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.     

A call admission and rate control scheme for multimedia support over IEEE 802.11 wireless LANs

Quality of service (QoS) support for multimedia services in the IEEE 802.11 wireless LAN is an important issue for such WLANs to become a viable wireless access to the Internet. In this paper, we endeavor to propose a practical scheme to achieve this goal without changing the channel access mechanism. To this end, a novel call admission and rate control (CARC) scheme is proposed. The key idea of this scheme is to regulate the arriving traffic of the WLAN such that the network can work at an optimal point. We first show that the channel busyness ratio is a good indicator of the network status in the sense that it is easy to obtain and can accurately and timely represent channel utilization. Then we propose two algorithms based on the channel busyness ratio. The call admission control algorithm is used to regulate the admission of real-time or streaming traffic and the rate control algorithm to control the transmission rate of best effort traffic. As a result, the real-time or streaming traffic is supported with statistical QoS guarantees and the best effort traffic can fully utilize the residual channel capacity left by the real-time and streaming traffic. In addition, the rate control algorithm itself provides a solution that could be used above the media access mechanism to approach the maximal theoretical channel utilization. A comprehensive simulation study in ns-2 has verified the performance of our proposed CARC scheme, showing that the original 802.11 DCF protocol can statically support strict QoS requirements, such as those required by voice over IP or streaming video, and at the same time, achieve a high channel utilization. Hongqiang Zhai received the B.E. and M.E. degrees in electrical engineering from Tsinghua University, Beijing, China, in July 1999 and January 2002 respectively. He worked as a research intern in Bell Labs Research China from June 2001 to December 2001, and in Microsoft Research Asia from January 2002 to July 2002. Currently he is pursuing the PhD degree in the Department of Electrical and Computer Engineering, University of Florida. He is a student member of IEEE. Xiang Chen received the B.E. and M.E. degrees in electrical engineering from Shanghai Jiao Tong University, Shanghai, China, in 1997 and 2000, respectively, and the Ph.D. degree in electrical and computer engineering from the University of Florida, Gainesville, in 2005. He is currently a Senior Research Engineer at Motorola Labs, Arlington Heights, IL. His research interests include resource management, medium access control, and quality of service (QoS) in wireless networks. He is a Member of Tau Beta Pi and a student member of IEEE. Yuguang Fang received a Ph.D degree in Systems and Control Engineering from Case Western Reserve University in January 1994, and a Ph.D degree in Electrical Engineering from Boston University in May 1997. From June 1997 to July 1998, he was a Visiting Assistant Professor in Department of Electrical Engineering at the University of Texas at Dallas. From July 1998 to May 2000, he was an Assistant Professor in the Department of Electrical and Computer Engineering at New Jersey Institute of Technology. In May 2000, he joined the Department of Electrical and Computer Engineering at University of Florida where he got the early promotion with tenure in August 2003 and has been an Associate Professor since then. He has published over one hundred (100) papers in refereed professional journals and conferences. He received the National Science Foundation Faculty Early Career Award in 2001 and the Office of Naval Research Young Investigator Award in 2002. He is currently serving as an Editor for many journals including IEEE Transactions on Communications, IEEE Transactions on Wireless Communications, IEEE Transactions on Mobile Computing, and ACM Wireless Networks. He is also actively participating in conference organization such as the Program Vice-Chair for IEEE INFOCOM’2005, Program Co-Chair for the Global Internet and Next Generation Networks Symposium in IEEE Globecom’2004 and the Program Vice Chair for 2000 IEEE Wireless Communications and Networking Conference (WCNC’2000).     

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.     

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     

非洲爪蟾卵提取物中200nm膜泡与环形片层及核被膜上核孔复合体形成的关系

将ＬａｍｂｄａＤＮＡ引入活化的非洲爪蟾卵提取物中，在由磷酸肌酸与磷酸肌酸激酶构成的ＡＴＰ再生系统的参与下，在这种非细胞体系中能够围绕由ＬａｍｂｄａＤＮＡ诱导形成的染色质重建核被膜结构，同时在染色质外出现类似核被膜结构的环形片层。在这两种膜结构中核孔复合体的形成都与直径２００ｎｍ左右的单层圆形小膜泡密切相关，这些小膜泡可以附着在染色质表面或独立于染色质之外相互融合成扁平囊状的双层膜片层，双层膜进一步融合形成核孔，与此同时，核孔复合体在核孔上完成装配。