Vol 17, No 1 (2019)

Experiments on rats showed that the individual resistance of the body to acute hypoxia is of decisive importance in the early recovery period after mechanical craniocerebral trauma. Antihypoxant ethomersol administration (25 mg/kg, 3 days, intraperitoneally) following trauma decreased behavioral impairments in rats with different levels of resistance to acute hypoxia, restored the structure of individual behavior, and prevented metabolic disturbances in the brain. Monotherapy of consequences of craniocerebral trauma with antidepressant pyrazidol (1 mg/kg) produced an anxiolytic effect in animals highly resistant to hypoxia and activating effect on low resistant animals. Treatment with bemithyl, an antihypoxant of benzimidazole structure, in a dose of 25 mg/kg produced a cerebroprotective effect and normalized individual behavioral characteristics, parameters of energy metabolism, and state of the antioxidant system in the brain of highly and low resistant rats. The effect of bemithyl was most pronounced in highly resistant animals. During combined treatment, pyrazidol and bemithyl had an additive effect in animals of both groups. They normalized behavioral reactions and prevented the development of metabolic disturbances in the brain.

Hypoxia plays an important role in the vital activity of the organism and practically accompanies any pathology. Hypoxia and tissue ischemia in the early stages are accompanied by the activation of lipid peroxidation. Derivatives of 9-dialkylaminoethyl imidazobenzimidazole with a 3,4-dioxyphenyl substitute showed high antioxidant activity. Therefore, they have been studied for antihypoxic activity in experimental models of hypobaric, histotoxic and hemic hypoxia, as well as in animals pre-typed for resistance to hypoxia, and it was shown that new condensed benzimidazole derivatives with antioxidant activity showed a wide range of antihypoxic activity. The most pronounced protective antihypoxic properties were demonstrated by compound RU-185.

The aim of the work was to study the effect of the complex compound of nicotine acid with antihypoxic activity under the code πQ-1043 on the function of the central nervous system. The experiments were performed on male mice of the SHR line. Influence of the compound on the function of the central nervous system was evaluated in the tests “open field”, conditioned-defense reflex of avoidance and corazole seizures. It was found that the compound πQ-1043 at a dose of 25 mg/kg increases emotional reactivity and reduces the coefficient of mobility of mice in the “open field” test, increases the latent time of the conditionally defensive reflex of avoidance, inhibits the development of seizures and increases the life expectancy of animals after administration of corazole. Such changes in the studied parameters indicate that the compound πQ-1043 has a depressing effect on the central nervous system function. It is assumed that the identified effect may be one of the components in the mechanism of antihypoxic action of the compound.

The aim of this study was to assess the effect of endothelial dysfunction caused by a decrease in the estrogen level on the severity of cerebral ischemia.

Methods. Endothelial dysfunction was caused by extirpation of the uterus with appendages and was confirmed by counting circulating endothelial cells and evaluating stimulated and basal secretion of nitric oxide. Focal cerebral ischemia was modeled by intravasal occlusion of the middle cerebral artery. The severity of ischemia was assessed according to the scales of neurological deficit (Combs & D’Alecy and McGraw), in the Rotarod test and in terms of the volume of necrosis.

Results. Estrogen deficiency resulted in an increase in the circulating endothelial cells by 88%, as well as a decrease in stimulated and basal nitric oxide secretion by 17.1% and 14.7% respectively. Focal cerebral ischemia in animals with endothelial dysfunction caused by estrogen deficiency resulted in greater cerebral damage, resulting in an increase in the level of neurological deficit on the Combs & D’Alecy and McGraw scales for 7 days, a decrease in the retention time on the rotating rod by 32%, as well as an increase in the infarct volume by 89% relative to the group of animals without sexual hormones failure.

Conclusion. It has been shown that endothelial dysfunction caused by estrogen deficiency complicates the severity of cerebral ischemia, causing a more pronounced neurological and motor deficit, and contributes to an increase in the size of infarct volume.

The article describes modern approaches for testing of drugs belonging to substrates and inhibitors of P-glycoprotein (Pgp, ABCB1-protein, MDR1-protein) according to the recommendations of Food and Drug Administration (United States) and European Medicines Agency. In vitro methods on cell lines with hyperexpression of the transporter are presented. The same analysis was done on human colon adenocarcinoma cell line (Caco-2).

The article deals with the state of cognitive functions (memory, attention and thought process) and asthenic disorders in stroke patients in the process of physical rehabilitation and pharmacotherapy. The study used conventional methods for determining the state of cognitive functions. To improve cognitive abilities in the process of physical rehabilitation in the experimental group of patients, traditional methods and special physical exercises in the form of training tasks for memory, attention and thought processes were used. In the control group of patients only traditional methods of restoration of cognitive functions were used. Both groups of patients took the same drugs to improve cognitive function and relieve symptoms of cerebrogenic asthenia, using classic nootropic drugs (Pyracetam, Phenotropil, Vinpotropil), peptide drugs (Cortexin, Cerebrolysin, Noopept, Semax), antidepressants and tranquilizers (benzodiazepines and non-benzodiazepine). It is determined that the most important indicator of memory quality is short-term memory. In the experimental group in the process of physical rehabilitation revealed an improvement in this memory in 50% of patients, the deterioration of this indicator in 34% of persons, and 16% memory remained at the same level. Short-term memory indices in post-stroke patients of the control group are lower and correspond to: improvement – in 35%, deterioration – in 40%, remained at the same level in 25% of patients. Since the rate of short-term memory is 7 ± 2 units of information, the study showed that in all patients after a stroke, the indicators of storing information in short-term memory have become normal. The study of attention stability revealed that in the control group of patients it is worse than in the experimental group, and that the stability of attention does not depend on the experience of the post-stroke state. Patients with 3 years of post-stroke experience show the same results as patients with 6-month stroke. The study of inductive thinking showed that in both groups of patients it is in good condition. As for the indicators of practical mathematical thinking, 83% of the participants coped with the task in the experimental group, and 17% failed. In the control group, 57% of patients coped with this task, and 43% failed. Only 50% of the patients in the experimental group and 42% of the control group coped with a more difficult task in this type of thinking. The same results were obtained in persons without stroke. This shows that the more difficult tasks of identifying this type of thinking are difficult for people after a stroke. It can be concluded that the mental processes of a person after a stroke are in optimal condition.