Discovery of a Histidine-Based Scaffold as an Inhibitor of Gut Microbial Choline Trimethylamine-Lyase

Anaerobic choline metabolism by human gut microbiota to produce trimethylamine (TMA) has recently evolved as a potential therapeutic target because of its association with chronic kidney disease and increased cardiovascular risks. Limited examples of choline analogues have been reported as inhibitors of bacterial enzyme choline TMA-lyase (CutC), a key enzyme regulating choline anaerobic metabolism. We used a new workflow to discover CutC inhibitors based on focused screening of a diversified library of small molecules for intestinal metabolic stability followed by in vitro CutC inhibitory assay. This workflow identified a histidine-based scaffold as a CutC inhibitor with an IC₅₀ value of 1.9±0.2 μM. Remarkably, the identified CutC inhibitor was able to reduce the production of TMA in whole-cell assays using various bacterial strains as well as in complex gut microbiota environment. The improved efficiency of the new scaffold identified in this study in comparison to previously reported CutC inhibitors would enable optimization of potential leads for in vivo screening and clinical translation. Finally, docking studies and molecular-dynamic simulations were used to predict putative interactions created between inhibitor and CutC.     

Drying Kinetics of Apple Tissue Treated by Pulsed Electric Field

The aim of this work was to study the influence of pulsed electric field (PEF) on the drying kinetics of apple tissue. Therefore, mathematical models that are commonly used in the literature were applied to describe the process. PEF treatment of the samples was carried out at an intensity of E = 5–10 kV/cm and 10–50 pulse numbers. Subsequently, the apples were convectively dried at 70°C and air velocity of 2 m/s. Based on electrical conductivity measurement, the cell disintegration index Z _p was computed. Midilli et al.'s(Drying Technology, Vol. 20, pp. 1503–1513, 2001) model was evaluated as the most adequate to describe the moisture transfer in PEF-treated and intact samples. PEF pretreatment induced a reduction in drying time of up to 12% when 10 kV/cm and 50 pulses were applied. For instance, after 60 min of drying, the dimensionless moisture ratio for PEF-treated (10 kV/cm, 50 pulses) samples was 0.18 compared to 0.26 for the untreated apples. The effective moisture diffusivity, calculated on the basis of the Fick's second law, was 1.04 × 10^?9 m/s for intact samples and from 1.09 × 10^?9 to 1.25 × 10^?9 m²/s for PEF-treated samples at 10 pulses at 5 kV/cm and 50 pulses at 10 kV/cm, respectively.     

Selected chemical and physico-chemical properties of microwave-convective dried herbs

The purpose of the presented study was to describe kinetics of microwave-convection drying of basil (Ocimum basilicum), lovage (Levisticum officinale), mint (Mentha sp.), oregano (Origanum vulgare), parsley (Petroselinum crispum), and rocket (Eruca vesicaria) by means of different mathematical models, as well as to describe changes of polyphenols content, color and sorption properties after drying. The analyzed leaves were dried using microwaves power level of 300 W, in a temperature of 40 °C. Logistic model provided best fit to the experimental data. No significant differences in the drying kinetics could be discerned, while significant influence of herbs species on polyphenols contents, color and sorption properties was noted. The highest retention of phenolic compound, good resistance to color degradation and the highest water vapor adsorption concerned Apiaceae family (lovage, parsley), while worse properties in terms of these parameters were noted in Lamiaceae (basil, oregano, mint) and Brassicaceae (rocket).     

UV-initiated crosslinking of photoreactive acrylic pressure-sensitive adhesives using excimer-laser

UV-initiated crosslinking technology is well established in the market and allows the production of a wide range of ultraviolet (UV)-crosslinkable pressure-sensitive adhesives (PSA) with interesting features. The balance between such properties as adhesive and cohesive strengths within the crosslinked self-adhesive coatings is critical for their performance. The UV crosslinking of acrylic PSA, especially for following properties: tack, peel adhesion, and shear strength of self-adhesive polymer layers, has been investigated using UV excimer-laser and UV lamp as UV sources. It was observed that after UV crosslinking of acrylic PSA using excimer-laser in comparison with typical UV lamp, high-quality PSA products with excellent properties, such as tack, peel adhesion, shear strength, and shrinkage were received.     

Influence of sodium alginate and methylcellulose on hydrolysis and physicochemical properties of α-TCP based materials

The effect of the sodium alginate and methylcellulose modifiers on hydrolysis, setting reaction, microstructure, mechanical and in vitro properties of α-TCP based materials was investigated. It was found that the presence of sodium alginate impeded α-TCP hydrolysis to hydroxyapatite, which may have a significant influence on resorbability, biodegradation and biological behavior of biomaterials. There were several reasons for these phenomena, such as: (I) the gelation of sodium alginate in the presence of Ca²⁺, (II) the creation of an organic layer which impedes the diffusion of water molecules to α-TCP and (III) the uptake of water molecules by sodium alginate. The inhibitory effect was not observed for methylcellulose and it was diminished in simulated body fluid. Additionally, it was demonstrated that the examined cements varied in their microstructure, setting times and compressive strengths, depending on the applied kind of a polymer additive. The cement containing sodium alginate had a higher compressive strength (20 ± 8 MPa) than the one with methylcellulose (17 ± 4 MPa) and the one lacking polymer (14 ± 4 MPa). All the developed materials exhibited high bioactivity in vitro.     

An analysis of the numerical model influence on the ground temperature profile determination

The estimation of the ground temperature profile with respect to the depth and time is the key issue in many engineering applications which use the ground as a source of thermal energy. In the present work, the influence of the model components on the calculated ground temperature distribution has been analysed in order to develop an accurate and robust model for the prediction of the ground temperature profile. The presented mathematical model takes into account all the key phenomena occurring in the soil and on its top surface. The impact of individual model elements on the temperature of the soil has been analysed. It has been found that the simplest models and the most complex model result in a similar temperature variation over the simulation period, but only at a low depth. A detailed analysis shows that a larger depth requires more complex models and the calculation with the use of simple models results in an incorrect temperature and a theoretical COP estimation.     

Antioxidative and anti‐inflammatory potential of phenolics from purple basil (Ocimum basilicum L.) leaves induced by jasmonic,arachidonic and β‐aminobutyric acid elicitation

The study presents changes in the phenolic levels, antioxidant and anti‐inflammatory potential of purple basil leaves caused by different chemical elicitors: arachidonic acid (AA), jasmonic acid (JA) and β‐aminobutyric acid (BABA). The application of the all tested elicitors increased the concentration of phenolic compounds, including flavonoids and phenolic acids; especially, in comparison with control (457.62 μg g^?1 FW), the rosmarinic acid level significantly increased after AA and JA treatment ‐ 705.0 and 596.5 μg g^?1 FW, respectively. Phenolics from AA‐elicited plants showed the highest anti‐inflammatory activities designated as lipoxygenase (EC₅₀ = 1.67 mg FW mL^?1) and cyclooxygenase inhibition (EC₅₀ = 0.31 mg FW mL^?1). Elicitors' treatments (especially AA and JA) may be a very useful biochemical tool for improving the production of phenolic compounds in purple basil leaves.