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A series of eight 5-nitrofuran-tagged oxazolyl tetrahydropyrazolopyridines (THPPs) has been prepared in six stages with excellent regioselectivity. The testing of these compounds against pathogens of the ESKAPE panel showed a good activity of lead compound 1-(2-methoxyethyl)-5-(5-nitro-2-furoyl)-3-(1,3-oxazol-5-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c] pyridine (13g), which is superior to nitrofurantoin. These results confirmed the benefit of combining a THPP scaffold with a nitrofuran warhead. Certain structure–activity relationships were established in the course of this study which were rationalized by the induced-fit docking experiments in silico. [ABSTRACT FROM AUTHOR]

The use of spirocycles in drug discovery and medicinal chemistry has been booming in the last two decades. This has clearly translated into the landscape of approved drugs. Among two dozen clinically used medicines containing a spirocycle, 50% have been approved in the 21st century. The present review focuses on the notable synthetic routes to such drugs invented in industry and academia, and is intended to serve as a useful reference source of synthetic as well as general drug information for researchers engaging in the design of new spirocyclic scaffolds for medicinal use or embarking upon analog syntheses inspired by the existing approved drugs. [ABSTRACT FROM AUTHOR]

Directed formation of the structure of the culture of living cells is the most important task of tissue engineering. New materials for 3D scaffolds of living tissue are critical for the mass adoption of regenerative medicine protocols. In this manuscript, we demonstrate the results of the molecular structure study of collagen from Dosidicus gigas and reveal the possibility of obtaining a thin membrane material. The collagen membrane is characterized by high flexibility and plasticity as well as mechanical strength. The technology of obtaining collagen scaffolds, as well as the results of studies of its mechanical properties, surface morphology, protein composition, and the process of cell proliferation on its surface, are shown in the given manuscript. The investigation of living tissue culture grown on the surface of a collagen scaffold by X-ray tomography on a synchrotron source made it possible to remodel the structure of the extracellular matrix. It was found that the scaffolds obtained from squid collagen are characterized by a high degree of fibril ordering and high surface roughness and provide efficient directed growth of the cell culture. The resulting material provides the formation of the extracellular matrix and is characterized by a short time to living tissue sorption. [ABSTRACT FROM AUTHOR]

Microalgae are rich in proteins, carbohydrates, lipids, polyunsaturated fatty acids, vitamins, pigments, enzymes, and other biologically active substances. This research aimed to study the composition and antioxidant and antimicrobial activity of proteins, lipids, and carbohydrates of microalgae found in the Filinskaya Bay of the Kaliningrad region. The chemical composition of Scenedesmus intermedius and Scenedesmus obliquus microalgae biomass was studied. Ultrasound was used to isolate valuable components of microalgae. It was found that microalgae are rich in protein and contain lipids and reducing sugars. To confirm the accuracy of the determination, the protein content was measured using two methods (Kjeldahl and Bradford). Protein content in S. intermedius and S. obliquus microalgae samples did not differ significantly when measured using different methods. Protein extraction by the Kjeldahl method was found to be 63.27% for S. intermedius microalgae samples and 60.11% for S. obliquus microalgae samples. Protein content in S. intermedius samples was 63.46%, compared to 60.07% in S. obliquus samples, as determined by the Bradford method. Lipids were 8.0–8.2 times less abundant than protein in both types of microalgae samples. It was determined that the content of reducing sugars in the samples of the studied microalgae was 5.9 times less than the protein content. The presence of biological activity (antioxidant) in proteins and lipids obtained from biomass samples of the studied microscopic algae was established, which opens up some possibilities for their application in the food, chemical, and pharmaceutical industries (as enzymes, hormones, vitamins, growth substances, antibiotics, and other biologically active compounds). [ABSTRACT FROM AUTHOR]

Miscanthus is a perennial wild plant that is vital for the production of paper and roofing, as well as horticulture and the development of new high-yielding crops in temperate climates. Chromosome-level assembly of the ancient tetraploid genome of miscanthus chromosomes is reported to provide resources that can link its chromosomes to related diploid sorghum and complex polyploid sugarcane. Analysis of Miscanthus sinensis and Miscanthus sacchariflorus showed intense mixing and interspecific hybridization and documented the origin of a high-yielding triploid bioenergetic plant, Miscanthus × giganteus. The Miscanthus genome expands comparative genomics functions to better understand the main abilities of Andropogoneae herbs. Miscanthus × giganteus is widely regarded as a promising lignocellulosic biomass crop due to its high-biomass yield, which does not emit toxic compounds into the environment, and ability to grow in depleted lands. The high production cost of lignocellulosic bioethanol limits its commercialization. The main components that inhibit the enzymatic reactions of fermentation and saccharification are lignin in the cell wall and its by-products released during the pre-treatment stage. One approach to overcoming this barrier could be to genetically modify the genes involved in lignin biosynthesis, manipulating the lignin content and composition of miscanthus. [ABSTRACT FROM AUTHOR]

The excess biomass of drifting algae and their casting to the Baltic Sea coast imposes a significant environmental burden. The analysis of beach-cast algae showed that the dominant species are macroalgae Ulva sp., Furcellaria lumbricalis, Cladophora sp., and Polysiphonia fucoides. The biomass of Furcellaria and Polysiphonia algae, containing 25.6% and 19.98% sugars, respectively, has the greatest resource potential in terms of obtaining carbohydrates. Fucose, glucose, and galactose were found to be the most common carbohydrates. The lipid content did not exceed 4.3% (2.3–4.3%), while the fatty acid composition was represented by saturated fatty acids (palmitic, stearic, methyloleic, behenic, etc.). The highest content of crude protein was found in samples of macroalgae of the genus Polysiphonia and amounted to 28.2%. A study of the elemental composition of drifting algae revealed that they have a high carbon content (31.3–37.5%) and a low hydrogen (4.96–5.82%), and sulfur (1.75–3.00%) content. Red algal biomass has the most resource potential in terms of biofuel generation, as it has a high number of lipids and proteins that can produce melanoidins during hydrothermal liquefaction, enhancing the fuel yield. The study noted the feasibility of using the biomass of the studied algae taxa to produce polysaccharides and biofuels. The analyses of antioxidant properties, fat content, and fat composition do not provide convincing evidence of the viability of using the aforementioned macroalgae for their production. [ABSTRACT FROM AUTHOR]

The article titled "The Dosidicus gigas Collagen for Scaffold Preparation and Cell Cultivation: Mechanical and Physicochemical Properties, Morphology, Composition and Cell Viability" has been retracted by the Polymers Editorial Office. Concerns were raised about the article's overlap with previously published work from different authorship groups. An investigation confirmed that there was an overlap of raw data without appropriate citation or permission. The article has been retracted in accordance with MDPI's retraction policy. The authors of the article have agreed to this retraction. [Extracted from the article]

This work aims to study the qualitative composition of biologically active substance (BAS) extracts in vitro callus, cell suspension, and root cultures of the medicinal plant Rhaponticum carthamoides. The research methodology is based on high-performance liquid chromatography, and 1H nuclear magnetic resonance (NMR) spectra, to study the qualitative and quantitative analysis of BAS. The results of the qualitative composition analysis of the dried biomass extracts of in vitro callus, cell suspension and root cultures showed that the main biologically active substances in the medicinal plant Rhaponticum carthamoides are 2-deoxy-5,20,26-trihydroxyecdyson (7 mg, yield 0.12%), 5,20,26-trihydroxyecdyson 20,22-acetonide (15 mg, yield 0.25%), 2-deoxy-5,20,26-trihydroxyecdyson 20,22-acetonide (6 mg, yield 0.10%), 20,26-dihydroxyecdyson 20,22-acetonidecdyson 20,22-acetonide (5 mg, yield 0.09%), and ecdyson 20,22-acetonide (6 mg, yield 0.10%). In the future, it is planned to study the antimicrobial, antioxidant, and antitumor activity of BAS of extracts of in vitro callus, cell suspension, and root cultures of the medicinal plant Rhaponticum carthamoides, for the production of pharmaceuticals and dietary supplements with antitumor, antimicrobial and antioxidant effects. [ABSTRACT FROM AUTHOR]

Plants of the Miscanthus genus (Miscanthus Anderss.) have a unique index of biomass production in relation to the occupied area. Miscanthus plants can be attributed to promising second-generation raw materials for the production of bioethanol and biofuel. Miscanthus plants are characterized by a high cellulose content. Herein, we report the results of a study on the obtained delignified cellulose with subsequent processing into bioethanol using microbial communities. In the course of the study, the optimal conditions for the delignification of the initial plant material for cellulose were selected. Ethanol with a high degree of conversion was successfully obtained from the isolated delignified cellulose. The article describes the pilot technological scheme for the conversion of Miscanthus plant biomass to bioethanol involving the delignification stages, followed by the conversion of the resulting cellulose into bioethanol by a consortium of microorganisms. As a result of the study, it was found that delignification using trifluoroacetic acid leads to the production of cellulose of high purity. Bioethanol with a yield of 3.1% to 3.4% in terms of the initial amount of biomass was successfully obtained by a microorganism consortium of Saccharomyces cerevisiae M Y-4242/Pachysolen tannophilus Y-3269, and Scheffersomyces stipitis Y-3264. [ABSTRACT FROM AUTHOR]

The lignocellulosic perennial crop miscanthus, especially Miscanthus × giganteus, is particularly interesting for bioenergy production as it combines high biomass production with low environmental impact. However, there are several varieties that pose a hazard due to susceptibility to disease. This review contains links showing genotype and ecological variability of important characteristics related to yield and biomass composition of miscanthus that may be useful in plant breeding programs to increase bioenergy production. Some clones of Miscanthus × giganteus and Miscanthus sinensis are particularly interesting due to their high biomass production per hectare. Although the compositional requirements for industrial biomass have not been fully defined for the various bioenergy conversion processes, the lignin-rich species Miscanthus × giganteus and Miscanthus sacchariflorus seem to be more suitable for thermochemical conversion processes. At the same time, the species Miscanthus sinensis and some clones of Miscanthus × giganteus with low lignin content are of interest for the biochemical transformation process. The species Miscanthus sacchariflorus is suitable for various bioenergy conversion processes due to its low ash content, so this species is also interesting as a pioneer in breeding programs. Mature miscanthus crops harvested in winter are favored by industrial enterprises to improve efficiency and reduce processing costs. This study can be attributed to other monocotyledonous plants and perennial crops that can be used as feedstock for biofuels. [ABSTRACT FROM AUTHOR]

Medicinal plants (Cotinus coggygria, Dactylorhiza maculata, Platanthera chlorantha) growing in various territories (Kaliningrad, Moscow, and Minsk regions) were the objects of research. This paper presents a study of the chemical composition of these plants. To analyze the qualitative and quantitative composition of biologically active substances, the method of high-performance liquid chromatography was used. Atomic absorption spectrometry was used to study the content of trace elements. The content of organic acids and vitamins was determined by capillary electrophoresis using the Kapel-105/105M capillary electrophoresis system with high negative polarity. Extracts of medicinal plants were obtained on a Soxhlet apparatus using 70% ethanol as an extractant. It was found that among the biologically active substances in the plants under discussion, hyperoside, rutin (C. coggygria), Ferulic acid and Gallic acid (D. maculata), triene hydrocarbon (3,7-Dimethyl-1,3,6-octatriene), unsaturated alcohol (3,7-Dimethyl-2,6-octadien-1-ol), and benzyl acetate (P. chlorantha) prevailed. Samples of these medicinal plants contained trace elements (phosphorus, potassium, calcium, sodium, magnesium, and sulfur) and many aliphatic organic acids (succinic acid, benzoic acid, fumaric acid, citric acid, oxalic acid, and tartaric acid). The largest amount of biologically active substances and secondary metabolites of the studied plants from the Eastern Baltic is associated with climatic and ecological differences from other regions. The composition of these plants determines the potential of their use in feed additives for livestock and poultry as part of measures to improve the quality of livestock products. The use of medicinal plants for the production of feed additives is relevant in terms of improving regional economies, as well as improving the quality of life and nation's health by providing ecologically clean livestock products. [ABSTRACT FROM AUTHOR]

Extremophilic microorganisms attract researchers by their unique characteristics, primarily antagonistic ones, acquired in the process of survival in extreme natural conditions. The antimicrobial potential of the metabolites of these microorganisms is quite broad, from the food industry to therapeutic drugs. Microbial mats of Lake Baikal are a source of unique and diverse microorganisms. The study aimed to evaluate the antimicrobial activity of bacterial strains isolated from the bottom sediments of the lake. Using heterotrophic growth conditions, seven bacterial strains were isolated from samples collected in several coastal zones of Lake Baikal. Thisstudy identified both widespread strains of the genera Pseudomonas and Bacillus and rare genera Micrococcus and Acinetobacterrepresentatives. Metabolites of five strains were found to have a broad spectrum of antimicrobial activity. Four large fractions of metabolites of the isolated strains wereidentified. Two peptides of the isolated fractions of metabolites (one is produced by microorganisms of all five isolated strains, another—only by Pseudomonas putida) are low molecular weight oligopeptides. These peptides were proved to be bacteriocins. [ABSTRACT FROM AUTHOR]

The medicinal plant Dactylorhiza maculata (L.) Soó (family Orchidaceae) is used to treat gastritis, colic, gastrointestinal tract, and bladder diseases. This study aimed to investigate the properties and characteristics of the in vitro Dactylorhiza maculata extract. The recommended parameters for producing Dactylorhiza maculata extract were determined: temperature 60 °C, process duration 60 min, hydro module 1:10. It is recommended to carry out the extraction using an aqueous ethyl alcohol solution with a mass fraction of the parent substance of 70%. It was found that such biologically active substances as rutin, quercetin, 3,3′,4′,5,5′,7-hexahydroxyflavonone, 3,3′,4′,5,5′,7-hexahydroxyflavonone-3-O-glycoside, gallic acid, and ferulic acid were dominant in Dactylorhiza maculata. A high phosphorus content was noted (2410.8 mg/kg dry matter). The studied Dactylorhizamaculata samples contained a large number of organic acids and water-soluble vitamins. The tested extracts were safe in terms of the content of heavy metals, pesticides, aflatoxin B1, and radionuclides, as well as pathogenic and opportunistic microorganisms; the content was significantly lower than the threshold limit values. The studied complex of biologically active substances from Dactylorhiza maculata extract samples had antimicrobial properties. It was found that the antioxidant activity of the samples was 217.89 ± 10.89 mg AA/g (AA—ascorbic acid). The high content of bioactive substances and the antimicrobial and antioxidant properties of Dactylorhizamaculata extract samples determine the application potential of this plant as a substitute for growth stimulants and feed antibiotics in the production of feed additives, aiming to increase the physiological and immune status of livestock and poultry. [ABSTRACT FROM AUTHOR]

The results of the studies have shown that to obtain an extract of a complex of biologically active substances of Cotinus coggygria, ethyl alcohol (mass fraction of alcohol 70%) with a hydromodule of 1:5 should be used, and the extraction should be carried out for 60 min at a temperature of 60 °C. The investigated plant extracts with the complex of bioactive substances from the Cotinus coggygria leaves and flowers are safe from the point of view of the content of heavy metals, pesticides, aflatoxin B1, radionuclides, as well as pathogenic and opportunistic microorganisms. It has been established that the Cotinus coggygria extract contains rutin, hyperoside, ferulic acid, quercetin, kaempferol, disulphuretin, sulphurein, sulphurein, gallic acid, methyl gallate, pentagalloyl glucose, 3,3′,4′,5,6,7-hexahydroxyflavonone, 3,3′,4′,5,5′,7-hexahydroxyflavonone, 3-O-α-L-rhamnofuranoside, 3,3′,4′,5,5′,7-hexahydroxyflavulium(1+), 7-O-β-D glucopyranoside, and 3,3′,4′,7-tetrahydroxyflavonone. The tested extracts have anticancer, antigenotoxic, and antimicrobial (against E. coli, S. aureus, P. vulgaris, C. albicans, L. mesenteroides) properties. The high antioxidant status of the tested extracts was established; the antioxidant activity of the samples was 145.09 mg AA/g (AA—ascorbic acid). [ABSTRACT FROM AUTHOR]

The cultivation of plants in the form of callus cultures constitutes a renewable source of secondary plant metabolites. The conditions for the cultivation of callus cultures affect the yield of target compounds. Callus cultures of Hyssopus officinalis were chosen for study. Nutrient media of various compositions were used for Hyssopus officinalis callus culture. For each culture, data on the quantitative contents of saponins, flavonoids and polyphenolic compounds, as well as antioxidant activity, were obtained. It was found that Murashige and Skoog medium supplemented with 1-naphthylacetic acid and kinetin led to the highest yield of secondary metabolites. [ABSTRACT FROM AUTHOR]

Spirocyclic motifs are emerging privileged structures for drug discovery. They are also omnipresent in the natural products domain. However, until today, no attempt to analyze the structural diversity of various spirocyclic motifs occurring in natural products and their relative populations with unique compounds reported in the literature has been undertaken. This review aims to fill that void and analyze the diversity of structurally unique natural products containing spirocyclic moieties of various sizes. [ABSTRACT FROM AUTHOR]

Cyclic hydroxamic acids can be viewed as effective binders of soluble iron and can therefore be useful moieties for employing in compounds to treat iron overload disease. Alternatively, they are analogs of bacterial siderophores (iron-scavenging metabolites) and can find utility in designing antibiotic constructs for targeted delivery. An earlier described three-component variant of the Castagnoli—Cushman reaction of homophthalic acid (via in situ cyclodehydration to the respective anhydride) was extended to involve hydroxylamine in lieu of the amine component of the reaction. Using hydroxylamine acetate and O-benzylhydroxylamine was key to the success of this transformation due to greater solubility of the reagents in refluxing toluene (compared to hydrochloride salt). The developed protocol was found suitable for multigram-scale syntheses of N-hydroxy- and N-(benzyloxy)tetrahydroisoquinolonic acids. The cyclic hydroxamic acids synthesized in the newly developed format have been tested and shown to be efficient ligands for Fe3+, which makes them suitable candidates for the above-mentioned applications. [ABSTRACT FROM AUTHOR]