Abstract: It was synthesized N-[5-(4-fluorobenzyl)-1,3-thiazol-2-yl]chroman-3-carboxamide. The
structure of the title compound was confirmed by 1H NMR spectroscopy and elemental analysis. The
synthesized compound complies with Lipinski, Muegge, Ghose, Veber, and Egan rules. ADME and
toxicity of the compound are analyzed, and Swiss target prediction of the compound has been carried
out to analyze the preferred target. The title compound exhibited remarkable anticancer activity against
all the tested cell lines and was more active than classical anticancer drugs – gefitinib, 5-fluorouracil,
cisplatin, and curcumin. The metabolic pathway mediated by Cytochrome P450 was evaluated for the
title compound. It was found that the main pathways are aromatic hydroxylation of fused benzene ring,
which should not cause toxic effects.
Keywords: thiazole; chroman; virtual screening; drug-like molecules; anticancer activity;
Cytochrome P450; metabolism.
Applied Nanoscience
Abstract
The biocompatibility of NPs to blood cells is a key issue when these NPs are planned for intravenous application because of potential contact with blood cells and proteins. In this work, γ-Fe2O3 NPs (~ 9 nm) and their poly(N,N-dimethylacrylamide) (PDMA) and SiO2-coated derivatives (γ-Fe2O3@PDMA and γ-Fe2O3@SiO2, respectively) were investigated. It was detected that both PDMA and SiO2 coatings decreased NPs’ aggregation in the buffer solutions, as well as in cell culture medium. Neither neat γ-Fe2O3 NPs nor their coated derivatives possessed hemolytic activity toward red blood cells. There was no significant loss of body weight observed after the intravenous injection to laboratory mice. The immune response to the injected NPs was assessed by the ELISA measuring. No antibodies of the IgM class were detected, which suggests lack of acute inflammation. On the 35th day of the experiment, there was a rise in the content of the anti-OVA IgG noticed in all three types of the NPs; however, this rise was lower compared to that induced by the positive control. The injected NPs were found to be spread and settled in the pouch cavity, and none of the tested NPs caused vascular damage or distinct signs of inflammation. Summarizing, γ-Fe2O3 NPs coated with the PDMA or SiO2 manifested good compatibility with blood cells in in vitro and in vivo investigations.
Keywords Maghemite · Nanoparticles · Poly(N,N-dimethylacrylamide) · Silica · Hemolytic action · Immune response
UDC 616.314-002-007.253:616.316-008.8]-018-039.71-053.2
The purpose of the study was to investigate the morphological properties of oral fluid in dynamics in the application of the developed set of measures for the prevention of fissure caries of the first permanent molars in children. Materials and methods. 62 children aged 6 years with fissure caries of the first permanent molars (main group) and 31 children without signs of carious lesions (control group) were examined. The study of the crystal formation of oral fluid was carried out according to the method of Leus P. A. (1977). The mineralizing potential of oral fluid was expressed as an average score depending on the types of crystals detected. Results and discussion. The analysis of the results of the study showed that 6 months after the start of preventive measures in the oral fluid of the children of the main group, a slight increase in type I crystals was noted in comparison with the initial data (40.18 ± 4.65% of cases, p>0.5), at the same time, the number of children, in whom type III crystals were observed, decreased in the main group (16.45 ± 2.32%, p>0.5), and increased in the control group (19.32 ± 2.47% of cases, p>0.5) in comparison with the initial data. After two years of observation, in the children of the main group, type I crystals were most often detected in the oral fluid (48.41 ± 4.23% of cases), in the children of the control group, on the contrary, the number of children with this type of crystals decreased and was almost one and a half times less than among children of the main group (p<0.05). On the other hand, the number of children in the control group, in whom type III crystals were detected, was two times higher than among children in the main group (22.34 ± 2.87% and 11.51 ± 2.56% of cases, respectively, p<0.05). Conclusion. It was established that in children who received a complex of preventive measures, 6 months after the implementation of preventive measures, the mineralizing potential of oral fluid was, on average, 2.73 ± 0.07 points, which is slightly higher compared to the fissure detected at the beginning of caries prevention (2.57 ± 0.12 points respectively, p>0.05). In the children of the control group, the mineralizing potential of oral fluid changed less noticeably (from 2.64 ± 0.11 points at the beginning of observation to 2.66 ± 0.11 points, p>0.5). After two years of observation, it was found that in the main group the mineralizing potential of oral fluid continued to increase, while in the children of the control group it decreased and reached almost the initial level (2.65 ± 0.07 points in the second year of observation and 2.64 ± 0.08 points at the beginning, p>0.05). Thus, it can be concluded that the proposed measures are quite effective.
616.31:616.24(048.8)
Abstract. The article reviews the factors of dental exposure that may have a potential risk for the development of pulmonary diseases.
Objective. To analyze the current national and foreign literature on the relationship between dental health and pulmonary disease, while exploring current data and future research directions.
Materials and Methods. The study used analytical and bibliosemantic methods. The search for scientific infor- mation on the medical research topic was conducted in the databases of the following search engines: the electronic library of abstracts and theses of the Vernadsky National Library of Ukraine, PubMed, Medline, MedNet, Embase, BMJ Group, Free Medical Journals, Free Medical Book, Scirus.
Research results and discussion. The analysis of literature data provides evidence of a host-pathogen interac- tion associated with the oropharyngeal microbiome and its metabolites.
Cross-species interactions between microorganisms create a symbiotic relationship with the host macroorganism by acting as a "sensor", "mediator" and "killer" of pathogens to prevent pathogens from colonising and integrating into the host. Conversely, the immune response of the macroorganism must balance between inflammation to destroy the pathogen and prevent unwanted immune responses against host tissue and its own microorganisms. When the composi- tion, activity and function of the oral microbiome is disturbed, it causes dysbiosis. In the presence of orthopaedic struc- tures in the oral cavity, the eubiotic balance is more or less shifted to a pathogenic state.
The article analyses the influence of structural materials and methods of their production, which are mainly used in prosthetic dentistry, on the formation of biofilm, changes in the oral microbiome, and the spread of an inflammatory reaction in the prosthetic bed.
The oral cavity is the first line of defence of the immune system against most foreign pathogens, which can affect the immune and inflammatory reactions of the body as a whole. This factor can spread systemic inflammation that affects other organs, including the lungs. The oral microbiota can influence the microbial community in the lungs through mi- croaspiration and dispersal. In general, the oral-pulmonary axis can exchange components of its microbiome
The most common respiratory diseases associated with dust among dentists and its irritating effects on the res- piratory system are also analyzed.
In general, ultrafine and nanoscale airborne particles have been studied for a long time, but with the development of new technologies, their acute or chronic effects on the health of healthcare workers associated with dental practice require more detailed study.
Conclusion. Understanding the relationship between oral health and systemic diseases, including pulmonary diseases, and studying a multidisciplinary approach to the treatment of a particular disease can be important in terms of extending healthy life expectancy and improving its quality. For effective health management, it remains an unsolved issue whether it is possible to prevent systemic diseases by influencing oral diseases (and vice versa).
Keywords: microbiome, dysbiosis, bacterial adhesion, pulmonary diseases, oral health, biofilm, aerosols, nano- particles, prosthetic materials, cross-species interaction of microorganisms.