Evaluation of the Antimicrobial Potential and Toxicity of a Newly Synthesised 4-(4-(Benzylamino)butoxy)-9H-carbazole

One of the greatest threats to human and animal health is posed by infections caused by drug-resistant bacterial strains. Therefore, newly synthesised substances are tested for their antimicrobial activity. Carbazole derivatives seem to be promising antibacterial agents. This study aimed at investigating the toxicity and activity of newly synthesised, functionalised carbazole derivative 2 (4-(4-(benzylamino)butoxy)-9H-carbazole) against various microorganisms. Its antimicrobial potential against Gram-positive and Gram-negative bacteria, yeast, and filamentous fungi was examined according to CLSI (Clinical and Laboratory Standards Institute) standards. The tested compound was found to efficiently inhibit the growth of Gram-positive strains. The addition of carbazole derivative 2 at the concentration of 30 µg/mL caused inhibition of bacterial growth by over 95%. Moreover, about 50 and 45% limitation of Pseudomonas aeruginosa and Aspergillus flavus growth was observed in the samples incubated with the addition of 20 and 60 µg/mL of the compound, respectively. Its addition to the microbial cultures caused an increase in the permeability of the cellular membrane. Slight haemolysis of red blood cells was observed after 24-h treatment with carbazole derivative 2. On the other hand, human fibroblasts were found to be more sensitive to its effects. The activity of the tested compound indicates a possibility of its further modification in order to obtain effective drugs, especially against drug-resistant staphylococci.     

Identification and determination of the glyceride and tris-(2-hydroxyethyl)isocyanurate structures in the average macromolecule of a polyester with carbon-13-NMR spectroscopy: Analysis of the polyester average structure

The ¹³C-NMR approach to quantitative analysis of a polyester resin synthesized from dimethylterephthalate, ethylene glycol, tris-(2-hydroxyethyl)isocyanurate (THEIC), and glycerol is presented. Various glyceride and isocyanurate structures formed during the esterification have been identified and analyzed, at first in simple model systems and then in the structure of the resin. The contents of particular structural units were determined as well as a hypothetical average macromolecule of the resin defined. The assignments of ¹³C-NMR signals were made and correlated with the ¹H shifts using a 2D-HETCOR experiment. © 1998 John Wiley & Sons, Inc. J. Appl. Polym. Sci. 70: 675–687, 1998     

Sevoflurane Effects on Neuronal Energy Metabolism Correlate with Activity States While Mitochondrial Function Remains Intact

During general anesthesia, alterations in neuronal metabolism may induce neurotoxicity and/or neuroprotection depending on the dose and type of the applied anesthetic. In this study, we investigate the effects of clinically relevant concentrations of sevoflurane (2% and 4%, i.e., 1 and 2 MAC) on different activity states in hippocampal slices of young Wistar rats. We combine electrophysiological recordings, partial tissue oxygen (p_tiO₂) measurements, and flavin adenine dinucleotide (FAD) imaging with computational modeling. Sevoflurane minimally decreased the cerebral metabolic rate of oxygen (CMRO₂) while decreasing synaptic transmission in naive slices. During pharmacologically induced gamma oscillations, sevoflurane impaired network activity, thereby decreasing CMRO₂. During stimulus-induced neuronal activation, sevoflurane decreased CMRO₂ and excitability while basal metabolism remained constant. In this line, stimulus-induced FAD transients decreased without changes in basal mitochondrial redox state. Integration of experimental data and computer modeling revealed no evidence for a direct effect of sevoflurane on key enzymes of the citric acid cycle or oxidative phosphorylation. Clinically relevant concentrations of sevoflurane generated a decent decrease in energy metabolism, which was proportional to the present neuronal activity. Mitochondrial function remained intact under sevoflurane, suggesting a better metabolic profile than isoflurane or propofol.     

Potential Therapeutic Application of Regulatory T Cells in Diabetes Mellitus Type 1

The autoimmune reaction against the beta cells of the pancreatic islets in type 1 diabetes mellitus (T1DM) patients is active in prediabetes and during the development of the clinical manifestation of T1DM, but it decreases within a few years of the clinical manifestation of this disease. A key role in the pathogenesis of T1DM is played by regulatory T cell (Treg) deficiency or dysfunction. Immune interventions, such as potential therapeutic applications or the induction of the Treg-cell population in T1DM, will be important in the development of new types of treatment. The aim of this study was to evaluate innovative immune interventions as treatments for T1DM. After an evaluation of full-length papers from the PubMed database from 2010 to 2021, 20 trials were included for the final analysis. The analysis led to the following conclusions: Treg cells play an important role in the limitation of the development of T1DM, the activation or application of Tregs may be more effective in the early stages of T1DM development, and the therapeutic use of Treg cells in T1DM is promising but requires long-term observation in a large group of patients.     

The Effect of Conjugation with Octaarginine,a Cell-Penetrating Peptide on Antifungal Activity of Imidazoacridinone Derivative

Acridine cell-penetrating peptide conjugates are an extremely important family of compounds in antitumor chemotherapy. These conjugates are not so widely analysed in antimicrobial therapy, although bioactive peptides could be used as nanocarriers to smuggle antimicrobial compounds. An octaarginine conjugate of an imidazoacridinone derivative (Compound 1-R8) synthetized by us exhibited high antifungal activity against reference and fluconazole-resistant clinical strains (MICs ≤ 4 μg mL⁻¹). Our results clearly demonstrate the qualitative difference in accumulation of the mother compound and Compound 1-R8 conjugate into fungal cells. Only the latter was transported and accumulated effectively. Microscopic and flow cytometry analysis provide some evidence that the killing activity of Compound 1-R8 may be associated with a change in the permeability of the fungal cell membrane. The conjugate exhibited low cytotoxicity against human embryonic kidney (HEK-293) and human liver (HEPG2) cancer cell lines. Nevertheless, the selectivity index value of the conjugate for human pathogenic strains remained favourable and no hemolytic activity was observed. The inhibitory effect of the analysed compound on yeast topoisomerase II activity suggested its molecular target. In summary, conjugation with R8 effectively increased imidazoacridinone derivative ability to enter the fungal cell and achieve a concentration inside the cell that resulted in a high antifungal effect.     

Drying Characteristics of Barley Grain Dried in a Spouted-Bed and Combined IR-Convection Dryers

A study was performed to determine the drying characteristics and quality of barley grain dried in a laboratory scale spouted-bed dryer at 30, 35, 40, and 45°C and an inlet air velocity of 23 m/s^?1, and in an IR-convection dryer under an infrared radiation intensity of 0.048, 0.061, 0.073, and 0.107 W cm^?2 at an air velocity of 0.5 m/s^?1. The results show that the first, relatively short, phase of a sharp decrease in the drying rate was followed by the phase of a slow decrease. The time of barley drying depended on temperature of inlet air in a spouted-bed dryer and on radiation intensities in an IR-convection dryer. Barley drying at 45°C in a spouted-bed dryer was accompanied by the lowest total energy consumption. The average specific energy consumption was lower and the average efficiency of drying was higher for drying in a spouted-bed dryer. The effective diffusivities were in the range 2.20–4.52 × 10^?11 m² s^?1 and 3.04–4.79 × 10^?11 m²/s^?1 for barley dried in a spouted-bed and in an IR-convection dryer, respectively. There were no significant differences in kernel germination energy and capacity between the two drying methods tested.     

The structure of the [Et2In(μ,λ-O2C)–C6H4–2–NH2]∞ coordination polymer: Competition of intramolecular hydrogen bonding with metal–ligand coordination preferences in determining the molecular and crystal structure

The X-ray structure analysis of [Et₂In(μ,λ-O₂C)–C₆H₄–2–NH₂]_n (1) reveals an extended one-dimensional chain comprised of an array of five-coordinate indium centers. The chain unit repeated along two-fold screw axis is defined by the diethylindium moiety chelated asymmetrically by the carboxylate group with one of the two carboxylate oxygens acting as bridge to the next indium center in the chain. The NH₂ group does not participate in the coordination of the metal center but is involved in an intermolecular hydrogen bond.     

Accelerated,Microwave‐Assisted,and Conventional Solvent Extraction Methods Affect Anthocyanin Composition from Colored Grains

Anthocyanins are important dietary components with diverse positive functions in human health. This study investigates effects of accelerated solvent extraction (ASE) and microwave‐assisted extraction (MAE) on anthocyanin composition and extraction efficiency from blue wheat, purple corn, and black rice in comparison with the commonly used solvent extraction (CSE). Factorial experimental design was employed to study effects of ASE and MAE variables, and anthocyanin extracts were analyzed by spectrophotometry, high‐performance liquid chromatography‐diode array detector (DAD), and liquid chromatography–mass spectrometry chromatography. The extraction efficiency of ASE and MAE was comparable with CSE at the optimal conditions. The greatest extraction by ASE was achieved at 50 °C, 2500 psi, 10 min using 5 cycles, and 100% flush. For MAE, a combination of 70 °C, 300 W, and 10 min in MAE was the most effective in extracting anthocyanins from blue wheat and purple corn compared with 50 °C, 1200 W, and 20 min for black rice. The anthocyanin composition of grain extracts was influenced by the extraction method. The ASE extraction method seems to be more appropriate in extracting anthocyanins from the colored grains as being comparable with the CSE method based on changes in anthocyanin composition. The method caused lower structural changes in anthocaynins compared with the MAE method. Changes in blue wheat anthocyanins were lower in comparison with purple corn or black rice perhaps due to the absence of acylated anthocyanin compounds in blue wheat. The results show significant differences in anthocyanins among the 3 extraction methods, which indicate a need to standardize a method for valid comparisons among studies and for quality assurance purposes.     

A hybrid multi-objective immune algorithm for predictive and reactive scheduling

The high productivity of a production process has a major impact on the reduction of the production cost and on a quick response to changing demands. Information about a failure-free machine operation time obtained in advance allows the users to plan preventive maintenance in order to keep the machine in a good operational condition. The introduction of maintenance work into a schedule reduces the frequency of unpredicted breaks caused by machine failures. It also results in higher productivity and in-time production. The foregoing of this constitutes the main idea of the predictive scheduling method proposed in the paper. Rescheduling of disrupted operations, with a minimal impact on the stability and robustness of a schedule, is the main idea of the reactive scheduling method proposed. The first objective of the paper is to present a hybrid multi-objective immune algorithm (H-MOIA) aided by heuristics: a minimal impact of disrupted operation on the schedule (MIDOS) for predictive scheduling and a minimal impact of rescheduled operation on the schedule (MIROS) for reactive scheduling. The second objective is to compare the H-MOIA with various methods for predictive and reactive scheduling. The H-MOIA + MIDOS is compared to two algorithms, identified in reference publications: (1) an algorithm based on priority rules: the least flexible job first (LFJ) and the longest processing time (LPT) (2) an Average Slack Method. The H-MOIA + MIROS is compared to: (1) an algorithm based on priority rules: the LFJ and LPT and (2) Shifted Gap-Reduction. This paper presents the research results and computer simulations.