Anti-fibrosis attributes: UHPLC-MS/MS-based pharmacokinetics profiling of a novel autotaxin inhibitor with excellent in vivo efficacy in rat

3,4-Difluorobenzyl(1-ethyl-5-(4-((4-hydroxypiperidin-1-yl)-methyl)thiazol-2-yl)-1H-indol-3-yl)carbamate (NAI59), a small molecule with outstanding therapeutic effectiveness to anti-pulmonary fibrosis, was developed as an autotaxin inhibitor candidate compound. To evaluate the pharmacokinetics and plasma protein binding of NAI59, a UPLC–MS/MS method was developed to quantify NAI59 in plasma and phosphate-buffered saline. The calibration curve linearity ranged from 9.95 to 1990.00 ng/mL in plasma. The accuracy was −6.8 to 5.9%, and the intra- and inter-day precision was within 15%. The matrix effect and recovery, as well as dilution integrity, were within the criteria. The chromatographic and mass spectrometric conditions were also feasible to determine phosphate-buffered saline samples, and it has been proved that this method exhibits good precision and accuracy in the range of 9.95–497.50 ng/mL in phosphate-buffered saline. This study is the first to determine the pharmacokinetics, absolute bioavailability, and plasma protein binding of NAI59 in rats using this established method. Therefore, the pharmacokinetic profiles of NAI59 showed a dose-dependent relationship after oral administration, and the absolute bioavailability in rats was 6.3%. In addition, the results of protein binding showed that the combining capacity of NAI59 with plasma protein attained 90% and increased with the increase in drug concentration.     

Determination of sulfa antibiotic residues in river and particulate matter by field-amplified sample injection-capillary zone electrophoresis

In the present research, field-amplified sample injection–CZE (FASI–CZE) coupled with a diode array detector was established to determine trace level sulfa antibiotic. Sulfathiazole, sulfadiazine, sulfamethazine, sulfadimethoxine, sulfamethoxazole, and sulfisoxazole were selected as analytes for the experiments. The background electrolyte solution consisted of 70.0 mmol/L borax and 60.0 mmol/L boric acid (including 10% methanol, pH 9.1). The plug was 2.5 mmol/L borax, which was injected into the capillary at a pressure of 0.5 psi for 5 s. Then the sample was injected into the capillary at an injection voltage of –10 kV for 20 s. The electrophoretic separation was carried out under a voltage of +19 kV. The capillary temperature was maintained at 20˚C throughout the analysis, and six sulfonamides were completely separated within 35 min. Compared with pressure injection-CZE, the sensitivity of FASI-CZE was increased by 6.25–10.0 times, and the LODs were reduced from 0.2–0.5 to 0.02–0.05 μg/mL. The method was applied to the determination of sulfonamides in river water and particulate matter samples. The recoveries were 78.59–106.59%. The intraday and interday precisions were 2.89–7.35% and 2.77–7.09%, respectively. This provides a simpler and faster method for the analysis of sulfa antibiotic residues in environmental samples.     

Electrochemiluminescence Enhanced by the Synergetic Effect of Porphyrin and Multi-walled Carbon Nanotubes for Uric Acid Detection

The design and exploration of efficient, stable and environmentally compatible organic emitters for an electrochemiluminescence (ECL) sensor is a promising topic. Herein, a novel environmentally-friendly luminophore, ZnBCBTP@MWCNTs, were fabricated via self-assembly of porphyrin molecules (ZnBCBTP) onto multi-walled carbon nanotubes (MWCNTs). The resulting luminophore ZnBCBTP@MWCNTs displayed not only the highly ECL property and but also the good accelerated electron mobility. Then, a label-free ECL biosensor based ZnBCBTP@MWCNTs was constructed for the ultrasensitive detection of uric acid. Excitingly, this proposed ECL biosensor performed a good linear relationship in the range of 0–300 μM with a low detection limit of 1.4 μM, thus offering another reliable and feasible sensing platform for clinical bioanalysis with good selectivity, stability, and repeatability.     

基于校园网的实验管理系统的设计

主要讨论了应用实验室管理系统的必要性,并从用户需求分析、系统总体设计、功能模块的设计等方面对B/S实验室管理系统的开发进行了详细的阐述。     

A method to collect an infrared spectrum in solution.

Herein we report a new method to collect a qualified infrared spectrum of a solute in solution by two solvent cells with different thickness during background single-beam spectrum scanning. By collecting the background spectrum with two cells (two stages), we successfully achieved accurate solvent compensation between a sample and a reference, namely, the solvent amounts in the sample and background measurements could become congruent. Therefore, the solvent bands were thoroughly suppressed in the infrared spectrum and a qualified spectrum of the solute was obtained.     

Fluorination of diamond — C4F9I and CF3I photochemistry on diamond (100)

The radiation-induced decomposition of C₄F₉I and CF₃I overlayers at 119 K on diamond (100) surfaces has been shown to be an efficient route to fluorination of the diamond surface. X-ray photoelectron spectroscopy has been used for photoactivation as well as for studying the photodecomposition of the fluoroalkyl iodide molecules, the attachment of the photofragments to the diamond surface, and the thermal decomposition of the fluoroalkyl ligands. Measured chemical shifts agree well with ab initio calculations of both C 1s and F 1s binding energies. It is found that chemisorbed CF₃ groups on diamond (100) decompose by 300 K whereas C₄F₉ groups decompose over the range 300 to 700 K and this reactivity difference is rationalized on steric grounds. Both of these thermal decomposition processes produce surface C---F bonds on the diamond. The surface C---F species thermally decompose over a wide temperature range extending up to 1500 K. Hydrogen passivation of the diamond surface is ineffective in preventing free radical attack from the photodissociated products of the fluoroalkyl iodides; I atoms produced photolytically abstract H from surface C---H bonds to yield hydrogen iodide at 119 K allowing diamond fluorination. The attachment of chemisorbed F species to the diamond (100) surface causes band bending as the surface states are occupied as a result of chemisorption. This results in a shift to higher binding energy of the diamond-related C 1s levels present in the surface and subsurface regions which are sampled by XPS on the diamond. The use of photoactivation of fluoroalkyl iodides for the fluorination of diamond surfaces provides a convenient route compared to other methods involving the action of atomic F, molecular F₂, XeF₂ and F-containing plasmas.     

THERMAL AND THERMO-ELASTIC-PLASTIC RESPONSE OF CERAMIC-METAL FUNCTIONALLY GRADED MATERIALS—THERMAL SHOCK PROBLEM

The thermal and thermo-elastic-plastic response of newly developed ceramic-metalfunctionally graded materials under a thermal shock load is studied.The materials are heated at the ce-ramic surface with a sudden high-intensity heat flux input,and cooled at the metal surface with aflowing liquid nitrogen.Emphasis is placed on two aspects:(1)the influence of the graded composi-tion of the materials on the temperature and stress response;and(2)the optimum design of the gradedcomposition from a unified viewpoint of the heat insulation property and stress relaxation property.Moreover,a comparison between the thermoelastic stress and the thermo-elastic-plastic stress is alsomade to indicate the plasticity effect.     

Experimental study of a plasma-filled backward wave oscillator

Experimental studies of a plasma-filled X-band backward-wave oscillator (BWO) are presented. Depending on the background gas pressure, microwave frequency upshifts of up to 1 GHz appeared along with an enhancement by a factor of 7 in the total microwave power emission. The bandwidth of the microwave emission increased from ⩽0.5 GHz to 2 GHz when the BWO was working at the RF power enhancement pressure region. The RF power enhancement appeared over a much wider pressure range in a high beam current case (10-100 mT for 3 kA) than in a lower beam case (80-115 mT for 1.6 kA). The plasma-filled BWO has higher power output than the vacuum BWO over a broader region of magnetic guide field strength. Trivelpiece-Gould modes (T-G modes) are observed with frequencies up to the background plasma frequency in a plasma-filled BWO. Mode competition between the T-G modes and the X-band Tm₀₁ mode prevailed when the background plasma density was below 6×10¹¹ cm^-3 . At a critical background plasma density of ≃8×10¹¹ cm^-3 power enhancement appeared in both X-band and the T-G modes. Power enhancement of the S-band in this mode collaboration region reached up to 8 dB. Electric fields measured by the Stark-effect method were as high as 34 kV/cm while the BWO power level was 80 MW. These electric fields lasted throughout the high-power microwave pulse     

互补型自适应滤波器在心磁信号处理中的应用

将心磁信号从干扰噪声中加以提取并有效地消除噪声干扰是心磁信号处理中尤为重要的环节 .从改进算法的角度出发，提出互补型自适应滤波器结构以实现心磁信号的消噪处理.该滤波器针对心磁这类非平稳信号进行设计，有效地解决了常规自适应滤波器应用于心磁信号处理时收敛速度和稳态误差的矛盾.通过仿真实验和心磁实验结果表明，该算法能有效地消除心磁信号的背景噪声和工频干扰噪声.同时该算法也可用于其他非平稳信号的消噪处理. 关键词： 自适应滤波 心磁图 最小均方误差