Combined intraarterial/intravenous thrombolysis for acute ischemic stroke

BACKGROUND AND PURPOSE: The intravenous use of recombinant tissue-type plasminogen activator (rTPA) in acute ischemic stroke has been investigated in three large trials. Limited series have reflected outcome after local intraarterial thrombolysis (LIT) in the cerebral territory. The purpose of this study was to evaluate the safety and efficacy of combined intraarterial/intravenous thrombolysis using rTPA (actilyse) for acute ischemic stroke. METHODS: Forty-five patients with acute onset of severe hemispheric stroke and without signs of major cerebral infarction on early CT scans were randomized by order of admission. Twelve patients were treated with 50 mg actilyse (maximal dose, 0.7 mg/kg); three had occlusion of the internal carotid artery and nine had occlusion of the middle cerebral artery. Thrombolysis was started by LIT and continued intravenously within 6 hours of stroke onset. Outcome, assessed after 1 and 12 months according to the modified Rankin scale (MRS), was considered good (MRS score, 0-3) for patients who were functionally independent and poor (MRS score, 4-5) for those who were dependent or had died. RESULTS: In the thrombolysis group, outcome was good in eight patients at 1 month and in 10 patients at 12 months; in the control group, outcome was good in seven (21%) and 11 (33%) patients, respectively. Of the eight patients with a good outcome after thrombolysis, four had complete and one had partial recanalization. In the control group, the rate of intracerebral hemorrhage was 6%. Mortality at 1 month in the thrombolysis and control groups was 17% and 48%, respectively. CONCLUSIONS: Combined intraarterial/intravenous thrombolysis with low-dose rTPA may be a safe and effective treatment for acute ischemic stroke within 6 hours in carefully selected patients.Peer reviewe

THE METHOD FOR DETERMINING THE ABSOLUTE CONFIGURATION USING NSUBSTITUTED CYCLIC AMINO ACIDS

Determining the absolute configuration of biologically active chiral substances is a current issue in drug development since biological properties of enantiomers may greatly vary. The absolute configuration of enantiomers can be determined using crystallography, circular dichroism, or by the method that involves chiral derivatizing agents and analysis of NMR spectra.This work was supported by the Russian Science Foundation, project no. 16-13-10358

Оценка противоречивости логической структуры учебного плана

Purpose of the study. The main purpose of creating a curriculum is to regulate academic disciplines in accordance with the logic of the learning process, defined by the relationship between the basic concepts of the disciplines. Violation of this logic becomes apparent only directly during the training sessions.A large variety of quantitative methods uses indicators that do not reveal structural deficiencies in the curriculum. This makes it difficult to improve the curriculum.The purpose of this work is to demonstrate the application of a general approach to the assessment of the structural inconsistency of systems in relation to the evaluation of the logical structure of the curriculum.Materials and methods. The paper applies a general approach to the assessment of structural integrity, developed on the basis of the provisions of the general theory of systems and graph theory. The approach involves the construction of three interrelated structural models of the system and using them to determine the initial data for calculating the index of inconsistency of the system structure.Results. The overall approach to the assessment of structural integrity is adapted to assess the logical structure of the curriculum. Three models of curriculum structure are developed:Elementary model of interdisciplinary communication;Curriculum network model;Hierarchical curriculum model.Based on the parameters of the hierarchical curriculum model, using three adapted algorithms, the value of the inconsistency index of the curriculum structure in the direction of preparation “Applied Informatics” is calculated. Recommendations on changing the structure of the studied curriculum to reduce the degree of its structural inconsistency are proposed. Conclusion. As a result of the research, the methods were proposed that allow identifying possible contradictions in the structure of the curriculum and evaluating its inconsistency. As the experiments have shown, it is extremely difficult to study the curricula in a manual manner, the number of disciplines in which exceeds 50. In this regard, the development of a complex of computer programs that will automate the assessment of the inconsistency of large curricula is being completed.Цель исследования. Основной целью создания учебного плана является упорядочение учебных дисциплин в соответствии с логикой процесса обучения, определенной взаимосвязями между основными понятиями дисциплин. Нарушение данной логики становится очевидным только непосредственно в ходе проведения учебных занятий.Большое разнообразие количественных методов используют показатели, которые не позволяют выявить структурные недоработки учебного плана. Это затрудняет процесс улучшения учебного плана.Целью данной работы является продемонстрировать применение общего подхода к оценке структурной противоречивости систем применительно к оценке логической структуры учебного плана.Материалы и методы. В работе применен общий подход к оценке структурной целостности, разработанный на основе положений общей теории систем и теория графов. Подход предусматривает построение трех взаимосвязанных структурных моделей системы и определения с их помощью исходных данных для расчета показателя противоречивости структуры системы.Результаты. Общий подход к оценке структурной целостности адаптирован для оценки логической структуры учебного плана. Разработаны три модели структуры учебного плана:– элементарная модель междисциплинарных связей;– сетевая модель учебного плана;– иерархическая модель учебного плана.На основе параметров иерархической модели учебного плана с использованием трех адаптированных алгоритмов рассчитано значение показателя противоречивости структуры учебного плана по направлению подготовки Прикладная информатика. Предложены рекомендации по изменению структуры исследуемого учебного плана для понижения степени его структурной противоречивости.Заключение. В результате проведенных исследований предложена методика, которая позволяет выявить возможные противоречия в структуре учебного плана и дать оценку его противоречивости.Как показали проведенные эксперименты, исследовать ручным способом учебные планы, количество дисциплин в которых превышает 50, крайне сложно. В связи с этим завершается разработка комплекса компьютерных программ, которые позволят автоматизировать оценку противоречивости больших учебных планов

Національна доповідь про стан і перспективи розвитку освіти в Україні: монографія (До 30-річчя незалежності України)

The publication provides a comprehensive analysis of the state and development of national education over the 30 years of Ukraine’s independence, identifies current problems in education, ascertains the causes of their emergence, offers scientifically reasoned ways to modernise domestic education in the context of globalisation, European integration, innovative development, and national self-identification. Designed for legislators, state officials, education institutions leaders, teaching and academic staff, the general public, all those who seek to increase the competitiveness of Ukrainian education in the context of civilisation changes.У виданні здійснено всебічний аналіз стану і розвитку національної освіти за 30-річний період незалежності України, визначено актуальні проблеми освітньої сфери, виявлено причини їх виникнення, запропоновано науково обґрунтовані шляхи модернізації вітчизняної освіти в умовах глобалізації, європейської інтеграції, інноваційного розвитку та національної самоідентифікації. Розраховано на законодавців, державних управлінців, керівників закладів освіти, педагогічних і науково-педагогічних працівників, широку громадськість, усіх, хто прагне підвищення конкурентоспроможності української освіти в контексті цивілізаційних змін

Inconsistency evaluation of the curriculum logical structure

Purpose of the study. The main purpose of creating a curriculum is to regulate academic disciplines in accordance with the logic of the learning process, defined by the relationship between the basic concepts of the disciplines. Violation of this logic becomes apparent only directly during the training sessions.A large variety of quantitative methods uses indicators that do not reveal structural deficiencies in the curriculum. This makes it difficult to improve the curriculum.The purpose of this work is to demonstrate the application of a general approach to the assessment of the structural inconsistency of systems in relation to the evaluation of the logical structure of the curriculum.Materials and methods. The paper applies a general approach to the assessment of structural integrity, developed on the basis of the provisions of the general theory of systems and graph theory. The approach involves the construction of three interrelated structural models of the system and using them to determine the initial data for calculating the index of inconsistency of the system structure.Results. The overall approach to the assessment of structural integrity is adapted to assess the logical structure of the curriculum. Three models of curriculum structure are developed:Elementary model of interdisciplinary communication;Curriculum network model;Hierarchical curriculum model.Based on the parameters of the hierarchical curriculum model, using three adapted algorithms, the value of the inconsistency index of the curriculum structure in the direction of preparation “Applied Informatics” is calculated. Recommendations on changing the structure of the studied curriculum to reduce the degree of its structural inconsistency are proposed. Conclusion. As a result of the research, the methods were proposed that allow identifying possible contradictions in the structure of the curriculum and evaluating its inconsistency. As the experiments have shown, it is extremely difficult to study the curricula in a manual manner, the number of disciplines in which exceeds 50. In this regard, the development of a complex of computer programs that will automate the assessment of the inconsistency of large curricula is being completed

Analysis of P‑Glycoprotein Transport Cycle Reveals a New Way to Identify Efflux Inhibitors

P-glycoprotein (P-gp) is found to be of considerable interest for the design of drugs capable of treating chemoresistant tumors. This transporter is an interesting target for which an efficient approach has not yet been developed in terms of computer simulation. In this work, we use a combination of docking, molecular dynamics, and metadynamics to fully explore the states that occur during the capture of a ligand and subsequent efflux by P-gp. The proposed approach allowed us to substantiate a number of experimentally established facts, as well as to develop a new criterion for identifying potential P-gp inhibitors

CCDC 924376: Experimental Crystal Structure Determination

An entry from the Cambridge Structural Database, the worlds repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures