Copper(II) complexes with pyridine-2,6-dicarboxylic acid from the oxidation of copper(I) iodide

Via an oxidation reaction of Cu(I) iodide with pyridine-2,6-dicarboxylic acid (H₂L) in DMF three copper(II) complexes, [(CH₃)₂NH₂]₂[CuL₂] (1), K₂[CuL₂]?H₂L?H₂O (2) and [Cu(L)(H₂O)]_n (3), were synthesized and characterized. The structures of 1–3 were determined by single crystal X-ray diffraction studies. In-situ DMF decomposition produces dimethylamine base under solvothermal conditions and a proton transfer reaction takes place for the complex formation of 1. 3-D networks are stabilized in 1 and 2 via hydrogen bonds. Complex 3 is a 1-D coordination polymer with Cu-O semi-coordination bonds. Thermal decomposition of the complexes results in the corresponding metal oxides. Also, the electrochemical behavior of 1 was determined to be a metal-centered and diffusion-controlled, one-electron reduction process.     

Atomic decompositions and Hardy’s inequality on weak Hardy-Morrey spaces

We introduce the weak Hardy-Morrey spaces in this paper. We also obtain the atomic decompositions of the weak Hardy-Morrey spaces. By using these decompositions, we establish the Hardy inequalities on the weak Hardy-Morrey spaces.     

Existence results for degenerate <Emphasis Type="Italic">p</Emphasis>(<Emphasis Type="Italic">x</Emphasis>)-Laplace equations with Leray-Lions type operators

We show the existence and multiplicity of solutions to degenerate p(x)-Laplace equations with Leray-Lions type operators using direct methods and critical point theories in Calculus of Variations and prove the uniqueness and nonnegativeness of solutions when the principal operator is monotone and the nonlinearity is nonincreasing. Our operator is of the most general form containing all previous ones and we also weaken assumptions on the operator and the nonlinearity to get the above results. Moreover, we do not impose the restricted condition on p(x) and the uniform monotonicity of the operator to show the existence of three distinct solutions.     

A note on fractional $${\varvec{}}$$-Lalacian roblems with singular weights

We study a class of fractional p-Laplacian problems with weights which are possibly singular on the boundary of the domain. We provide existence and multiplicity results as well as characterizations of critical groups and related applications.     

Effect of Water and Ethanol Extracts from Hericium erinaceus Solid-State Fermented Wheat Product on the Protection and Repair of Brain Cells in Zebrafish Embryos

Extracts from Hericium erinaceus can cause neural cells to produce nerve growth factor (NGF) and protect against neuron death. The objective of this study was to evaluate the effects of ethanol and hot water extracts from H. erinaceus solid-state fermented wheat product on the brain cells of zebrafish embryos in both pre-dosing protection mode and post-dosing repair mode. The results showed that 1% ethanol could effectively promote zebrafish embryo brain cell death. Both 200 ppm of ethanol and water extracts from H. erinaceus solid-state fermented wheat product protected brain cells and significantly reduced the death of brain cells caused by 1% ethanol treatment in zebrafish. Moreover, the zebrafish embryos were immersed in 1% ethanol for 4 h to cause brain cell damage and were then transferred and soaked in the 200 ppm of ethanol and water extracts from H. erinaceus solid-state fermented wheat product to restore the brain cells damaged by the 1% ethanol. However, the 200 ppm extracts from the unfermented wheat medium had no protective and repairing effects. Moreover, 200 ppm of ethanol and water extracts from H. erinaceus fruiting body had less significant protective and restorative effects on the brain cells of zebrafish embryos. Both the ethanol and hot water extracts from H. erinaceus solid-state fermented wheat product could protect and repair the brain cells of zebrafish embryos damaged by 1% ethanol. Therefore, it has great potential as a raw material for neuroprotective health product.     

Combinatorial Therapeutic Effect of Inhibitors of Aldehyde Dehydrogenase and Mitochondrial Complex I,and the Chemotherapeutic Drug,Temozolomide against Glioblastoma Tumorspheres

Resident cancer cells with stem cell-like features induce drug tolerance, facilitating survival of glioblastoma (GBM). We previously showed that strategies targeting tumor bioenergetics present a novel emerging avenue for treatment of GBM. The objective of this study was to enhance the therapeutic effects of dual inhibition of tumor bioenergetics by combination of gossypol, an aldehyde dehydrogenase inhibitor, and phenformin, a biguanide compound that depletes oxidative phosphorylation, with the chemotherapeutic drug, temozolomide (TMZ), to block proliferation, stemness, and invasiveness of GBM tumorspheres (TSs). Combination therapy with gossypol, phenformin, and TMZ induced a significant reduction in ATP levels, cell viability, stemness, and invasiveness compared to TMZ monotherapy and dual therapy with gossypol and phenformin. Analysis of differentially expressed genes revealed up-regulation of genes involved in programmed cell death, autophagy, and protein metabolism and down-regulation of those associated with cell metabolism, cycle, and adhesion. Combination of TMZ with dual inhibitors of tumor bioenergetics may, therefore, present an effective strategy against GBM by enhancing therapeutic effects through multiple mechanisms of action.     

Chrysin Derivative CM1 and Exhibited Anti-Inflammatory Action by Upregulating Toll-Interacting Protein Expression in Lipopolysaccharide-Stimulated RAW264.7 Macrophage Cells

Although our previous study revealed that gamma-irradiated chrysin enhanced anti-inflammatory activity compared to intact chrysin, it remains unclear whether the chrysin derivative, CM1, produced by gamma irradiation, negatively regulates toll-like receptor (TLR) signaling. In this study, we investigated the molecular basis for the downregulation of TLR4 signal transduction by CM1 in macrophages. We initially determined the appropriate concentration of CM1 and found no cellular toxicity below 2 μg/mL. Upon stimulation with lipopolysaccharide (LPS), CM1 modulated LPS-stimulated inflammatory action by suppressing the release of proinflammatory mediators (cytokines TNF-α and IL-6) and nitric oxide (NO) and downregulated the mitogen-activated protein kinase (MAPK) and nuclear factor-κB (NF-κB) signaling pathways. Furthermore, CM1 markedly elevated the expression of the TLR negative regulator toll-interacting protein (Tollip) in dose- and time-dependent manners. LPS-induced expression of cell surface molecules (CD80, CD86, and MHC class I/II), proinflammatory cytokines (TNF-α and IL-6), COX-2, and iNOS-mediated NO were inhibited by CM1; these effects were prevented by the knockdown of Tollip expression. Additionally, CM1 did not affect the downregulation of LPS-induced expression of MAPKs and NF-κB signaling in Tollip-downregulated cells. These findings provide insight into effective therapeutic intervention of inflammatory disease by increasing the understanding of the negative regulation of TLR signaling induced by CM1.     

Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations

The incorporation of permeation enhancers in topical preparations has been recognized as a simple and valuable approach to improve the penetration of antifungal agents into toenails. In this study, to improve the toenail delivery of efinaconazole (EFN), a triazole derivative for onychomycosis treatment, topical solutions containing different penetration enhancers were designed, and the permeation profiles were evaluated using bovine hoof models. In an in vitro permeation study in a Franz diffusion cell, hydroalcoholic solutions (HSs) containing lipophilic enhancers, particularly prepared with propylene glycol dicaprylocaprate (Labrafac PG), had 41% higher penetration than the HS base. Moreover, the combination of hydroxypropyl-β-cyclodextrin with Labrafac PG further facilitated the penetration of EFN across the hoof membrane. In addition, this novel topical solution prepared with both lipophilic and hydrophilic enhancers was physicochemically stable, with no drug degradation under ambient conditions (25 °C, for 10 months). Therefore, this HS system can be a promising tool for enhancing the toenail permeability and therapeutic efficacy of EFN.     

Macrocycle Dynamics in a Branched [8]Catenane Controlled by Three Different Stimuli in Three Different Regions

A branched [8]catenane from an efficient one-pot synthesis (72 % HPLC yield, 59 % isolated yield) featuring the simultaneous use of three kinds of templates and cucurbit[6]uril-mediated azide–alkyne cycloaddition (CBAAC) for ring-closing is reported. Design and assembly of the [8]catenane precursors are unexpectedly complex that can involve cooperating, competing and non-influencing interactions. Due to the branched structure, dynamics of the [8]catenane can be modulated in different extent by rigidifying/loosening the mechanical bonds at different regions by using solvent polarity, acid-base and metal ions as the stimuli. This work not only highlights the importance of understanding the delicate interplay of the weak and non-obvious supramolecular interactions in the synthesis of high-order [n]catenane, but also demonstrates a complex control of dynamics and flexibility for exploiting [n]catenanes applications.     

Analysis of buoyancy-aided convection heat transfer from a horizontal cylinder in a vertical duct at low Reynolds number

This paper reports a numerical study on buoyancy-aided steady convection heat transfer from a horizontal cylinder situated in a vertical adiabatic duct. Numerical results have been generated forH ₁/D=2.5, 4, 8,H/D=8, 16, 24,S/D=2, 4, 6, 20Re60, andRi up to 4. The placing of a horizontal cylinder in a vertical duct of smaller width results in significantly enhanced pure forced convection due to the blockage effect, but degrades appreciably the extent of buoyancy-aided enhancement in the heat transfer rate. Nevertheless, the presence of a vertical duct leads to an overall enhancement of mixed convection heat transfer coefficient relative to that without the confining duct. Moreover, the average Nusselt number is rather insensitive to the variation of either the position of the cylinder in the duct or the duct height in the investigated ranges of these geometric parameters.Dieser Artikel beschreibt eine numerische Studie über auftriebsunterstützte konvektive Wärmeübertragung von einem horizontalen Zylinder der in einem vertikalen adiabaten Kanal positioniert ist. Die numerischen Ergebnisse sind fürH ₁/D=2, 5, 4, 8,H/D=8, 16, 24,S/D=2, 4, 6 sowie 20Re60 undRi bis 4 berechnet worden. Die Anordnung des horizontalen Zylinders in einem schmaleren vertikalen Kanal führt auf Grund des Blockierungs-effektes zu einem deutlichen Anstieg der reinen Zwangskonvektion. Aber sie verschlechtert deutlich den Betrag der auftriebsbedingten Steigerung in der Wärmeübergangsrate. Trotzdem führt die Anwesenheit des vertikalen Kanals insgesamt zu einer Steigerung des Wärmeübergangskoeffizienten bei Mischkonvektion im Vergleich zur Abwesenheit des begrenzenden Kanals. Des weiteren ist die durchschnittliche Nusseltzahl von der Variation der Zylinderposition im Kanal oder der Kanalhöhe abhängig.