A Dual Inhibitor of DYRK1A and GSK3β for β-Cell Proliferation: Aminopyrazine Derivative GNF4877

Loss of β-cell mass and function can lead to insufficient insulin levels and ultimately to hyperglycemia and diabetes mellitus. The mainstream treatment approach involves regulation of insulin levels; however, approaches intended to increase β-cell mass are less developed. Promoting β-cell proliferation with low-molecular-weight inhibitors of dual-specificity tyrosine-regulated kinase 1A (DYRK1A) offers the potential to treat diabetes with oral therapies by restoring β-cell mass, insulin content and glycemic control. GNF4877, a potent dual inhibitor of DYRK1A and glycogen synthase kinase 3β (GSK3β) was previously reported to induce primary human β-cell proliferation in vitro and in vivo. Herein, we describe the lead optimization that lead to the identification of GNF4877 from an aminopyrazine hit identified in a phenotypic high-throughput screening campaign measuring β-cell proliferation.     

人工监督神经网络在煤层裂缝发育区识别中的应用

针对在地震属性应用中难以精细识别煤层裂缝发育区边界的难题,开展了基于人工监督神经网络技术的煤层裂缝发育区应用研究。从地震资料中获取倾角导向体以提取高质量的地震属性,以多属性为指导进行人工拾取样点,并基于多层感知器进行神经网络机器训练学习,建立裂缝的最优属性集,拓展整体数据后获得裂缝概率体,从而识别划分出煤层裂缝发育区。该技术在山西阳泉新元矿区进行了应用,煤层裂缝发育区的识别结果明显优于属性直接识别,但勘探区内暂无钻井资料,预测效果还有待进一步验证。     

Thermoplastic and low dielectric constants polyimides based on BPADA-BAPP

ABSTRACT

The thermoplastic and low dielectric constants polyimides were introduced. The polyimides were prepared by pyromellitic dianhydride (PMDA) or 4,4?-(4,4?-Isopropylidenediphenoxy)diphthalic anhydride (BPADA) as anhydride monomer and 4,4?-oxydianiline (ODA) or 2,2-bis(4-(4-aminephenoxy)phenyl)propane (BAPP) as amine monomer. The polyimides were well characterized by FT-IR, thermogravimetric analysis, dynamic thermomechanical analysis, dielectric measurement, and tensile test. The dielectric constants were 2.32–2.95 compared with 3.10 of ODA-PMDA polyimide, while partly polyimides were thermoplastic. The results indicated anhydride monomers, containing lateral methyl groups, made polyimides become thermoplastic. The results of molecular simulations via Materials Studio also proved this conclusion.     

湖北省保康县荆山玉地球化学特征及其成因分析

荆山玉是湖北省保康县新发现的一个玉石品种,形成于大陆边缘—洋盆区过渡带的热水沉积环境,为晚震旦世—早寒武世灯影组的一种硅质角砾岩:原地震碎角砾岩,由角砾和胶结物二部分构成,角砾局部可拼接;角砾成分为早期硅质岩碎裂产物,胶结物除早期硅质岩碎裂产物外,还有少量后期充填的石英、铁质等,受角砾、胶结物颗粒大小、裂隙发育程度不同的影响,后期热液改造程度不同,角砾和胶结物化学成分存在一定的差异,色调与铁质有关。荆山玉的形成主要经历了三个阶段的演化:第一阶段,低温150～225℃、弱氧化—弱还原条件下热水成因的硅质岩形成;第二阶段,热力膨胀外力作用下,硅质岩局部原地震碎形成硅质角砾岩,热水温度243～340℃,富氧氧化—贫氧过渡环境,红褐色的Fe~(3+)在胶结物、裂隙中富集;第三阶段,热水温度116～127℃、缺氧还原条件,黄色的Fe~(2+)在胶结物、裂隙中富集。     

Effect of hybrid polysphosphazene coating treatment on carbon fibers on the interfacial properties of CF/PA6 composites

Carbon fiber (CF) reinforced polyamide 6 (PA6) composite has an extensive application. However, the performances of CF/PA6 composite are constrained by the poor interfacial adhesion between CF and PA6 matrix. In this article, in order to strengthen the interfacial adhesion of CF/PA6 composite, a layer of poly(cyclotriphosphazene-co-4,4′-sulfonyldiphonel) (PZS) hybrid coating with plenty of PZS microspheres (PZSMS) was successfully introduced onto CF surface through facile in situ polymerization. After surface modification, the surface morphologies and the surface chemical structures of fibers changed distinctly. On one hand, the PZSMS provided more contact points and increased mechanical interlocking between CF and PA6 matrix. On the other hand, numerous hydrogen bonds between CF and PA6 were formed due to a great amount of unique polar groups on modified CF surface. Consequently, in comparison with untreated CF, the interfacial shear strength of CF-PZSMS/PA6 composites was improved from 37.68 ± 3.16 to 53.79 ± 3.38 MPa, by 42.75 ± 3.02%. The results indicated that PZS hybrid coating on fiber surface effectively improved the interfacial adhesion of CF/PA6 composites, and the stronger hydrogen bonding and the enhanced mechanical interlocking synergistically played a major role in such significant improvements.     

The bottom-up synthesis for aramid nanofibers: The influence of copolymerization

Aramid based on poly (p-phenylene terephthalamide) (PPTA) is widely concerned as high-performance materials. Herein, copolymerized aramid nanofibers (CANFs) were prepared for the first time by a direct bottom-up polymerization method without additives. Three kinds of third monomers of m-phenylenediamine, 4,4′-diaminodiphenyl ether, and 2,5-dichloro-1,4-phenylenediamine were separately copolymerized in PPTA and transformed into nanofiber dispersions in water medium. The characterization results revealed the relationship between the morphology of products and the structure as well as dosages of the different kinds of monomers, which was explained by the influence on conjugate regularities of the PPTA molecules. Furthermore, CANFs were used to build aramid paper blended in pure PPTA nanofibers, and the mechanical and insulation properties of composite paper were improved significantly, which would be of potential use as the new building block for aramid composite materials.     

Fabrication and photocatalytic performance of one-dimensional Ag3PO4 sensitized SrTiO3 nanowire

The 1D Ag₃PO₄ sensitized SrTiO₃ nanowires are prepared by simple route of electrospinning-in situ deposition technique. The results of the thermogravimetry (TG), X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive Spectrometer (EDS), transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS) and UV–Visible diffuse reflectance spectroscopy (UV–Vis) indicate that the Ag₃PO₄ nanoparticles has been deposited on the surface of the SrTiO₃ nanowires successfully. Experimental results showed that compared with pure SrTiO₃, the as-prepared 1D Ag₃PO₄ sensitized SrTiO₃ nanowires exhibit obvious enhancement of photocatalytic performance and stability. Especially, the Ag₃PO₄/SrTiO₃ (3AS sample) had a satisfactory photocatalytic activity for degrading methylene blue (MB) more than 98% under visible light irradiation. As to pure SrTiO₃ and Ag₃PO₄, only 9.8% and 49% of MB was decomposed after 35?min irradiation respectively. Furthermore, the mechanism of the enhancing photocatalytic activity could be ascribed to the nano-heterojunction of the Ag₃PO₄/SrTiO₃, the visible light response of the Ag₃PO₄, and the 1D structure of the nanowires.     

Embedding Ag or Au nanoparticles within the nano-sized wall of YbPO4:Er3+ inverse opals and resulting enhanced upconversion luminescence

Metal nanoparticles preparation in the interior of nanoscale skeleton of inverse opals made up of crystallized matrix is more difficult than the preparation of pure inverse opals. In the present work, the Ag or Au nanoparticles embedded YbPO₄:Er³⁺ inverse opals were prepared by a simple approach, which involved the infiltration of opal template by using the transparent YbPO₄:Er³⁺ sol including silver nitrate or chloroauric acid and the sintering at high temperature. The 20–30?nm Au or 5–10?nm Ag nanoparticles were formed in the interior of nanoscale skeleton in the YbPO₄:Er³⁺ inverse opals, and the Ag or Au nanoparticles embedded YbPO₄:Er³⁺ inverse opals were prepared. The influence of Ag or Au nanoparticles on the upconversion photoluminescence of YbPO₄:Er³⁺ inverse opal was studied, and the upconversion luminescence enhancement induced by the Ag or Au nanoparticles was observed. The mechanisms of upconversion luminescence enhancement of YbPO₄:Er³⁺ inverse opals induced by Ag or Au nanoparticles were discussed. The enhancement of upconversion luminescence induced by Ag nanoparticles was attributed to the enhancement of the excitation field, and the enhancement of upconversion emission induced by Au nanoparticles was related to the increasing of the radiation decay rate of Er³⁺.     

AlF3-modified LiCoPO4 for an advanced cathode towards high energy lithium-ion battery

Surface-interface reaction between the electrode and electrolyte plays a key role in lithium-ion storage properties, especially for high voltage cathode such as LiCoPO₄ and Ni-riched cathode. Generally, surface modification is an effective method to improve the electrochemical performance of electrode materials. Herein, in order to revise the LiCoPO₄ cathode with desirable properties, uniform AlF₃-modified LiCoPO₄ (LiCoPO₄@AlF₃) cathode materials in nano-sized distribution are synthesized. XRD result indicates that there is no structural transformation observed after AlF₃ coating. TEM characterization and XPS analysis reveal that the surface of LiCoPO₄ particle is coated by a nano-sized uniform AlF₃ layer. Further, the electrochemical results indicate that AlF₃ layer significantly improves the cycling and rate performances of LiCoPO₄ cathode within the voltage range of 3.0–5.0 V. After a series of optimization, 4 mol% AlF₃-coated LiCoPO₄ material exhibits the best properties including an initial discharge capacity of 159 mA h g^?1 at 0.1 C with 91% capacity retention after 50 cycles, especially a discharge capacity of 90 mA h g^?1 can be obtained at 1 C rate. CV curves indicate that the polarization of cathode is reduced by AlF₃ layer and EIS curves reveal that AlF₃ layer relieves the increase of resistance to facilitate Li-ion transfer at the interface between electrode and electrolyte during the cycling process. The enhanced electrochemical performances are attributed to that the AlF₃ layer can stabilize the interface between the cathode and electrolyte, form steady SEI film and suppress the electrolyte continuous decomposition at 5 V high voltages. This feasible strategy and novel characteristics of LiCoPO₄@AlF₃ could promise the prospective applications in the stat-art of special lithium-ion battery with high energy and/or power density.     

Microstructures and mechanical properties of B4C-TiB2-SiC composites fabricated by ball milling and hot pressing

B₄C-TiB₂-SiC composites were fabricated via hot pressing using ball milled B₄C, TiB₂, and SiC powder mixtures as the starting materials. The impact of ball milling on the densification behaviors, mechanical properties, and microstructures of the ceramic composites were investigated. The results showed that the refinement of the powder mixtures and the removal of the oxide impurities played an important role in the improvement of densification and properties. Moreover, the formation of the liquid phases during the sintering was deemed beneficial for densification. The typical values of relative density, hardness, bending strength, and fracture toughness of the composites reached 99.20%, 32.84?GPa, 858?MPa and 8.21?MPa?m^1/2, respectively. Crack deflection, crack bridging, crack branching, and microcracking were considered to be the potential toughening mechanisms in the composites. Furthermore, numerous nano-sized intergranular/intragranular phases and twin structures were observed in the B₄C-TiB₂-SiC composite.