（S）-噻吗洛尔半水合物的合成及表征

为了开发β受体阻断剂新药（S）-噻吗洛尔半水合物，采用3-吗啉-4-氯-1，2，5-噻二唑为起始原料，经水解反应得到中间体1（3-吗啉-4-羟基-1，2，5-噻二唑）。中间体1与R-环氧氯丙烷发生醚化反应，经后处理及重结晶得到中间体2 {（R）-4-［4-（环氧乙烷-2-基甲氧基）-1，2，5-噻二唑-3-基］吗啉}。中间体2经胺化反应、马来酸成盐及重结晶得到（S）-马来酸噻吗洛尔。（S）-马来酸噻吗洛尔经游离、纯水转晶得到符合药典标准的（S）-噻吗洛尔半水合物，总收率14.05%且e.e.值为99.66%。最终成品经IR、1H-NMR、13C-NMR、MS、TGA、DSC表征，并优化各步反应条件。结果表明:以三乙胺为醚化反应缚酸剂75 ℃反应最佳；以乙醇为胺化反应溶剂46 ℃反应16 h最佳；S-噻吗洛尔的转晶拆分以水作溶剂，比传统不对称合成工艺安全稳定，操作简单，适合工业化生产。     

陕南山地烟田不同植烟年限土壤养分的变化

为给陕南山地烟草生产布局及有针对性的施肥措施提供依据,分析了陕南山地烟田不同植烟年限(0~15年)与土壤养分含量的关系。结果表明:随着植烟年限延长,有机质线性下降,全氮和速效钾显著上升,有效磷先上升后下降;氯、有效铁、有效锰、有效硼和有效铜无显著变化或变化很小,有效锌则在第1年急剧下降,之后保持稳定,10年后再次显著下降。认为陕南山地烟区烟叶生产中应适当增加有机肥的施用而合理控制氮肥、磷肥和钾肥的施用,并要注意锌肥的补充。     

Combination of heat treatment and chitosan coating to improve postharvest quality of wolfberry (Lycium barbarum)

The synergistic application of hot water dip at 42 °C for 30 min and 1% chitosan coating on differentiation in postharvest quality traits, microstructure as well as microbiological evolution of wolfberry fruits was investigated. Fresh wolfberry fruits were stored at 2 ± 0.5 °C and 90% relative humidity (RH) for 28 days. Results indicated the combination of prestorage heat treatment and chitosan coating maintained higher levels of ascorbic acid, total phenolic contents and antioxidant capacity as well as lower decay, compared with untreated wolfberry fruits. The possible mechanism was that the heat treatment almost sealed open stomata to limit the sites of pathogen penetration into fruits independently, followed by the biofilm formed by chitosan which controlled secondary infections as well as slowed changes in fruit respiration and metabolic activity in wolfberries. The synergistically treated fruit also exhibited a higher acceptability obtained by sensory analysis after cold storage. In this sense, the integrated application of heat treatment and chitosan coating could be regarded as an effective strategy to extend storage life and maintain the postharvest quality of wolfberry fruits.     

Metal-polyphenol-network coated CaCO3 as pH-responsive nanocarriers to enable effective intratumoral penetration and reversal of multidrug resistance for augmented cancer treatments

Construction of multifunctional stimuli-responsive nanotherapeutics enabling improved intratumoral penetration of therapeutics and reversal of multiple-drug resistance (MDR) is potent to achieve effective cancer treatment. Herein, we report a general method to synthesize pH-dissociable calcium carbonate (CaCO₃) hollow nanoparticles with amorphous CaCO₃ as the template, gallic acid (GA) as the organic ligand, and ferrous ions as the metallic center via a one-pot coordination reaction. The obtained GA–Fe@CaCO₃ exhibits high loading efficiencies to both oxidized cisplatin prodrug and doxorubicin, yielding drug loaded GA–Fe@CaCO₃ nanotherapeutics featured in pH-responsive size shrinkage, drug release, and Fenton catalytic activity. Compared to nonresponsive GA–Fe@silica nanoparticles prepared with silica nanoparticles as the template, such GA–Fe@CaCO₃ confers significantly improved intratumoral penetration capacity. Moreover, both types of drug-loaded GA–Fe@CaCO₃ nanotherapeutics exhibit synergistic therapeutic efficacies to corresponding MDR cancer cells because of the GA–Fe mediated intracellular oxidative stress amplification that could reduce the efflux of engulfed drugs by impairing the mitochondrial-mediated production of adenosine triphosphate (ATP). As a result, it is found that the doxorubicin loaded GA–Fe@CaCO₃ exhibits superior therapeutic effect towards doxorubicin-resistant 4T1 breast tumors via combined chemodynamic and chemo-therapies. This work highlights the preparation of pH-dissociable CaCO₃-based nanotherapeutics to enable effective tumor penetration for enhanced treatment of drug-resistant tumors.

     

面向航空通信应用的边沿触发器教学设计

研究和分析了面向航空通信应用的边沿触发器教学设计。以边沿触发电路实现原理为核心,引导边沿触发机制的探究式学习；以航空机载网络通信为具体应用背景,引入科学研究和工程实现中实际问题,设计曼切斯特码检测系统实验；使得边沿触发器教学成为“知识再创造”的过程和创新实践的新载体,以期培养新工科背景下的独立、创新和实践精神。     

改进HSR-FCN的服装图像识别分类算法研究

目前网络上的服装图像数量增长迅猛，对于大量服装图像实现智能分类的需求日益增加。将基于区域的全卷积网络（Region-Based Fully Convolutional Networks，R-FCN）引入到服装图像识别中，针对服装图像分类中网络训练时间长、形变服装图像识别率低的问题，提出一种新颖的改进框架HSR-FCN。新框架将R-FCN中的区域建议网络和HyperNet网络相融合，改变图片特征学习方式，使得HSR-FCN可以在更短的训练时间内达到更高的准确率。在模型中引入了空间转换网络，对输入服装图像和特征图进行了空间变换及对齐，加强了对多角度服装和形变服装的特征学习。实验结果表明，改进后的HSR-FCN模型有效地加强了对形变服装图像的学习，且在训练时间更短的情况下，比原来的网络模型R-FCN平均准确率提高了大约3个百分点，达到96.69%。