A Reduction‐responsive Amphiphilic Methotrexate‐Podophyllotoxin Conjugate for Targeted Chemotherapy

Owing to the naturally high toxicity, poor water solubility, and other side effects of podophyllotoxin (PPT), its applications are limited. To address these issues, we developed a new PPT delivery system, in which the hydrophilic drug methotrexate (MTX) and the hydrophobic drug PPT were linked by a reduction‐responsive disulfide bond to form an amphiphilic drug‐drug conjugate prodrug (MTX‐SS‐PPT). The conjugate could self‐assemble into spherical nanoaggregates in aqueous solution and self‐deliver to tumor tissues. In addition, MTX could target to folate‐receptor‐positive cells. Over‐expression of glutathione in tumor cells broke the disulfide bonds and released the free drug. In vitro and in vivo experiments indicated that the nanodrug could effectively improve the biocompatibility and reduce the toxicity of PPT.     

Synergy of Single‐ion Conductive and Thermo‐responsive Copolymer Hydrogels Achieving Anti‐Arrhenius Ionic Conductivity

Artificial intelligence sensations have aroused scientific interest from electronic conductors to bio‐inspired ionic conductors. The conductivity of electrons decreases with increasing temperature, while the ionic conductivity agrees with an Arrhenius equation or a modified Vogel–Tammann–Fulcher (VTF) equation. Herein, thermo‐responsive poly(N‐isopropyl amide) (PNIPAm) and single‐ion‐conducting poly(2‐acrylamido‐2‐methyl‐1‐propanesulfonic lithium salt) (PAMPSLi) were copolymerized via a facile radical polymerization to demonstrate a very intriguing anti‐Arrhenius ionic conductivity behaviour during thermally induced volume‐phase transition. These smart hydrogels presented very promising scaffolds for architecting flexible, wearable or advanced functional ionic devices.     

球形WC增强铁基复合等离子堆焊层的组织与摩擦学性能

为提高304不锈钢的摩擦学性能,将质量分数为30%和60%的球形WC添加到铁基复合粉末,采用等离子堆焊技术在其表面制备了WC增强铁基复合涂层.分析其显微组织结构、物相和显微硬度,在恒定载荷(50 N)和滑动速度(20 mm/s)下进行干摩擦磨损试验,研究其干滑动摩擦学性能.结果表明:富含Cr的固溶强化奥氏体、高硬度的Cr7C3和WC增强相的存在,提高了WC增强铁基堆焊层的硬度,30%WC和60%WC涂层的显微硬度达到HV0.2665和HV0.2724,比铁基涂层提高了21.1%和31.9%,是304基体的3.7和4倍;30%WC和60%WC涂层的摩擦系数和磨损率分别为0.59和2.639×10~(–6) mm~3·N~(–1)·m~(–1),0.42和1.111×10~(–6) mm~3·N~(–1)·m~(–1).30%WC和60%WC涂层均表现出优异的耐磨性能,其磨损机理分别为黏着磨损和二体磨粒磨损的混合机制,和三体磨粒磨损.     

Design and Synthesis of Proteolysis Targeting Chimeras for Inducing BRD4 Protein Degradation

In this paper, we synthesized a series of proteolysis targeting chimeras(PROTACs) using VHL E3 ligase ligands for BRD4 protein degradation. One of the most promising compound 19g exhibited robust potency of BRD4 inhibition with IC₅₀ value of (18.6±1.3) nmol/L, respectively. Furthermore, compound 19g potently inhibited cell proliferation in BRD4-sensitive cell lines RS4;11 with IC₅₀ value of (34.2±4.3) nmol/L and capable of inducing degradation of BRD4 protein at 0.4—0.6 µmol/L in the RS4;11 leukemia cells. These data show that compound 19g is a highly potent and efficacious BRD4 degrader.     

A Simple,Low-cost Method to Fabricate Drag-reducing Coatings on a Macroscopic Model Ship

A low-cost method was used to fabricate superhydrophobic coatings on a macroscopic model ship and the drag-reducing effect was investigated at both low and high speed. Hierarchical structures of the superhydrophobic copper coatings were characterized by means of scanning electron microscopy(SEM) and X-ray diffraction(XRD). Drag coefficient tests on surfaces with different wettability(superhydrophilic, hydrophilic, hydrophobic and superhydrophobic surfaces) showed that the as-prepared superhydrophobic surface exhibited a high remarkable drag reduction of 81% at a low speed of 1 mm/s. In the drag-reducing tests with model ship, the superhydrophobic coatings also exhibited around 16% drag reduction at a velocity of 0.3 m/s.     

New bi-level programming model for routing and spectrum assignment in elastic optical network

The routing and spectrum assignment problems in elastic optical networks are well-known NP-hard problem, and are even more complex and challenging when the energy consumption is taken into account. To tackle this challenging problem, we establish a bi-level programming model with the energy consumption of the optical networks and the maximum index of used frequency slots as the leader’s and follower’s objectives to be minimized, respectively, which are used to determine the optimal schemes of routing and spectrum assignments. To solve the model effectively, a hybrid genetic algorithm framework integrating a heuristic algorithm into a genetic algorithm is proposed. We use heuristic algorithm to sort the connection requests and design a genetic algorithm with tailor-made crossover, mutation and local search operator to look for an optimal routing and spectrum assignment scheme. Finally, simulation experiments are conducted, and the experimental results indicate the effectiveness of the proposed model and algorithms.     

分块式空间望远镜波前传感及控制方法的仿真研究

分块式空间望远镜的波前传感及控制方法是实现高分辨率成像的关键.空间望远镜在轨展开后,由于空间环境及光学系统本身的特点,存在位置和面形误差,波前误差动态范围大、空间频率覆盖宽,需要采用分级校正的方法逐步减小误差.给出了波前校正流程及相应的波前传感及控制方法.利用Zemax软件建立了同轴偏场三反射镜系统仿真模型,并对主镜进行了分块设计.针对该系统模型,建立了分块式空间望远镜系统波前传感及控制集成仿真软件,通过分析分块主镜的波前误差校正过程验证了算法的可行性.     

Performance of dispersed Rayleigh interferometer on the active cophasing and alignment testbed

We report the laboratory experiment on a segmented mirror testbed that shows the use of a dispersed Rayleigh interferometer to phase segmented mirrors.Segment alignment of tip-tilt is fulfilled by overlapping diffraction pattern centroids of the three individual segments on the focal plane.A spherical interferometer is introduced to evaluate the performance of piston, tip-tilt sensing, and control closed-loop, and finally a total residual root-mean-square (RMS) surface error of about 45 nm is achieved, in which a typical error of about 20 nm is contributed by piston.These results demonstrate that the dispersed Rayleigh interferometer can successfully sense the piston of segmented mirrors and be used in phasing segmented telescopes under extensive studies.     

微波辐射下吡啶[2,3-d]嘧啶衍生物的高效合成

本文以等摩尔的芳醛,巴比妥酸（或1,3-二甲基巴比妥酸）,5-氨基-2-甲基苯[d]噻唑为原料,以醋酸和乙二醇为溶剂,微波辐射下多组分一锅法合成了一系列新的吡啶[2,3-d]嘧啶衍生物。这种方法具有产率高,操作简便,反应时间短等优点。