In Vitro Effects of Fungal Phytotoxins on Cancer Cell Viability: First Insight into Structure Activity Relationship of a Potent Metabolite of Cochliobolus australiensis Radicinin

Natural compounds have always represented an important source for new drugs. Although fungi represent one such viable source, to date, no fungal metabolite has been marketed as an anticancer drug. Based on our work with phytotoxins as potential chemical scaffolds and our recent findings involving three phytopathogenic fungi, i.e., Cochliobolus australiensis, Kalmusia variispora and Hymenoscyphus fraxineus, herein, we evaluate the in vitro anti-cancer activity of the metabolites of these fungi by MTT assays on three cancer cell models harboring various resistance levels to chemotherapeutic drugs. Radicinin, a phytotoxic dihydropyranopyran-4,5-dione produced by Cochliobolus australiensis, with great potential for the biocontrol of the invasive weed buffelgrass (Cenchrus ciliaris), showed significant anticancer activity in the micromolar range. Furthermore, a SAR study was carried out using radicinin, some natural analogues and hemisynthetic derivatives prepared by synthetic methods developed as part of work aimed at the potential application of these molecules as bioherbicides. This investigation opens new avenues for the design and synthesis of novel radicinin analogues as potential anticancer agents

Metal-free transannulation reaction of indoles with nitrostyrenes: a simple practical synthesis of 3-substituted 2-quinolones

3-Substituted 2-quinolones are obtained via a novel, metal-free transannulation reaction of 2-substituted indoles with 2-nitroalkenes in polyphosphoric acid. The reaction can be used in conjunction with the Fisher indole synthesis offering a practical three-component heteroannulation methodology to produce 2-quinolones from arylhydrazines, 2-nitroalkenes and acetophenone

Анализ ассортимента древесно-кустарниковых растений, используемых в озеленении г. Саратова

The article deals with the history of green space expansion in the city of Saratov based on comparative analysis of the range of green spaces for 1966, 1998, and 2017. The authors note the expansion tendency of the wood species range applied in city landscaping due to the inclusion of invasive plants and decorative forms of trees and bushes. The results of a comprehensive assessment of the current state of the range of plants at the sites of urban landscaping and long-term observations of them allowed determining the types and varieties of trees, shrubs, and lianas, which had successfully adapted to the urban environment states. The authors have developed a broad range of plants, which includes 138 names of tree and bush species recommended for application on landscaping sites of various categories in Saratov.El artículo considera la historia de la construcción verde en la ciudad de Saratov, se realiza un análisis comparativo de la variedad de espacios verdes para 1966, 1998 y 2017. Existe una tendencia a expandir la variedad de especies utilizadas en el paisajismo de la ciudad debido a la inclusión de introductores y formas decorativas de árboles y arbustos en ella. Los resultados de una evaluación exhaustiva del estado actual del surtido de plantas en las instalaciones de paisajismo de la ciudad y las observaciones a largo plazo de ellos permitieron determinar los tipos y variedades de especies de árboles, arbustos y enredaderas que se adaptaron con éxito a las condiciones del entorno urbano. Sobre la base de los datos obtenidos, se desarrolló una variedad de 138 nombres de especies de arbustos arbóreos recomendados para su uso en objetos de varias categorías de espacios verdes de la ciudad de Saratov.В статье рассмотрена история зеленого строительства в г. Саратове, выполнен сравнительный анализ ассортимента зеленых насаждений за 1966, 1998 и 2017 годы. Отмечена тенденция расширения ассортимента применяемых в озеленении города пород за счет включения в него интродуцентов и декоративных форм деревьев и кустарников. Результаты комплексной оценки современного состояния ассортимента растений на объектах озеленения города и многолетние наблюдения за ними позволили определить виды и сорта древесных, кустарниковых пород и лиан, которые успешно адаптировались к условиям городской среды. На основании полученных данных разработан ассортимент из 138 наименований древесно-кустарниковых видов, рекомендованных к применению на объектах различных категорий зеленых насаждений г. Саратова

The development of the solution search method based on the improved bee colony algorithm

Active digitization of people's daily life leads to the use of the decision-making support systems (DMSS). DMSS is actively used in data processing, forecasting the course of various processes, providing informational support for the decision-making process by decision makers. However, a number of problems arise while evaluating monitoring objects, namely: a large number of destabilizing factors affecting the efficiency of the processes of information collection, processing and transmission; high dynamism of changes in the state and composition of heterogeneous monitoring objects during the conduct of hostilities (operations); high dynamism of conducting hostilities (operations); the uncertainty of the initial situation and the noise of the initial data. In this article, a method of finding solutions based on an improved bee colony algorithm was developed. The efficiency of information processing is achieved by learning the architecture of artificial neural networks; taking into account the type of uncertainty of the information to be evaluated; the use of an improved algorithm of the bee colony, the use of an unordered linguistic scale of measurements with adjustment coefficients for the degree of awareness and the degree of noise of the initial data. An approbation of the use of the proposed method was carried out on the example of assessing the state of the operational grouping of troops (forces). The method is proposed to be used in the development of software for automated systems of control of troops and weapons, namely, in the modernization of existing and development of new automated systems of control of troops and weapons. The evaluation of the effectiveness of the proposed method showed an increase in the efficiency of the evaluation at the level of 21–28 % in terms of the efficiency of information processin

Deniable encryption protocols based on probabilistic public-key encryption

The paper proposes a new method for designing deniable encryption protocols characterized in using RSA-like probabilistic public-key encryption algorithms. Sender-, receiver-, and bi-deniable protocols are described. To provide bi-deniability in the case of attacks perfored by an active coercer stage of entity authentication is used in one of described protocols

The state and dynamics of the intellectual infrastructure of technological development of industrial enterprises: methodological tools for assessing sustainability

The article presents the results of research in the field of formation of methods of organization of intellectual infrastructure of technological development of industrial enterprises, focused on methodological issues of measuring and assessing its sustainability. The relevance of the research is due to modern trends in the intellectualization of the economy under the influence of technological processes of digitalization, which determine the need for the formation of new infrastructure institutions necessary to solve modern problems of technological development in industry. As a result of this research stage, the structural characteristics and parameters that determine the state and dynamics of the intellectual infrastructure of technological development of industrial enterprises have been clarified, which allowed us to offer methodological tools for assessing the state of stability of the intellectual infrastructure and the prospects for its positive dynamics focused on the digital transformation of business processes of industrial production. Thus, as structural elements that determine the organizational level of the intellectual infrastructure of technological development of industrial enterprises, the following are defined: the level of material resources used in the production of products; the availability of logistics routes; the environmental impact of the results of resource processing, including the cost of disposal of residues; the state of fixed assets. The author’s approach to the assessment of the intellectual infrastructure of technological development of industrial enterprises has been developed, based on the identification of key elements of the studied infrastructure, classification of resource blocks, justification of indicators and factors of resource components that affect the stability of the intellectual infrastructure of technological development. This approach makes it possible to develop and improve methodological tools for analytical assessment of the organizational level of stability of the intellectual infrastructure of technological development, identifying trends in its dynamics, as well as controlling unacceptable deviations

Structural features of Ni-Cr-Si-B materials obtained by different technologies

This study considers the structural features of Ni-Cr-Si-B (Ni - base; 15.1 % Cr; 2 % Si; 2 % B; 0.4 % C) materials obtained by different methods. The self-fluxing coatings were deposited by plasma spraying on the tubes from low carbon steel. Bulk cylinder specimens of 20 mm diameter and 15 mm height were obtained by spark plasma sintering (SPS). The structure and phase composition of these materials were investigated by optical microscopy (OM), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and X-ray diffractometry (XRD). The major phases of coatings and sintered materials are [gamma]-Ni, Ni[3]B, CrB and Cr[7]C[3]. We demonstrate that the particle unmelted in the process of plasma spraying or SPS consist of [gamma]-Ni-NEB eutectic and also CrB and Cr[7]C[3] inclusions. The prolonged exposure of powder to high temperatures as well as slow cooling rates by SPS provide for the growth of the structural components as compared to those of plasma coatings materials. High cooling rates at the plasma spraying by melted particles contribute to the formation of supersaturated solid solution of Cr, Si and Fe in [gamma]-Ni. The structure of the melted particles in sintering material has gradient composition: the core constituted of Ni grains of 10 μm with [gamma]-Ni-Ni[3]B eutectic on the edges. The results of the experiment demonstrate that the sintering material has a smaller microhardness in comparison with plasma coatings (650 and 850 MPa, respectively), but at the same time the material has higher density (porosity less than 1 %) than plasma coatings (porosity about 2.. .3 %)

Application of DICOM in Electrical Impedance Tomography

Medical imaging devices including EIT systems are required to be integrated in the clinical information systems. Combining DICOM industrial standard with Open EIT file format can lead to the result, appropriate both to clinical requirements and research community. Successful implementation of the DICOM format for data storage in real EIT system is described here

Higginsianins A and B, Two Diterpenoid α-Pyrones Produced by Colletotrichum higginsianum, with in Vitro Cytostatic Activity

Two new diterpenoid α-pyrones, named higginsianins A (1) and B (2), were isolated from the mycelium of the fungus Colletotrichum higginsianum grown in liquid culture. They were characterized as 3-[5a,9b-dimethyl-7-methylene-2-(2-methylpropenyl)dodecahydronaphtho[2,1-b]furan-6-ylmethyl]-4-hydroxy-5,6-dimethylpyran-2-one and 4-hydroxy-3-[6-hydroxy-5,8a-dimethyl-2-methylene-5-(4-methylpent-3-enyl)decahydronaphthalen-1-ylmethyl]-5,6-dimethylpyran-2-one, respectively, by using NMR, HRESIMS, and chemical methods. The structure and relative configuration of higginsianin A (1) were confirmed by X-ray diffractometric analysis, while its absolute configuration was assigned by electronic circular dichroism (ECD) experiments and calculations using a solid-state ECD/TDDFT method. The relative and absolute configuration of higginsianin B (2), which did not afford crystals suitable for X-ray analysis, were determined by NMR analysis and by ECD in comparison with higginsianin A. 1 and 2 were the C-8 epimers of subglutinol A and diterpenoid BR-050, respectively. The evaluation of 1 and 2 for antiproliferative activity against a panel of six cancer cell lines revealed that the IC50 values, obtained with cells reported to be sensitive to pro-apoptotic stimuli, are by more than 1 order of magnitude lower than their apoptosis-resistant counterparts (1 vs >80 μM). Finally, three hemisynthetic derivatives of 1 were prepared and evaluated for antiproliferative activity. Two of these possessed IC50 values and differential sensitivity profiles similar to those of 1

Розроблення методики обґрунтування потреби у зразках озброєння та цілерозподілу при застосуванні розвідувально-вогневої системи

This paper proposes an algorithm to substantiate the need for weapons samples, as well as targeting when using a reconnaissance firing system taking into consideration the peculiarities of functioning of such systems. The algorithm essentially implies streamlining the stages in determining the magnitude of the reduction of the enemy's combat potential and, on its basis, the formation of the need for the number of weapons by type. The algorithm makes it possible to take into consideration the nonlinearity of functions that describe both different types of weapons and targets. In addition, this algorithm is based on a modified method of nonlinear programming (two functions). The modification involves the use of a normalized share of the weight of each target as weight coefficients. This allows for targeting while taking into consideration the established level of the combat potential of an enemy. A procedure for determining the need for samples of weapons and targeting in the use of reconnaissance firing systems has been devised. It was determined that in order to achieve the goal of enemy fire damage, it is not typically necessary to use all weapons samples. In general, the procedure makes it possible to take into consideration the peculiarities of the samples of weapons and their suitability to hit a certain target. That could prevent problems with overspending of resources, failures in the detection-defeat cycle, non-fulfillment (not fully performing) tasks during enemy fire damage. In general, the algorithm and procedure for determining the need for the samples of weapons and targeting when using a reconnaissance firing system testify to devising a methodology for justifying the need for weapons samples and targeting. The performance and adequacy of this procedure have been tested by considering an example of determining the need for weapons samples and targeting and obtaining the result confirmed by the experience in the use of reconnaissance firing systemsПредложен алгоритм обоснования потребности в образцах вооружения и целераспределения при применении разведывательно-огневой системы с учетом особенностей функционирования таких систем. Сущность алгоритма заключается в упорядочении этапов по определению величины снижения боевого потенциала противника и на его основании формирование потребности в количестве вооружения по типам. Указанный алгоритм позволяет учесть нелинейность функций, которые описывают как различные типы вооружения, так и цели. К тому же этот алгоритм базируется на модифицированном методе нелинейного программирования (двух функций). Модификация заключается в использовании в качестве весовых коэффициентов нормированных долей веса каждой цели. Это позволяет проводить целераспределение с учетом установленного уровня боевого потенциала противника. Разработана процедура определения потребности в образцах вооружения и целераспределения при применении разведывательно-огневых систем. Определено, что для достижения цели огневого поражения противника, как правило, не требуется использовать все образцы вооружения. В целом же указанная процедура позволяет учитывать особенности образцов вооружения и их пригодность к поражению определенной цели. Это позволит предотвратить возникновение проблем по перерасходу ресурсов, сбоям в цикле обнаружения-поражения, невыполнение (не в полной мере выполнения) задач во время огневого поражения противника. В целом же алгоритм и процедура определения потребности в образцах вооружения и целераспределения при применении разведывательно-огневой системы свидетельствует о разработке методики обоснования потребности в образцах вооружения и целераспределения. Работоспособность и адекватность этой методики проверены путем рассмотрения примера определения потребности в образцах вооружения и целераспределения и получении результата, подтвержденного опытом применения разведывательно-огневых системЗапропоновано алгоритм обґрунтування потреби у зразках озброєння та цілерозподілу при застосуванні розвідувально-вогневої системи з урахуванням особливостей функціонування таких систем. Сутність алгоритму полягає у впорядкуванні етапів щодо визначення величини зниження бойового потенціалу противника та його підставі формування потреби у кількості озброєння за типами. Означений алгоритм дозволяє врахувати нелінійність функцій, які описують як різні типи озброєння, так і цілі. До того ж, цей алгоритм базується на модифікованому методі нелінійного програмування (двох функцій). Модифікація полягає у використанні у якості вагових коефіцієнтів нормованих часток ваги кожної цілі. Це дозволяє проводити цілерозподіл з урахуванням встановленого рівня бойового потенціалу противника. Розроблено процедуру визначення потреби у зразках озброєння та цілерозподілу при застосуванні розвідувально-вогневих систем. Визначено, що для досягнення мети вогневого ураження противника, як правило, не потрібно використовувати всі зразки озброєння. Загалом же зазначена процедура дозволяє враховувати особливості зразків озброєння та їх придатність до ураження певної цілі. Це дозволить запобігти виникненню проблем щодо перевитрати ресурсів, збоїв у циклі виявлення-ураження, невиконання (не у повній мірі виконання) завдань під час вогневого ураження противника. Загалом же алгоритм та процедура визначення потреби у зразках озброєння та цілерозподілу при застосуванні розвідувально-вогневої системи свідчить про розроблення методики обґрунтування потреби у зразках озброєння та цілерозподілу. Працездатність та адекватність цієї методики перевірені шляхом розгляду прикладу визначення потреби у зразках озброєння та цілерозподілу та отриманні результату, підтвердженого досвідом застосування розвідувально-вогневих систе