Synthesis of Moracin C and Its Derivatives with a 2-arylbenzofuran Motif and Evaluation of Their PCSK9 Inhibitory Effects in HepG2 Cells

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key factor in several cardiovascular diseases, as it is responsible for the elevation of circulating low-density lipoprotein cholesterol (LDL-C) levels in blood plasma by direct interaction with the LDL receptor. The development of orally available drugs to inhibit this PCSK9-LDLR interaction is a highly desirable objective. Here, we report the synthesis of naturally occurring moracin compounds and their derivatives with a 2-arylbenzofuran motif to inhibit PCSK9 expression. In addition, we discuss a short approach involving the three-step synthesis of moracin C and a divergent method to obtain various analogs from one starting material. Among the tested derivatives, compound 7 (97.1%) was identified as a more potent inhibitor of PCSK9 expression in HepG2 cells than berberine (60.9%). These results provide a better understanding of the structure–activity relationships of moracin derivatives for the inhibition of PCSK9 expression in human hepatocytes.     

近紫外激发Gd2ZnTiO6∶Eu3+,Li+红色荧光粉的制备及荧光性能

采用溶胶-凝胶法成功制备出系列Eu³⁺掺杂和Li⁺、Eu³⁺共掺杂Gd₂ZnTiO₆红色荧光粉,并研究Li⁺、Eu³⁺掺杂对样品的晶体结构、微观形貌及发光性能的影响。结果显示,所制备的Gd₂ZnTiO₆∶Eu³⁺,Li⁺(GZT∶Eu³⁺,Li⁺) 荧光粉为双钙钛矿结构,属于单斜晶系(空间群:P2₁/n),大小为10 μm的无规则形状的颗粒。在395 nm近紫外光的激发下,GZT∶Eu³⁺的发射光谱展示出典型的Eu³⁺线状特征光谱,发射峰中心位于615 nm处,归属于Eu³⁺的⁵D₀→⁷F₂跃迁。Eu³⁺的最佳掺杂浓度为0.07(摩尔分数),样品显示明显的浓度猝灭效应,其机制为电偶极子-电偶极子(d-d)相互作用。此外,研究还发现,Li⁺掺杂对样品的晶体结构、微观形貌没有影响,但是一定量的Li⁺掺杂可以显著增强样品的荧光强度。当Li⁺浓度为0.05时,荧光粉发射主峰强度增强程度最大,提高至原来的4.3倍,说明通过Li⁺、Eu³⁺共掺杂可以获得高亮度的GZT红色荧光粉。GZT∶0.14Eu³⁺,0.05Li⁺荧光粉的CIE色坐标为(0.631 1,0.375 3)与标准红光色坐标(0.670,0.330)较为接近,是一种潜在的LED用红色荧光粉。     

Role of FTFSI Anion Asymmetry on Physical Properties of AFTFSI (A=Li,Na and K) Based Electrolytes and Consequences on Supercapacitor Application

This study compares the physicochemical properties of six electrolytes comprising of three salts: LiFTFSI, NaFTFSI and KFTFSI in two solvent mixtures, the binary (3EC/7EMC) and the ternary (EC/PC/3DMC). The transport properties (conductivity, viscosity) as a function of temperature and concentration were modeled using the extended Jones-Dole-Kaminsky equation, the Arrhenius model, and the Eyring theory of transition state for activated complexes. Results are discussed in terms of ionicity, solvation shell, and cross-interactions between electrolyte components. The application of the six formulated electrolytes in symmetrical activated carbon (AC)//AC supercapacitors (SCs) was characterized by cyclic voltammetry (CV), galvanostatic cycling with potential limitation (GCPL), electrochemical impedance spectroscopy (EIS) and accelerated aging. Results revealed that the geometrical flexibility of the FTFSI anion allows it to access and diffuse easily in AC whereas its counter ions (Li⁺, Na⁺ or K⁺) can remain trapped in porosity. However, this drawback was partially resolved by mixing LiFTFSI and KFTFSI salts in the electrolyte.     

Highly stretchable,self-adhesive,and self-healable double network hydrogel based on alginate/polyacrylamide with tunable mechanical properties

A number of synthetic hydrogels suffer from low mechanical strength. Despite of the recent advances in the fabrication of tough hydrogels, it is still a great challenge to simultaneously construct high stretchability, and self-adhesive and self-healing capability in a hydrogel. Herein, a new type of double network hydrogel was prepared based on irreversible cross-linking of polyacrylamide chains and Schiff-base reversible cross-linking between glycidyl methacrylate-grafted ethylenediamine and oxidized sodium alginate (OSA). The combination of both cross-linkings and their synergistic effect provided a novel hydrogel with high strength, stretchable, rapid self-healing, and self-adhesiveness to different material. Besides, the hydrogels with diverse OSA content could maintain their original shapes after loading–unloading tensile test. The resulting hydrogel has a great potential in various fields for supporting and load-bearing substance.     

Microvascular blood flow with heat transfer in a wavy channel having electroosmotic effects

The present paper addresses microvascular blood flow with heat and mass transfer in complex wavy microchannel modulated by electroosmosis. Investigation is carried out with joule heating and chemical reaction effects. Further, viscous dissipation is also considered. Using Debye–Huckel, lubrication theory, and long wavelength approximations, analytical solutions of dimensionless boundary value problems are obtained. The impacts of different parameters are examined for temperature and concentration profile. Furthermore, nature of pressure rise is also investigated to analyze the pumping characteristics. Important results of flow phenomena are explored by means of graphs.     

On actions of Drinfel'd doubles on finite dimensional algebras

Let q be an nth root of unity for $n>2$ and let $T_n(q)$ be the Taft (Hopf) algebra of dimension $n^2$. In 2001, Susan Montgomery and Hans-Jürgen Schneider classified all non-trivial $T_n(q)$-module algebra structures on an n-dimensional associative algebra A. They further showed that each such module structure extends uniquely to make A a module algebra over the Drinfel'd double of $T_n(q)$. We explore what it is about the Taft algebras that leads to this uniqueness, by examining actions of (the Drinfel'd double of) Hopf algebras H “close” to the Taft algebras on finite-dimensional algebras analogous to A above. Such Hopf algebras H include the Sweedler (Hopf) algebra of dimension 4, bosonizations of quantum linear spaces, and the Frobenius–Lusztig kernel $u_q({\mathfrak{sl}}_2)$.