Репозитарій

Heterocycles are commonly known for their unique features, e.g., antibacterial or anticancer properties. Although many synthetic heterocycles, such as 4-thiazolidinone (4-TZD), have been synthesized, their potential applications have not yet been fully investigated. However, many researchers have reported relevant results that can be a basis for the search for new potential drugs. Therefore, the aim of this study was to evaluate the cytotoxic, cytostatic, and antibacterial effects of certain 4-thiazolidinone-based derivatives, Les-3166, Les-5935, Les-6009, and Les-6166, on human fibroblasts (BJ), neuroblastoma (SH-SY5Y), epithelial lung carcinoma (A549), and colorectal adenocarcinoma (CACO-2) cell lines in vitro. All tested compounds applied in a concentration range from 10 to 100 µM were able to decrease metabolic activity in the BJ, A549, and SH-SY5Y cell lines. However, the action of Les-3166 was mainly based on the ROS-independent pathway, similarly to Les-6009. In turn, Les-5935 and Les-6166 were able to promote ROS production in BJ, A549, and SH-SY5Y cells, compared to the control. Les-3166, Les-6009, and Les-6166 significantly increased the caspase-3 activity, especially at the concentrations of 50 µM and 100 µM. However, Les-5935 did not induce apoptosis. Only Les-5935 showed a minor cytostatic effect on SH-SY5Y cells. Additionally, the antibacterial properties of the tested compounds against P. aeruginosa bacterial biofilm can be ranked as follows: Les-3166 > Les-5935 > Les-6009. Les-6166 did not show any anti-biofilm activity. In summary, the study showed that Les-5935, Les-6009, and Les-6166 were characterized by anticancer properties, especially in the human lung cancer cell. In cases of BJ, SH-SY5Y, and CACO-2 cells the anticancer usage of such compounds is limited due to effect visible only at 50 and 100 µM.

Новину відредагував: library-lnmu - 2-01-2025, 10:25

Tlre possible role of viral persistence as an epigenetic factor in the development of
psoriasis is discussed when a specific antigen (virus, especially type 1,2 (HSV 1,2)) is considered as a trigger factor
for direct or indirect action on immunocompetent cells.
The purposeTo evaluate the peculiarities of blood lyrnphocytes phenotyping in patients with psoriasis and
activated chronic Herpes slmplex virus infection compared to patients with psoriasis, activated chronic Herpes
virus infection, and healthy persons during treatment

UDC: 615.277.3:547.78].012:542.9

In vitro study and characterization of anticancer activity of heterocyclic derivative — [3-allyl-4-(4¹-methoxyphenyl)-3H-thiazole-2-ylidene]-(3²-trifluoromethylphenyl)amine hydrobromide

UDC: 547.673.5+547.789.13

Synthesis and study of new polyfunctionalized 2-hydrazinoanthraquinone derivatives as potential antimicrobial agents. Methods. Organic synthesis, NMR and LC-MS spectroscopy, agar diffusion and broth microdilution methods. Results. A series of anthraquinonehydrazone derivatives are synthesized using the reaction of 2-(morpholinodiazenyl)anthracene-9,10-dione with methylene active compounds in the acetic acid medium. The screening of antimicrobial activity identified the compounds with significant effects against the tested microorganisms with MIC value <186.9 μM. Compounds 5 and 11 with MIC <93.5 μM are effective against yeast fungi whereas compound 5 with MIC <186.9 μM is effective against P.putida, which is multidrug resistant to antibiotics.

BACKGROUND: A decrease in the incidence of syphilis has been observed in the world and in Ukraine in recent years. At the same time, an increase in cases of neurosyphilis is recorded. Diagnosis of neurosyphilis is quite difficult and based on the correct interpretation of the complex of various diagnostic tests.
OBJECTIVES: The paper is aimed to determine diagnostic potential of treponemal tests (TTs) and evaluate effectiveness of Treponema pallidum immunoblot (TPI) while research on cerebrospinal fluid (CSF) in differential diagnosis of neurosyphilis.
MATERIALS AND METHODS: The research object was CSF of patients with late forms of syphilis. The regulated serological and immunological methods in accordance with current guidelines and orders of the Ministry of Healthcare of Ukraine were used for laboratory diagnosis of neurosyphilis: Enzyme immunoassays (EIA), fluorescent treponemal antibody (FTA), T. pallidum hemagglutination assay (TPHA), and TPI.
RESULTS: Effectiveness of TTs in the diagnosis of neurosyphilis while research on 23 samples of CSF was carried out by the following methods: EIA (Immunoglobulin [Ig]M + IgG), FTA, andTPHA. The above-mentioned TTs used in serological diagnosis of CSF do not always meet the problem of confirming neurosyphilis diagnosis. According to these investigations, both positive and false positive results were obtained. In order to verify the diagnosis, a study on positive and false positive samples of CSF by TPI method was carried out. Positive results were obtained in 13 samples with the established duration of the disease.
CONCLUSIONS: TPI is an optimal treponemal immunological method of examination of CSF to diagnose neurosyphilis with a high degree of reliability. The use of TPI while research on CSF makes it possible to verify the diagnosis of neurosyphilis by differentiated detection of antibodies to the most immunogenic antigens of T. pallidum eliminating the subjective factor of the reaction and simplifies diagnostic procedure.