Home – Home – Jornals – Advanced Search

The article presents and discusses the statement of the problem, goals and objectives, methodology, tools, software and research results obtained during the development of the prototype information and analytical system “Ecological Barometer”. A review of research in the area of knowledge under discussion has been completed. A system of characteristics for measuring the level of environmental safety is outlined. Sources of primary data are described in detail. The system involves the implementation of monitoring and analysis of key characteristics of the state of the environment based on data obtained using artificial intelligence technologies.

The article deals with the use of interactive seminar model for the development of professional competencies and activation of scientific activity of students in the discipline “Life Safety”. Traditional formats of seminars in higher education have their disadvantages. The interactive workshop model developed by the author, using the “Workshop” module in the Moodle learning management system, includes such elements as discussions, collective assessment, small group work, surveys, questionnaires and webinars. These activities promote critical thinking, collaboration, and active student participation. This model addresses the shortcomings of traditional seminars and improves the quality of research papers, deepens the understanding of compulsory disciplines and prepares students for scientific endeavors.

The authors propose a sequence of acquisition and interpretation of geospatial data obtained using different methods and means during mineral mining toward the accuracy increase in evaluation of industrially disturbed land. This approach uses the concept of stage-wise transition from the areas of industrial facilities to their individual points. The integration of data of satellite surveys, ground-based laser scanning and unmanned aerial surveillance in the digital models of land areas is described. It is highlighted that the rational combination of different methods of geospatial data acquisition and interpretation produces a high-accurate geoinformation system of digital twins of various subsoil use facilities.

The content and composition of 19 priority polycyclic aromatic hydrocarbons (PAH) in the rocks and soils of dumps, mushrooms growing on them ( Verpa bohemica and Suillus luteus ), as well as infiltrated and thawed snow waters on the territory of the Gorlovo anthracite deposit were evaluated. It is shown that the main source of PAH in the components of technogenic and adjacent natural landscapes of the deposit are fine coal particles and products of their transformation of non-pyrogenic nature. The flux of PAH into the components of the environment occurs due to: 1) dust fallout near the road along which the extracted coal is transported; 2) transformation of anthracite inclusions in the upper horizons of coal-bearing soils of dumps; 3) migration of transformation products with infiltrated waters. A distinctive feature of the composition of PAH in the samples of the studied objects is the predominance of light PAH (LPAH) in rocks and coals and heavy PAH (HPAH) in infiltrated and thawed snow waters. The composition of the polyarenes of rocks is dominated by PHE (phenanthrene) > FLT fluoranthene) > NAP (naphthalene), waters - FLT > PYR (pyrene) > CHR (chrysene). The composition of PAH of soils depends on the presence of coal inclusions. For carbonaceous soils, the predominant polyarenes are FLT > PYR > PHE = CHR. With depth in soils, the composition of PAHs changes and becomes close to the composition of soil-forming rocks. Mushrooms have a selective ability to absorb PAH. Regardless of the presence of coal in the soils on which the mushrooms grow, the predominant compounds are FLT for V. bohemica and PHE for S. luteus . Based on the results of the analysis of the main components, as well as the correlation of the priority PAH indices with their total content and the content of carcinogenic polyarenes, it has been found that the most representative ratios for assessing the impact of technogenic sources associated with anthracite extraction and transportation are PHE/(PHE + CHR) and ΣLPAH/ΣHPAH.

The anti-inflammatory and analgesic activity of three azaadamantane analogues of amantadine 1 was investigated. The tested azaadamantanes containing nitrogen atoms in the polycyclic framework were: 5,7-dimethyl-1,3-diazaadamantane-6-one 2, 6-amino-5,7-dimethyl-1,3-diazaadamantane 3 and 7-amino-1,3,5-triazaadamantane 4. Experiments were carried out on male mice of CD1 and CBA lines. Compounds were administered intraperitoneally at doses of 20 and 50 mg/kg. Anti-inflammatory activity was studied on the standard models of inflammatory edema induced by histamine or concanavaline inflammation by injecting the phlogogens in the aponeurosis of the hind paw of mice. The analgesic activity was assessed using the hot plate and acetic writhing tests. It is shown that the introduction of heteroatoms into the adamantane core does not reduce the anti-inflammatory activity of diazaadamantanes (2, 3) and enhances that of triazaadamantane (4) compared to amantadine. Modification of the adamantane backbone with nitrogen atoms leads to a change in the analgesic properties of the molecule, which is manifested as hyperalgesia in the acetic writhing test. This phenomenon is presumably related to the effect of azaadamantanes on nocigenic transient receptor potential channels (TRPV1).

Tyrosyl-DNA phosphodiesterases 1 and 2 (Tdp1 and Tdp2) are DNA repair enzymes that are considered as potential targets for antitumour supporting therapy in combination with topoisomerase inhibitors. The most effective Tdp1 inhibitors were found among the derivatives of the lichen secondary metabolite usnic acid. The sensitising effect of these compounds in combination with the topoisomerase 1 inhibitor topotecan was confirmed in cell culture experiments and animal models. In the present work, we describe new derivatives of usnic acid synthesized on the basis of previously obtained Tdp1 inhibitors by introducing the pyrazole cycle annelated with the C ring in dibenzofuran backbone, which makes it possible to reduce the intrinsic toxicity of the obtained compounds. New dual Tdp1 and Tdp2 inhibitors in the micromolar range of concentrations are found.

A new usnic acid derivative containing cyanethyl and isoniazid fragments is synthesised. The compound inhibits the activity of DNA repair enzyme Tdp1 with IC₅₀ = 1.2 μM, is inactive against Tdp2 and does not affect cell survival for a panel of passaged cell lines in the concentration range up to 20 μM. It is shown that the compound in combinations with the certain concentrations of antitumour drugs can sensitise the effect of antitumour drugs olaparib and temozolomide on some cell lines.

15-Acetyl- and 16-acetylfuranolabdanoids were synthesised by the acetylation of the methyl ester of lambertianic acid with acetic anhydride in the presence of Mg(ClO₄)₂ and used as starting compounds for the preparation of 15- or 16-(3-aminopropanoyl)methyllambertianates. The proposed approach involved silylation of 15-acetyl- or 16-acetylmethyllambertianate and the Mannich reaction of the resulting enol silyl ester with N,N-disubstituted methyleneiminium salts. The synthesized compounds possessed cytotoxicity on tumour cell lines CCRF CEM, MCF7 and PC-3 (MTT test). The compounds containing a 3-morpholinopropanoyl or 3-pyrrolidinopropanoyl substituent at the C-16 position of methyl lambertianate selectively inhibited the growth of human T-cell leukemia cells (GI₅₀ was 5.8-6.1 μM) and exhibited cytotoxicity an order of magnitude higher than the parent compound lambertianic acid.

The use of the available synthetic platform of 5-ethynyl-N-(acetyl)anthranilic acid in the synthesis of a chemical library of 2,4-diaryl-3H-1,5-benzodiazepines is proposed. The key step of the synthesis included the reaction of in situ generated methyl 2-acetylamino-5-[3-(4-aryl)propiolyl]benzoate with o-phenylenediamine. The selected conditions were used for the synthesis of a chemical library of 3H-1,5-benzodiazepines containing an anthranilic acid methyl ester fragment in the C-2 position. The physicochemical characteristics of intermediately formed α,β-alkynyl ketones are also described.

The dependence of mechanical characteristics (hardness and tensile strength) of polyurethane on the content of MgFeGa layered triple hydroxide additive and the electron beam irradiation dose is investigated. The optimal amount of layered hydroxides and the optimal irradiation dose, causing a substantial increase in tensile strength and hardness of polyurethane, are determined. Polyurethane modification by adding magnesium/iron/gallium layered triple hydroxides in the amount of 3 wt% causes an increase in tensile strength and hardness by 30.0 and 5.4%, respectively. Modification of pure polyurethane by irradiation with the optimal dose (100 kGy) promotes an increase in tensile strength by 27.1% and hardness by 4.6%.