ABSTRACT
Compound PDMpT.HCI reduces intensity of lipoperoxidation, activates antioxidant system and increases animal life expectancy under hypoxic circumstance.
Subject(s)
Antioxidants/pharmacology , Hypoxia-Ischemia, Brain/drug therapy , Pyrimidines/pharmacology , Pyrimidinones/pharmacology , Reperfusion Injury/drug therapy , Toluene/analogs & derivatives , Animals , Animals, Outbred Strains , Antioxidants/chemistry , Gravitation , Hypoxia-Ischemia, Brain/metabolism , Hypoxia-Ischemia, Brain/physiopathology , Lipid Peroxidation/drug effects , Longevity/drug effects , Male , Mice , Picolines/pharmacology , Pyrimidines/chemistry , Pyrimidinones/chemistry , Rats , Reperfusion Injury/metabolism , Reperfusion Injury/physiopathology , Superoxide Dismutase/metabolism , Toluene/chemistry , Toluene/pharmacologyABSTRACT
It is established that flavonoid flavicin improves antithrombotic and vasodilating functions of blood vessels in rats with endothelial dysfunction caused by streptozotocin-induced diabetes.
Subject(s)
Diabetes Mellitus, Experimental/metabolism , Endothelium, Vascular/metabolism , Fibrinolytic Agents/pharmacology , Flavonoids/pharmacology , Vasodilation/drug effects , Animals , Diabetes Mellitus, Experimental/physiopathology , Endothelium, Vascular/physiopathology , Male , Rats , Rats, WistarABSTRACT
Quantum-chemical calculations of a series of molecules with primary amino groups were carried out, and the results were compared with experimental data on the in vivo acetylation degree. A criterion of the interaction efficiency of primary amines with arylamine N-acetyltransferase was suggested. An analysis of the known data and the results of our calculations showed that the interaction peculiarities of xenobiotics containing primary amino groups with the acetylating system of an organism largely define the spectrum of side effects of these xenobiotics.
Subject(s)
Acetyltransferases/metabolism , Xenobiotics/metabolism , Acetylation , Animals , Humans , Xenobiotics/toxicityABSTRACT
Calculations of valerolactam and N-methylacetamide dimers by the method of molecular orbitals in CNDO/2H, MINDO/3, MINDO/3H, MNDO, MNDO/H, AM1, and PM3 approximations showed that the PM3 was the most suitable method for the description of geometrical and thermodynamic characteristics of hydrogen bonds between their amide groups. The calculation of the H-bound dimers of N-acetylalanine methylamide, which mimicked the beta structure of protein macromolecule, showed that the antiparallel conformation of the dimer is by 2.85 kcal/mol more stable than the parallel conformation. According to the data obtained by using the AM1 approximation, the parallel type dimer has the enhanced ability to transmit the electron disturbance along the chain of amide-amide hydrogen bonds. The formation of the complexes of the antiparallel and the parallel types lead to the increase of the H-bonding ability of the outer oxygen atom of the amide group in comparison with the monomer.
Subject(s)
Proteins/chemistry , Electrons , Hydrogen Bonding , Protein Conformation , ThermodynamicsABSTRACT
The antiallergic effects of new novel synthetic coumarine-3-carboxylic acid derivatives were studied in a rat model of passive cutaneous anaphylaxis. The most potent agent was found and tested for mechanisms of its specific pharmacological action. Its capacity of suppressing immediate hypersensitivity in various animal species was demonstrated to be due to its concomitant action on the pathochemical and pathophysiological stages of the allergic process.