Conjugates of nucleobases with triazole-hydroxamic acids for the reactivation of acetylcholinesterase and treatment of delayed neurodegeneration induced by organophosphate poisoning.

A series of new uncharged conjugates of adenine, 3,6-dimetyl-, 1,6-dimethyl- and 6-methyluracil with 1,2,4-triazole-3-hydroxamic and 1,2,3-triazole-4-hydroxamic acid moieties were synthesized and studied as reactivators of organophosphate-inhibited cholinesterase. It is shown that triazole-hydroxamic acids can reactivate acetylcholinesterase (AChE) inhibited by paraoxon (POX) in vitro, offering reactivation constants comparable to those of pralidoxime (2-PAM). However, in contrast to 2-PAM, triazole-hydroxamic acids demonstrated the ability to reactivate AChE in the brain of rats poisoned with POX.

Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety.

We report herein the design, synthesis and biological evaluation of series of 7-substituted fluoroquinolones with pyridoxine derivatives. In vitro screening of antibacterial activity and toxicity of 39 synthesized fluoroquinolones defined compounds 7 and 28 as lead compounds for further investigations. On various clinical isolates lead compounds 7 and 28 exhibited antibacterial activity comparable with reference fluoroqinolones.

A Switch from Latent to Typical Infection during -Tobacco Interactions: Predicted and True Molecular Players.

Phytopathogenic microorganisms, being able to cause plant diseases, usually interact with hosts asymptomatically, resulting in the development of latent infections. Knowledge of the mechanisms that trigger a switch from latent to typical, symptomatic infection is of great importance from the perspectives of both fundamental science and disease management. No studies to date have compared, at the systemic molecular level, the physiological portraits of plants when different infection types (typical and latent) are developed.

Integrated Multiresonator Quantum Memory.

We develop an integrated efficient multiresonator quantum memory scheme based on a system of three interacting resonators coupled through a common resonator to an external waveguide via switchable coupler. It is shown that high-precision parameter matching based on step-by-step optimization makes it possible to efficiently store the signal field and enables on-demand retrieval of the signal at specified time moments. Possible experimental implementations and practical applications of the proposed quantum memory scheme are discussed.

The Role of Intercellular Signaling in the Regulation of Bacterial Adaptive Proliferation.

Bacterial adaptation is regulated at the population level with the involvement of intercellular communication (quorum sensing). When the population density is insufficient for adaptation under starvation, bacteria can adjust it to a quorum level through cell divisions at the expense of endogenous resources. This phenomenon has been described for the phytopathogenic bacterium (), and it is called, in our study, adaptive proliferation.

Sympathetic Innervation and Endogenous Catecholamines in Neuromuscular Preparations of Muscles with Different Functional Profiles.

Influence of the sympathetic nervous system on the work of skeletal muscles contractile apparatus is now beyond doubt. However, until recently there was no evidence that the endings of sympathetic nerves can be located in close proximity to the neuromuscular synapses, and there is also no reliable data on how much endogenous adrenaline and noradrenaline can be contained near the synaptic contact in skeletal muscles. In this research, using fluorescent analysis, immunohistochemical and enzyme immunoassays the isolated neuromuscular preparations of three skeletal muscles of different functional profiles and containing different types of muscle fibers were examined.

Improving meat qualities of pigs after deworming against ascariasis with administered glycyrrhizic acid.

The present paper describes the effect of glycyrrhizic acid contained in licorice roots on the quality of pork produced. The study uses advanced research methods as ion-exchange chromatography, inductively coupled plasma mass spectrometry, drying of an average sample of muscle, and pressing method. The paper set out to investigate the effect of glycyrrhizic acid on the pig meat quality after deworming.

Complete Genome Sequences of sp. Strains B-10 and H-1, Isolated from the Water in the Shulgan-Tash Cave.

In this article, we report the complete genome sequences of sp. strains B-10 (RCAM05335) and H-1 (RCAM05339), which were isolated from the water of the Dal'nee Verkhnee Lake in the Shulgan-Tash cave in Russia (53°2'0″N, 57°3'0″E). The sequences were obtained using an Oxford Nanopore Technologies MinION system.

First genome-scale insights into the virulence of the snow mold causal fungus Microdochium nivale.

Pink snow mold, caused by a phytopathogenic and psychrotolerant fungus, Microdochium nivale, is a severe disease of winter cereals and grasses that predominantly occurs under snow cover or shortly after its melt. Snow mold has significantly progressed during the past decade, often reaching epiphytotic levels in northern countries and resulting in dramatic yield losses. In addition, M.

Isolation and Characterization of 1-Hydroxy-2,6,6-trimethyl-4-oxo-2-cyclohexene-1-acetic Acid, a Metabolite in Bacterial Transformation of Abscisic Acid.

We report the discovery of a new abscisic acid (ABA) metabolite, found in the course of a mass spectrometric study of ABA metabolism by the rhizosphere bacterium sp. P1Y. Analogue of (+)-ABA, enriched in tritium in the cyclohexene moiety, was fed in bacterial cells, and extracts containing radioactive metabolites were purified and analyzed to determine their structure.

Resistance to Snow Mold as a Target Trait for Rye Breeding.

Winter rye is a versatile crop widely used for food and industry. Although rye is resistant to abiotic stressors and many phytopathogens, it is severely damaged by pink snow mold (SM)-a progressive disease caused by the psychrotolerant fungus under the snow cover or during prolonged periods of wet and cool conditions. Due to little use of the SM resistance sources in contemporary breeding, varieties with at least moderate resistance to SM are limited.

Plant Polysaccharide Array for Studying Carbohydrate-Binding Proteins.

The specificity of the most plant carbohydrate-binding proteins (CBP), many of which are known only through bioinformatic analysis of the genome, has either not been studied at all or characterized to a limited extent. The task of deciphering the carbohydrate specificity of the proteins can be solved using glycoarrays composed of many tens or even hundreds of glycans immobilized on a glass surface. Plant carbohydrates are the most significant natural ligands for plant proteins; this work shows that plant polysaccharides without additional modification can be immobilized on the surface, bearing N-hydroxysuccinimide activated carboxyl groups.

Is RsfS a Hibernation Factor or a Ribosome Biogenesis Factor?

Solving the structures of bacterial, archaeal, and eukaryotic ribosomes by crystallography and cryo-electron microscopy has given an impetus for studying intracellular regulatory proteins affecting various stages of protein translation. Among them are ribosome hibernation factors, which have been actively investigated during the last decade. These factors are involved in the regulation of protein biosynthesis under stressful conditions.

Stone Age genomes shed light on the early evolution, diversity, and ecology of plague.

The bacterial pathogen Yersinia pestis gave rise to devastating outbreaks throughout human history, and ancient DNA evidence has shown it afflicted human populations as far back as the Neolithic. Y. pestis genomes recovered from the Eurasian Late Neolithic/Early Bronze Age (LNBA) period have uncovered key evolutionary steps that led to its emergence from a Yersinia pseudotuberculosis-like progenitor; however, the number of reconstructed LNBA genomes are too few to explore its diversity during this critical period of development.

Alterations in the Transcriptome of Rye Plants following the Infection: Identification of Resistance/Susceptibility-Related Reactions Based on RNA-Seq Analysis.

is a progressive and devastating phytopathogen that causes different types of cereal crop and grass diseases that are poorly characterized at the molecular level. Although rye ( L.) is one of the most resistant crops to most of the phytopathogens, it is severely damaged by .

α-tocopherol, a slow-binding inhibitor of acetylcholinesterase.

Acetylcholinesterase (AChE) is reversibly inhibited by α-tocopherol (α-T). Steady state kinetic analysis shows that α-T is a mixed slow-binding inhibitor of type A of human enzyme (K = 0.49 μM; K = 1.

Cappable-Seq Reveals Specific Patterns of Metabolism and Virulence for Typhimurium Intracellular Survival within .

The bacterial pathogen , which causes enteritis, has a broad host range and extensive environmental longevity. In water and soil, Salmonella interacts with protozoa and multiplies inside their phagosomes. Although this relationship resembles that between and mammalian phagocytes, the interaction mechanisms and bacterial genes involved are unclear.

Protective effects of m-(tert-butyl) trifluoroacetophenone, a transition state analogue of acetylcholine, against paraoxon toxicity and memory impairments.

m-(Tert-butyl) trifluoroacetophenone (TFK), a slow-binding inhibitor of acetylcholinesterase (AChE), a transition state analog of acetylcholine, was investigated as a potential neuroprotectant of central and peripheral AChE against organophosphate paraoxon (POX) toxicity. Acute toxicity and pharmacological effects of TFK were investigated on mice and rats. Intraperitoneal administered TFK has low acute toxicity in mice (LD ≈ 19 mg/kg).

The protealysin operon encodes emfourin, a prototype of a novel family of protein metalloprotease inhibitors.

Protealysin is a Serratia proteamaculans metalloproteinase of the M4 peptidase family and the prototype of a large group of protealysin-like proteases (PLPs). PLPs are likely involved in bacterial interaction with plants and animals as well as in bacterial pathogenesis. We demonstrated that the PLP genes in bacteria colocalize with the genes of putative conserved proteins.

1-(3--Butylphenyl)-2,2,2-Trifluoroethanone as a Potent Transition-State Analogue Slow-Binding Inhibitor of Human Acetylcholinesterase: Kinetic, MD and QM/MM Studies.

Kinetic studies and molecular modeling of human acetylcholinesterase (AChE) inhibition by a fluorinated acetophenone derivative, 1-(3-tert-butylphenyl)-2,2,2-trifluoroethanone (TFK), were performed. Fast reversible inhibition of AChE by TFK is of competitive type with = 5.15 nM.

Slow-binding reversible inhibitor of acetylcholinesterase with long-lasting action for prophylaxis of organophosphate poisoning.

Organophosphorus (OP) compounds represent a serious health hazard worldwide. The dominant mechanism of their action results from covalent inhibition of acetylcholinesterase (AChE). Standard therapy of acute OP poisoning is partially effective.

Platinum-Catalyzed Hydrosilylation in Polymer Chemistry.

This paper addresses a review of platinum-based hydrosilylation catalysts. The main field of application of these catalysts is the curing of silicone polymers. Since the 1960s, this area has developed rapidly in connection with the emergence of new polymer compositions and new areas of application.

Interpretation of the Nature of the Mixed Form of Resonance Lines of the Electron Paramagnetic Resonance Spectrum in a New Paradigm of Spin Exchange: Abnormal "Resonance" of Non-Resonant Spins.

It is shown that the asymmetric shape of lines in the electron paramagnetic resonance spectra of paramagnetic particle solutions caused by spin exchange in bimolecular particle collisions is due to the fact that, in the experiment, under the conditions of slow spin exchange, an absorption signal of nominally resonant spins and a "resonance" dispersion signal of nominally nonresonant spins with an abnormal phase of their quantum coherence are registered simultaneously. The mixing of these two signals is different for different resonance lines in the observed spectrum. A phenomenological model is proposed that can be used to find the phase of the "resonance" signal of non-resonant spins.

Melanin from the Lichens Cetraria islandica and Pseudevernia furfuracea: Structural Features and Physicochemical Properties.

Lichens are symbiotic photosynthesizing organisms with thalli formed by fungi and algae/cyanobacteria that possess high stress tolerance. One of the factors that contributes to the ability of a lichen to tolerate harsh environmental conditions is the presence of unique metabolites, including high-molecular-weight dark pigments termed melanins. The chemical composition and structure of lichen melanins remain poorly studied.

Observation of Acoustically Induced Transparency for γ-Ray Photons.

We report an observation of a 148-fold suppression of resonant absorption of 14.4 keV photons from exp(-5.2) to exp(-0.