Metallocenyl 7-ACA Conjugates: Antibacterial Activity Studies and Atomic-Resolution X-ray Crystal Structure with CTX-M β-Lactamase

The conjugation of organometallic groups to current β-lactam antibiotics is a field of increasing study due to the ability of certain organometallic groups to enhance the antibiotic potency of these drugs. Herein, we report the antibacterial properties of two metallocenyl (ferrocenyl and ruthenocenyl) 7-aminocephalosporanic acid (7-ACA) antibiotic conjugates. Continuing a trend we found in our previous studies, the ruthenocenyl conjugate showed greater antibacterial activity than its ferrocenyl counterpart. Compared with the previously published 7-aminodesacetoxycephalosporanic acid (7-ADCA) conjugates, the 3-acetyloxymethyl group significantly improved the compounds’ activity. Furthermore, the Rc-7-ACA compound was more active against clinical Staphylococcus aureus isolates than the ampicillin reference. Noticeably, neither of the two new compounds showed an undesirable toxic effect in HeLa and L929 cells at the concentrations at which they displayed strong antibacterial effects. The antibacterial activity of the two metallocenyl 7-ACA derivatives was further confirmed by scanning electron microscopy (SEM). SEM micrographs showed that bacteria treated with metallocenyl 7-ACA derivatives feature cell wall damage and morphology changes. Using a CTX-M-14 β-lactamase competition assay based on nitrocefin hydrolysis, we showed that the Rc-7-ACA bound more favorably to CTX-M-14 than its ferrocenyl counterpart, again confirming the superiority of the ruthenocenyl moiety over the ferrocenyl one in interacting with proteins. We also report a 1.47 Å resolution crystal structure of Rc-7-ACA in complex with the CTX-M-14 E166A mutant, an enzyme sharing a similar active site configuration with penicillin-binding proteins, the molecular target of β-lactam antibiotics. These results strengthen the case for the antibacterial utility of the Rc and Fc groups.     

Enhancing the permeability of reverse osmosis membrane by embedding the star-like rigid supports in the substrate

Thin film composite (TFC) reverse osmosis (RO) membranes with high permeability have been prepared by interfacial polymerization based on tailoring the polysulfone (PSf) substrate structure by in situ embedded poly(p-phenylene terephthamide) (PPTA) star-like rigid supports. The star-like rigid supports were observed by the polarizing optical microscopy (POM) and transmission electron microscope (TEM). The surface properties of the substrates were investigated by FTIR, the water contact angle (WCA), FESEM and AFM. The WCA was decreased from 88.5° to 72.3° with the PPTA increasing from 0% to 8%, and the surface roughness increased from 24.2, 25.1, 33.5 and 58.6 nm, respectively. Furthermore, numerous interconnect micro-structures were constructed in the substrate when the PPTA content was up to 8%. The pure water flux of 8% PPTA/92%PSf substrate was up to 377.0 L m⁻² h⁻¹ and the flux decline rate was lowest (64%) after compacted at 5.5 MPa for 30 min. Otherwise, increasing the PPTA contents in the substrate enhanced the roughness, encouraged nanosheet formation and improved the permeability of TFC RO membranes. The pure water flux of the TFC RO membranes increased from 36.32 to 58.42 L m⁻² h⁻¹, where the NaCl rejection was about 99.5% at 5.5 MPa.     

Test sample allocation method for testability verification test

An extended failure mode effect and criticality analysis (FMECA)-based sample allocation method for testability verification is presented in this study to deal with the poor representativeness of test sample sets and the randomness of the testability evaluation results caused by unreasonable selection of failure samples. First, the fault propagation intensity is introduced as part of the extended information of FMECA, and the sample allocation impact factors of component units and failure modes are determined under this framework. Then, the failure mode similarity and impact factor support are defined, and the game decision method for weighing the relationship between similarity and support is proposed to obtain the weight of failure mode impact factor. Finally, a two-step allocation framework of test samples is formulated to realize the sample allocation of component units and failure modes. This method is applied to the testability verification test of a launch control system. Results show that this method can obtain more representative test samples compared with the traditional sample allocation method while effectively reducing randomness of single testability evaluation result.     

钢铁生产的水能关系分析

从钢铁生产过程中水资源使用时的能耗角度研究了钢铁联合企业的水能关系，提出了水能强度的概念来评价企业生产过程中水资源利用的节能水平，建立了钢铁企业的水能关系模型。以中国某大型钢铁联合企业为例，计算并分析了该企业的水能关系。该企业总的水能量为55 709 kW·h/h，重复用水水能量占整个钢铁企业全部水能量的82%，补水水能量占16%，排水水能量占1%；各工序中热轧工序占比最大，其次是炼铁、炼钢工序，冷轧、烧结和炼焦工序较低。该企业的吨钢水能强度为0.208 kW·h/m3，炼铁工序的水能强度最高，热轧、炼钢工序次之，烧结、冷轧和炼焦工序较低。最后，从钢铁生产过程水资源利用的角度得到节能的方向及措施。     

Improve Semi-supervised Learning with Metric Learning Clusters and Auxiliary Fake Samples

Neural Processing Letters - Because it is very expensive to collect a large number of labeled samples to train deep neural networks in certain fields, semi-supervised learning (SSL) researcher has...     

The reduction of Eu to Eu in air and luminescence properties of Eu activated ZnO–B2O3–P2O5 glasses

A valence change from Eu³⁺ to Eu²⁺ was observed in the europium ion-doped ZnO–B₂O₃–P₂O₅ glasses prepared at high temperature in air. The fluorescence emission spectrum of the sample consists of a broad emission band ascribed to the 5d–4f transition of Eu²⁺ ion and sharp emission peaks assigned to the transitions of ⁵D_o–⁷F_J (J = 0, 1, 2, 3, and 4) of Eu³⁺ ion, indicating that part of Eu³⁺ can be reduced into Eu²⁺ in the glass. A charge compensation model is proposed. The rigid tetrahedral network structure of glasses plays an important role in stability of Eu²⁺. The fabrication conditions are also studied.     

曲轴磨床磨削进给和砂轮修整控制的研究与实现

通过研究曲轴曲拐径磨床磨削进给和砂轮修整的工艺过程，对磨床进行数控系统改造，用PLC和NC相结合的方式在不改变原来PLC程序的前提下实现了砂轮修整和磨削进给的控制。     

CFD在柴油机螺旋进气道评价中的应用

本文用CFD软件对直喷柴油机螺旋进气道进行了三维数值模拟；通过气道稳流试验台对模拟计算得到的Ricardo和FEV评价参数进行了验证，得出两者趋势吻合良好的结论；指出了CFD在评价柴油机螺旋进气道性能中的实用价值。     

非线性互联系统的分散镇定

研究非线性互联系统的分散镇定问题。利用向量 L yapunov函数 ,对一类具有互联结构的非线性大系统给出了 L yapunov型的分散镇定条件 ,并给出了分散镇定的反馈控制律