Bis[1]benzothieno[1,4]thiazines: Planarity,Enhanced Redox Activity and Luminescence by Thieno-Expansion of Phenothiazine

Twofold Buchwald–Hartwig aminations selectively furnish three regioisomers of bis[1]benzothieno[1,4]thiazines; X-ray structure analyses and DFT calculations were corroborated for correlation of their electronic properties. All regioisomers outscore the parent compound phenothiazine with respect to a low-lying oxidation potential and reversible redox activity. The anti-anti bis[1]benzothieno[3,2-b:2′,3′-e][1,4]thiazines possess the lowest oxidation potentials in this series and displayed pronounced green luminescence in solution (Φ_F≈20 %) and in the solid state. Syn-anti regioisomers were only weakly luminescent in solution, but showed aggregation-induced emission enhancement and solid-state luminescence. Most interestingly, X-ray structure analyses revealed that anti-anti derivatives have an amazingly coplanar structure of the pentacyclic anellated 1,4-thiazine system, emphasizing a structural similarity to heteroacenes. The calculated theoretical nucleus-independent chemical shifts additionally suggested that these 8π-electron core systems can be considered as the first electronically unbiased anellated 1,4-thiazines with antiaromatic character.     

The wait-and-judge scenario approach applied to antenna array design

Computational Management Science - The scenario optimisation approach is a methodology for finding solutions to uncertain convex problems by resorting to a sample of data, which are called...     

Hydrolysis of the low gelatinization temperature Araucaria angustifolia pine seed starch

Journal of Thermal Analysis and Calorimetry - The effect of compressor speed, initial refrigerant charge and volume concentrations of SiO2/PAG nanolubricant on the performance of automotive...     

Preclinical Evaluation of Cetuximab and Benzoporphyrin Derivative-Mediated Intraperitoneal Photodynamic Therapy in a Canine Model

Peritoneal carcinomatosis (PC) can occur as an advanced consequence of multiple primary malignancies. Surgical resection, radiation or systemic interventions alone have proven inadequate for this aggressive cancer presentation, since PC still has a poor survival profile. Photodynamic therapy (PDT), in which photosensitive drugs are exposed to light to generate cytotoxic reactive oxygen species, may be an ideal treatment for PC because of its ability to deliver treatment to a depth appropriate for peritoneal surface tumors. Additionally, epidermal growth factor receptor (EGFR) signaling plays a variety of roles in cancer progression and survival as well as PDT-mediated cytotoxicity, so EGFR inhibitors may be valuable in enhancing the therapeutic index of intraperitoneal PDT. This study examines escalating doses of benzoporphyrin derivative (BPD)-mediated intraperitoneal PDT combined with the EGFR-inhibitor cetuximab in a canine model. In the presence or absence of small bowel resection (SBR) and cetuximab, we observed a tolerable safety and toxicity profile related to the light dose received. Additionally, our findings that BPD levels are higher in the small bowel compared with other anatomical regions, and that the risk of anastomotic failure decreases at lower light doses will help to inform the design of similar PC treatments in humans.     

A complete solution to the infinite Oberwolfach problem

Let F be a 2‐regular graph of order v. The Oberwolfach problem, OP(F), asks for a 2‐factorization of the complete graph on v vertices in which each 2‐factor is isomorphic to F. In this paper, we give a complete solution to the Oberwolfach problem over infinite complete graphs, proving the existence of solutions that are regular under the action of a given involution free group G. We will also consider the same problem in the more general context of graphs F that are spanning subgraphs of an infinite complete graph $\mathbb{K}$ and we provide a solution when F is locally finite. Moreover, we characterize the infinite subgraphs L of F such that there exists a solution to OP(F) containing a solution to OP(L).     

Differential Algebra-Based Multiple Gaussian Particle Filter for Orbit Determination

Journal of Optimization Theory and Applications - The nonlinear filtering problem plays a fundamental role in multiple space-related applications. This paper offers a new filtering technique that...     

Penalty alternating direction methods for mixed-integer optimal control with combinatorial constraints

Mathematical Programming - We consider mixed-integer optimal control problems with combinatorial constraints that couple over time such as minimum dwell times. We analyze a lifting and...     

Transmembrane Transport of Bicarbonate Unravelled**

Anion receptors can be used to transport ions across lipid bilayers, which has potential for therapeutic applications. Synthetic bicarbonate transporters are of particular interest, as defects in transmembrane transport of bicarbonate are associated with various diseases. However, no convenient method exists to directly observe bicarbonate transport and study the mechanisms involved. Here, an assay is presented that allows the kinetics of bicarbonate transport into liposomes to be monitored directly and with great sensitivity. The assay utilises an encapsulated europium(III) complex, which exhibits a large increase in emission intensity upon binding bicarbonate. Mechanisms involving CO₂ diffusion and the dissipation of a pH gradient are shown to be able to lead to an increase in bicarbonate concentration within liposomes, without transport of the anion occurring at all. By distinguishing these alternative mechanisms from actual bicarbonate transport, this assay will inform the future development of bicarbonate transporters.     

Anti-Inflammatory and Neuromodulatory Effects Induced by Tanacetum parthenium Water Extract: Results from In Silico,In Vitro and Ex Vivo Studies

Tanacetum parthenium (feverfew) has traditionally been employed as a phytotherapeutic remedy in the treatment of migraine. In this study, a commercial T. parthenium water extract was investigated to explore its anti-inflammatory and neuromodulatory effects. Isolated mouse cortexes were exposed to a K⁺ 60 mM Krebs-Ringer buffer and treated with T. parthenium water extract. The prostaglandin E₂ (PGE₂) level, brain-derived neurotrophic factor (BDNF), interleukin-10 (IL-10), and IL-1β gene expression were evaluated in the cortex. The effects on dopamine (DA) release and dopamine transporter (DAT) gene expression were assayed in hypothalamic HypoE22 cells. A bioinformatics analysis was conducted to further investigate the mechanism of action. The extract was effective in reducing cortex PGE₂ release and IL-1β gene expression. In the same experimental system, IL-10 and BDNF gene expressions increased, and in HypoE22 cells, the extract decreased the extracellular dopamine level and increased the DAT gene expression due to the direct interaction of parthenolide with the DAT. Overall, the present findings highlight the efficacy of T. parthenium water extract in controlling the inflammatory pathways that occur during cortical-spreading depression. Additionally, the inhibition of the hypothalamic DA release observed in this study further supports the role of dopaminergic pathways as key targets for novel pharmacological approaches in the management of migraine attacks.