use of steel angles for the connection of laminated glass beams: Experiments and modelling
2012
Abstract In the present paper the experimental results relative to three-point bending tests on multilayer glass beams and on semi-rigid connections realised with stainless double web angles are presented and discussed. Small and medium size glass beams were tested and load–deflection curves and crack patterns at failure were recorded. The laminated glass specimens, of equal cross-section, were characterised by three different combinations of annealed float and fully thermally tempered glass plies and different interlayers. Steel joints constituted by double web angles to connect two glass beams were tested adopting several geometrical configurations and using stainless steel bolts preloade…
Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis
2018
Abstract: Chemotherapy is currently the only effective approach to treat all forms of leishmaniasis. However, its effectiveness is severely limited due to high toxicity, long treatment length, drug resistance, or inadequate mode of administration. As a consequence, there is a need to identify new molecular scaffolds and targets as potential therapeutics for the treatment of this disease. We report a small series of 1,2‐substituted‐1H‐benzo[d]imidazole derivatives (9ad) showing affinity in the submicromolar range (Ki = 0.150.69 μM) toward Leishmania mexicanaCPB2.8ΔCTE, one of the more promising targets for antileishmanial drug design. The compounds confirmed activity in vitro against intrace…
GSK-3? Can Regulate the Sensitivity of MIA-PaCa-2 Pancreatic and MCF-7 Breast Cancer Cells to Chemotherapeutic Drugs, Targeted Therapeutics and Nutra…
2021
Glycogen synthase kinase-3 (GSK-3) is a regulator of signaling pathways. KRas is frequently mutated in pancreatic cancers. The growth of certain pancreatic cancers is KRas-dependent and can be suppressed by GSK-3 inhibitors, documenting a link between KRas and GSK-3. To further elucidate the roles of GSK-3β in drug-resistance, we transfected KRas-dependent MIA-PaCa-2 pancreatic cells with wild-type (WT) and kinase-dead (KD) forms of GSK-3β. Transfection of MIA-PaCa-2 cells with WT-GSK-3β increased their resistance to various chemotherapeutic drugs and certain small molecule inhibitors. Transfection of cells with KD-GSK-3β often increased therapeutic sensitivity. An exception was observed wi…