Histone deacetylase (HDAC) activity is modulated in vivo by post-translational modifications and formation of multiprotein complexes. Novel chemical tools to study how these factors affect engagement of HDAC isoforms by HDAC inhibitors (HDACi) in cells and tissues are needed. In this study, a synthetic strategy to access chemically diverse photoreactive probes (PRPs) was developed and used to prepare seven novel HDAC PRPs 9 – 15 . The class I HDAC isoform engagement by PRPs was determined in biochemical assays and photolabeling experiments in live SET-2, HepG2, HuH7, and HEK293T cell lines and in mouse liver tissue. Unlike the HDAC protein abundance and biochemical activity against recombinant HDACs, the chemotype of the PRPs and the type of cells were key in defining the engagement of HDAC isoforms in live cells. Our findings suggest that engagement of HDAC isoforms by HDACi in vivo may be substantially modulated in a cell- and tissue-type-dependent manner. 相似文献
This paper is concerned with Electroencephalography (EEG) seizure prediction, which means the detection of the pre-ictal state prior to ictal activity occurrence. The basic idea of the proposed approach for EEG seizure prediction is to work on the signals in the Hilbert domain. The operation in the Hilbert domain guarantees working on the low-pass spectra of EEG signal segments to avoid artifacts. Signal attributes in the Hilbert domain including amplitude, derivative, local mean, local variance, and median are analyzed statistically to perform the channel selection and seizure prediction tasks. Pre-defined prediction and false-alarm probabilities are set to select the channels, the attributes, and bins of probability density functions (PDFs) that can be useful for seizure prediction. Due to the multi-channel nature of this process, there is a need for a majority voting strategy to take a decision for each signal segment. Simulation results reveal an average prediction rate of 96.46%, an average false-alarm rate of 0.028077/h and an average prediction time of 60.1595 min for a 90-min prediction horizon.
The corrosion inhibition characteristics of 2-amino thiophenol (ATP) and 2-cyanomethyl benzothiazole (CNMBT) on two types of steel in 1m HCl medium were investigated at different temperatures (25, 30, 35, 40 and 50°C). The pitting corrosion behaviour for the same system was studied using a potentiodynamic technique. The pitting corrosion resistance of steel samples increased with increase in concentration of the ATP and CNMBT. Some samples were examined by scanning electron microscopy. The effects of the inhibitors on the general corrosion of the two samples were investigated by using gravimetric and galvanostatic polarization techniques. The inhibition efficiencies increased with increase their concentration but decreased with increase in temperature. Free energies of activation, enthalpies and entropies for the inhibition processes were determined from rate constant data measured and different temperatures at different concentrations of ATP and CNMBT. Results were compared with fits obtained from the application of the Langmuir isotherm. Results were correlated to the chemical structure of the inhibitors. The inhibition efficiency of CNMBT is higher than that of ATP. 相似文献
Two sensitive, spectrophotometric and atomic absorption spectrometric procedures are developed for the determination of ramipril and perindopril. Both methods are based on the formation of a ternary complex, extractable with chloroform, between copper(II), eosin and the two cited drugs. Spectrophotometrically under the optimum condition, the ternary complexes showed an absorption maximum at 535 nm, with apparent molar absorptivities of 6.55 and 4.00 x 10(3) mol(-1) x cm(-1) and Sandell's sensitivities of 5.80 x 10(-2) and 1.04 x 10(-1) microg x cm(-2) for perindopril and ramipril, respectively. The solution of ternary complex obeyed Beer's law in concentration ranges 10-60 and 20-100 microg x ml(-1) for perindopril and ramipril, respectively. The proposed method was applied to the determination of the two cited drugs in pharmaceutical tablets. The atomic absorption spectrometric method, directly through the quantitative determination of copper content of the organic extract of the complex, was also investigated for the purpose of enhancing the sensitivity of the determination. The spectrophotometric and atomic absorption spectrometric procedures hold their accuracy and precision well when applied to the determination of ramipril and perindopril dosage forms. 相似文献
The aim of the present work was to study the effect of quartz on the hydration characteristics of hydrothermally hardened granulated slag-alite pastes. The pastes, of water: solid ratio 0.20, were moulded at a pressure of 50 kg cm–2 and autoclaved at 10 atm for 0.5, 2, 6, 12 and 24 h. Compressive strengths of the hardened product were determined, and the kinetics of reaction were studied by the quantitative determination of free lime and combined water contents. The phases formed after autoclaving were determined using XRD techniques. The reaction mechanism of the system under investigation was discussed and correlated to the strength of the hardened product. It can be concluded that the addition of quartz to slag-alite mixture increases the strength of the final product. The strength obtained for samples with high alite content are higher than that of low-alite content. Finally, the addition of quartz assists the formation of tobermorite in the hardened specimens. 相似文献
Problems have occurred with dykes constructed on the Lisan Marl to retain brine pumped from the Dead Sea, which is chemically
processed to produce potash. In this study the engineering behavior, collapse potential and compressibility of the Lisan Marl
were assessed by undertaking laboratory tests with both natural, distilled water and brine as the media. The results showed
that the liquid limit and fine particles increased when the soil was mixed with fresh/distilled water compared with brine
water. The soil can be classified as highly compressible with a low undrained shear strength. In terms of collapsibility,
the soil could be classified as slightly collapsible upon inundation with distilled water and moderately collapsible when
soaked in Dead Sea brine. The results are important when determining the height and nature of the dykes.
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A novel methodology for the solvent free auto-oxidation of methylbenzenes under mild conditions is disclosed. The new scheme is based on a combination of metallic salt (cobalt chloride) and a quaternary ammonium phase transfer catalyst (didecyldimethylammonium bromide) which together form a complex soluble catalyst in the organic phase. Major reaction parameters are studied and optimized and the procedure is applied for the conversion of several substituted toluenes to the corresponding benzoic acids in excellent isolated yields. 相似文献
Microalloyed steels are characterised by their mechanical properties. Nowadays, they are used in a wide range of applications. The convenience and simplicity of hardness tests permit to obtain economically and rapidly information on the structure of steels and control their treatments. This study has been carried out to derive equations for prediction of the mechanical properties of microalloyed steels by hardness measurement. With this objective, V‐ and Ti‐microalloyed plain carbon steel bars were melted, hot rolled, heat treated and machined for the measurement of their mechanical properties and to reach a correlation between both ultimate tensile strength, yield strength and uniform elongation and Vickers hardness. The obtained data were treated using different mathematical fittings. They are mathematically treated as groups according to the heat treatment processes and as one group. The derived equations show good agreement with each other and with most of the little relations found in the literature. General equations for deducing mechanical properties values from the easily measured Vickers hardness values were derived. The equations derived from one group without regarding the treatment processes are more reliable. 相似文献