Rapid Synthesis and Antiproliferative Properties of Polyazamacrocycle-Based Bi- and Tetra-Gold(I) Phosphine Dithiocarbamate Complexes

A family of bi- and tetrametallic gold(I) phosphine dithiocarbamate complexes were synthesized, starting from cyclam and dimethylcyclam polyazamacrocycles, respectively, along with their monometallic gold(I) chloridophosphine precursors. Their antiproliferative properties were evaluated on two cancer cell lines (A549 and NSCLC-N6-L16). Most of the mono- and bimetallic complexes displayed strong activities and, in particular, one bimetallic derivative showed antiproliferative properties in the low micromolar range. Insights into the structure–activity relationships are given, along with determination of the thioredoxin reductase inhibition potential, two-photon imaging of the fluorescent derivatives, and evaluation of gold uptake.     

18F-NaF注射液的制备及新西兰兔骨折显像

由外伤或肿瘤骨转移造成的隐匿性骨折和愈合情况的准确诊断对制定合适的治疗方案具有非常重要的意义。为考查¹⁸F-NaF PET显像用于骨折诊断的诊断效能，本研究制备了¹⁸F-NaF注射液，并对其进行了质量控制和稳定性研究，然后建立新西兰兔骨折动物模型，模型建立约2周后进行了¹⁸F-NaF PET显像和⁹⁹Tc^m-亚甲基二磷酸盐（⁹⁹Tc^m-MDP）SPECT显像的自身对照实验，并对显像效果进行了比较。结果表明：¹⁸F-NaF的产量大于37 GBq，各项检验结果均符合质控要求，40 ℃下放置8 h和30 ℃下放置10 h所有检验结果均无明显变化；¹⁸F-NaF PET和⁹⁹Tc^m-MDP SPECT两种显像方式均可见全身骨骼，骨折部位呈明显放射性浓聚，但¹⁸F-NaF给药后30 min即可进行PET显像，骨折部位显示更为清晰，骨折部位与对侧正常骨骼的放射性摄取比（T/NT）明显高于⁹⁹Tc^m-MDP，而⁹⁹Tc^m-MDP需在给药后2 h才能进行SPECT显像。本研究表明¹⁸F-NaF PET对骨折的显像性能优于⁹⁹Tc^m-MDP，可明显提高检查流通量和诊断效能。     

Covalently Assembled Dipeptide Nanoparticles with Adjustable Fluorescence Emission for Multicolor Bioimaging

Peptide self-assembly, inspired by the naturally occurring fabrication principle, remains the most attractive in constructing fluorescent nanoagents towards bioimaging. However, the noncovalent interactions that drive peptide self-assembly are usually susceptible to the complex physiological environment; thus leading to disassembly and dysfunction of fluorescent nanoagents. Herein, a covalently crosslinked assembly strategy for fabrication of stable peptide-based nanoparticles with adjustable emission is introduced. In the process of cationic diphenylalanine peptide (H-Phe-Phe-NH₂ ⋅ HCl) self-assembly, glutaraldehyde is used as a crosslinker and the resulting product of the Schiff base reaction can be fluorescent. More importantly, the emission wavelength can be readily tuned by controlling the covalent reaction time. It has been demonstrated that the nanoparticles are stable, even after intracellular uptake, and can be used for sustainable multicolor fluorescent imaging. The strategy with integrating peptide self-assembly and covalent crosslinking could be promising for the design and engineering of functional fluorescent nanoparticles with robust physiological stability and adjustable emission towards improved bioimaging applications.     

A Versatile Theranostic Nanoemulsion for Architecture‐Dependent Multimodal Imaging and Dually Augmented Photodynamic Therapy

To design a clinically translatable nanomedicine for photodynamic theranostics, the ingredients should be carefully considered. A high content of nanocarriers may cause extra toxicity in metabolism, and multiple theranostic agents would complicate the preparation process. These issues would be of less concern if the nanocarrier itself has most of the theranostic functions. In this work, a poly(ethylene glycol)‐boron dipyrromethene amphiphile (PEG‐F₅₄‐BODIPY) with 54 fluorine‐19 (¹⁹F) is synthesized and employed to emulsify perfluorohexane (PFH) into a theranostic nanoemulsion (PFH@PEG‐F₅₄‐BODIPY). The as‐prepared PFH@PEG‐F₅₄‐BODIPY can perform architecture‐dependent fluorescence/photoacoustic/¹⁹F magnetic resonance multimodal imaging, providing more information about the in vivo structure evolution of nanomedicine. Importantly, this nanoemulsion significantly enhances the therapeutic effect of BODIPY through both the high oxygen dissolving capability and less self‐quenching of BODIPY molecules. More interestingly, PFH@PEG‐F₅₄‐BODIPY shows high level of tumor accumulation and long tumor retention time, allowing a repeated light irradiation after a single‐dose intravenous injection. The “all‐in‐one” photodynamic theranostic nanoemulsion has simple composition, remarkable theranostic efficacy, and novel treatment pattern, and thus presents an intriguing avenue to developing clinically translatable theranostic agents.     

基于自回归谱外推的全聚焦成像分辨力提升

针对相邻缺陷全聚焦超声成像混叠问题，结合低阶、宽有效频带自回归谱外推方法，压缩超声波时域脉冲宽度，实现亚波长级全聚焦（Total focusing method，TFM）成像分辨力。建立碳钢试块模型，设置两个中心间距1.8 mm，直径1.3 mm圆孔，选用中心频率2.25 MHz，32阵元相控阵探头采集全矩阵数据。针对全矩阵数据，选择自回归阶数为2，信号频谱最大幅值下降14 dB为有效频带，建立自回归模型并外推有效频带外的高频与低频成分，随后对全矩阵数据进行延迟叠加处理和TFM成像。仿真结果表明，低阶、宽有效频带自回归谱外推处理方法具有较高的鲁棒性和准确性，TFM成像后可有效分离中心间距0.7λ（λ为超声波长）圆孔，保留缺陷横向位置信息的同时，定位误差不超过0.73%。对碳钢试块中相同位置及尺寸的圆孔进行试验验证，定位误差不超过1.06%，有效地提高TFM成像分辨力。     

激光立体成形TC4钛合金的热力场演化

激光立体成形能够实现高性能复杂零件的精确成形，但成形过程中的高温度梯度极易导致残余应力和变形，最终影响构件的几何精度和力学性能。通过搭建基板单边夹持原位热变形测量系统，探究了多道多层TC4钛合金成形件在激光立体成形过程中基板温度、变形的演化规律，分析了不同扫描策略对构件热应力场的影响。研究结果表明，构件的变形发展受其热历史驱使，扫描策略对成形件的热变形具有显著影响。     

老矿山残矿资源回收方案设计中三维探测及建模技术的应用

目前我国绝大多数中小型老矿山残矿回收面临一系列问题，包括资料缺失无法准确判定老采空区及剩余资源位置，无法准确掌握剩余资源形态及可回收量，回收方案设计与实际资源相差较大等。通过将三维探测及建模技术应用于老矿山残矿资源精准定位及回收方案设计中，有助于解决以上问题。以福建浦城屏峰硫铅锌矿为例，通过对老采空区采用三维激光扫描构建采空区三维模型，结合三维建模计算，构建了目前可回收的剩余资源三维模型。通过模型划分及切割，按照矿体实际形态，在三维模型中布设采切及穿孔工程，并将其导入平面施工图中，不仅可以减少设计工作量，而且能够精准匹配矿体，减少设计偏差。由于周边存在大量老采空区，为保障安全，在采空区及剩余资源精准三维模型的基础上，制定了采空区稳定性监测方案，布设了监测传感器，保障了资源回收安全。     

Mapping haze-komi on rice koji grains using β-glucuronidase expressing Aspergillus oryzae and mass spectrometry imaging

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