В сучасних умовах ВООЗ об’єднала зусилля у боротьбі з глобальним тягарем раку. Необхідно підвищення обізнаності в системі правовідносин «лікар-пацієнт-фармацевт». Підтримуюча фармакотерапія важлива для пацієнтів з колоректальним раком. Для виявлення лікувальної дії інфузійного препарату Сорбілакт в оперованих хворих на рак прямої кишки для корекції активності амінотрансфераз у плазмі крові обстежено дві групи онкологічних хворих (основна і контрольна). Основній групі онкологічних хворих після передньої резекції прямої кишки у ранньому післяопераційному періоді внутрішньовенно вводили інфузійний препарат Сорбілакт у дозі 600,0 мл на добу з швидкістю 30 крапель за хвилину протягом 5-ти днів. Контрольній групі - інфузійну терапію здійснювали 5% розчином глюкози у дозі 800,0 мл. Виявлено зростання активності аланін-амінотрансферази і аспартат-амінотрансферази у плазмі крові. при фармакотерапії препаратом Сорбілакт. Інфузійний препарат Сорбілакт рекомендується до широкого медичного застосування в онкологічних хворих після передньої резекції прямої кишки для попередження післяопераційних ускладнень, особливо у ранньому
післяопераційному періоді.
Ключові слова: рак прямої кишки, пацієнти, інфузійний препарат Сорбілакт, показники активності амінотрансфераз плазми крові.

UDC 615.276:547.789:542.91

Aim. The screening of antimicrobial and cytotoxic activities of thiazolo[4,5-b]pyridine derivatives was accomplished. Methods. The antibacterial and antifungal activities of synthesized thiazolopyridines were evaluated in vitro with the agar diffusion and broth microdilution methods using clinical and reference strains of Gram-positive, Gram-negative bacteria and yeasts. The structure-antibacterial/antifungal activity relationships of the screened compounds were established. The target compounds were screened for their cytotoxicity effects on HaCaT and HEK293 cells using MTT assay. Results. The highest antimicrobial activity was observed for compound V 2-oxo-7-thiophen-2-yl-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid with minimal inhibitory concentration (MIC) 12.5 μg/mL against Candida albicans. At the same time, the synthesized compounds were explored in the interaction with amoxicillin against multidrug resistant clinical isolates of ESβL+ Klebsiella pneumonie and Staphylococcus haemolyticus (MRSH). The best synergistic activity with amoxicillin was exhibited by compound VI. HaCaT human keratinocytes and HEK293 human embryonic kidney cells demonstrated resistance to the thiazolopyridine derivatives treatment and did not reach the IC50 value up to 100 µM. Conclusions. The tested thiazolopyridines constitute an interesting background for further development of new chemotherapeutic agents. K e y w o r d s: heterocyclic compounds, thiazolidinones, thiazolo[4,5-b]pyridines, antimicrobial activity, antiproliferative activity

UDC 616–093+547.789

Aim. Synthesis, structure determination, in vivo study of anti-inflammatory (anti-exudative) and ulcerogenic activity, estimation of an impact of novel pyrazolin-5-one bearing thiazolidin4-ones on liver function. Methods. Organic synthesis: multicomponent reactions (MCRs), [2+3]-cycloaddition reactions. Spectral methods: IR, LC-MS, 1H NMR. Biological methods: study of anti-cancer activity (NCI NIH, USA) protocol for 3-cell line panel); carrageenin-induced inflammatory paw edema model of white rats, biochemical laboratory tests (ALT, AST, ALP, γ-GGT levels determination); evaluation of ulcerogenic action. Results. The series of novel C-5 and N-3 substituted 2-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl) amino/imino]thiazolidin-4-ones had been synthesized using MCR and [2+3]-cycloaddition reactions as potential biologically active compounds. The results of screening anti-exudative activity revealed that the tested derivatives possess promising anti-inflammatory effect. The SARs were formed and possible mechanisms of their action were discussed. Conclusions. The results presented in paper suggest that the design and synthesis of new pyrazolin-5-on/ thiazolidin-4-one hybrids as potential molecules are an attractive area for the search for novel agents with promising pharmacological properties.
K e y w o r d s: antipyrine, pyrazolin-5-one, thiazolidin-4-one, hybrids, multicomponent reactions, tautomers/rotamers; anticancer/anti-inflammatory activity

UDC: 616.155.3-097.37:612.176:612.017.1:575.75.8

Abstract
The aim of our study is to elucidate changes in the content of pro-inflammatory interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) and anti-inflammatory cytokines interleukin-10 (IL-10) in the blood serum of guinea pigs in the dynamics of experimental immobilization stress. The dynamics of the immobilization stress is accompanied by a pronounced progression of the proinflammatory group of cytokines - TNF-α and IL-6 against theт background of declining functional activity of IL-10 at all stages of their formation (3 rd, 5 th and 15 th days) with an advantage on the 3 rd day of the experiment. The data obtained indicate an imbalance of pro- and anti-inflammatory cytokines and impaired cytokinogenesis, which is important for the pathogenesis in immobilization stress.
Key words: immobilization stress; tumor necrosis factor – α; interleukins; cytokines.

UDC: 616.314.18-002.4-099]-092.4/.9

Abstract The aim of our work was to investigate the peculiarities of changes in endogenous rates: medium mass molecules (MMM) and erythrocyte intoxication index (EII) in the blood of guinea pigs in the experimental periodontitis formation. The results of biochemical studies showed that at all stages of the development of experimental periodontitis, there is a consistent increase in the degree of endogenous with their dominance on the 15 th of the experiment relative to the control, namely, the content of medium-mass molecules (МMМ254, МMМ280) and the erythrocyte intoxication index (EII) increased in blood, respectively, by 24.8% (р≤0.05), 28.2% (р≤0.05) and 34.7% (р≤0.05) compared to the first group of animals, which indicates an increase in the processes and the important role of metabolites of endogenous intoxication and their participation in the mechanisms of formation of experimental periodontitis. 
Key words: periodontitis; stress; endogenous intoxication; medium mass molecules; erythrocyte intoxication index