Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9‐Epipolygodial against Drug‐Resistant Cancer Cells

Polygodial, a terpenoid dialdehyde isolated from Polygonum hydropiper L., is a known agonist of the transient receptor potential vanilloid 1 (TRPV1). In this investigation a series of polygodial analogues were prepared and investigated for TRPV1‐agonist and anticancer activities. These experiments led to the identification of 9‐epipolygodial, which has antiproliferative potency significantly exceeding that of polygodial. 9‐Epipolygodial was found to maintain potency against apoptosis‐resistant cancer cells as well as those displaying the multidrug‐resistant (MDR) phenotype. In addition, the chemical feasibility for the previously proposed mechanism of action of polygodial, involving the formation of a Paal–Knorr pyrrole with a lysine residue on the target protein, was demonstrated by the synthesis of a stable polygodial pyrrole derivative. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives. These compounds should inspire further work in this area aimed at the development of new pharmacological agents, or the exploration of novel mechanisms of covalent modification of biological molecules with natural products.     

基于FPGA的多路视频通道控制

根据织布机告警系统的需求,提出一种开关设计思想,阐述开关设计过程中遇到的问题以及解决方法。首先在FPGA中设计一个开关控制信号,利用这个信号结合双口RAM中的编码数据识别两个拨动开关状态．从而达到控制多路视频通道的目的,使本告警系统更方便的应用于实际工业中。介绍整个控制系统的工作原理,给出硬件结构图和软件设计过程,然后利用QnartusⅡ中的SignalTapⅡLogic Analyzer工具对控制信号进行实时采样分析．最后在织布机告警系统中成功实现视频通道控制功能。     

卫星信道中高阶APSK调制的非线性失真补偿算法

针对高阶APSK调制在卫星信道中存在有记忆非线性失真的现象,提出一种联合补偿算法,该算法充分利用APSK调制信号星座图的特点,在大幅度减小无记忆数据预失真计算量的基础上,联合非线性均衡实现对有记忆非线性卫星信道的自适应补偿.其优点是存储量和计算复杂度随调制阶数的增加变化很小.仿真结果表明,该算法能够达到有记忆数据预失真的补偿性能,且最佳工作点提高0.2 dB.     

基于零点消除的无线OFDM系统 信道缩短均衡器

针对无线信道的有限冲激响应及其全零点特性,本文设计了一种基于零点消除的无线正交频分复用(OFDM)系统信道缩短均衡器,该均衡器利用零点消除的方式有效地缩短信道时延扩展长度,并采用反馈滤波器的形式来实现无限冲激响应滤波器,该方案不仅降低了信道缩短均衡器算法的复杂度,而且也大大简化了无线OFDM系统的设计与实现.仿真结果验证了上述方案和算法的有效性.     

NOC路由节点VLSI设计

基于wormhole交换策略和目的地址确定性路由算法,采用三级流水线的结构实现了片上网络中的路由节点.该路由节点适用于Mesh和Torus拓扑,并采用虚通道技术增加吞吐量.在Xilinx的FPGA上实现后可知,该路由节点最高可工作在130MHz的时钟频率上,传输带宽为20.8Gb/s.     

Ablation behaviour of Csf/ZrB2-SiC composites fabricated by direct ink writing and reactive melt infiltration

Pitch-based short carbon fibres reinforced C_sf/ZrB₂-SiC composites were fabricated by direct ink writing of short carbon fibres, followed by slurry impregnation and reactive melt infiltration. Ablation behaviour of the C_sf/ZrB₂-SiC composite was studied by air plasma test. It is indicated that the skeleton of the oriented short carbon fibres provides heat diffusion channels. Consequently, temperatures at the ablation surface are as low as ∼1730 ^oC and ∼2000 ^oC respectively at 4 MW/m² and 5 MW/m². The composite presents outstanding ablation-resistant performance with a linear recession rate of ∼ − 0.04 µm/s and mass recession rate of ∼ − 3.40 mg/s at 4 MW/m², ∼ − 0.17 µm/s and ∼ 3.58 mg/s at 5 MW/m². It is revealed that the fibres area and matrix area of the composite present different ablation mechanisms. The fibres area is ablated severely, while the matrix area presents excellent ablation-resistance with continuous ZrO₂-SiO₂ protective layer.     

Fabrication of powder components with internal channels by spark plasma sintering and additive manufacturing

A novel method of producing complex ceramic and metallic parts with designed internal channels is developed. The method utilizes a combination of the additive manufacturing technique of solvent jetting and spark plasma sintering (SPS.) The developed manufacturing approach brings benefits in producing complex shapes with internal channels. Along with geometric customization of the 3D printed mold, a major advantage of this method is the removal of the need for a long debinding process, usually necessary with other 3D printing methods, by using the SPS. High density ceramic and metallic complex parts with internal channels were successfully produced with close to theoretical densities. The conducted studies include the development of a model that can predict the evolution and/or distortions of the complex-shaped powder assembly during the sintering process. The model is based on the continuum theory of sintering formulations embedded in a finite element code.     

基于巴特沃思滤波器的纸张定量信号处理

针对纸张定量在线检测信号受“温漂”噪声影响稳定性差、补偿效果不理想的问题,从定量检测原理出发对噪声干扰源及主要耦合通道进行了时-频域分析和研究,并根据定量信号和噪声不同的频谱分布规律,构造了相应的巴特沃思滤波器处理定量信号。     

Expanding the Genetic Code in Xenopus laevis Oocytes

Heterologous expression of ligand‐gated ion channels (LGICs) in Xenopus laevis oocytes combined with site‐directed mutagenesis has been demonstrated to be a powerful approach to study structure–function relationships. In particular, introducing unnatural amino acids (UAAs) has enabled modifications that are not found in natural proteins. However, the current strategy relies on the technically demanding in vitro synthesis of aminoacylated suppressor tRNA. We report here a general method that circumvents this limitation by utilizing orthogonal aminoacyl‐tRNA synthetase (aaRS)/suppressor tRNA_CUA pairs to genetically encode UAAs in Xenopus oocytes. We show that UAAs inserted in the N‐terminal domain of N‐methyl‐D ‐aspartate receptors (NMDARs) serve as photo‐crosslinkers that lock the receptor in a discrete conformational state in response to UV photo treatment. Our method should be generally applicable to studies of other LGICs in Xenopus oocytes.     

Optogenetics Comes of Age: Novel Inhibitory Light‐Gated Anionic Channels Allow Efficient Silencing of Neural Function

Optogenetics, the developing field of research that uses light‐switchable biochemical tools in a sophisticated technological approach to monitor or control neural function, is rapidly evolving with the discovery and development of novel microbial rhodopsins. Light‐absorbing membrane proteins, as tools for brain research, are promoting new applications within the discipline of optogenetics. Light‐gated rhodopsin ion channels with better intrinsic light sensitivity and improved resolution are needed to overcome some of the current limitations of existing molecules. The recent discovery of light‐gated inhibitory anion channels opens new opportunities for studying physiological neural processes and, at the same time, represent a powerful approach for elucidating the mechanisms of neurological and mental disorders that could benefit from this approach.