Smart photopharmacological agents: LaVO:Eu@vinyl phosphonate combining luminescence imaging and photoswitchable butyrylcholinesterase inhibition.

The combination of photoswitchability and bioactivity in one compound provides interesting opportunities for photopharmacology. Here, we report a hybrid compound that in addition allows for its visual localization. It is the first demonstration of its kind and it even shows high photoswitchability.

[The impact of digital technologies on labor organization in health care scope].

Enhancement of the health care system in Russia continues to be one of key directions of National development. In conditions of deficiency of personnel, systemic changes are needed to transit to qualitatively new level. The application of digital platforms permits to resolve a number of issues related to accessibility and quality of medical services.

All-in-One Photoactivated Inhibition of Butyrylcholinesterase Combined with Luminescence as an Activation and Localization Indicator: Carbon Quantum Dots@Phosphonate Hybrids.

Photopharmacology is a booming research area requiring a new generation of agents possessing simultaneous functions of photoswitching and pharmacophore. It is important that any practical implementation of photopharmacology ideally requires spatial control of the medicinal treatment zone. Thus, advances in the study of substances meeting all the listed requirements will lead to breakthrough research in the coming years.

Artificial genetic polymers against human pathologies.

Originally discovered by Nielsen in 1991, peptide nucleic acids and other artificial genetic polymers have gained a lot of interest from the scientific community. Due to their unique biophysical features these artificial hybrid polymers are now being employed in various areas of theranostics (therapy and diagnostics). The current review provides an overview of their structure, principles of rational design, and biophysical features as well as highlights the areas of their successful implementation in biology and biomedicine.

Photoswitchable Phosphonate-Fullerene Hybrids with Cholinesterase Activity.

Modern progress in photopharmocology calls for new generation of compounds joining bioactivity, photoswitchable properties and high selectivity of response to light wavelength. Introduced here, phosphonate-fullerene hybrids are the first representatives of such compounds. Phosphonate-fullerene hybrids were synthesized on a base of fullerene C and organophosphates with the function of photoswitchable cholinesterase activity-phosphorylated thiazolotriazole and aminomalonate compounds and studied with FTIR, UV-VIS spectroscopy and IPC-micro neurotoxin amperometric analysis.

Theranostic Platforms Based on Silica and Magnetic Nanoparticles Containing Quinacrine, Chitosan, Fluorophores, and Quantum Dots.

In this paper, we describe the synthesis of multilayer nanoparticles as a platform for the diagnosis and treatment of ischemic injuries. The platform is based on magnetite (MNP) and silica (SNP) nanoparticles, while quinacrine is used as an anti-ischemic agent. The synthesis includes the surface modification of nanoparticles with (3-glycidyloxypropyl)trimethoxysilane (GPMS), the immobilization of quinacrine, and the formation of a chitosan coating, which is used to fix the fluorophore indocyanine green (ICG) and colloidal quantum dots AgInS/ZnS (CQDs), which serve as secondary radiation sources.

[Nutrition and body composition in young women with various leptin and ghrelin levels].

Body mass and its composition depend on the energy equilibrium due to the consumption of energy-intensive macronutrients and energy expenditure under strict neuroendocrine control. Leptin and ghrelin are the most important regulators of the energy balance; they modulate the redistribution of substrate flows in metabolic pathways. of the research was the assessment of nutrient intake in conjunction with the analysis of body composition and primarily hormonal regulators of energy balance in young women with various body mass index (BMI) values.

Preliminary Assessment of the Anti-inflammatory Activity of New Structural Honokiol Analogs with a 4'--(2-Fluoroethyl) Moiety and the Potential of Their F-Labeled Derivatives for Neuroinflammation Imaging.

Neolignans honokiol and 4'--methylhonokiol (MH) and their derivatives have pronounced anti-inflammatory activity, as evidenced by numerous pharmacological studies. Literature data suggested that cyclooxygenase type 2 (COX-2) may be a target for these compounds in vitro and in vivo. Recent studies of [C]MPbP () biodistribution in LPS (lipopolysaccharide)-treated rats have confirmed the high potential of MH derivatives for imaging neuroinflammation.

Inhibition of Neutrophil Elastase and Cathepsin G As a New Approach to the Treatment of Psoriasis: From Fundamental Biology to Development of New Target-Specific Drugs.

Psoriasis therapy remains an extremely relevant area of modern drug design, due to necessity of adverse reaction reduction, inherent for actual methods of therapy. It was established that two serine proteases-neutrophil elastase 1 (HNE1) and cathepsin G (CatG)-are the key agents in psoriasis development. The collected molecular data for the presented targets form the basis for the molecular modeling strategy for the search for and identification of new target-specific inhibitors.

An Integrated Method of Instrumental Microbiotesting of Environmental Safety of Various Products, Wastes, and Territories.

The described microbiotesting technique provides the recording of pH changes, redox potential, electrical conductivity, optical density, light scattering and luminescence intensities, and other parameters of samples with viable test microorganisms incubated in a liquid nutrient medium in the presence and absence of the tested factors. The results of using this system for the analysis of pro- and antibiotic activity of various oil products, as well as weak electromagnetic fields of the megahertz range, are presented. It has been shown that the proposed technique, compared to the standard methods, yields more detailed and objective information and is less time- and labor-consuming.

Flow cytometric HyPer-based assay for hydrogen peroxide.

HyPer is a genetically encoded fluorogenic sensor for hydrogen peroxide which is generally used for the ratiometric imaging of HO fluxes in living cells. Here, we demonstrate the advantages of HyPer-based ratiometric flow cytometry assay for HO, by using K562 and human mesenchymal stem cell lines expressing HyPer. We show that flow cytometry analysis is suitable to detect HyPer response to submicromolar concentrations of extracellularly added HO that is much lower than concentrations addressed previously in the other HyPer-based assays (such as cell imaging or fluorimetry).

Luminescence of Eu ions in hybrid polymer-inorganic composites based on poly(methyl methacrylate) and zirconia nanoparticles.

Spherical nanoparticles of ZrO with 2 and 10 mol% EuO up to 20 nm size were prepared by the method of hydrothermal synthesis for luminescent functionalization of the polymer-inorganic nanocomposites based on poly(methyl methacrylate). Surface modification of oxide nanoparticles was carried out by 3-(trimethoxysilyl)propyl methacrylate, dimethoxymethylvinyl silane and 2-hydroxyethyl methacrylate to provide uniform distribution and to prevent agglomeration of nanosized filler in the polymer matrix. Polymer-inorganic composites were synthesized by in situ free radical polymerization in bulk.

A new tridecapeptide with an octaarginine vector has analgesic therapeutic potential and prevents morphine-induced tolerance.

A growing body of evidence suggests that peptides may possess analgesic effects without tolerance development. The synthetic tetrapeptide Tyr-d-Arg-Phe-Gly-NH was modified with the inclusion of a (d-Arg) vector to prevent the action of endopeptidase and to increase the duration of the analgesic action of the tetrapeptide when administered orally. The aim of this study was to estimate the analgesic efficacy of the tetrapeptide with (d-Arg) (tridecapeptide, TDP) in experimental models of acute and chronic pain.

Biodegradable Micellar HPMA-Based Polymer-Drug Conjugates with Betulinic Acid for Passive Tumor Targeting.

Here, we present the synthesis, physicochemical, and preliminary biological characterization of micellar polymer-betulinic acid (BA) conjugates based on N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer carriers, enabling the controlled release of cytotoxic BA derivatives in solid tumors or tumor cells. Various HPMA copolymer conjugates differing in the structure of the spacer between the drug and the carrier were synthesized, all designed for pH-triggered drug release in tumor tissue or tumor cells. The high molecular weight of the micellar conjugates should improve the uptake of the drug in solid tumors due to the Enhanced permeability and retention (EPR) effect.

The 26S proteasome is a multifaceted target for anti-cancer therapies.

Proteasomes play a critical role in the fate of proteins that are involved in major cellular processes, including signal transduction, gene expression, cell cycle, replication, differentiation, immune response, cellular response to stress, etc. In contrast to non-specific degradation by lysosomes, proteasomes are highly selective and destroy only the proteins that are covalently labelled with small proteins, called ubiquitins. Importantly, many diseases, including neurodegenerative diseases and cancers, are intimately connected to the activity of proteasomes making them an important pharmacological target.

[Activity of the key enzymes in xylose-assimilating yeasts at different rates of oxygen transfer to the fermentation medium].

The activities of xylitol dehydrogenase and xylose reductase in the yeasts Candida shehatae, C. didensiae, C. intermediae, C.

[The activity of xylose reductase and xylitol dehydrogenase in yeasts].

The activity and the cofactor specificity of xylose reductase and xylitol dehydrogenase were studied in extracts of yeasts from the genera Candida, Kluyveromyces, Pachysolen, Pichia, and Torulopsis grown under microaerobic conditions. It was found that xylitol dehydrogenase in all of the yeast species studied is specific for NAD+; xylose reductase in the xylitol-producing species C. didensiae, C.

[Mycelial waste of tetracycline production as a component of the nutrient medium].

A new composition of the nutrient medium for cultivation of the tetracycline-producing organism was developed with the fermentative hydrolysate of the tetracycline production mycelial waste as a source of nitrogen: 0.02 to 0.04 g/l by amino nitrogen.