Drug self-assembly: A phenomenon at the nanometer scale with major impact in the structure–biological properties relationship and the treatment of disease

Under water-rich conditions, small amphiphilic and hydrophobic drug molecules self-assemble into supramolecular nanostructures. Thus, substantial modifications in their interaction with cellular structures and the ability to reach intracellular targets could happen. Additionally, drug aggregates could be more toxic than the non-aggregated counterparts, or vice versa. Moreover, since self-aggregation reduces the number of effective “monomeric” molecules that interact with the target, the drug potency could be underestimated. In other cases, the activity could be ascribed to the non-aggregated molecule while it stems from its aggregates. Thus, drug self-assembly could mislead from drug throughput screening assays to advanced preclinical and clinical trials. Finally, aggregates could serve as crystallization nuclei. The impact that this phenomenon has on the biological performance of active compounds, the inconsistent and often controversial nature of the published data and the need for recommendations/guidelines as preamble of more harmonized research protocols to characterize drug self-aggregation were main motivations for this review. First, the key molecular and environmental parameters governing drug self-aggregation, the main drug families for which this phenomenon and the methods used for its characterization are described. Then, promising nanotechnology platforms investigated to prevent/control it towards a more efficient drug development process are briefly discussed.     

基于溢流环换能器液腔的水听器校准系统

针对溢流环换能器液腔振动表现出的优秀低频特性,提出利用溢流环换能器液腔内部声场进行低频校准的校准方法。首先分析了溢流环换能器液腔特性,并在现有刚性罐体的基础上,构造出了一套无须激振台,以溢流环换能器为低频声源,溢流环换能器液腔为两端开口振动液柱的低频比较法校准系统。通过实验测量确定了液柱高度为15 cm处的圆心位置为最佳的比较法测量点,实验测试该点在100~1400 Hz频段的径向声压变化不超过5%。对Ф20 mm球型水听器进行比较法测量,在100~1000 Hz频段的测量结果与标准校准结果最大偏差为0.8 dB,测量不确定度为1 dB。结果表明,以溢流环液腔为基础构造的低频校准系统是可行的。     

不同缓冲材料的堆码包装振动特性分析

目的 研究物流运输中采用不同缓冲材料的堆码包装件的振动特性。方法 以缓冲材料聚乙烯泡沫(EPE)和聚苯乙烯泡沫(EPS)为研究对象,采用三维建模软件SoildWorks和有限元仿真软件Workbench建立有限元模型进行模态与谐响应分析,结合扫频振动试验和随机振动试验对各层堆码件的振动响应特性进行分析。结果 2类包装件共振频率处的第一激励能量都大于第二激励能量,振动幅值随层数增加而升高。EPE包装件第一和第二共振频率的激励能量占比分别为35.7%和3%,EPS包装件第一和第二共振频率的激励能量占比分别为26.8%和16.8%。EPE包装件共振区域主要分布于15～40 Hz,而EPS包装件共振频率区域分布于15～40 Hz和60～80 Hz。三层堆码件的中上层包装件受第一共振频率控制,EPS材料的底层包装件受多个共振频率影响,EPE材料的底层包装件受到第二共振频率控制。结论 经过循环载荷作用后的EPE的吸振缓冲性能优于EPS的。通过试验与有限元仿真数据绘制了相应的防振性能曲线,同时验证了有限元仿真的可靠性。这为堆码产品选择不同缓冲材料组合提供了的理论指导。     

铝合金曲轴后端盖压铸模浇注与排溢系统优化设计

为满足某发动机曲轴后端盖铸件高质量的外观与密封要求,针对该铝合金零件进行了高压铸造模具的浇注与排溢系统优化设计。首先根据铸件形貌和尺寸特征进行浇道、内浇口和排溢槽的理论设计,随后采用ProCAST软件模拟高压铸造充型、凝固过程,对铸件的卷气、缩松、缩孔及组织进行预测分析。研究发现,方案1的平直型横浇道浇注方案,金属液冲击型芯容易产生紊流和飞溅,且设置在铸件中间和下部的排溢系统不能减少紊流,易形成裹气和大的缩孔缺陷;而方案2为钳形浇道,去除方案1铸件中部的溢流槽并将下部连通溢流槽改为两个,明显改善铸件内裹气和缩孔现象,确定方案2为最终方案。试模铸件外观质量良好,经X射线探伤发现铸件无裂纹,厚大缩孔位置与缺陷仿真预测良好吻合;金相显微镜(OM)、扫描电镜(SEM)和电子背散射衍射(EBSD)观察组织发现,铸件晶粒细小、组织致密,晶粒取向差小,内部应力小,与组织和应力仿真结果一致;能谱分析(EDS)、X射线衍射(XRD)分析表明,铸件成分均匀,组织内部无杂质。本研究可为端盖类铝合金压铸件模具及工艺开发提供参考。     

强酸强碱溶液“缓冲容量”的讨论

本文从缓冲微分方程式说明强酸、强碱溶液具有缓冲能力,并且比同总浓度的由共轭酸碱对组成的缓冲溶液的缓冲容量大。     

使用固态硬盘管理主存KV数据库的虚拟内存

主存键值(key-value,KV)数据库具有高效性、易用性和可扩展性.由于主存容量有限,一些数据量较大的应用必须使用磁盘进行数据交换.而固态硬盘(solid state disk,SSD)有高速的随机读特点,使用固态硬盘作为主存KV数据库的虚拟内存会提高对不在主存中的数据的读性能.但是固态硬盘的随机写性能较差,于是提...     

Protecting Against Address Space Layout Randomisation （ASLR） Compromises and Return-to-Libc Attacks Using Network Intrusion Detection Systems

Writable XOR executable (W⊕X) and address space layout randomisation (ASLR) have elevated the understanding necessary to perpetrate buffer overflow exploits[1]. However, they have not proved to be a panacea[1–3], and so other mechanisms, such as stack guards and prelinking, have been introduced. In this paper, we show that host-based protection still does not offer a complete solution. To demonstrate the protection inadequacies, we perform an over the network brute force return-to-libc attack against a preforking concurrent server to gain remote access to a shell. The attack defeats host protection including W⊕X and ASLR. We then demonstrate that deploying a network intrusion detection systems (NIDS) with appropriate signatures can detect this attack efficiently.     

以太网交换控制芯片的缓存结构

为实现交换控制,需要为以太网交换控制芯片选择合理的数据缓存结构。采用数据包缓存空间的分页管理模式、空闲缓存空间的调度方法和出口端口队列管理技术,通过数据包缓存空间描述符设计方法和对应的目的端口结构分析,提高交换控制芯片缓存空间的使用效率并增强芯片性能。     

用于缓冲区生成的随机算法

缓冲区分析是GIS中重要的空间分析方法之一。针对现有方法处理大数据量矢量地图时的低效率问题,提出一种易于并行处理和编程实现的缓冲区生成的随机算法,并设计适用于多种形式的应用模式,以适应缓冲区分析普适性应用。采用舍伍德随机算法优化计算效率,利用可伸缩矢量图形遮罩对象解决可视化问题。测试结果证明,该算法可以提高大数据集的处理效率。     

基于DSP和VDK内核的USB通信系统

针对ADSP-TS201 DSP的USB通信需求,设计一个完整的USB通信系统,其中,硬件系统采用CY7C68013A USB控制器和FPGA扩展USB主机接口,软件系统引入VDK实时内核、消息函数注册机制和数据缓冲队列。该通信系统可以提高USB通信资源的利用率,提供友好的通信接口,便于应用程序调用。