Searching for new types of biological activities among preliminarily identified hit compounds is a key challenge in modern medicinal chemistry. In our study, a previously studied 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl]-propionic acid (Les-6614) was screened for antimicrobial, antifungal, anti-allergic, and antitumor activities. Moreover, cytotoxicity, molecular docking, and SwissAdme online target screening were accomplished. It was determined that the Les-6614 has slight antimicrobial and antitumor activity. However, the studied compound decreased IgE levels in sensitized guinea pigs by 33–86% and reduced IgA, IgM, IL-2, and TNF-α, indicating anti-inflammatory and anti-allergic aactivities. According to the SwissADME web tool, target predictions for Les-6614 potentially have an affinity for lysosomal protective protein, Thromboxane-A synthase, and PPARγ. The molecular docking confirmed that the studied 2-thioxo-4-thiazolidinone derivative showed good bonding with LLP and TXAS, leading to stable protein–ligand complexes. Additionally, Les-6614 is a potential PPARγ modulator, which is important in the pathogenesis of allergy, cancer, and cardiovascular diseases.

The aim. To study the cell immunity status under influence of 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-propionic acid, as a prominent 4-thiazolidinone derivative and a class of biologically active compounds with polypharmacological properties. Materials and methods. Experimental method on the model of laboratory animals (guinea pigs); intradermal allergy tests; relative and absolute content in the peripheral blood of T- and B-lymphocytes subpopulations; hematological indexies: index of the ratio of lymphocytes and monocytes, index of the ratio of neutrophils and monocytes, index of the ratio of neutrophils and eosinophils, phagocytic index, phagocytic number; ELISA; organic synthesis; pharmacological screening. Results. The effect of 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-propionic acid has antifungal properties and affect cellular component of immunity in vivo in the guinea pigs model. There are no changes in the skin of guinea pigs during and after chemical applications of the skin and after intradermal tests. The compound stimulate the immune cells, in particular the lymphocyte (increase in the absolute number of CD3 T-lymphocytes by 21.46 % and the absolute number of CD8 T-suppressors by 27.15 %), but with a selective inhibitory effect on certain units (decrease the relative number of NK cells CD16 by 11.57 % and B-lymphocytes CD22 by 23.08 %). There was an increase in the activity of the macrophage phagocytic system (increase in PN by 439.87 % and PI by 62.73 % at 120 minutes), which indicates the reliability of the absorbing function of phagocytes, but with a decrease in their ability to endocytosis (PCI decreased significantly by 78,72 %). Conclusions. Synthesized 3-[5-(1H-indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-propionic acid has a selective activating effect on certain parts of cellular immunity and on phagocytic activity. Derivate influence on the phagocytic activity of neutrophils is ambiguous, and the effect of the compound directed to the cellular part of the immune system does not cause cellular immunodeficiency. The studied derivative is promising for further study of the drug-like molecule with antifungal and antitumor effects

Background. An integral part of a child’s physical and mental development is a balanced diet. Insufficient or inadequate for a child developing organism’s needs nutrition in preschool age leads to a delay in physical, cognitive, and mental development. The study was aimed to assess the macro-and micronutrient provision status of preschool children with psychomotor developmental delay, identify the presence of macro- and micronutrient deficiencies, define the connection between macro- and micronutrient levels in patient’s serum and psychomotor developmental disorders. Materials and methods. The study analyzed the results of biochemical blood tests of blood serum samples for total calcium, magnesium, and iron level in 30 preschool children with psychomotor developmental disorders. Results. Mental retardation was observed in 53.33 % of examined children, autism spectrum disorders — in 20 % of exami­ned children; minimal brain dysfunction — in 13.33 %, attention deficit hyperactivity disorder (ADHD) — in 13.33 %. 93.33 % of exami­ned children had a deficiency of total calcium, magnesium — in 63.33 %, iron — in 20 %. Ten percent of patients had a deficiency of both total calcium, magnesium, and iron; one child (3.33 %) had no deficits. The most common deficiency in almost all subgroups of examined children was a combined deficiency of total calcium and magnesium. Only in the minimal brain dysfunction subgroup, in 50 % of cases, there was a combined deficiency of total calcium and magnesium, and in other 50 % of cases — an isolated deficiency of total calcium. This study identified a reliable inverse correlation of moderate strength between the level of total calcium and psychomotor development disorders and between the level of magnesium and the hyperexcitability syndrome. This study detected a weak unreliable correlation between the levels of magnesium and neurological disorders; an inverse unreliable weak correlation was found between iron and psychomotor developmental disorders. Conclusions. The most common deficiency in almost all subgroups of examined children was a combined deficiency of total calcium and magnesium. This study identified a reliable inverse correlation of moderate strength between the level of total calcium and psychomotor developmental disorders and between the level of magnesium and the hyperexcitability syndrome. There is also a weak direct unreliable correlation between magnesium level and psychomotor disorders. An inverse unreliable weak correlation was detected between the concentration of iron and psychomotor disorders.

Ìåòà. Åêñïåðèìåíòàëüíî äîñë³äèòè àëåðãîíåáåçïåêó ïîáóòîâèõ á³îïðåïàðàò³â ÑÀÍÅÊÑ âèãîòîâëåíèõ íà îñíîâ³ åíçèì³â, âèðîáíèöòâà Nviron Biosolutions Incorporation, Êàíàäà. Ìàòåð³àë ³ ìåòîäè. Âèâ÷àëè ³ìóíîòîêñè÷íèé âïëèâ á³îïðåïàðàò³â ÑÀÍÅÊÑ: Àíòèçàïàõ êîíöåíòðàò ³ Àíòèòàáàê â ðîç÷èí³. Äîñë³äaeåííÿ ïðåïàðàò³â ïðîâîäèëè íà áàç³ öåíòðàëüíî¿ íàóêîâî-äîñë³äíî¿ ëàáîðà-òî𳿠òà ëàáîðàòî𳿠ïðîìèñëîâî¿ òîêñèêîëî´³¿ Ëüâ³âñüêîãî íàö³îíàëüíîãî ìåäè÷íîãî óí³âåðñèòåòó ³ìåí³ Äàíèëà Ãàëèöüêîãî.  åêñïåðèìåíò áðàëè íåë³í³éíèõ á³ëèõ ùóð³â-ñàìîê ìàñîþ 175-210 ´.  åêñïåðèìåíòàõ ïðîâåäåíî ñåíñèá³ë³çàö³þ øëÿõîì îäíîðàçîâîãî ³íãàëÿö³éíîãî ââåäåííÿ 0,25 ñì 3 ïðåïàðàòó. Ñòóï³íü ñåíñèá³ë³çàö³¿ âñòàíîâëþâàëè çà ðåçóëüòàòàìè òåñò³â in vivo òà in vitro. ³ðîã³äí³ñòü îòðèìàíèõ çì³í îö³íþâàëè ç âèêîðèñòàííÿì t-êðèòåð³þ Ñòüþäåíòà. Ðåçóëüòàòè é îáãîâîðåííÿ. ²íãàëÿö³éíà ñåíñèá³ë³çà-ö³ÿ á³îïðåïàðàòàìè âèêëèêàëà çì³íè ó ëåéêîöèòàðí³é ôîðìóë³ ó ï³ääîñë³äíèõ òâàðèí (á³ëèõ ùóð³â-ñàìîê). Âì³ñò åðèòðîöèò³â òà ìàñîâà êîíöåíòðàö³ÿ ãåìî-ëîá³íó á³ëèõ ùóð³â, ÿê³ ñåíñèá³ë³çîâàí³ ïðåïàðàòàìè Àíòèòàáàê ³ Àíòèçàïàõ, â³ðîã³äíî çìåíøåí³.  ëåé-êîöèòàðí³é ôîðìóë³ ï³ääîñë³äíèõ òâàðèí â³äì³÷àºòüñÿ â³ðîã³äíå çá³ëüøåííÿ âì³ñòó åîçèíîô³ë³â.  òåñòàõ in vitro, âèÿâëåíî â³ðîã³äíå ïîñèëåííÿ ðåàêö³¿ ñïåöè-ô³÷íîãî ë³çèñó ëåéêîöèò³â òà ðåàêö³¿ ñïåöèô³÷íî¿ àãëîìåðàö³¿ ëåéêîöèò³â ïðè ðîçâåäåíí³ 1:10. Ñåðåä äî-ñë³äaeåíèõ ïîêàçíèê³â êë³òèííîãî ³ìóí³òåòó ó åêñïåðèìåíòàëüíèõ òâàðèí â³ðîã³äíèõ çì³í íå âèÿâëåíî, ò³ëüêè ó òâàðèí, ÿê³ ñåíñèá³ë³çîâàí³ á³îïðåïàðàòîì Àíòèçàïàõ â³äì³÷åíî â³ðîã³äíå çá³ëüøåííÿ âì³ñòó öè-òîòîêñè÷íèõ ë³ìôîöèò³â (ÑÄ8). Çíà÷åííÿ ³ìóíîðåãóëÿòîðíîãî ³íäåêñó â³ðîã³äíî çìåíøèëîñü ó òâàðèí ñåíñèá³ë³çîâàíèõ á³îïðåïàðàòîì Àíòèòàáàê. Âèñíîâêè. Á³îïðåïàðàòè Àíòèòàáàê â ðîç÷èí³ ³ Àíòèçàïàõ êîíöåíòðàò ìîaeóòü ïðèçâåñòè äî ðîçâèòêó àíå쳿 ó åêñïåðèìåíòàëüíèõ òâàðèí ïðè ³íãàëÿö³éíîìó âïëèâ³. Äîñë³äaeåí³ á³îïðåïàðàòè âîëîä³þòü ïîì³ðíèì àëåðãîïîòåíö³àëîì.

Probable changes were studied in rats’ immune status under experimental conditions with inhalation route of type I pyrethroid–imiprotrin administration, which is the main component of a number of household insecticidal agents. The drug at a concentration of 45.0 mg/m3 interrupts immunological homeostasis in experimental animals. Nonspecific cellular component parameters of immune system have changed significantly. Imiprotrin is capable of inducing delayed hypersensitivity. Imiprotrin induces sensibilization under experimental conditions in more than half of the experimental animals, but the magnitude of the reactions to the intradermal administration of the drug has no probable differences, which allows imiprotin to be attributed to substances with moderate sensibilization potential