The possibility of increasing metabolism and resistance in an organism of animals under the influence of biologically active substances of natural origin is considered in the paper. In the current study, we investigated the effect of 40% ethanolic extract of common nettle (Urtica dioica L.) on hematologic indexes (hemoglobin concentration, erythrocytes and leukocytes content), protein metabolism (total protein, aspartate aminotransferase (AST), alanine aminotransferase activities (ALT)), glutathione metabolism (peroxidase (GP), glutathione reductase (GR) and reduced glutathione content (GSH)), antioxidant defense systems (superoxide dismutase (SOD), catalase (CAT)), and indicators of free radical processes (lipid hydroperoxidation products (LHP), TBA-active products and carbonyl groups of protein (CP)) in the blood and tissues of normal and adrenalin-stressed rats. White Wistar rats (male) with body weight 180–200 g were used in the experiments. The animals were divided into 4 groups (control and 3 experimental), each containing 7 animals. The animals of experimental groups D2 and D3 received 40% ethanolic extract of common nettle in a dose of 5 mL/kg of body weight during 4 weeks. After 29 days of the experiment, the animals of D1 and D3 groups were intramuscularly administered 0.1% solution of adrenaline hydrochloride at a dose of 1 mg/kg of body weight. One day after the administration of adrenaline, the animals were decapitated under ether anesthesia. The objects of the study were blood and homogenates of liver, heart, and kidneys of the rats. Our results have shown that adrenaline stress causes a decrease in the concentration of hemoglobin, LHP, SOD activity and increase in activities of AST, GP, GR, and GSH content in the blood of rats. Stress induced by adrenaline was accompanied by decrease in CP content, activities of SOD, CAT, and increase in the glutathione chain of antioxidant defense system in the liver of the animals while in the heart and kidneys, there was an increase in oxidative stress parameters and decrease in antioxidant enzyme activities (SOD, CAT, GP, GR). The administration of ethanolic extract of nettle caused an increase within the physiological range in the erythrocytes and leucocytes content, hemoglobin concentration, and normalization of protein metabolism (decrease in the activity of AST and increase in protein concentration) in the blood of the stressed rats. The activation of the antioxidant defense system (increase in activities of SOD, GP, CAT, GR) and inhibition of free radical processes (decrease in concentration of LHP, TBA-active products and CP) was observed in the tissues of animals of D2 and D3 groups. Our results suggested that using a complex of biologically active substances of the common nettle ethanolic extract prevents metabolic disorders and stresses of different etiology through the activation of the antioxidant defense system, the normalization of protein metabolism and stimulation of hematopoiesis both in normal and stressed rats.

We studied the effects of the newly synthesized biologically active compound potassium aminobenzene thiosulfonate on electrophysiological parameters of the embryos of weatherfish (Misgurnus fossіlis L.), in particular the dynamics of transmembrane potential (TMP) of the plasmatic membranes of the weatherfish and the activity of the membrane enzyme Na+/K+–ATPase during synchronous cleavage of blastomeres in early embryogenesis. A slight impairment of electrogenesis of the cellular membranes under the action of potassium aminobenzene thiosulfonate indicates changes in the permeability of plasmatic membrane and transport of electrogenic ions. This was related to the inhibition of biosynthetic processes in the first hours of the development of embryos, which led to 60.6 ± 2.6% decrease in the activity of membrane pump when subject to high (10–3 М) concentration of potassium aminobenzene thiosulfonate. Its activity further recovered to the level of the control only in 10–8 М concentration. Also, we conducted a comparative analysis of the effects potassium aminobenzenethiosulfonate had on the activity of the membrane pump of embryos in in vivo and in vitro experiments. We determined that the action of the examined compound depends on the presence of a correspondding concentration in the embryo incubation medium. To characterize the variability of changes in the activity of membrane pump of the embryos in the conditions of action of potassium aminobenzene thiosulfonate, we determined constants of semi-inhibition (І50) by linearization of the developed concentration-effect curves using Hill’s plot. To determine which factors contribute to the changes in the activity of membrane pump the most, namely, various concentrations of potassium p-aminobenzene thiosulfonate, duration of the development of embryos or other factors that had not been taken into account, we performed a dispersion analysis of how these factors affect the variability of the studied parameter. We determined that the extent of variability of the activity of the membrane pump is also determined by the effect of different concentrations of potassium p-aminobenzene thiosulfonate, and the factor of time of embryo development. The electronic-microscopic study of weatherfish’s blastomeres subject to potassium p-aminobenzene thiosulfonate revealed the changes in the ultrastructure of mitochondria, which led to inhibition of their matrix and electron transport chain, and therefore decrease the efficiency of ATP production and energy-dependent processes.

Проведено комп'ютерне прогнозування фармакологічної активності ряду екзофункціоналізованих похідних 9,10-антрахінону з амінокислотними та тіазольними фрагментами з метою пошуку сполук з антиоксидантним ефектом за допомогою програм вебресурсу Way2Drug. Здійснено експериментальне тестування відібраних похідних у дослідженнях гепатоцитів in vitro на здатність пероксидного окиснення ліпідів (ПОЛ) з визначенням вмісту тіобарбітурактивних (ТБК-активних) продуктів та окисної модифікації білка (ОМБ) через кількість утворених додаткових карбонільних груп (КГ) у бічних ланцюгах білків. Виявлено сполуки з антиоксидатною дією порівняно з контролем та в межах дії відомого антиоксиданту кверцетину за двома показниками оксидативного стресу ПОЛ та ОМБ серед досліджених похідних 9,10-антрацендіону, що спрогнозовані даними in silico прогнозу та узгоджуються із ними. Ключові слова: 9,10-антрахінон, амінокислота, тіазол, in silico прогнозування, експериментальне тестування, антиоксидантна активність.

The synthesis of new N-(9,10-dioxo-9,10-dihydroanthracen-1(2)-yl)-2-(R-thio) acetamides was carried out using reaction of 2-chloro-N-(9,10-dioxo-9,10-dihydroanthracene-1(2)-yl)acetamides with functionalized thiols in the presence of potassium carbonate in N,N-dimethylformamide (DMF) at room temperature. Evaluation of the synthesized compounds on such indicators of radical scavenging activity as lipid peroxidation (LP) and oxidative modification of proteins (OMP) in vitro in rat liver homogenate was carried out. It was determined that the compounds with a substituent in the first position of anthracedione core showed better antioxidant properties than their isomers with a substituent in the second position. The compounds 6 and 7 with the best indicators of radical-scavenging activity were determined. Antioxidant effect in OMP processes was also determined for compound 10. The antiplatelet activity study in vitro revealed compound 10 with the inhibited effect of ADP-induced aggregation.

By means of morphological studies, it was established that the influence of thiosulfonate solutions of different structure doesn’t show an inhibition of blastomere division and germ layer formation of the freshwater bony fish, namely weatherfish (MisgurnusfossіlisL). However, under the effect of potassium nitrobenzenethiosulfonate (NTK), at the pre-hatching stage (36thdevelopment stage), that is responsible for the establishment of erythrocyte circulation, external gills predevelopment and the appearance of pigmentation, we observed a delay for approximately 13-16 hours with the imminent vascular pathology. The pronounced changes of cardio-vascular system, which manifested itself in vasodilation, were spotted later on after the NTK influence.The results showed evidence of thiosulfate acid’s derivatives, namely NTK, being promising, highly efficient, non-toxic antithrombotic and antiplatelet remedies.