Glycosphingolipids (GSL) are functionally important components of the cell membrane and recognition of their glycan "head" by the immune system is a key part of normal and pathological processes. Recognition of glycolipid antigens on a living cell, their structure, "context" (microenvironment and clustering), presentation including orientation and distance from the plasma membrane, as well as molecular dynamics are important. GSL antigens are targets for the development of anticancer vaccines and therapeutic antibodies, therefore, control of the presentation of their glycans by synthetic methods opens up new possibilities in medicine.
View Article and Find Full Text PDFStereocontrolled 1,2-trans-α-arabinofuranosylation using polysilylated mono- and disaccharide glycosyl donors was investigated. A complete α-stereoselectivity of 1,2-trans-arabinofuranosylation was found for Ara-β-(1 → 2)-Ara disaccharide glycosyl donors containing five triisopropylsilyl (TIPS) groups with arylthiol (1) (as shown in our previous publications) or N-phenyltrifluoroacetimidoyl (2) (this work) leaving groups. Conversely, in case of monosaccharide thioglycosides polysilylated with acyclic silyl groups (TIPS, TBDPS), stereoselectivity of glycosylation was lower (α:β = 7-8:1), although the desired α-isomer still dominated.
View Article and Find Full Text PDFThe closed-loop control of pathological brain activity is a challenging task. In this study, we investigated the sensitivity of continuous epileptiform short discharge generation to electrical stimulation applied at different phases between the discharges using an in vitro 4-AP-based model of epilepsy in rat hippocampal slices. As a measure of stimulation effectiveness, we introduced a sensitivity function, which we then measured in experiments and analyzed with different biophysical and abstract mathematical models, namely, (i) the two-order subsystem of our previous Epileptor-2 model, describing short discharge generation governed by synaptic resource dynamics; (ii) a similar model governed by shunting conductance dynamics (Epileptor-2B); (iii) the stochastic leaky integrate-and-fire (LIF)-like model applied for the network; (iv) the LIF model with potassium M-channels (LIF+KM), belonging to Class II of excitability; and (v) the Epileptor-2B model with after-spike depolarization.
View Article and Find Full Text PDFLeukemia is the most common cancer in children. Its incidence has been increasing worldwide since 1910th, suggesting the presence of common sources of the disease, most likely related to people's lifestyle and environment. Understanding the relationship between childhood leukemia and environmental conditions is critical to preventing the disease.
View Article and Find Full Text PDFThe rapid increase in the antibiotic resistance of microorganisms, capable of causing diseases in humans as destroying cultural heritage sites, is a great challenge for modern science. In this regard, it is necessary to develop fundamentally novel and highly active compounds. In this study, a series of -alkylcytidines, including 5- and 6-methylcytidine derivatives, with extended alkyl substituents, were obtained in order to develop a new generation of antibacterial and antifungal biocides based on nucleoside derivatives.
View Article and Find Full Text PDFGlycosyl halides are historically one of the first glycosyl donors used in glycosylation reactions, and interest in glycosylation reactions involving this class of glycosyl donors is currently increasing. New methods for their activation have been proposed and effective syntheses of oligosaccharides with their participation have been developed. At the same time, the possibilities of using these approaches to the synthesis of sialosides are restricted by the limited diversity of known sialyl halides (previously, mainly sialyl chlorides, less often sialyl bromides and sialyl fluorides, with acetyl (Ac) groups at the oxygen atoms and AcNH, AcN and N groups at C-5 were used).
View Article and Find Full Text PDFThe marine flavobacterium Krokinobactereikastus light-driven sodium pump (KR2) generates an outward sodium ion current under 530 nm light stimulation, representing a promising optogenetic tool for seizure control. However, the specifics of KR2 application to suppress epileptic activity have not yet been addressed. In the present study, we investigated the possibility of KR2 photostimulation to suppress epileptiform activity in mouse brain slices using the 4-aminopyrindine (4-AP) model.
View Article and Find Full Text PDFApparent motion is a visual illusion in which stationary stimuli, flashing in distinct spatial locations at certain time intervals, are perceived as one stimulus moving between these locations. In the primary visual cortex, apparent-motion stimuli produce smooth spatio-temporal patterns of activity similar to those produced by continuously moving stimuli. An important prerequisite for producing such activity patterns is prolongation of responses to brief stimuli.
View Article and Find Full Text PDFA variety of ribo-, 2'-deoxyribo-, and 5'-norcarbocyclic derivatives of the 8-aza-7-deazahypoxanthine fleximer scaffolds were designed, synthesized, and screened for antibacterial activity. Both chemical and chemoenzymatic methods of synthesis for the 8-aza-7-deazainosine fleximers were compared. In the case of the 8-aza-7-deazahypoxanthine fleximer, the transglycosylation reaction proceeded with the formation of side products.
View Article and Find Full Text PDFThe reaction of aromatic ring-substituted isoselenocyanates with 2-thiopheacetic and 4-pyridinecarboxylic acid hydrazides yielded selenosemicarbazides which were further converted into previously unknown 1,2,4-triazole-3-selones and 3,3'-di(4H-1, 2,4-triazolyl)diselenides. The structures of the obtained compounds were studied by NMR spectroscopy, IR spectroscopy, and high-resolution mass spectroscopy (HR-MS). The bactericidal and fungicidal activity of some obtained compounds was evaluated in molecular modeling studies such as docking and simulation studies.
View Article and Find Full Text PDFBase-promoted (MeONa in MeOH or imidazole in DMF) isomerization of a series of 3,4,6-tri-O-benzyl-d-gluco- and d-mannopyranose derivatives with triisopropylsilyl (TIPS) substituents was studied. The presence of a bulky TIPS group at O-1 or O-2 was shown to be favorable for the isomerization of benzyl protected d-gluco- and d-mannopyranose derivatives to d-fructofuranose derivatives, in which the bulky silyl group occupies less sterically hindered primary position. The highest yield (33%) of the fructofuranose derivative was achieved when 3,4,6-tri-O-benzyl-2-O-triisopropylsilyl-d-mannopyranose was treated with MeONa in MeON at 50 °C.
View Article and Find Full Text PDFFor single neuron models, reproducing characteristics of neuronal activity such as the firing rate, amplitude of spikes, and threshold potentials as functions of both synaptic current and conductance is a challenging task. In the present work, we measure these characteristics of regular spiking cortical neurons using the dynamic patch-clamp technique, compare the data with predictions from the standard Hodgkin-Huxley and Izhikevich models, and propose a relatively simple five-dimensional dynamical system model, based on threshold criteria. The model contains a single sodium channel with slow inactivation, fast activation and moderate deactivation, as well as, two fast repolarizing and slow shunting potassium channels.
View Article and Find Full Text PDFBackground: This study explores the regional variations in toxic metal accumulation among RUDN University students from various global regions.
Methods: This comparative analysis examined hair samples from students hailing from different regions, including Russia, Asia, the Middle East, Africa, and Latin America. The concentrations of Aluminium (Al), Arsenic (As), Cadmium (Cd), Mercury (Hg), Lead (Pb), and Tin (Sn) were measured in the hair samples.
The emergence of drug-resistant strains of pathogenic microorganisms necessitates the creation of new drugs. A series of uridine derivatives containing an extended substituent at the C-5 position as well as C-5 alkyloxymethyl, alkylthiomethyl, alkyltriazolylmethyl, alkylsulfinylmethyl and alkylsulfonylmethyl uridines were obtained in order to explore their antimicrobial properties and solubility. It has been shown that new ribonucleoside derivatives have an order of magnitude better solubility in water compared to their 2'-deoxy analogues and effectively inhibit the growth of a number of Gram-positive bacteria, including resistant strains of Mycobacterium smegmatis (MIC=15-200 μg/mL) and Staphylococcus aureus (MIC=25-100 μg/mL).
View Article and Find Full Text PDFThe paper simulates the process of the migration of a single energy excitation along a chain of tryptophans in cell microtubules connected by dipole-dipole interaction. The paper shows that the excited states propagation rate falls within the range of nerve impulse velocity. It was shown that such a process also causes a transfer of quantum entanglement between tryptophans, so that microtubules can be considered as signaling system, the basis for transmitting information via the quantum channel.
View Article and Find Full Text PDFThe biogenic polyamines, spermidine (Spd) and spermine (Spm), are present at millimolar concentrations in all eukaryotic cells, where they participate in the regulation of vitally important cellular functions. Polyamine analogs and derivatives are a traditional and important instrument for the investigation of the cellular functions of polyamines, enzymes of their metabolism, and the regulation of the biosynthesis of antizyme-a key downregulator of polyamine homeostasis. Here, we describe convenient gram-scale syntheses of a set of -methylated analogs of Spd.
View Article and Find Full Text PDFZinc oxide is one of the well-known photocatalysts, the potential applications of which are of great importance in photoactivated gas sensing, water and air purification, photocatalytic synthesis, among others. However, the photocatalytic performance of ZnO strongly depends on its morphology, composition of impurities, defect structure, and other parameters. In this paper, we present a route for the synthesis of highly active nanocrystalline ZnO using commercial ZnO micropowder and ammonium bicarbonate as starting precursors in aqueous solutions under mild conditions.
View Article and Find Full Text PDFis a critical priority nosocomial pathogen that produces a variety of capsular polysaccharides (CPSs), the primary receptors for specific depolymerase-carrying phages. In this study, the tailspike depolymerases (TSDs) encoded in genomes of six novel Friunaviruses, APK09, APK14, APK16, APK86, APK127v, APK128, and one previously described phage, APK37.1, were characterized.
View Article and Find Full Text PDFPhotoactivation by UV and visible radiation is a promising approach for the development of semiconductor gas sensors with reduced power consumption, high sensitivity, and stability. Although many hopeful results were achieved in this direction, the theoretical basis for the processes responsible for the photoactivated gas sensitivity still needs to be clarified. In this work, we investigated the mechanisms of UV-activated processes on the surface of nanocrystalline ZnO, InO, and SnO by in situ mass spectrometry and compared the obtained results with the gas sensitivity to oxygen in the dark and at UV irradiation.
View Article and Find Full Text PDFLow-frequency electrical stimulation is used to treat some drug-resistant forms of epilepsy. Despite the effectiveness of the method in suppressing seizures, there is a considerable risk of side effects. An optogenetic approach allows the targeting of specific populations of neurons, which can increase the effectiveness and safety of low-frequency stimulation.
View Article and Find Full Text PDFIn this work, colloidal perovskite nanocrystals (PNCs) are used to sensitize the photoconductivity of nanocrystalline ZnO films in the visible range. Nanocrystalline ZnO with a crystallite size of 12-16 nm was synthesized by precipitation of a zinc basic carbonate from an aqueous solution, followed by annealing at 300 °C. Perovskite oleic acid- and oleylamine-capped CsPbBr, CsPb(Cl/Br) and CsPb(Br/I) PNCs with a size of 6-13 nm were synthesized by a hot injection method at 170 °C in 1-octadecene.
View Article and Find Full Text PDFA structurally diverse capsular polysaccharide (CPS) in the outer cell envelope plays an important role in the virulence of the important bacterial pathogen, Acinetobacter baumannii. More than 75 different CPS structures have been determined for the species to date, and many CPSs include isomers of a higher sugar, namely 5,7-diamino-3,5,7,9-tetradeoxynon-2-ulosonic acid. Recently, a novel isomer having the d-glycero-l-manno configuration (5,7-di-N-acetyl-8-epipseudaminic acid; 8ePse5Ac7Ac) has been identified in the CPS from A.
View Article and Find Full Text PDFCytokinins, classical phytohormones, affect all stages of plant ontogenesis, but their application in agriculture is limited because of the lack of appropriate ligands, including those specific for individual cytokinin receptors. In this work, a series of chiral -benzyladenine derivatives were studied as potential cytokinins or anticytokinins. All compounds contained a methyl group at the α-carbon atom of the benzyl moiety, making them - or -enantiomers.
View Article and Find Full Text PDFMolecules
September 2022
A practical method for the synthesis of 2-selenoxo-1,2,3,4-tetrahydro-4-quinazolinone was reported. The latter compounds were found to undergo facile oxidation with HO into corresponding diselenides. Novel organoselenium derivatives were characterized by the H, Se, and C NMR spectroscopies, high-resolution electrospray ionization mass spectrometry, IR, elemental analyses (C, H, N), and X-ray diffraction analysis for several of them.
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