Unraveling the reactivity of a cationic iminoborane: avenues to unusual boron cations

A cationic terminal iminoborane [Mes*N B ← IPr₂Me₂][AlBr₄] (3⁺[AlBr₄]⁻) (Mes* = 2,4,6-tri-tert-butylphenyl and IPr₂Me₂ = 1,3-diisopropyl-4,5-dimethylimidazol-2-ylidene) has been synthesized and characterized. The employment of an aryl group and N-heterocyclic carbene (NHC) ligand enables 3⁺[AlBr₄]⁻ to exhibit both B-centered Lewis acidity and BN multiple bond reactivities, thus allowing for the construction of tri-coordinate boron cations 5⁺–12⁺. More importantly, initial reactions involving coordination, addition, and [2 + 3] cycloadditions have been observed for the cationic iminoborane, demonstrating the potential to build numerous organoboron species via several synthetic routes.

An NHC-stabilized aryliminoboryl cation exhibits both boron-centered Lewis acidity and multiple bond reactivity and could be utilized as an effective synthon for unusual cationic boron species.     

Impact of drifts in the ASDEX upgrade upper open divertor using SOLPS-ITER

SOLPS-ITER L-mode-like simulations with the full set of currents and drift velocities activated, and fluid neutrals have been carried out to interpret experimental results obtained in AUG. Drifts are critical to quantitatively reproduce the experimental results; however, simulations without drifts can also reproduce some trends qualitatively. The magnitude and dependence of the peak heat flux onto both targets on the upstream collisionality are, in general, in quantitative agreement within uncertainties with infrared thermography measurements in favourable field direction. The onset of power detachment is observed. In unfavourable toroidal field direction, a more symmetrical inner/outer target solution with regards to the power distribution is predicted, in agreement with experimental observations. However, also in unfavourable toroidal field direction, insufficient power is dissipated in the simulations and therefore q_{peak, inn} is overpredicted by up to a factor of 4 and q_{peak, out} by up to a factor of 1.5. The largest contribution to the sources due to radial transport in the energy balance equation is the radial divergence of the energy flux due to V_{E × B}.     

Recent Analytical Approaches for the Study of Bioavailability and Metabolism of Bioactive Phenolic Compounds

The study of the bioavailability of bioactive compounds is a fundamental step for the development of applications based on them, such as nutraceuticals, functional foods or cosmeceuticals. It is well-known that these compounds can undergo metabolic reactions before reaching therapeutic targets, which may also affect their bioactivity and possible applications. All recent studies that have focused on bioavailability and metabolism of phenolic and terpenoid compounds have been developed because of the advances in analytical chemistry and metabolomics approaches. The purpose of this review is to show the role of analytical chemistry and metabolomics in this field of knowledge. In this context, the different steps of the analytical chemistry workflow (design study, sample treatment, analytical techniques and data processing) applied in bioavailability and metabolism in vivo studies are detailed, as well as the most relevant results obtained from them.     

Synthetic Diphenylacetylene-Based Retinoids Induce DNA Damage in Chinese Hamster Ovary Cells without Altering Viability

All-trans-retinoic acid (ATRA), the active metabolite of vitamin A, plays a pivotal role in cell differentiation, proliferation and embryonic development. It is an effective therapy for dermatological disorders and malignancies. ATRA is prone to isomerization and oxidation, which can affect its activity and selectivity. Novel diphenylacetylene-based ATRA analogues with increased stability can help to overcome these problems and may offer significant potential as therapeutics for a variety of cancers and neurodegenerative diseases, including amyotrophic lateral sclerosis. Here, we investigated the effects of these retinoids on cell viability and genotoxicity in the widely used model system of the rapidly proliferating Chinese hamster ovary cell line. DC360 is a fluorescent ATRA analogue and DC324 is a non-active derivative of DC360. EC23, DC525, DC540, DC645, and DC712 are promising analogues with increased bioactivity. The cytotoxic activity of the compounds was evaluated by ATP assay and DNA damage was tested by comet assay. No cytotoxicity was observed in the 10⁻⁶–10⁻⁵ M concentration range. All compounds induced DNA migration similar to ATRA, but DC324, DC360 and EC23 did so to a greater extent, particularly at higher concentrations. We believe that retinoid receptor-independent genotoxicity is a general characteristic of these compounds; however, further studies are needed to identify the molecular mechanisms and understand their complex biological functions.     

Effects of Frankincense Compounds on Infection,Inflammation, and Oral Health

Boswellia trees, found throughout the Middle East and parts of Africa and Asia, are the source of frankincense oil. Since antiquity, frankincense has been traded as a precious commodity, but it has also been used for the treatment of chronic disease, inflammation, oral health, and microbial infection. More recently, the bioactive components of Boswellia trees have been identified and characterized for their effects on cancer, microbial infection (especially infection by oral pathogens), and inflammation. Most studies have focused on cell lines, but more recent research has also investigated effects in animal models of disease. As natural products are considered to be safer than synthetic drugs, there is growing interest in further developing the use of substances such as frankincense oil for therapeutic treatment.     

Steroidal Antimetabolites Protect Mice against Trypanosoma brucei

Trypanosoma brucei, the causative agent for human African trypanosomiasis, is an emerging ergosterol-dependent parasite that produces chokepoint enzymes, sterol methyltransferases (SMT), not synthesized in their animal hosts that can regulate cell viability. Here, we report the lethal effects of two recently described natural product antimetabolites that disrupt Acanthamoeba sterol methylation and growth, cholesta-5,7,22,24-tetraenol (CHT) and ergosta-5,7,22,24(28)-tetraenol (ERGT) that can equally target T. brucei. We found that CHT/ERGT inhibited cell growth in vitro, yielding EC₅₀ values in the low nanomolar range with washout experiments showing cidal activity against the bloodstream form, consistent with their predicted mode of suicide inhibition on SMT activity and ergosterol production. Antimetabolite treatment generated altered T. brucei cell morphology and death rapidly within hours. Notably, in vivo ERGT/CHT protected mice infected with T. brucei, doubling their survival time following daily treatment for 8–10 days at 50 mg/kg or 100 mg/kg. The current study demonstrates a new class of lead antibiotics, in the form of common fungal sterols, for antitrypanosomal drug development.     

Die Grundlagen der Physik

Ohne Zusammenfassung     

Prix Bolyai. avec un rapport par Henri Poincaré

Conclusions Après cet exposé, un long commentaire serait inutile. On voit quelle a été la variété des recherches deM. Hilbert, l'importance des problèmes auxquelles il s'est attaqué. Nous signalerons l'élégance et la simplicité des méthodes, la clarté de l'exposition, le souci de l'absolue riguer. En cherchant à être parfaitement rigoureux, on risque parfois d'être long, et ce n'est pas là acheter trop cher une correction sans laquelle les mathématiques ne seraient rien. MaisM. Hilbert a su éviter ce que ces longueurs auraient pu avoir d'un peu pénible pour ses lecteurs, en ne leur laissant jamais perdre de vue le fil conducteur qui lui a servi à s'orienter. On voit toujours aisément par quel encha?nement d'idées il a été amené à se poser un problème et à en trouver la solution. On sent que, plus analyste que géomètre au sensordinaire du mot, il a néanmoins aper?u l'ensemble de son travail d'un coup d'œil, avant d'en distinguer les détails, et il sait faire profiter le lecteur de cette vue d'ensemble. M. Hilbert a exercé une influence considérable sur les progrès récents des sciences mathématiques, non seulement par ses travaux personnels, mais par son enseignement, par les conseils qu'il donait à ses élèves et qui leur permettaient de contribuer à leur tour à ce développement de nos connaissances en se servant des méthodes créées par leur ma?tre. Il n'est pas besion, ce semble, d'en dire davantage pour justifier le choix de la Commission qui a été unanime à attribuer àM. Hilbert le prix Bolyai pour la période 1905–1909.     

Hermann Minkowski

Ohne ZusammenfassungGedächtnisrede, gehalten in der öffentlichen Sitzung der Kgl. Gesellschaft der Wissenschaften zu Göttingen am 1. Mai 1909.     

Neue Begründung der Bolyai-Lobatschefskyschen Geometrie

Ohne Zusammenfassung