A Pyropheophorbide Analogue Containing a Fused Methoxy Cyclohexenone Ring System Shows Promising Cancer-Imaging Ability

Herein we report the synthesis, photophysical properties, positron emission tomography (PET) imaging and photodynamic therapy (PDT) efficacy of methyl 3-(1′-m-iodobenzyloxy)ethyl-3-devinyl-verdin 4 (with or without the ¹²⁴I isotope). The PET imaging ability and ex vivo biodistribution of [¹²⁴I] 4 were compared with the well-studied methyl [3-(¹²⁴1′-m-iodobenzyloxy)ethyl]-3-devinyl-pyropheophorbide-a methyl ester (PET-ONCO or [¹²⁴I] 2 ) and [¹⁸F]fluorodeoxyglucose ([¹⁸F]FDG) in BALB/c mice bearing colon-26 tumors. Whole-body PET images of [¹²⁴I] 4 containing a fused methoxy cyclohexenone ring system showed excellent tumor contrast with time (72>48>24 h post-injection). Ex vivo biodistribution results indicate that relative to the current clinical standard [¹⁸F]FDG and [¹²⁴I] 2 in 2 % ethanol formulation, [¹²⁴I] 4 , at the same radioactive dose (25 μCi per mouse), showed higher tumor uptake at 24 h post-injection and longer tumor retention. In biological environments, compound 4 showed lower fluorescence and lower singlet oxygen yield than 2 , which is possibly due to higher aggregation caused by the presence of a fused cyclohexenone ring system, resulting in limited in vitro/in vivo PDT efficacy. Therefore, the chlorophyll-a analogue [¹²⁴I] 4 provides easy access to a novel PET imaging agent (with no skin phototoxicity) to image cancer types—brain, renal carcinomas, pancreas—in which [¹⁸F]FDG shows limitations.     

基于声发射和高斯混合模型的灰岩破裂特征识别研究

通过单轴压缩条件下灰岩破裂过程的声发射试验研究,利用高斯混合模型(GMM)对加载过程声发射信号波形特征进行深入分析,探索性识别灰岩破裂失稳过程的裂纹模式及其前兆特征。分析结果表明,灰岩在单轴加载过程中先后主要存在张拉和剪切两种破裂模式。其中,张拉破裂的声发射信号波形特征在AF-RA坐标空间呈现低A_F值、高R_A值分布;剪切破裂的声发射信号波形特征在AF-RA坐标空间呈现低R_A值、高A_F值,且随着应力的增加分布中心向A_F轴靠拢。GMM分析结果揭示了灰岩在整个应力加载过程中以张拉裂纹为主,在加载前中期几乎全为张拉裂纹,临近破坏阶段过渡到剪切破坏为主。剪切裂纹所占比例的最大值出现在(0.8～0.9)σ_c阶段,也是AF-RA坐标轴分布呈现最大A_F值时。研究结果可为预测早期灰岩破裂失稳提供参考,同时为深入研究识别岩石破裂失稳前兆信号特征提供了一种分析方法。     

Synthesis and Preliminary Evaluation of 11C-Labeled VU0467485/AZ13713945 and Its Analogues for Imaging Muscarinic Acetylcholine Receptor Subtype 4

Muscarinic acetylcholine receptors (mAChRs) have five distinct subunits (M₁–M₅) and are involved in the action of the neurotransmitter acetylcholine in the central and peripheral nervous system. Attributed to the promising clinical efficacy of xanomeline, an M₁/M₄-preferring agonist, in patients of schizophrenia and Alzheimer's disease, M₁- or M₄-selective mAChR modulators have been developed that target the topographically distinct allosteric sites. Herein we report the synthesis and preliminary evaluation of ¹¹C-labeled positron emission tomography (PET) ligands based on a validated M₄R positive allosteric modulator VU0467485 (AZ13713945) to facilitate drug discovery. [¹¹C]VU0467485 and two other ligands were prepared in high radiochemical yields (>30 %, decay-corrected) with high radiochemical purity (>99 %) and high molar activity (>74 GBq μmol⁻¹). In vitro autoradiography studies indicated that these three ligands possess moderate-to-high in vitro specific binding to M₄R. Nevertheless, further physiochemical property optimization is necessary to overcome the challenges associated with limited brain permeability.     

考虑节点过载的碳排放空间关联系统级联失效模型

为提高突发事件级联失效对现实碳排放关联系统破坏程度的评估可信性，在传统复杂网络的"负载-容量"级联失效模型基础上，考虑个体成员对负载的冗余能力，提出一种过载失效概率，构建了考虑节点过载状态的级联失效模型，并基于节点特性提出了6种过载节点负载分配策略。仿真结果表明：在过载节点负载分配策略中，综合分配策略整体上较优，能够有效控制级联失效的规模，增加网络鲁棒性；在一定范围内提升过载参数有助于降低级联失效的影响，但提升到一定程度时改善效果不明显；在不同负载分配策略下，剩余系数存在一个最优值，容量可调参数存在最优区间，可以使碳排放关联网络保持较好鲁棒性的同时，花费较小的构建成本，其中紧密度分配策略对应的网络构建成本较高。     

基于瓦斯涌出特征的钱家营矿掘进工作面突出预警系统应用

为实现钱家营矿掘进工作面煤与瓦斯突出实时预警,提出一种基于瓦斯涌出特征的预警方法。依据巷道高低浓度甲烷传感器实时监测数据,通过离散回归理论分析煤与瓦斯突出前的瓦斯涌出量,建立预警指标特征序列,确定掘进工作面煤与瓦斯突出预警指标危险临界值:方差0.018,波峰差0.41,波动斜率±0.027。在此基础上构建了非接触式煤与瓦斯突出可视化预警系统并在钱家营矿进行现场应用。结果表明,以瓦斯涌出特征值作为预警指标,能够准确监测到井下瓦斯异常现象,达到瓦斯数据实时解算和可视化预警的目的,为钱家营矿掘进工作面防突工作提供技术借鉴。     

阳泉矿区煤样不同应力状态下声发射特性分析

为探索原煤煤样的力学性能和不同应力状态下的声发射活动特性,对阳泉矿区新景矿、平舒矿主采煤层的煤样进行了单轴、三轴压缩和巴西劈裂的声发射试验,分析了2种煤样力学性能及不同加载过程的声发射活动规律。证明通过监测声发射(微震)活动分析煤样或煤岩体内部破坏状态是一种方便有效的手段。     

牵引车载荷对NOx排放和排温影响的试验研究

在五轴动力总成试验台架上对牵引车在不同载荷下进行同一路谱的排放试验,研究牵引车在不同载荷下NOx排放和排温的变化,得到载荷与排放物和选择性催化还原(selective catalytic reduction,SCR)上游排温的变化关系。结果表明:载荷为标定载荷的60%以下时,NOx比排放值与载荷基本呈线性相关;载荷超过标定载荷的75%时,NOx比排放值与载荷呈二次项相关;载荷在为标定载荷的23%以上时,NOx比排放值与SCR上游排温基本呈线性相关。利用该试验结论可以通过只进行单一载荷排放试验,判断车辆在其他载荷下的排放水平是否满足国家标准要求,并可通过载荷对排温的影响规律预判排放水平。     

基于车载排放法商用车排放影响因素研究

为研究商用车实际道路排放试验的影响因素,基于便携式排放测量系统(portable emission measurement system,PEMS)测试技术,进行多组车载排放试验。通过试验数据定性分析试验工况、整车速比、整车载荷、试验海拔等对整车PEMS测试结果的影响。研究表明,整车变速箱、后桥配置存在最佳速比匹配区间,稳定的驾驶工况有利于整车排放,高海拔地区排放变差,且高负荷工况恶化严重,整车载荷、空气湿度与排放结果呈负相关。并从排放检测试验过程、整车配置、整车ECU数据等方面对试验数据进行分析,确定试验条件变化影响整车后处理转化效率和发动机燃烧性能,导致发动机排放性能变化。     

Measurement of chemical emission rates from cigarette butts into air

This study examined airborne emissions from cigarette butts for styrene, 2-methyl-2-cyclopenten-1-one, naphthalene, triacetin, and nicotine. Ten experiments were conducted by placing butts in a stainless steel chamber and measuring the chemical concentrations in chamber air. Emission rates were determined from the concentrations. Triacetin and nicotine concentrations were roughly 50% of initial concentrations after 100 hours, while concentrations of other chemicals decayed to less than 10% of initial concentrations within 24 hours. Initial emission rates per cigarette butt ranged from 200 to 3500 ng h⁻¹. Triacetin and nicotine emission rates at 25°C were 1.6 to 2.2 times higher than the rates at 20°C, while the emission rates of other chemicals at 25°C were 1.1 to 1.3 times higher than the rates at 20°C only during the first sampling period. The chemical concentrations and emission rates at 30°C were comparable or lower than the values at 25°C, possibly due to different batches of cigarettes used. The 24-hours emitted mass of nicotine from a cigarette butt at 25°C could be up to 14% of the literature reported nicotine masses emitted from a burning cigarette.     

300MWCFB锅炉配套半干法烟气脱硫的汞排放试验研究

某300 MW循环流化床(CFB)锅炉采用炉内脱硫、SNCR、预电除尘器和烟气循环流化床半干法脱硫装置实现了超低排放。对不同工况下不同位置的烟气汞浓度和灰渣等固体副产物中的汞含量进行测试分析,研究结果表明:燃煤在循环流化床锅炉燃烧产生的汞主要以气态汞和颗粒汞形式存在;锅炉负荷提高,烟气中气态汞和颗粒汞浓度均有所提高,炉内脱硫对原始汞排放特性几乎没有影响;烟气循环流化床半干法脱硫装置可脱除71%～77%的气态汞和86%～88%的颗粒汞;采用预电除尘器与烟气循环流化床半干法脱硫结合的超低排放路线,总汞脱除率可达到82%～87%,使烟囱排放的汞浓度不高于1.5μg/m~3。副产物分析结果表明,烟气中脱除的汞主要富集于粉煤灰和半干法脱硫灰中。