Synthesis, conformation and biological evaluation of the enantiomers of 3-fluoro-gamma-aminobutyric acid ((R)- and (S)-3F-GABA): an analogue of the neurotransmitter GABA

Gamma-aminobutyric acid or GABA (1) is one of the major inhibitory amino acid neurotransmitters of the central nervous system. This article describes the first synthesis of both the (R)- and (S)- enantiomers of 3-fluoro-GABA (2, 3F-GABA). DFT calculations were carried out in a continuum solvent model (PCM-B3LYP) to estimate the preferred conformations of 3F-GABA in aqueous solution. NMR coupling constants were calculated for each conformer and were then used to simulate the NMR spectra to evaluate the solution conformation of 3F-GABA. A preliminary evaluation of the 3F-GABA enantiomers shows that they act similarly as agonists of cloned GABA(A) receptors; however, they behave quite differently in a whole animal (Xenopus laevis tadpole model).     

Betontechnologie und Dauerhaftigkeit von glasfaserbewehrten Bauteilen

Concrete Technology and Durability of Glass Fibre Reinforced Structures The durability of glass fibre reinforced concrete structures is significantly determined by matrix composition, the type of glass and its surface quality including necessary coatings. In the paper an experimental overview is given concerning special material influences and their interaction in the composite.     

BSA Hydrogel Beads Functionalized with a Specific Aptamer Library for Capturing Pseudomonas aeruginosa in Serum and Blood

Systemic blood stream infections are a major threat to human health and are dramatically increasing worldwide. Pseudomonas aeruginosa is a WHO-alerted multi-resistant pathogen of extreme importance as a cause of sepsis. Septicemia patients have significantly increased survival chances if sepsis is diagnosed in the early stages. Affinity materials can not only represent attractive tools for specific diagnostics of pathogens in the blood but can prospectively also serve as the technical foundation of therapeutic filtration devices. Based on the recently developed aptamers directed against P. aeruginosa, we here present aptamer-functionalized beads for specific binding of this pathogen in blood samples. These aptamer capture beads (ACBs) are manufactured by crosslinking bovine serum albumin (BSA) in an emulsion and subsequent functionalization with the amino-modified aptamers on the bead surface using the thiol- and amino-reactive bispecific crosslinker PEG₄-SPDP. Specific and quantitative binding of P. aeruginosa as the dedicated target of the ACBs was demonstrated in serum and blood. These initial but promising results may open new routes for the development of ACBs as a platform technology for fast and reliable diagnosis of bloodstream infections and, in the long term, blood filtration techniques in the fight against sepsis.     

Phenazine and meso-1, 2-Diphenyl-1,2-ethanediol – Partners in Photochromic Cocrystals

A hydrogen-bonded network in a 1:1 cocrystal of phenazine and meso-1,2-diphenyl-1,2-ethandiol places phenazine and diol in such a way that a thermally reversible photochromism is produced. The structure of the cocrystal is determined by X-ray crystallography. Thermally reversible changes in the UV/Vis and IR spectrum on irradiation, in combination with the generation of paramagnetism (ESR) lead to the interpretation that a light induced electron transfer between two phenazine molecules is followed by a double proton transfer to the nitrogen atoms of the radical anion of phenazine.     

Aziridide-based inhibitors of cathepsin L: synthesis, inhibition activity, and docking studies

A comprehensive screening of N-acylated aziridine (aziridide) based cysteine protease inhibitors containing either Boc-Leu-Caa (Caa=cyclic amino acid), Boc-Gly-Caa, or Boc-Phe-Ala attached to the aziridine nitrogen atom revealed Boc-(S)-Leu-(S)-Azy-(S,S)-Azi(OBn)(2) (18 a) as a highly potent cathepsin L (CL) inhibitor (K(i)=13 nM) (Azy=aziridine-2-carboxylate, Azi=aziridine-2,3-dicarboxylate). Docking studies, which also accounted for the unusual bonding situations (the flexibility and hybridization of the aziridides) predict that the inhibitor adopts a Y shape and spans across the entire active site cleft, binding into both the nonprimed and primed sites of CL.     

In Vivo Performance and Structural Relaxation of Biodegradable Bone Implants Made from Mg?Zn?Ca Bulk Metallic Glasses

A study of Mg‐based bulk metallic glasses (BMGs) as biodegradable bone implants is presented. The implantation site can affect performance, so the BMGs were evaluated in vivo in rat femurs using µ‐CT scans at various times for more than 90 days. Estimates of H₂ evolution correlate well with previous in vitro studies and bone–implant contact is similar to that for Ti pins. One potential drawback of Mg‐based BMGs in this application is embrittlement due to structural relaxation. Here, relaxation at 20 and 37 °C is examined, and an increase in the characteristic relaxation time, from 10 to 30 days at 20 °C, is observed as Zn increases from 29 to 32 at.%, correlating with dramatically reduced hydrogen evolution.     

Potassium Chloride‐Based Salt Substitutes: A Critical Review with a Focus on the Patent Literature

High dietary sodium intake (DSI) represents a major health‐related public issue in most countries all over the world. Such a diet can lead to increased risk of hypertension and related cardiovascular diseases. This situation has resulted in important public policies for various salt reduction strategies. One of these is based on the use of salt substitutes or salts with reduced sodium content. Among several options, potassium chloride (KCl) has proved to be a key nutritional ingredient for this purpose. It provides similar properties like common salt (NaCl), but with several unwanted side effects, of which the most important have relatively offensive side tastes: bitter, acrid, and metallic. To successfully formulate KCl‐based salt substitutes, numerous taste‐improving agents and formulation concepts have been used. The field of salt substitutes is mainly described in the patent literature. Since patents are both scientific and legal documents, careful and critical consideration is required when using them as a source of scientific information. This review brings a deep insight into the area of KCl‐based salt substitutes with a focus on the patent literature through the eyes of food science and technology. The most important classes of taste‐improving agents that have been employed in numerous formulation concepts of KCl‐based salt substitutes are nutritionally acceptable mineral salts; food acids, amino acids, and their nutritionally acceptable salts; simple carbohydrates and sugar substitutes; food polymers; umami ingredients; spices, vegetables, and flavors; miscellaneous taste improvers; as well as a plethora of their specific combinations. A critical review of the respective patent literature is given.