Within the recent years, xenobiochemistry (establishing biological action mechanism of chemical compounds, alien to the living organism, i.e. xenobiotics) gains extreme development, mostly due to brand new numerous substances, which are produced by organic synthesis industry. This fully concerns the new group of compounds – crown-ethers, the molecular core of which is represented by macroheterocyclic systems with 9-60 atoms in the cycle. One third of the atoms are etherized oxygens, which are separated by ethane groups. The most important property of macrocyclic polyethers is their capacity of forming stable complexes with salts of alkaline and other metals including the metal cation to their molecular niche. Objective.Investigation of biological action of 18-crawn-6, 21-crawn-7, cyclohexyl-18-crawn-6, and diketo-18-crown-6 1/1000 LD 50 upon Vistar line rats organism TTH-T 3 , T 4 system. Materials and methods.Applying a model of chronic experiment (6 months) and using 50 (10 per an experimental group) Vistar line male rats 1/1000 LD 50 of 18-crown-6 (0.00127 g/kg), 21-crown-7 (0.0032 g/kg), cyclohexyl-18-crown-6 (0.00265 g/kg), and diketo-18-crown-6 (0.00185 g/kg) was studied to influence concentrations of blood serum thyrotropic hormone (TTH), triiodothyronine (T 3 ), thyroxine (T 4 ). The experimental animals were administered water emulsions of the investigated compounds daily, on an empty stomach, per orally, with the usage of oral catheter. The rats of the control group were given the correspondent volumes of water. Since synthesis and secretion of TTH-releasing factor in hypothalamus is controlled by norepinephrine, which has high affinity to alpha2-adrenoreceptors (α 2 -AR) in this brain structure, we studied the action of crown-ethers on norepinephrine contents and 3 Н-rawolcine binding parameters in rats hypothalamus. Besides, activity of guanylate cyclase, and cGMP contents in hypothalamus were investigated. Results. The results showed the significant increase in norepinephrine and cGMP contents, and enhance of guanylate cyclase activity induced by norepinephrine in rats experimental groups hypothalamus. The influence of 18-crown-6 and diketo-18-crown-6 led to the increase in active forms of α 2 -adrenoreceptors in hypothalamus synaptosomes, whilst the action of cyclohexyl-18-crawn-6 and 21-crawn-7 was not that pronounced, and the index had only a tendency to rising. At the conditions of experimental substances action, TTH and T 3 blood serum concentrations grew increased, whereas T 4 blood serum concentration got significantly diminished. Cytochrome oxidase and K + -Na + , Ca 2+ -, Mg 2+ -ATPases activities became induced in the organism of rats experimental groups. Generally, crown-ethers were established to have a significant influence upon the activity level of ТТГ-Т3 , Т 4 system and the links, which control the system and are controlled by it.
crown-ethers, thyrotropin, triiodthyronine, thyroxine, norepinephrine, α 2 -adrenoreceptors, guanilate cyclase, cGMP, cytochrome oxidase, ATPases
«Bulletin of problems biology and medicine» Issue 1 Part 1 (142), 2018 year, 68-72 pages, index UDK 57.017.053:615.91
