scholarly journals Isothiazoles in the Design and Synthesis of Biologically Active Substances and Ligands for Metal Complexes

Synthesis ◽  
2019 ◽  
Vol 52 (02) ◽  
pp. 159-188 ◽  
Author(s):  
Alexey V. Kletskov ◽  
Nikolay A. Bumagin ◽  
Fedor I. Zubkov ◽  
Dmitry G. Grudinin ◽  
Vladimir I. Potkin
Keyword(s):  
Metal Complexes ◽  
Plant Protection ◽  
Cross Coupling ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
New Drugs ◽  
Bioactive Substances ◽  
High Biological Activity ◽  
Wide Range ◽  
Active Substances

The chemistry of isothiazoles is being intensively developed, which is evidenced by the wide range of selective transformations involving the isothiazole heterocycle and the high biological activity of its derivatives that can be used as effective new drugs and plant protection chemicals. Some representatives of isothiazoles have proven to be synergists of bioactive substances, which opens the way to lower the doses of drugs used and is especially important in cancer chemotherapy. In the framework of the present review, the accomplishments in the chemistry of isothiazoles over the past 18 years are examined, whilst current strategies for the synthesis of isothiazole-containing molecules and key directions of studies in this field of heterocyclic chemistry are discussed. Considerable attention is paid to chlorinated isothiazoles and strategies for their use in the synthesis of biologically active substances. In addition, a comprehensive review of existing literature in the field of metal complexes of isothiazoles is given, including the results and prospects for the practical use of isothiazole–metal complexes as catalysts for cross-coupling reactions in aqueous and aqueous–alcoholic media (‘green chemistry’).1 Introduction2 Synthesis by Ring-Forming Reactions2.1 Intramolecular Cyclization2.2 (4+1)-Heterocyclization2.3 (3+2)-Heterocyclization2.4 Syntheses by Ring Transformations3 Isothiazoles by Ring Functionalization Reactions: Nucleophilic Substitution, Cross-Coupling and Side-Chain Functionalization4 Selected Syntheses of Biologically Active Isothiazole Derivatives5 Isothiazoles in the Synthesis of Transition-Metal Complexes and in Metal-Complex Catalysis6 Conclusion

scholarly journals Comparative study of phenolic compounds of the herb of Betonica L. genus species of flora of Ukraine

2021 ◽  
pp. 66-75
Author(s):  
Iryna Sas ◽  
Andrii Hrytsyk ◽  
Taras Koliadzhyn ◽  
Oleh Koshovyi
Keyword(s):  
Phenolic Compounds ◽  
Comparative Study ◽  
Hydroxycinnamic Acids ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
New Drugs ◽  
Raw Material ◽  
Wide Range ◽  
Nitrogen Containing Compounds ◽  
Active Substances

Species of Betonica L. genus are widespread in Ukraine and contain different groups of biologically active substances: hydroxycinnamic acids, flavonoids, tannins, iridoids, terpenoids, steroids, essential oil, organic acids, vitamin K, nitrogen-containing compounds, phenylethanoid glycosides. Species of Betonica L. genus show a wide range of pharmacological activity (anti-inflammatory, antioxidant, choleretic, diuretic, sedative, antitumor, antihypertensive, etc.) and phenolic compounds are one of the most important and promising groups of biologically active substances of these plants. The aim. The aim of the work was to conduct a comparative study of the phenolic compounds of the herb of Betonica L. genus species of flora of Ukraine. Materials and methods. The object of the study was the herb of Betonica peraucta and Betonica brachydonta harvested in the phase of mass flowering of the plant in Ivano-Frankivsk region. The study of phenolic compounds was carried out by paper chromatography, HPLC and spectrophotometry. Results. 7 components of tannins, 4 flavonoids, 5 hydroxycinnamic acids, 2 coumarins were identified and quantified by HPLC in the studied raw material. The quantitative content of the main groups of phenolic compounds in the herb of Betonica peraucta and Betonica brachydonta was determined by the method of absorption spectrophotometry: polyphenols – 5.96 % and 4.82 %, tannins – 1.62 % and 0.68 %, flavonoids – 2.07 % and 1.13 %, hydroxycinnamic acids – 7.01 % and 3.58 %, respectively. Conclusions. As a result of the conducted studies it was found that the content of phenolic compounds in the herb of Betonica peraucta is significantly higher than in the herb of Betonica brachydonta. Therefore, this species is promising for further research and creation of new drugs

The content of decenoic acids in drone brood preparations and combined preparations based on it

Biomics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 389-393
Author(s):  
D.V. Mitrofanov ◽  
N.V. Budnikova
Keyword(s):  
Royal Jelly ◽  
Storage Conditions ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Strict Adherence ◽  
Drone Brood ◽  
Wide Range ◽  
Active Substances ◽  
Melanin Complex

The drone brood contains a large number of substances with antioxidant activity. These substances require stabilization and strict adherence to storage conditions. Among these substances are unique decenoic acids, the content of which is an indicator of the quality of drone brood and products based on it. The ability of drone brood to reduce the manifestations of oxidative stress is shown. There are dietary supplements for food and drugs based on drone brood, which are used for a wide range of diseases. Together with drone brood, chitosan-containing products, propolis, royal jelly can be used. They enrich the composition with their own biologically active substances and affect the preservation of the biologically active substances of the drone brood. Promising are the products containing, in addition to the drone brood, a chitin-chitosan-melanin complex from bees, propolis, royal jelly. The chitin-chitosan-melanin complex in the amount of 5% in the composition of the adsorbent practically does not affect the preservation of decenic acids, while in the amount of 2% and 10% it somewhat worsens. The acid-soluble and water-soluble chitosan of marine crustaceans significantly worsens the preservation of decenoic acids in the product. Drone brood with royal jelly demonstrates a rather high content of decenoic acids. When propolis is introduced into the composition of the product, the content of decenoic acids increases according to the content of propolis.

scholarly journals Biologically Active Substances of Siberian Medical Plants in Functional Wgey-Based Drinks

2019 ◽  
Vol 49 (1) ◽  
pp. 14-22
Author(s):  
Светлана Иванова ◽  
Svetlana Ivanova ◽  
Ирина Милентьева ◽  
Irina Milenteva ◽  
Людмила Асякина ◽  
...  
Keyword(s):  
Callus Cultures ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Rhodiola Rosea ◽  
Plant Materials ◽  
Rhaponticum Carthamoides ◽  
Wide Range ◽  
Mountain Ash ◽  
Active Substances ◽  
Mineral Base

The use of infusions and extracts from domestic plant materials is a promising direction in the development of functional beverages since they contain a wide range of substances of various pharmacological properties. Drinks fortified with physiologically active natural components maintain a certain level of this content in human body. They can have a healing or prophylactic effect. However, there is a lack of technologies for the effective production of biologically active substances from plant materials. Moreover, the development of cultivated botanical medicinal plant species remains quite poor. The present study features the qualitative and quantitative composition of biologically active substances of medicinal plants that are endemics of Siberia. They are Rhodiola rosea (Rhodiola rosea L.) and maral root (Rhaponticum carthamoides). The paper introduces a method for increasing their biosynthetic activity. An experiment helped to select a composition of the nutrient medium for the cultivation of callus cultures of Rhodiola rosea (Rhodiola rosea L.) and maral root (Rhaponticum carthamoides) in vitro, which contributed to an increase in the biosynthesis of biologically active substances. For callus cultures of Rhodiola Rosea (line R.r-1k) the following composition was used: mineral base – MS; sucrose – 30 g; inositol – 100 mg; thiamine – 1.0 mg; pyridoxine – 1.0 mg; Ca-panthetonate – 10 mg; kinetin – 0.05 g; naphthyl acetic acid – 0.1 g; 2.4-D – 0.5. For callus cultures of maral root (line R.c -2k): mineral base – SH; sucrose – 30 g; inositol – 100 mg; thiamine – 5.0 mg; pyridoxine – 0.5 mg; nicotinic acid – 5.0 mg; kinetin – 0.1 g; indoleacetic acid – 1.0 g. The authors developed a technology for the production of functional whey-based tonic drink fortified with extract of carotenoids isolated from the fruits of mountain ash and the extract of biologically active substances Rhodiola rosea and maral root. The presence of biologically active substances in the plant and medicinal raw materials gives the drink antioxidant and bactericidal properties, as well as helps to raise the overall state of the organizm and strengthen the immune system.

scholarly journals Comparative study of technologies for extraction of biologically active substances from the raw material of animal origin

2021 ◽  
Vol 6 (3) ◽  
pp. 226-235
Author(s):  
E. R. Vasilevskaya ◽  
M. A. Aryuzina ◽  
E. S. Vetrova
Keyword(s):  
Molecular Weight ◽  
Trichloroacetic Acid ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Animal Origin ◽  
Low Molecular Weight ◽  
Acid Extraction ◽  
Trichloroacetic Acid Solution ◽  
Wide Range ◽  
Active Substances

Technologies of isolation and concentration of biologically active substances, developed in the middle of the 20th century, need adjustment and adaptation to modern conditions both to increase the activity of substances and for greater economic efficiency. The aim of the research is the comparison of dynamics of biologically active compounds extraction from porcines pancreas in two methods: the saline method based on 0.9% sodium chloride solution, and the acidic method based on 2.4% trichloroacetic acid solution. Also the purpose of research is to assess the possibilities for further optimization of technologies. The total protein concentration based on the biuret reaction in the samples taken during the extraction, as well as the calculation and analysis of the point degrees and rates of extraction are chosen as the controlled parameters. Local maxima of the protein yields into the extractant media at the 60th, 135th and 255th minute were recorded during saline extraction; and at the 75th and 135th minute during acid extraction. Also the proteomic profile of the extracts was studied. Wide range of compounds with molecular weight of less than 52 kDa was found in extracts based on physiological saline solution, and protein substances of whole presented range of molecular weights in trichloroacetic acid based extracts were considered. The predominance of low molecular weight protein fraction of interest was noted also in this method of extraction in comparison with the other methods of extraction. According to the UniProt database, we assume availability of probable compounds with a molecular weight of less than 30 kDa in the purified acidic extract. The presence of some proteins absent in the final saline extract was noted. The acidic erythrograms showed a weak degrading effect of both types of extracts on the membranes of rat erythrocytes, as well as the cytoprotective effect of acidic ultrafiltrates (less than 3 kDa). The obtained results prove a better efficiency of trichloroacetic acid extraction method used for obtaining a mixture of a wide range of compounds, including biologically active substances of low molecular weight.

scholarly journals Study of the Properties of In Vitro Dactylorhiza maculata (L.) Soó (Family Orchidaceae) Extracts

Plants ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1330
Author(s):  
Stanislav Sukhikh ◽  
Svetlana Noskova ◽  
Svetlana Ivanova ◽  
Liubov Skrypnik ◽  
Artem Pungin ◽  
...  
Keyword(s):  
Antioxidant Properties ◽  
Antimicrobial Properties ◽  
Feed Additives ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Bioactive Substances ◽  
Limit Values ◽  
Active Substances

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 Dactylorhiza maculata 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 Dactylorhiza maculata 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.

scholarly journals DEVELOPMENT OF A DRUG BASED ON THE FRUITS OF CHOKEBERRY (ARÓNIA MELANOCÁRPA (MICHX.) EL-LIOT) IMPROVING THE EFFICIENCY OF CANCER CHEMOTHERAPY

2020 ◽  
pp. 219-226
Author(s):  
Valeriya Yur'yevna Andreyeva ◽  
Vladimir Viktorovich Sheykin ◽  
Galina Il'inichna Kalinkina ◽  
Tat'yana Georgiyevna Razina ◽  
Yelena Petrovna Zuyeva ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Raw Materials ◽  
Combined Treatment ◽  
Latin Square ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
New Drugs ◽  
Raw Material ◽  
Black Chokeberry ◽  
Active Substances

Black chokeberry is an official drug raw material and is used as a multivitamin drug. Black chokeberry guarantees the supply of raw materials as it grows all over the Russian Federation end is a promising sourse of phenolic compounds for new drugs. Objective: to develop the most favorable conditions for extraction of bioactive compounds from black chokeberry and to assess its anti-metastatic activity. To extract bioactive compounds from black chokeberry the method of multistep repercolation with completed cycle was used. To assess the factors controlling the raw material extraction the technique of mathematic simulation for latin square. The technique of liquid anthocyanins and catechins rich black chokeberry extraction was given with the following parameters: extragent – 95% acidified alcohol, phase relation – 1 : 5, number of percolators – 5. The content of biologically active substances in the extract obtained with 95% acidified ethyl alcohol was determined by conventional methods. In the composition of the extract, the content of anthocyanins (5.83±0.25%), catechins (0.22±0.02%), tannins (4.65±0.30%), phenolic acids (0.27±0.01%) and other biologically active substances was determined. To assess the antitumor properties of the chokeberry fruit extract, the Lewis lung carcinoma model was used. It was found that the proposed extract reliably inhibits the development of metastases and increases the antimetastatic activity of cyclophosphamide in combined treatment, is of interest as a means for increasing the effectiveness of tumor chemotherapy.

scholarly journals INFLUENCE OF BIOTECHNOLOGICAL FACTORS ON THE YIELD OF BIOLOGICALLY ACTIVE COMPOUNDS FROM SORBUS AUCUPARIA

2021 ◽  
pp. 291-300
Author(s):  
Elena Nikolaevna Sokolova ◽  
Tat'yana Vladimirovna Yuraskina ◽  
Yuliya Aleksandrovna Borshcheva ◽  
Natal'ya Aleksandrovna Fursova ◽  
Anton Yur'yevich Sharikov ◽  
...  
Keyword(s):  
Amino Acids ◽  
Biologically Active Compounds ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Theoretical Research ◽  
Sorbus Aucuparia ◽  
Plant Materials ◽  
Active Compounds ◽  
Wide Range ◽  
Active Substances

Currently, the diet of almost all population groups in Russia is characterized by a deficiency of vitamins, essential amino acids, macro- and micronutrients, as well as biologically active substances (flavonoids, carotenoids, etc.). Replenishment of the lack of these components in the diet of the population due to natural sources of plant origin is an important and actual task of national health care. The rational use of natural components of plant materials containing a wide range of natural biologically active substances using biocatalytic methods, as well as the selection of optimal conditions for obtaining commodity forms of ingredients, will allow to create preventive products that have a beneficial effect on the human body. Theoretical research in the field of promising sources of food and biologically active ingredients among wild species of plant materials were carried out. Biomedical properties of Sorbus aucuparia were described. The technological characteristics of the biologically active substances extraction from dried plant raw materials was investigated. Thus, it was revealed that the degree of dried berries grinding about 0.2–0.8 mm, the hydromodule 1 : 10 and the extraction duration 240 minutes are most effective for the extractive substances yield. The enzymatic complex, allowing the maximum to release biologically valuable components to extract was selected. The amino acid composition of rowanberry with the use of high-performance liquid chromatography was investigated. Produced fermentalizates contain complex of biologically active compounds, including amino acids, vitamins, carotenoids, phenolic substances, that makes these ingredients promising for creation of various foodstuffs to improve quality, nutritional and biological value, taste and other consumer properties.

scholarly journals VARIATION OF CHEMICAL COMPOSITION OF FRUITS OF BOG BLUEBERRY (VACCINIUM ULIGINOSUM L.) WHEN INTRODUCING

2018 ◽  
pp. 107-114
Author(s):  
Татьяна (Tat'yana) Ивановна (Ivanovna) Снакина (Snakina) ◽  
Татьяна (Tat'yana) Абдулхаиловна (Аbdulkhailovna) Кукушкина (Kukushkina)
Keyword(s):  
Biochemical Study ◽  
West Siberia ◽  
Botanical Garden ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Forest Steppe ◽  
Planting Material ◽  
Wide Range ◽  
Pharmaceutical Industries ◽  
Active Substances

Bog blueberry berries are a source material for food and pharmaceutical industries. However, industrial harvesting of bog blueberry is hardly carried out as plants grow in hard-to-access areas and safekeeping of berries is low during transportation to the processing plants.Special-purpose plantations of bog blueberry at the processing plants may solve the problem. To do this would require planting material noted for a high content of biologically active substances. Central Siberian Botanical Garden is a leading center of introduction and breeding of blueberry in Russia.In this connection, biochemical study of dry substance, ascorbic acid, sugars, acids, anthocyans, catechins, pectins and protopectins of berries of promising bog blueberry forms was conducted in the forest-steppe zone of West Siberia in 2011–2015.The results of research showed a wide range of variability of chemical characters due to individual peculiarities of bog blueberry forms and weather conditions in various years. Protopectins, catechins and pectins exhibited the greatest interannual distinctions.Bog blueberry samples with the greatest content of biologically active substances which can be recommended as planting material for creation of production plantations were revealed.

scholarly journals TECHNOLOGICAL PARAMETERS OF COUNTERCURRENT EXTRACTION: DERIVING BIOACTIVE COMPOUNDS FROM PLANT RAW MATERIALS

2016 ◽  
pp. 8-15
Author(s):  
Sergey Garmashov ◽  
Sergey Garmashov ◽  
Alexander Izgaryshev ◽  
Alexander Izgaryshev ◽  
Egor Kashirskih ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Plant Material ◽  
Continuous Process ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Wild Plant ◽  
Countercurrent Extraction ◽  
Mineral Salts ◽  
Wide Range ◽  
Active Substances

Wild-growing plants produce a wide range of vitamins, macro- and microelements, mineral salts and other biologically active substances. Even in minute quantities, these constituents can mediate the healing effect on a human body. To date, the most promising method of extracting biologically active compounds from crude wild plant material is solvent extraction. The intensification of the extraction process has seen a new development in the last few years. This paper focuses on obtaining maximum yield of bioactive compounds from wild-growing plants, such as ordinary cowberry, prickly wild rose, sea-buckthorn, ordinary rowan, guelder-rose by a countercurrent extraction method, a continuous process where the plant material moves against the solvent. With that, it examines various extraction agents and their mixtures in relation to the extractives and total flavonoid content, the optimal time of the duration of the extraction. The optimal temperature of the process was found to be corresponding to the boiling point of the solvent. In the future, this study might contribute to the development of high quality new galenical preparations with maximum content of biologically active substances identical to the composition of the source plants to produce pharmaceutical drugs, food supplements, functional foods and cosmetics.

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