Cytotoxic Potential of a-Azepano- and 3-Amino-3,4-SeCo-Triterpenoids

Semi-synthetic triterpenoids, holding an amino substituted seven-membered A-ring (azepano-ring), which could be synthesized from triterpenic oximes through a Beckmann type rearrangement followed by a reduction of lactame fragment, are considered to be novel promising agents exhibiting anti-microbial, alpha-glucosidase, and butyrylcholinesterase inhibitory activities. In this study, in an attempt to develop new antitumor candidates, a series of A-ring azepano- and 3-amino-3,4-seco-derivatives of betulin, oleanolic, ursolic, and glycyrrhetinic acids were evaluated for their cytotoxic activity against five human cancer cell lines and non-malignant mouse fibroblasts by means of a colorimetric sulforhodamine assay. Azepanoallobetulinic acid amide derivative 11 was the most cytotoxic compound of this series but showed little selectivity between the different human tumor cell lines. Flow cytometry experiments showed compound 11 to act mainly by apoptosis (44.3%) and late apoptosis (21.4%). The compounds were further screened at the National Cancer Institute towards a panel of 60 cancer cell lines. It was found that compounds 3, 4, 7, 8, 9, 11, 15, 16, 19, and 20 showed growth inhibitory (GI₅₀) against the most sensitive cell lines at submicromolar concentrations (0.20–0.94 μM), and their cytotoxic activity (LC₅₀) was also high (1–6 μM). Derivatives 3, 8, 11, 15, and 16 demonstrated a certain selectivity profile at GI₅₀ level from 5.16 to 9.56 towards K-562, CCRF-CEM, HL-60(TB), and RPMI-8226 (Leukemia), HT29 (Colon cancer), and OVCAR-4 (Ovarian cancer) cell lines. Selectivity indexes of azepanoerythrodiol 3 at TGI level ranged from 5.93 (CNS cancer cell lines SF-539, SNB-19 and SNB-75) to 14.89 for HCT-116 (colon cancer) with SI 9.56 at GI₅₀ level for the leukemia cell line K-562. The present study highlighted the importance of A-azepano-ring in the triterpenic core for the development of novel antitumor agents, and a future aim to increase the selectivity profile will thus lie in the area of modifications of azepano-triterpenic acids at their carboxyl group.     

Antimicrobial and Amyloidogenic Activity of Peptides. Can Antimicrobial Peptides Be Used against SARS-CoV-2?

At present, much attention is paid to the use of antimicrobial peptides (AMPs) of natural and artificial origin to combat pathogens. AMPs have several points that determine their biological activity. We analyzed the structural properties of AMPs, as well as described their mechanism of action and impact on pathogenic bacteria and viruses. Recently published data on the development of new AMP drugs based on a combination of molecular design and genetic engineering approaches are presented. In this article, we have focused on information on the amyloidogenic properties of AMP. This review examines AMP development strategies from the perspective of the current high prevalence of antibiotic-resistant bacteria, and the potential prospects and challenges of using AMPs against infection caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2).     

Detection of RDX traces at the surface with sonic aerosol flow desorption

The use of a high-speed aerosol flow is proposed for sampling RDX from the surface followed by chromatographic analysis. The aerosol is generated from different solvents by means of a coaxial nebulizer. The effect of the aerosol flow parameters (solvent flowrate, an angle of the nebulizer inclination with respect to the surface) and various solvents (water, acetone, and hexane) on the efficiency of the RDX desorption was investigated. The optimal angle of the nebulizer was found to be 30°, under these conditions, the desorption of RDX from the surfaces of different structure (metal, glass, leather, cotton fabric, and paper) has also been studied. It is shown that under the action of an aerosol created using water and acetone, desorption from a smooth surface occurs most efficiently (1.5 times higher than with hexane). In this case, the sample removes almost completely (about 80%) by the aerosol flow in a few seconds. A relationship between the desorption efficiency and the amount of the solvent sprayed (that is the amount of aerosol particles in desorbing flow) has a characteristic maximum which location depends on the properties of the solvent spray. This effect is associated with a rate of solvent evaporation. Under optimal conditions for desorption of RDX from a smooth surface using an aqueous aerosol, an LOD of ～10?ng can be achieved. For porous and rough surfaces, the efficiency of the analyte desorption decreases (three times for leather and cotton fabric). The results of the experiments conducted allow one to conclude that the RDX solubility in the solvent used does not affect considerably the efficiency of the RDX desorption. It is assumed that small aerosol drops are very active and can capture the particles of the target analyte. This promotes the desorption of RDX molecules from the surface.

© 2018 American Association for Aerosol Research     

An investigation of the elastic properties of viscoelastic clusters of particles: A comparison between two methods

Most industrial process lines involve mixing complex dispersions, which can include non-Newtonian liquids and viscoelastic particles. Knowledge of the parameters of these components may provide a key for understanding how dispersions are formed and how equipment should be designed. One parameter is the shear modulus, which describes the ability of particles to resist mechanical stresses. This parameter may play the main role in the mixing process, when a dispersion is formed by the mechanical influence of a rotor (slice or shear in a rotor-stator mixer). In this work, two methods were chosen for measuring the shear modulus: the evaluation method, based on the Warner-Bratzler cut test, and the oscillatory method. Both methods were used for measuring viscoelastic clusters of particles, and the results were adjusted for the purposes of the comparison. The comparison shows that the shear modulus values obtained from Warner-Bratzler are higher than the values obtained from the oscillatory test for the same conditions. This difference can be explained by differences in the mechanical processes during the experiments.     

The effect of mechanical recycling on the microstructure and properties of PA66 composites reinforced with carbon fibers

This article aims to prepare by injection molding recycled polymeric composites based on PA66 reinforced with short carbon fibers after artificial aging for applications in the automotive field. The aging cycles involves the combined action of UV radiation, moisture, and temperature in order to simulate the common outdoor conditions. The 100% recycled composites are obtained by the regranulation of the aged specimens followed by the remelting and re‐injection molding. The study is focused on the comparison between the mechanical behavior and the microstructure of the composites before and after mechanical recycling. The results of mechanical, thermal, and morphological investigations reveal that the recycling process had no significant effect on the final properties and microstructure of the recycled composites. Therefore the recycled PA66CF30 composites could be successfully used for structural or semi‐structural automotive applications guaranteeing good final performances and advantages from the environmental point of view. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42275.     

Formic Acid Production Via Methane Peroxide Oxidation Over Oxalic Acid Activated Fe-MFI Catalysts

Topics in Catalysis - The process of synthesis of formic acid via partial peroxide oxidation of methane over Fe-MFI zeolites, as well as the influence of the catalyst activation by oxalic acid on...     

Environmentally Benign Oxidation of Alkylphenols to p-Benzoquinones: A Comparative Study of Various Ti-Containing Catalysts

Catalytic properties of Ti-containing porous solids were compared in the oxidation of 2,3,6-trimethylphenol (TMP) with H₂O₂ to produce 2,3,5-trimethyl-1,4-benzoquinone (TMBQ, vitamin E key intermediate). Mesoporous titanium–silicates with di(oligo)nuclear Ti centers, metal–organic framework MIL-125 and amorphous TiO₂ demonstrated 100 % selectivity toward TMBQ. Titanium–silicates prepared by evaporation-induced self-assembly revealed superior performance in terms of product yield and catalyst reusability.

     

Coal mining in the Russian Donetsk Basin

The activities of coal companies in the Russian Donetsk Basin (Rostov oblast) are considered, as well as the basic coal characteristics, the potential value of local reserves, and the prospects for the region in current economic conditions.     

CO adsorption in PdxCoyXz (X = Au,Mo, Ni) tertiary alloy nanocatalysts for PEM fuel cells—a theoretical analysis

Application of tertiary alloy nanoparticles is becoming more important, however, the local structure of such alloyed particles, which is critical for tailoring their properties, is not yet very clearly understood. In this study, we present detailed theoretical analysis on the atomistic structure and CO adsorption in Pd₇₀Co₂₀X₁₀ (X=Au, Mo, Ni) tertiary composite alloys for their application in fuel cells toward oxygen reduction reaction (ORR). Basic structure and the most stable configurations for all the three composites are determined. Quantum mechanical approaches and classic molecular dynamics methods are applied to model the structure and to determine the lowest energy configurations. Our theoretical results agree well with the experimental results of XRD patterns. Considering those structures as the base, simulations were performed to determine the magnitude of CO poisoning. The results obtained by ab‐initio calculations allow us to estimate the CO‐tolerance that these catalysts might have, along with those obtained for Pd‐Co‐Ni (70:20:10 atom %) tertiary alloy, and compared with commercial Pt (1 1 0) catalyst. From these results, a comparison has been made to show different CO adsorption strengths. This is the first step to fabricate an efficient engineering design that allows us to obtain high‐performance, low‐cost nanostructured catalysts. Copyright © 2010 John Wiley & Sons, Ltd.