The effect of unmodified chitosan nanoparticles with a size of ~100 nm and a weakly positive charge on blood coagulation, metabolic activity of cultured cardiomyocytes, general toxicity, biodistribution, and reactive changes in rat organs in response to their single intravenous administration at doses of 1, 2, and 4 mg/kg was studied. Chitosan nanoparticles (CNPs) have a small cytotoxic effect and have a weak antiplatelet and anticoagulant effect. Intravenous administration of CNPs does not cause significant hemodynamic changes, and 30 min after the CNPs administration, they mainly accumulate in the liver and lungs, without causing hemolysis and leukocytosis. The toxicity of chitosan nanoparticles was manifested in a dose-dependent short-term delay in weight gain with subsequent recovery, while in the 2-week observation period no signs of pain and distress were observed in rats. Granulomas found in the lungs and liver indicate slow biodegradation of chitosan nanoparticles. In general, the obtained results indicate a good tolerance of intravenous administration of an unmodified chitosan suspension in the studied dose range.
The increased complexity due to the emergence and rapid spread of new viral infections prompts researchers to search for potential antiviral and protective agents for mucous membranes among various natural objects, for example, plant raw materials, their individual components, as well as the products of their chemical modification. Due to their structure, resin acids are valuable raw materials of natural origin to synthesize various bioactive substances. Therefore, the purpose of this study was to confirm the possibility of using resin acid derivatives for the drug design. As a result, we studied the cytotoxicity and biological activity of resin acid derivatives. It was shown that a slight decrease in the viral load in the supernatants was observed upon stimulation of cells (II) compared with the control. When using PASS-online modeling (Prediction of Activity Spectra for Substances), the prediction of the biological activity spectrum showed that compound (I) is capable of exhibiting antiviral activity against the influenza virus. The use of the SWISS-ADME webserver to reveal the drug-like properties of compounds did not directly indicate the presence of antiviral activity. These results indicate the potential of resin acid derivatives as a starting point for extensive research in the study of biological activity.
Introduction. The article presents the results of the research investigation on identifying key narratives in the perception of the external social environment by university students on the example of St. Petersburg Peter the Great Polytechnic University (hereinafter referred to as SPbPU). The aim of the article is to identify key narratives (images of the present, past, and future) to assess students’ perception of social reality, to substantiate key needs of students in the field of soft skills development and to summarize the practices in the field of teaching these skills in SPbPU. Materials and Methods. The key methods of obtaining research data include the survey, participant observation of the research team members within the framework of professional activities, analysis of documents on the issues of teaching and assessment of teaching Soft Skills disciplines. The methods of semantic analysis, generalization, comparison, data visualization, and verification were used in order to collect data, process and present them. Results. The authors identified key narratives in the perception of the external social environment by university students, including peculiarities of the perception of enlarged groups in social, humanitarian and technical fields of study. The data on the key needs of young people within the framework of Soft Skills acquisition and the experience of implementing such disciplines on the example of SPbPU were generalized. During the study, a search semantic analysis of existing evaluative acronyms was applied to investigate the existing image of reality perception in the target group, and the DICE acronym was introduced to summarize the desired image of the future in university students. The practical results of the research consist in the possibilities to assess the potential of practices in the disciplines within the framework of «Soft Skills» in SPbPU and modernization of similar practices in other universities. Conclusions. The article concludes about the need to build an effective feedback system with university students, which will allow, based on specialized Soft Skills practices, to respond flexibly to needs in the field of deficit skills and competencies of students and ensure their acquisition. In addition, the importance of identifying the existing narratives in the youth environment in the field of perception of social environment and social time to realize the educational, communicative and moral functions of higher education institutions is shown.
Background. Derivatives of diterpenes, in particular, resin acids, are of interest for the creation of pharmacological substances with a wide spectrum of action.Objective. To perform a predictive assessment of the biological activity of oxidation products of fluorinated esters of resin acids.Design and methods. Predictive assessment of the biological activity of the oxidation products of fluorinated esters of resin acids (I–VIII) was carried out using the PASS-online software. The prediction of physico-chemical and pharmacological properties of the studied compounds was carried out using the SWISS-ADME web server and SwissTargetPrediction.Results. A predictive assessment of the spectrum of biological activity, physico-chemical and pharmacological properties of oxidation products of fluorinated esters of resin acids was carried out using PASS-online modeling and the SWISS-ADME and SwissTargetPrediction web server. All the studied compounds (I–VIII) are capable of exhibiting antiviral, antitumor, and dermatological activity. These results indicate the potential of using oxidized fluorinated esters of resin acids as a platform for the creation of pharmacological substances. Using SwissTargetPrediction, it was demonstrated that the most likely target (92 %) for compound (I) is a cholesterol ester transporter protein.Conclusion. Based on the results of a predictive assessment of the spectrum of biological activity using the PASS-online and SWISS-ADME programs, the possibility of using oxidation products of fluorinated esters of resin acids as pharmaceutical substances was revealed.
28 March 2024 in Proceedings of universities. Applied chemistry and biotechnology
Biologically active substances that confer antiviral, anti-tumour and antimicrobial effects, which are found among the components of plant raw materials, as well as the products of their chemical modification, are the subject of considerable research interest. These objects include tricyclic diterpenoids – extractives of wood of abietic and pimaric types (resin acids). The presence of two reaction centres (double bonds and a carboxyl group) in the structure of resin acids opens up a wide range of possibilities for synthesising useful compounds on their basis. One of the most promising areas for the study of resin acids and their derivatives consists assessing their fungicidal properties to inform their introduction into compositions as additives, as well as in the application of protective films to increase the resistance of composite building materials against the aggressive effects of microorganisms. In the present work, the fungicidal activity of the N-phenylimide of maleopimaric acid and its polyfluoroalkyl ethers synthesised by us was evaluated on the cells of the filamentous fungi Aspergillus niger, Alternaria alternata and Penicillium sp. by the rate of colony formation and growth. A comparative analysis of the biological activity of resin acids and their in silico derivatives was performed. According to the AntiBag Pred forecast, the test compounds having the maximum values of the probabilities of the presence and absence of each type of activity are characterised by the manifestation of antibacterial activity in relation to strains of gram-positive bacteria. The results of the predictive model are consistent with previous experimental data. However, AntiFun Pred data related to the calculation of fungicidal activity were not confirmed in vitro.