Discovery of Heterocyclic Nonacetamide Synaptic Vesicle Protein 2A (SV2A) Ligands with Single‐Digit Nanomolar Potency: Opening Avenues towards the First SV2A Positron Emission Tomography (PET) Ligands

The role of the synaptic vesicle protein 2A (SV2A) protein, target of the antiepileptic drug levetiracetam, is still mostly unknown. Considering its potential to provide in vivo functional insights into the role of SV2A in epileptic patients, the development of an SV2A positron emission tomography (PET) tracer has been undertaken. Using a 3D pharmacophore model based on close analogues of levetiracetam, we report the rationale design of three heterocyclic non‐acetamide lead compounds, UCB‐A, UCB‐H and UCB‐J, the first single‐digit nanomolar SV2A ligands with suitable properties for development as PET tracers.     

Deep‐black‐coloring effect of fabrics made of noncircular cross‐section polyester filaments

The effects of noncircular cross‐section (NCCS) poly ethylene terephthalate (PET) filaments and its shape factor on deep‐black‐coloring of dyed fabrics were investigated by comparing to that of the circular cross‐section PET ones. Indexes such as K/S, L* and Integ values were used for characterizing the deep‐black‐coloring effect on fabrics. The results indicated that fabrics made with NCCS PET filaments exhibited good deep‐black‐coloring effects. The calculated shape factor of the NCCS PET fiber had a significant correlation with the degree of deep‐black‐coloring exhibited by the fabric made from the fibers. A qualitative optical analysis of the NCCS PET fibers was carried out to explain the causes of the deep‐coloring of the NCCS fibers. This analysis implies that the contours of the NCCS fiber composed of surfaces with varied curvature increase the scattering of light by lowering specular reflection and increasing interior reflected and refracted light. This, in turn, strengthens the deep‐coloring effect. © 2013 Wiley Periodicals, Inc. Col Res Appl, 39, 511–518, 2014     

纳米TiQ/炭黑改性PET织物及其导电与光活性的表征

对聚对苯二甲酸乙二醇酯(PET)织物进行碱性水解预处理.通过浸渍法以十二烷基硫酸钠作为分散剂在原始的和经预处理的PET中加入纳米炭黑(CB1515和CB156),纳米二氧化钛(NTO)-NCBs(CB1515或CB156)混合物.以柠檬酸(CA)和次磷酸钠(SHP)分别为交联剂和催化剂,分别在预处理前后的PETs中加入NTO+CB1515和NTO+CB156作对比研究.结果表明,CB156比CB1515更能有效地降低样品的电阻率.加入NTO后,由原始PET所制样品比预处理PET所制样品具有更低的电阻率.然而,这与不加NTO所制样品结果相反.通过增加添加量和改善NCBs和NTO在织物中的分散均匀性,采用CA和SHP可明显降低样品的电阻率.发现NCBs与NTO的协同效应可提高预处理织物的紫外吸收.由原始PET中加入NCB和NTO所制样品比预处理的PET对亚甲基蓝降解具有更高活性.通过添加NTO或CA-SHP可提高活性,前者比后者更有效.     

Antibody-Based Tracers for PET/SPECT Imaging of Chronic Inflammatory Diseases

Chronic inflammatory diseases are often progressive, resulting not only in physical damage to patients but also social and economic burdens, making early diagnosis of them critical. Nuclear medicine techniques can enhance the detection of inflammation by providing functional as well as anatomical information when combined with other modalities such as magnetic resonance imaging, computed tomography or ultrasonography. Although small molecules and peptides were mainly used for the treatment and imaging of chronic inflammatory diseases in the past, antibodies and their fragments have also been emerging for chronic inflammatory diseases as they show high specificity to their targets and can have various biological half-lives depending on how they are engineered. In addition, imaging with antibodies or their fragments can visualize the in vivo biodistribution of the probes or help monitor therapeutic responses, thereby providing physicians with a greater understanding of drug behavior in vivo and another means of monitoring their patients. In this review, we introduce various targets and radiolabeled antibody-based probes for the molecular imaging of chronic inflammatory diseases in preclinical and clinical studies. Targets can be classified into three different categories: 1) cell-adhesion molecules, 2) surface markers on immune cells, and 3) cytokines or enzymes. The limitations and future directions of using radiolabeled antibodies for imaging inflammatory diseases are also discussed.     

Effect of recycled content and rPET quality on the properties of PET bottles,part II: Migration

Polyethylene terephthalate (PET) bottles were produced from three types of recycled PET (rPET) with four levels of recycled content. The migration of substances from these bottles to water was studied. Several migrated substances were detected. The migrated amounts of acetaldehyde and ethylene glycol complied with the limits given in the food contact material (FCM) legislation. Migration of 2-methyl-1,3-dioxolane was below the limit of 10 μg·L⁻¹, which is conventionally applied for non-intentionally added substances (NIAS) not classified as ‘carcinogenic’, ‘mutagenic’ or ‘toxic to reproduction’ (CMR). Limonene, acetone, butanone and furan were also detected as migrants, of which limonene is a natural fragrant, and the other three are probably residues from solvents used to clean and protect the mould at the small-scale production facility. Finally, benzene and styrene were also found as migrants from rPET. These migrants appear to originate from heat-induced reactions within the PET matrix, which involve contaminants. The formation of benzene in rPET is attributed to polyvinylchloride as contaminant. The migrated amounts of benzene from the PET bottles with recycled content to the water simulant are relatively small (0.03–0.44 μg·L⁻¹) after 10 days at 40°C. Consequently, the margin of exposure is 3.10⁵–8.10⁶. Hence, the level of concern for the public health is low, and the migrated amount represents a low priority for risk management. The FCM legislation demands a risk assessment for migrating NIAS. Depending on the underlying data and exposure scenario, different threshold limits in the food can be derived which can still be considered as safe.     

Synthesis of 16-Epiestriol and its Radiolabeling Procedure

To explore novel synthetic routes of 16-epiestriol (Estra-1, 3, 5(10)-triene-3, 16β, 17β-triol), we used the estrone as the starting material. After some simple synthetic steps, 16-epiestriol was yielded. Identification and purity of intermediates in the synthetic routes were characterized by melting point and ¹H NMR spectrum analysis, respectively. In addition, the structure of 16-epiestriol was modified and radiolabeled with¹⁸F-fluoride to yield¹⁸F-FES. The corresponding quality control analysis of the injection were performed. The yield of two synthetic routes of 16-epiestriol were about 20% starting from estrone. Radiosynthesis of¹⁸F-FES was finished in 60 minutes with a radiochemical yield of (30±4)% and radiochemical purity greater than 99%. The¹⁸F-FES injection was colorless and clear and the pH value was 6.5-7.5. The specific activity of the injection saline was (1.75±0.25) Ci/μmol. In this study, 16-Epiestriol was yielded with a relatively high yield in two novel routes.¹⁸F-FES was finally yielded after structure modification of 16-epiestriol and the corresponding radiolabeling procudure. The quality control results of the¹⁸F-FES injection could meet the need in clinical examination.     

Dynamic viscoelasticity and molecular orientation in uniaxially drawn PC/PET blends

The dependence of dynamic viscoelasticity on molecular orientation of the hot-drawn polycarbonate (PC)/poly(ethylene terephthalate) blends was studied experimentally. The oriented states of samples were investigated by wide-angle X-ray diffraction and quantified by Hermans' factor. The viscoelasticity was probed by dynamic mechanical analysis. For the fitting curves of dynamic modulus versus orientation, the PC-rich blends with different compositions had an opposite concavity and convexity compared with the neat PC. The difference revealed the influence of molecular mobility on orientation and viscoelasticity. The assumption on the phase morphological change from sea-island to local sandwich-like structure in blends was proposed and used to interpret the variation of slope of fitting curves. The relationship between orientation and viscoelasticity was observed in PC-rich blends, which can help understand the mechanism of molecular orientation and develop the constitutive relations for simulation. © 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136, 47514.     

酯化釜设备故障时的工艺控制

介绍了酯化釜设备故障情况,如酯化釜液位计故障,酯化反应泵机封EG内漏及对生产的影响。指出了在故障情况下稳定生产的对策,包括利用相关工艺点变化间接控制酯化二室液位及酯化机封泄露时羧基的控制。     

The use of SVM-FFA in estimating fatigue life of polyethylene terephthalate modified asphalt mixtures

To predict fatigue life of Polyethylene Terephthalate (PET) modified asphalt mixture, various soft computing methods such as Genetic Programming (GP), Artificial Neural Network (ANN), and Fuzzy Logic-based methods have been employed. In this study, an application of Support Vector Machine Firefly Algorithm (SVM-FFA) is implemented to predict fatigue life of PET modified asphalt mixture. The inputs are PET percentages, stress levels and environmental temperatures. The performance of proposed method is validated against observed experiment data. The results of the prediction using SVM-FFA are then compared to those of applying ANN and GP approach and it is concluded that SVM-FFA leads to more accurate results when compared to observed experiment data.     

Numerical simulation of the wire‐pinning process in PET film casting: Steady‐state results

Poly(ethylene terephthalate) (PET) film casting involves melt flow through a slot die, across a small span, and onto a fast moving quench drum. In the “wire‐pinning” casting process, a thin electrified wire close to the line of contact with the drum creates a strong pinning force that delays air entrainment to higher line speeds. Nonuniform wetting of the die lips by the extruded melt is thought to be responsible for the formation of streaks, a defect in the machine direction. A finite element model of the film casting process with wire pinning was developed to assist in understanding what causes significant wetting of the lips and whether this can be avoided by electrostatic pinning. The solution of the governing equations provide the location of the static and dynamic contact lines, thus finding the wetting and pinning points in the process. The simulations investigate the sensitivity of the static wetting line locations on the die lands to the imposed values of static contact angle and die‐lip gap. It was found that while the contact angle has a small effect on the extent of die‐lip wetting within the parameter ranges examined, there is a considerable chance that the feed slot surfaces can be dewetted. This seems to be the greatest danger for causing streaks rather than excessive wetting of the die lands. © 2011 American Institute of Chemical Engineers AIChE J, 2012