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Information × Registration Number 0214U005078, 0111U000176 , R & D reports Title The determine the biological activity and safety of biotransformation products of antidiabetic preparation phensueccinal popup.stage_title Head Kudria Maria Yakivna, Кандидат біологічних наук Registration Date 31-01-2014 Organization Ukrainian Research Institute of Endocrine Diseases Pharmacotherapy popup.description2 Objects of the study: metabolites of phensukcynal biotransformation in phase I - beta- phenylethylsukcynamid (beta-PESA) is the 2-hydroxiphenilsukcynamid (2 HPSA), anti-hyperglycemic activity, functional and metabolic state of individual systems and organs of the body, pro- and antioxidant system, the metabolism of nitric oxide, nonspecific resistance. Purpose of work: the clarify the features of the biological action of metabolites antidiabetic agent of phensukcynal and the mechanisms of their damaging effects on the body. Research methods: organic synthesis, physical and chemical analysis, toxicological, physiological, rheological, biochemical and immunological. It was identified potential metabolites of I phase biotransformation of phensukcynal - beta-2-PESA that HPSA. It has been established that they do not show antihyperglycemic activity in intact rats at a single oral glucose load, are moderately expressed in the test antioxidant properties in vitro. Beta-PESA at doses of 18 mg/kg, that of 72 mg/kg accelerates the process of platelet aggregation and blood clotting. 2 HPSA in dose 17 mg/kg inhibits the formation of a fibrin clot in the final stage of coagulation. Both metabolites fensuktsinala at doses equimolar its effective dose, increases the activity of enzymes of glycolysis and mitochondrial energy metabolism of different units, and also has antiatherogenic potential. At these doses, both metabolite cause retardation of peroxide oxidation of lipids and proteins in the serum and liver in subtoxic doses, conversely, enhance these processes. Beta- 2- and PESA HPSA regardless of the dose causing a decrease of NO-synthase activity and a stable end products of NO metabolites in plasma and blood. Beta-PESA regardless of dose level activates the glutathione system and other antioxidant enzymes, 2-HPSA has different effect on the antioxidant defense system. Proved that the antioxidant, antioxidant and anti-atherogenic activity energy-stimulated of phensukcynal effective in dose may be due to the action of its active metabolites 2-HPSA that beta-PESA. Application area: pharmacology, medical toxicology, chemical and pharmaceutical industries. Product Description popup.authors Бурма Тетяна Юхимівна Жураковська Марія Володимирівна Завадська Наталія Володимирівна Карножицька Тетяна Михайлівна Кравченко Світлана Вікторівна Кудря Марія Яківна Ліпсон Вікторія Вікторівна Лалименко Ольга Сергіївна Мельниківська Наталія Вікторівна Нікішина Людмила Євгенівна Павленко Тетяна Олексіївна Палагіна Ірина Анатоліївна Сидорова Ірина Василівна Сукова Юлія Петрівна Устенко Нонна Василівна popup.nrat_date 2020-04-02 Close