Registration Number
0217U004456,
0116U002639
, R & D reports
Title
Pyrrole derivatives as anti-inflammatory and anti-tumor compounds of new generation.
popup.stage_title
Head
Vladimir Rybalchenko, Доктор біологічних наук
Registration Date
03-02-2017
Organization
Taras Shevchenko Kiev University
popup.description2
Subject of research: general and specific toxicity, antioxidant, membranotropna activity genotoxicity pyrrole derivatives, fullerene C60. Object of study: pyrrole derivatives of D-1 and Mi-1 as a therapeutic compound of the new generation, their derivatives, C60 fullerenes. Purpose - to study the safety of compounds 5-amino-4- (1,3-benzotiazol-2-yl) -1- (3-methoxyphenyl) -1,2-dihydro-3H-pyrrole-3-one (D-1) and 1- (4-hlorbenzyl) -3-chloro-4- (trifluoromethyl-fenilamino) -1H-pyrrole-2,5-dione (MI-1); assessment of their genetic, membranotropnoyi activity, antioxidant properties, evaluation of antioxidant properties of fullerene C60 Methods: Histological, hematological, genetic, biochemical and biophysical methods and morphometric and statistical analyzes. It is shown that pyrrole derivatives 1- (4-Cl-benzyl) -3-Cl-4- (CF3-fenilamino) -1H-pyrrole-2,5-dione (MI-1) and 5-amino-4- (1 3-benzotiazol-2-yl) -1- (3-methoxyphenyl) -1,2-dihydro-3H-pyrrole-3-one (D1) for the actions of a relatively effective (2.7 mg / kg and 2.3 mg / kg, respectively), 5-fold and 10-fold dose of it to the general state of the rats no effect. The toxic effects of compounds dose-dependent increase, but even in maximal doses of these compounds do not cause significant damage and change morpho-functional state of the mucous membrane of the colon and blood. MI-1 D1 and correcting the effects of oxidative stress in the colon mucosa in its inflammation. Established that MI-1 does not affect the survival, growth and fecundity of Drosophila melanogaster line Oregon R (R) and shows no mutagenic effects in the test in breach of DNA repair in line mei-9a mei-41D5 / FM7c; mwh. Modification of side radicals (atoms interchange Cl and F) at positions 1 and 4 molecules MI-1 did not significantly affect the nature and intensity of its interaction with artificial bilipidnymy membranes. Fullerene C60 when exposed to a dose of 0.5 mg / kg virtually no effect on the activity of antioxidant enzymes and glutathione system in hepatocytes under conditions of oxidative stress, ¬pry action in higher doses (0.8, 1.6 and 3, 2 mg / kg) did not affect the content of lipid peroxidation products plasma membrane of hepatocytes, but causing multidirectional changes in the activity of superoxide dismutase and catalase. The data indicate safety pyrrole derivatives and C60 fullerenes and their ability to correct the effects of oxidative stress.
Product Description
popup.authors
Бєлінська І.В.
Бичко А.В.
Гурмач В.В.
Гурняк О.М.
Дзюбенко Н.В.
Дудка О.А.
Кузнєцова Г.М.
Линчак О.В.
Рибальченко В.К.
Т.В.Рибальченко
Цивінська С.М.
Ю.І. Прилуцький
popup.nrat_date
2020-04-02
