Сосудистые заболевания головного мозга -одна из главных причин заболеваемости, смертности и инвалидизации населения стран Евросоюза, США и Японии.Ежегодно в мире переносят инсульт около 6 млн человек.Увеличение распространенности инсульта наблюдается у лиц работоспособного возраста -до 60 лет.Согласно международным эпидемиологическим исследованиям, в мире от инсульта ежегодно умирает 4,7 млн человек.В большинстве промышленно развитых стран инсульт занимает 2-3 место в структуре общей смертности населения, уступая лишь кардиоваскулярной патологии.Ранняя 30-дневная летальность после инсульта составляет в среднем 30-40 %, а в течение года умирает около 50 % больных.Инсульт является основной причиной инвалидизации населения.Лишь около 20 % выживших больных могут вернуться к прежней работе.По данным ВОЗ, средняя стоимость прямых и непрямых расходов на одного больного составляет около 80 тыс.долл.США в год.Таким образом, сосудистые заболевания головного мозга являются чрезвычайно важной проблемой современной медицины.

The continuous research of new effective drugs is associated with a significant number of diseases, pathological conditions. Conventional treatment with existing drugs could be ineffective, or addictive, and have a large number of side effects. Therefore, the aim of modern pharmacy is to minimize the toxicity of drugs and create new modern domestic medicine that would be more effective in relation to their activity and relatively non-toxic. Derivatives of 1,2,4-triazol have considerable synthetic, pharmacological potential. That’s why study of the synthetic methods of the new structures obtain, its physical, physico-chemical, biological properties may become the basic for their spector of the synthesized derivatives and biological activity widening. The aim of the work: choice on the investigation ground in silico the basic structures 1,2,4-triazol-3-thione and the special purpose synthesis of the new potential biological active compounds, definition its structure and physic-chemical properties mark of antiexudative activity. The synthesis of pyroline derivatives of 2-((4-amino-5-(furan-2-il)-1,2,4-triazol-4H-3-il)-sulfanyl)-N-acetamides was accomplished by stages. The article describes the synthesis of new pyrolin derivatives 2-((4-amino-5(furan-2-yl)-1,2,4-triazol-4H-3-il)-sulfanyl)-N-acetamide. Acetamides were obtained by alkylation of 2-((4-amino-5(furan-2-yl)-1,2,4-triazol-3-thione N-aryl-substituted α-chloroacetamides in the presence of KOH. Using Paal-Knorr condensation of the amino group at 4th position of the triazole ring modified into pyrolium fragment. Physical and chemical characteristics, chemical structure and anti-exudative activity of the obtained compounds were established. Anti-exudative activity of compounds was investigated in the experiments on the white rats in the doses 10 mg/kg comparately with reference drug-diclophenac natrium in formalin edema modulation. The paw size was measured by pletismography before drugs introduction. For the first time 24 compounds have been synthesized: 4 pyroline derivatives 2-((4-amino-5-(furan-2-il)-1,2,4-triazol-4H-3-il)-sulfanyl)-N-acetamides. In 91% of the new synthesized derivatives the antiexudative properties have been found, 5 compounds (10.9, 10.10, 10.15, 10.21, 10.1) by anti-exudative activity have exceeded the reference drug. It is considered that the investigations of these compounds by presence or absence analgesics activities are perspective.

Оригінальний метаболітотропний препарат -елгацин: квантово-хімічні властивості та особливості фармакологічної діїПредставлено членом-кореспондентом НАН України І

Phosphorus plays the important role in metabolic processes comes in composition of nucleic acids, macroergic compounds, phosphorus is contained in the bone tissue, less in the brain tissue, muscles, blood. Phosphorus is in the structure of drugs. Thanks to the nanotechnology, phosphorus is received as the nаnophosphorus particles that is able for agglomeration, have a paramagnetic sensitivity. Nanophosphorus is used for the means’ creation on visualization, many-sided nanoprobes and drugs transporters. Phosphorus is in the phosphides’ structure, combination with the metals that is used in tomography.

The use of laboratory animals in pharmacological and toxicological studies is axiomatic from the point of experimental science and will always be conducted. But these studies are laborious, require additional personnel, the presence of a vivarium, cause the suffering of animals and their death. Therefore, since the late 80's of the last century in the scientific community of Europe and the US actively discusses the issue of toxicological studies in vitro and, in particular, neurotoxicological studies in vitro. But the use of various molecular and biochemical markers of the central nervous system in neurotoxicological studies in vitro, as well as the morphometric parameters of a neuron, can be difficult, because they can be changed by neuroprotective, and not neurotoxic, action of a potential drug. That's why, it is necessary to identify and use molecular or bioche72 I. S. Chekman et al. mical markers, that make it possible to clearly judge about only the neurotoxicity of the drugs. We first discovered a correlation of the expression of 70 kDa protein-chaperones with the disruption of the functioning of the glutathione unit of the thiol-disulfide system on the background of injection of the neurotoxin MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine). Injection of MPTP caused a decrease in the reduced form of glutathione and indirectly led to the deprivation of HSP70 protein expression. The revealed mechanism can be one of the manifestations of the neurotoxic effect of some neuropsychoric drugs. We revealed statistically significant linear dependence of the development of neurological deficit from the functioning of the conjugate system "nitric oxide reduced thiols". The obtained results reveal the importance of the neuron glutathione system as an important target of neuroprotective therapy in ischemic stroke and are the experimental justification for the clinical application of thiol-disulphide system modulators. The coefficient of the ratio of nitrotyrosine to reduced glutathione can be used for the purpose of early laboratory diagnosis of cognitive-mnestic disorders in patients with cerebral pathology. Thus, we identified specific markers for in vitro experiments, that had the greatest potential in providing information on some important mechanisms of neurotoxicity.

Фосфор відіграє важливу роль в обмінних процесах, входить до складу нуклеїнових кислот, макроергічних сполук, фосфоліпідів. Значна кількість фосфору міститься в кістковій тканині, менша - у тканинах мозку, м’язах, крові. Фосфор входить до складу лікарських засобів. Завдяки нанотехнологіям фосфор отримують у вигляді частинок нанофосфору що виявляють парамагнітну чутливість. Нанофосфор застосовують для створення засобів візуалізації багатофункціональних нанозондів, транспортерів лікарських засобів. Фосфор входить до складу фосфідів, сполук з металами, які використовують в томографії.

Квантово-хімічні властивості дикло фенакуДиклофенак натрію -нестероїдний протизапальний засіб, який широко використовується в медичній практиці.Вивчено квантово-хімічні властивості молекули диклофенаку

Summary: Article is devoted to a new direction of nanopharmacology - functioning nanoparticles, nanocom­posites comprising nanomotors that mimic the dynamics of natural motors. The natural nanomotors include ATP-ase. Degree of activation of ATP-ase protein kinesin associated with the hydrolysis of ATP and its synthesis. Wherein a transition of the chemical energy into mechanical energy. Each conformational cycle is set a certain number of reactions. Identify the operation and the mechanism of molecular motors which include Ca2 + ATP-ase myosin, DNA polymerase, etc. Establishment mechanisms of nanomotors contributes to finding new methods of diagnostics and treatment.

Doxorubicin – basic drug for the neoplastic diseases treatment, it’s main adverse effect is cardiotoxicity. The development of this complication is connected with the energy metabolism, prooxidant-antioxidant homeostasis, disturbances and influence on the genetic apparatus. The aim of the study – to state the succin acid’ derivatives – yakton and mexicor influence on indicators of glycolysis, glyconeogenesis and energoproduct function of mitochondria in the rats’ myocardium in the conditions of doxorubicin cardiomyopathy. Results. In was found that myocardial pyruvate, malate, isocitrate, glycogen, glucose-6-phosphate level and malatdegidrogenase activity were decreased in rats with doxorubicin cardiomyopathy. In comparison lactate lactate level increased. Conclusion. Succin acid’ derivatives – yakton and mexicor, administering with doxorubicin, protect glycolysis, glyconeogenesis and energoproduct function of mitochondria in the rats’ myocardium.

У статті наведено перелік деяких різновидів алотропних модифікацій вуглецю, проаналізовано їх характеристики і властивості. Узагальнено відо- мості про раціональне використання нанокарбонових структур у науці й техніці. Викладено історію їх відкриття і перспективні шляхи подальшого розвитку. Особливу увагу приділено біомедичному застосуванню нанокарбонових сполук та обґрунтовано необхідність евалюації їх токсичного впливу на живі системи.

Doxorubicin, which is included in the scheme of cancer treatment, possesses cardiotoxicity that requires effective cardioprotectors searching. Aim. The aim of the study was to compare the influence of yacton and mexicor on the antioxidant system, oxidative modification of proteins, protein synthesis in the myocardium of rats in conditions of doxorubicin cardiomyopathy. Methods and results. The content of prooxidant-antioxidant homeostasis indicators - SOD, GPR, GR, AFG, KFG and proteinsynthesis – the protein content in the cytoplasma and mitochondria and protective effect of derivatives of succinic acid (yacton, mexicor) were studied in the myocardium of rats in the conditions doxorubicin cardiomyopathy with wellknown methods. Conclusion. It is stated that yakton similar to mexicor has protective influence on the prooxidant-antioxidant homeostasis, protein synthesis in the rats myocardium in conditions of doxorubicin cardiomyopathy.

The aim of the work was to estimate biosafety of iron nanoparticles’ substance according to in vitro and in vivo tests. Materials and Methods: biosafety of the substance of 40 nm sized spherical zero-valent iron nanoparticles has been established in vitro using cytotoxicity and genotoxicity tests. Biosafety in vivo has been determined according to the acute toxicity parameter (LD50) and the effect on cardiac function and state of rabbits’ hemodynamics. Results: there were no cytotoxic and genotoxic effects of iron nanoparticles’ substance on the test culture of eukaryotic cells. In case of intravenous injection of nanoparticles the average LD50 for BALB/с mice was 220.3 mg/kg. Iron nanoparticles’ substance injected intravenously was safe according to hemodynamic parameters. Conclusion: obtained data on biosafety estimation denotes low level of potential risks associated with iron nanoparticles’ substance.