MECHANOCHEMICAL ACTIVATION OF PHARMACEUTICAL SUBSTANCES AS A FACTOR FOR MODIFICATION OF THEIR PHYSICAL, CHEMICAL AND BIOLOGICAL PROPERTIES

Objective: Study the influence of the mechanical preparation methods (grinding, fluidization) of solid pharmaceutical substances (PS) and herbal raw material on their physicochemical properties and biological activities. Methods: Test substances and solvents-Lactose monohydrate (DFE Pharma, Germany). Sodium chloride, bendazol hydrochloride (all Sigma-Aldrich, USA) and herbal raw material (Callisia fragrans). The dispersity and native structure of pharmaceutical substances were analyzed by several methods: optical microscopy–Altami BIO 2 microscope (Russia); low angle laser light scattering (LALLS) method (Malvern Instruments, UK); Spirotox method–Quasichemical kinetic of cell transition of cellular biosensor Spirostomum ambiguum; Fourier-transform infrared spectroscopy–the analysis in the middle IR region was carried out using an IR Cary 630 Fourier spectrometer (Agilent Technologies, USA). The analysis of dried leaves of C. fragrans before and after mechanical activation was performed using Shimadzu EDX-7000 X-ray fluorescence spectrophotometer without mineralization (Shimadzu, Japan). Results: It was established that the mechanical change, such as dispersion and drying, alters the biological activity of PS and herbal raw materials. The observed increase in the influence of the dispersed substance on the biosensor S. ambiguum is quantitatively estimated from the values of the activation energy (obsEa), which turns to be valued 1,5 (P≤0,05) times more than for the native form substance. In the study of the dependence of the availability of chemical elements K, Ca, Zn on the degree of dispersion of herbal raw materials was established a quantitative 4-fold (P≤0,05) increase in the concentration of elements in mechano-activated raw materials. Conclusion: By the example of the biological model of Spirotox (single-celled biosensor S. ambiguum) and herbal raw materials obtained from C. fragrans, the increase of biological activity of PS at the dispersion of initial preparations was proved.

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Rose Flowers—A Delicate Perfume or a Natural Healer?

Biomolecules ◽

10.3390/biom11010127 ◽

2021 ◽

Vol 11 (1) ◽

pp. 127

Author(s):

Milka Mileva ◽

Yana Ilieva ◽

Gabriele Jovtchev ◽

Svetla Gateva ◽

Maya Margaritova Zaharieva ◽

...

Keyword(s):

Essential Oils ◽

Food Industry ◽

Raw Materials ◽

Biological Activities ◽

Biological Properties ◽

Rosa Damascena ◽

Oil Sand ◽

Rosa Gallica ◽

Therapeutic Properties ◽

Phytochemical Profile

Plants from the Rosacea family are rich in natural molecules with beneficial biological properties, and they are widely appreciated and used in the food industry, perfumery, and cosmetics. In this review, we are considering Rosa damascena Mill., Rosa alba L., Rosa centifolia L., and Rosa gallica L. as raw materials important for producing commercial products, analyzing and comparing the main biological activities of their essential oils, hydrolates, and extracts. A literature search was performed to find materials describing (i) botanical characteristics; (ii) the phytochemical profile; and (iii) biological properties of the essential oil sand extracts of these so called “old roses” that are cultivated in Bulgaria, Turkey, India, and the Middle East. The information used is from databases PubMed, Science Direct, and Google Scholar. Roses have beneficial healing properties due to their richness of beneficial components, the secondary metabolites as flavonoids (e.g., flavones, flavonols, anthocyanins), fragrant components (essential oils, e.g., monoterpenes, sesquiterpenes), and hydrolysable and condensed tannins. Rose essential oils and extracts with their therapeutic properties—as respiratory antiseptics, anti-inflammatories, mucolytics, expectorants, decongestants, and antioxidants—are able to act as symptomatic prophylactics and drugs, and in this way alleviate dramatic sufferings during severe diseases.

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Structural Analysis of Fucoidans

Natural Product Communications ◽

10.1177/1934578x0800301011 ◽

2008 ◽

Vol 3 (10) ◽

pp. 1934578X0800301 ◽

Cited By ~ 13

Author(s):

Maria I. Bilan ◽

Anatolii I. Usov

Keyword(s):

Biological Activity ◽

Structural Analysis ◽

Charge Density ◽

Brown Algae ◽

Uronic Acid ◽

Chemical Structure ◽

Biological Activities ◽

Biological Properties ◽

Sulfated Polysaccharides ◽

New Information

Sulfated polysaccharides of brown algae (“fucoidans”) constitute a wide variety of biopolymers from simple sulfated fucans up to complex heteropolysaccharides composed of several neutral monosaccharides, uronic acid and sulfate. The increased interest in this class of polysaccharides is explained by their high and versatile biological activities, and hence, by their possible use in new drug design. Structural analysis of several fucoidans demonstrates that their biological properties are determined not only by charge density, but also by fine chemical structure, although distinct correlations between structure and biological activity cannot be formulated at present. The aim of this review is to describe the methods of structural analysis currently used in fucoidan chemistry, and to discuss some new information on the structures of fucoidans presented in recent publications.

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Cornus mas L. Stones: A Valuable by-Product as an Ellagitannin Source with High Antioxidant Potential

Molecules ◽

10.3390/molecules25204646 ◽

2020 ◽

Vol 25 (20) ◽

pp. 4646

Author(s):

Dominika Przybylska ◽

Alicja Z. Kucharska ◽

Iwona Cybulska ◽

Tomasz Sozański ◽

Narcyz Piórecki ◽

...

Keyword(s):

Biological Activities ◽

Antioxidant Properties ◽

Biological Properties ◽

Raw Material ◽

Hydrolyzable Tannins ◽

Cornus Mas ◽

Fruit Processing ◽

High Antioxidant Activity ◽

Total Polyphenolic Content ◽

First Time

The stone of Cornus mas L. remains the least known morphological part of this plant, whereas the fruit is appreciated for both consumption purposes and biological activity. The stone is considered to be a byproduct of fruit processing and very little is known about its phytochemical composition and biological properties. In this study, the complete qualitative determination of hydrolyzable tannins, their quantitative analysis, total polyphenolic content, and antioxidant properties of the stone of C. mas are presented for the first time. The 37 identified compounds included the following: various gallotannins (11), monomeric ellagitannins (7), dimeric ellagitannins (10), and trimeric ellagitannins (7). The presence of free gallic acid and ellagic acid was also reported. Our results demonstrate that C. mas stone is a source of various bioactive hydrolyzable tannins and shows high antioxidant activity which could allow potential utilization of this raw material for recovery of valuable pharmaceutical or nutraceutical substances. The principal novelty of our findings is that hydrolyzable tannins, unlike other polyphenols, have been earlier omitted in the evaluation of the biological activities of C. mas. Additionally, the potential recovery of these bioactive chemicals from the byproduct is in line with the ideas of green chemistry and sustainable production.

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Isatis tinctoria L. (Woad): A Review of Its Botany, Ethnobotanical Uses, Phytochemistry, Biological Activities, and Biotechnological Studies

Plants ◽

10.3390/plants9030298 ◽

2020 ◽

Vol 9 (3) ◽

pp. 298 ◽

Cited By ~ 3

Author(s):

Jasmine Speranza ◽

Natalizia Miceli ◽

Maria Fernanda Taviano ◽

Salvatore Ragusa ◽

Inga Kwiecień ◽

...

Keyword(s):

Therapeutic Potential ◽

Antioxidant Activities ◽

Biological Activities ◽

Biological Properties ◽

Biologically Active ◽

Raw Material ◽

Future Research ◽

Shoot Cultures ◽

Isatis Tinctoria ◽

Enhanced Production

Isatis tinctoria L. (Brassicaceae), which is commonly known as woad, is a species with an ancient and well-documented history as an indigo dye and medicinal plant. Currently, I. tinctoria is utilized more often as medicinal remedy and also as a cosmetic ingredient. In 2011, I. tinctoria root was accepted in the official European phytotherapy by introducing its monograph in the European Pharmacopoeia. The biological properties of raw material have been known from Traditional Chinese Medicine (TCM). Over recent decades, I. tinctoria has been investigated both from a phytochemical and a biological point of view. The modern in vitro and in vivo scientific studies proved anti-inflammatory, anti-tumour, antimicrobial, antiviral, analgesic, and antioxidant activities. The phytochemical composition of I. tinctoria has been thoroughly investigated and the plant was proven to contain many valuable biologically active compounds, including several alkaloids, among which tryptanthrin, indirubin, indolinone, phenolic compounds, and polysaccharides as well as glucosinolates, carotenoids, volatile constituents, and fatty acids. This article provides a general botanical and ethnobotanical overview that summarizes the up-to-date knowledge on the phytochemistry and biological properties of this valuable plant in order to support its therapeutic potential. Moreover, the biotechnological studies on I. tinctoria, which mainly focused on hairy root cultures for the enhanced production of flavonoids and alkaloids as well as on the establishment of shoot cultures and micropropagation protocols, were reviewed. They provide input for future research prospects.

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The Preparation of ZrO2 and the Influence of the Calcination Temperature

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.1095.67 ◽

2015 ◽

Vol 1095 ◽

pp. 67-71

Author(s):

Yan Zhu ◽

Xiao Zhang ◽

Shuai Yuan

Keyword(s):

Electron Diffraction ◽

Calcination Temperature ◽

Surface Activity ◽

Raw Materials ◽

Raw Material ◽

Ceramic Powders ◽

Preparation Technology ◽

Preparation Methods ◽

Optimum Technology ◽

Scherrer Formula

nanoZrO2ceramic powders have excellent properties in many field. In order to obtain nanoZrO2powder with excellent properties, the study of preparation methods become a hotspot. The nanoZrO2powders new preparation technology from cheap raw materials is target of this paper. nanoZrO2powers were preparated from ZrOCl2and NaCO3as raw material. The optimum technology parameters were determined as follow, namely at 40°C, C (ZrOCl2) =0.4mol/L, C (NaCO3) =1.0mol/L, 2% the surface activity agent. nanoZrO2powders preparated were characterized by XRD, TEM and Electron Diffraction . The results show that the ZrO2powders prepared are crystal and the sizes are nanometer. The ZrO2average sizes were calculated with the scherrer formula. The nanoZrO2sizes change with temperature was discussed. The result is ageerment with that calculated with the scherrer formula.

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Coordination Compounds of Platinum and Palladium with Mixed Ligands (Usnic Acid and 1-(o-Tolyl) Biguanide) � Synthesis, Spectral Characterization and Biological Activity

Revista de Chimie ◽

10.37358/rc.20.4.8073 ◽

2020 ◽

Vol 71 (4) ◽

pp. 336-346

Author(s):

Mirela Calinescu ◽

Ovidiu Oprea ◽

Catalina Stoica ◽

Mihai Nita-Lazar ◽

Madalina Mihalache

Keyword(s):

Staphylococcus Aureus ◽

Pseudomonas Aeruginosa ◽

Biological Activity ◽

Coordination Compounds ◽

Antitumor Agents ◽

Biological Activities ◽

Usnic Acid ◽

Biological Properties ◽

Mixed Ligands

Four coordination compounds of Pd(II), Pt(II) and Pt(IV) with usnic acid (H3AU) and 1-(o-tolyl)biguanide (TB) as ligands have been synthesized in view of their potential as antimicrobial, antifungal and antitumor agents. The metal complexes have been characterized by elemental and thermogravimetrical analyses, infrared and electronic spectra. Based on these studies, the following formulas have been proposed for the complexes: [Pd(TB)(H3AU)]PdCl4 (C1), [Pd(TB)(H2AU)] CH3COO (C2), [Pt(TB)(H2AU)Cl2]Cl (C3) and [Pt(TB)(H2AU)]Cl (C4), where H2AU is deprotonated usnic acid. The in vitro biological activities of the new complexes were tested against Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Candida albicans ATCC 10231 and HeLa tumor cells. All complexes were found to have good biological properties and therefore they can be further explored in therapeutic applications.

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Improving the Technology of Extraction, Preparation and Conservation of Musk Deer Extract for the Standardization and Production of Pharmaceutical Substances

Biomeditsina ◽

10.33647/2074-5982-16-1-28-41 ◽

2020 ◽

Vol 16 (1) ◽

pp. 28-41

Author(s):

S. L. Lyublinskiy ◽

I. N. Lyublinskaya ◽

V. P. Galochkina ◽

E. M. Koloskova ◽

V. N. Karkischenko ◽

...

Keyword(s):

Electron Beam ◽

Raw Materials ◽

Absorbed Dose ◽

Antimicrobial Effect ◽

Biologically Active ◽

Raw Material ◽

Musk Deer ◽

Beam Radiation ◽

Research Attention ◽

Pharmaceutical Substances

The development of new methods for the conservation of biological raw materials, which can be used in the production of active pharmaceutical substances, is increasingly attracting research attention. This article presents the results of comparative studies into the effectiveness of biological conservation using cryopreservation, electron beam treatment and the lactoperoxidase system. Electron beam technologies demonstrated a pronounced antimicrobial effect in the treatment of musk deer extract and other biologically active substances. A recommendation was formulated to treat musk extract with electron-beam radiation at an absorbed dose of 6 kGy (9.5 MeV) following cryopreservation at –25°C over the period of 1 year. The data obtained using the method of accelerated testing allows an extended shelf life of up to 48 months to be predicted.For the ﬁrst time, the main indicators of the quality and safety of musk deer extract as a potential raw material for the production of active pharmaceutical substances and medicinal animal raw materials were determined. A standard for the quality of musk deer extract as a raw material, as well as an experimental-industrial regulation for its preparation and preservation, were developed.

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Syntheses and Biological Activities of triazole-based Sulfonamides

Current Organic Chemistry ◽

10.2174/1385272823666191021115023 ◽

2020 ◽

Vol 23 (21) ◽

pp. 2319-2349 ◽

Cited By ~ 2

Author(s):

Ali Ramazani ◽

Hamed Sadighian ◽

Farideh Gouranlou ◽

Sang W. Joo

Keyword(s):

Biological Activity ◽

Biological Activities ◽

Biological Properties ◽

Biologically Active ◽

Potential Biological Activity

: The triazole and sulfonamide compounds are known as biologically active agents that were employed for medicinal applications. These compounds were obtained in different forms by a variety of techniques to vast ranges of applications. The broad biological properties of these compounds have encouraged researchers to design and synthesize triazole-based sulfonamide derivatives as compounds with potential biological activity. In this review, we summarized the synthetic procedures of triazole-based sulfonamide compounds together with their biological activities during the last two decades.

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BIOTECHNOLOGICAL FEATURES OF OBTAINING CO2 EXTRACTS FROM GRAIN AND NUT RAW MATERIALS

Известия вузов. Пищевая технология ◽

10.26297/0579-3009.2019.5-6.13 ◽

2019 ◽

Author(s):

А.М. МЕДВЕДЕВ ◽

К.Ш. САКИБАЕВ

Keyword(s):

Electromagnetic Field ◽

Electromagnetic Waves ◽

Raw Materials ◽

Low Frequency ◽

Extraction Process ◽

Raw Material ◽

Grape Seeds ◽

Before And After ◽

Extractive Substances ◽

Vegetable Raw Materials

Разработана технология получения СО2экстрактов с повышенным выходом СО2экстрактивных веществ после предварительной обработки зернового и орехового сырья электромагнитным полем низкой частоты (ЭМП НЧ) 28,36 Гц. Растительное сырье семена амаранта, винограда, расторопши пятнистой, ростки пшеницы, арахис, миндаль, ядра фисташковых и ореха грецкого подвергли измельчению в крупку размером 2 3 мм для дальнейшей обработки на вальцевом станке (d 0,2 мм). Измельченное сырье помещали в радиопрозрачный короб и трижды подвергали воздействию ЭМП НЧ по 20 мин с перерывом по 30 мин. Обработанное электромагнитным полем сырье заключили в сетчатую кассету и загрузили внутрь СО2экстрактора, работающего в докритическом режиме при давлении 6,5 МПа и температуре 22С. Продолжительность процесса экстракции сырья, ч: орехового 4,0 зернового 2,5. Установлено увеличение выхода биокомпонентов в экстракт из орехов и зерна, подвергнутых воздействию электромагнитных волн, по сравнению с контрольными образцами без обработки ЭМП НЧ. Выход СО2экстрактивных веществ из сырья до обработки и после обработки ЭМП НЧ составил, : арахис 8,0 и 14,1 орех грецкий 10,2 и 16,3 семена амаранта 4,7 и 5,4 семена винограда 6,0 и 6,5 соответственно. Концентрация фенольных веществ в экстрактах повысилась на 15, витаминов С и Р на 6,2 и 7,0 соответственно. Применение электромагнитного излучения НЧ привело к сокращению продолжительности экстракции из зернового и орехового сырья в 1,2 раза. A technology has been developed for producing CO2 extracts with an increased yield of CO2 extractives after preliminary processing of grain and nut raw materials with a low frequency electromagnetic field (LF EMF) of 28,36 Hz. Vegetable raw materials amaranth seeds, grapes, milk thistle, wheat germ, peanuts, almonds, pistachio kernels and walnuts kernels were crushed into a grain size of 2 3 mm for further processing on a roller machine (d 0,2 mm). The crushed raw material was placed in a radiotransparent box and exposed to LF EMF three times for 20 min with a break of 30 min. The raw material processed by the electromagnetic field was enclosed in a mesh cassette and loaded inside a CO2 extractor operating in a subcritical mode at a pressure of 6,5 MPa and a temperature of 22C. The duration of the extraction process of raw materials, h: nut 4,0 grain 2,5. An increase in the yield of biocomponents in the extract from nuts and grains exposed to electromagnetic waves was established compared with the control samples without processing the LF EMF. The yield of СО2 extractive substances from the raw materials before and after the treatment of LF EMF was, : peanuts 8,0 and 14,1 walnut 10,2 and 16,3 amaranth seeds 4,7 and 5,4 grape seeds 6,0 and 6,5, respectively. The concentration of phenolic substances in the extracts increased by 15, vitamins C and P by 6,2 and 7,0, respectively. The use of electromagnetic radiation of low frequency led to a reduction in the duration of extraction from grain and nut raw materials by 1,2 times.

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Essential oils biological activity of the Lippia alba (Verbenaceae) shrub

Revista de Biología Tropical ◽

10.15517/rbt.v68i1.39153 ◽

2020 ◽

Vol 68 (1) ◽

Author(s):

Mailen Ortega Cuadros ◽

Emma E Acosta de Guevara ◽

Ailen D Molina Castillo ◽

Clara Gutiérrez Castañeda ◽

Glorismar Castro Amarís ◽

...

Keyword(s):

Biological Activity ◽

Essential Oils ◽

Biological Activities ◽

Biological Properties ◽

Research Groups ◽

Lippia Alba ◽

Sedative Effects ◽

Aromatic Species ◽

Meta Analyses ◽

The Relationship

Introduction: Lippia alba is an aromatic species belonging to the Verbenaceae family. Its essential oils have been used in different industries, because of its biological properties. Objective: Identify the perspectives of the biotechnological applications of Lippia alba essential oils. Methodology: A scoping review was conducted on the biological activity of Lippia alba essential oils registered until October, 2018 in EBSCO, Embase, Scopus, and Lilacs databases. Results: Chemotypes I and III have been reported for different biological activities from the evaluations performed on microorganisms, fish, arthropods, small mammals, and cell lines; fundamentally associated with antibacterial, antifungal, cytotoxic, antioxidant, and sedative effects, among others. Records focused mainly on the health, fishing industry, and agrifood sectors. Conclusion: Studies on the effect of essential oil are promising, but do not reflect a continuity of the research toward prototypes or finished commercial products. Research groups must unify evaluation methodologies and include in all studies the relationship between phytochemical and biological activity for the meta-analyses to be possible. Likewise, they must join efforts through the National System for Agricultural Innovation (SNIA, for the term in Spanish) to generate finished products that impact upon society and facilitate progress in the country’s bio-economy.

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