scholarly journals BIOMIMETIC APPROACHES TO STUDY OF PROPERTIES OF MEDICINAL SUBSTANCES

2019 ◽  
Vol 62 (10) ◽  
pp. 4-29
Author(s):  
Nina B. Melnikova ◽  
Olga N. Solovyova ◽  
Evgeni N. Evgeni N. Kochetkov
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Lipid Bilayers ◽  
Superoxide Anion ◽  
Molecular Form ◽  
Biologically Active ◽  
New Drugs ◽  
In Vitro Experiments ◽  
Medicinal Substances

The review is devoted to an assessment of the current level of use of biomimetic approaches to the study of the properties of known drugs and the development of new drugs. In this review, we consider the main biological functions of superoxide dismutase, namely the catalytic decomposition of toxic superoxide anion of oxygen to the molecular form of oxygen and protection against induced apoptosis. The biomimetic enzymes-Mn- and TEMPO-containing equivalents of superoxide dismutase SOD with antitumor and antioxidant activity were discussed more detail. The relationship between the properties and activity of SOD mimetics with their structure among them the nature of the anion and ligands, the coordination number, the geometry of the presence of conjugated bonds, and other parameters of the molecules. The study of the properties of Mn-SOD mimetics makes it possible to develop a new class of drugs successfully tested by in vivo and in vitro experiments and which are at the stages of clinical trials. Stable TEMPO radicals containing compounds are able to perform SOD functions, exhibiting antioxidant activity in relation not only to superoxide-anion, but also to peroxynitrile, and moreover to act as a spin label. The biomimetic membrane systems (monolayers, planar lipid bilayers, liposomes and other nano-sized objects) are discussed too for studying properties in in vitro experiments and for delivering potent and medicinal substances. The biomimetic approach combination allows to create the new promising drugs, including those based on SOD mimetics, and to develop the synthetic analogues of biologically active substances and methods of their delivery. The advantages of such dosage forms are lower toxicity of the preparations, lack of immunogenicity and a decrease in the dose of potent drugs.

Synthesis and antioxidant activity of new selenium-containing quinolines

2020 ◽  
Vol 16 ◽  
Author(s):  
Benedetta Bocchini ◽  
Bruna Goldani ◽  
Fernanda S.S. Sousa ◽  
Paloma T. Birmann ◽  
Cesar A. Brüning ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Radical Scavenging ◽  
Building Blocks ◽  
Antioxidant Potential ◽  
In Vitro Assays ◽  
Pharmacological Activities ◽  
Antioxidant Power ◽  
Antioxidant Agents

Background: Quinoline derivatives have been attracted much attention in drug discovery and synthetic derivatives of these scaffolds present a range of pharmacological activities. Therefore, organoselenium compounds are valuable scaffolds in organic synthesis because their pharmacological activities and their use as versatile building blocks for regio-, chemio-and stereoselective reactions. Thus, the synthesis of selenium-containing quinolines has great significance, and their applicability range from simple antioxidant agents, to selective DNA-binding and photocleaving agents. Objective: In the present study we describe the synthesis and antioxidant activity in vitro of new 7-chloroN(arylselanyl)quinolin-4-amines 5 by the reaction of 4,7-dichloroquinoline 4 with (arylselanyl)-amines 3. Methods: For the synthesis of 7-chloro-N(arylselanyl)quinolin-4-amines 5, we performed the reaction of (arylselanyl)- amines 3 with 4,7-dichloroquinoline 4 in the presence of Et3N at 120 °C in a sealed tube. The antioxidant activities of the compounds 5 were evaluated by the following in vitro assays: 2,2- diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), ferric ion reducing antioxidant power (FRAP), nitric oxide (NO) scavenging and superoxide dismutase-like activity (SOD-Like). Results: 7-Chloro-N(arylselanyl)quinolin-4-amines 5a-d has been synthesized in yields ranging from 68% to 82% by the reaction of 4,7-dichloroquinoline 4 with arylselanyl-amines 3a-d using Et3N as base, at 120 °C, in a sealed tube for 24 hours and tolerates different substituents, such as -OMe and -Cl, in the arylselanyl moiety. The obtained compounds 5a-d presented significant results with respect to the antioxidant potential, which had effect in the tests of inhibition of radical’s DPPH, ABTS+ and NO, as well as in the test that evaluates the capacity (FRAP) and in the superoxide dismutase-like activity assay (SOD-Like). It is worth mentioning that 7-chloro-N(arylselanyl)quinolin-4-amine 5b presented excellent results, demonstrating a better antioxidant capacity when compared to the others. Conclusion: According to the obtained results 7-chloro-N(arylselanyl)quinolin-4-amines 5 were synthesized in good yields by the reaction of 4,7-dichloroquinoline with arylselanyl-amines and tolerates different substituents in the arylselanyl moiety. The tested compounds presented significant antioxidant potential in the tests of inhibition of DPPH, ABTS+ and NO radicals, as well as in the FRAP and superoxide dismutase-like activity assays (SOD-Like).

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

scholarly journals Health benefits of new symbiotic “NAR”

2014 ◽  
Vol 2 ◽  
Author(s):  
Saule Saduakhasova ◽  
Almagul Kushugulova ◽  
Samat Kozhakhmetov ◽  
Gulnara Shakhabayeva ◽  
Adil Supiyev ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Superoxide Dismutase ◽  
Glutathione Reductase ◽  
Inflammatory Mediators ◽  
Antioxidant Activities ◽  
Reductase Activity ◽  
Protein A ◽  
Intact Cells ◽  
Total Antioxidant

Introduction: The immune-modulatory effects of synbiotics and their ability to reduce free radical levels may be useful for functional food that is able to be active throughout whole period of colonization of the gastrointestinal tract.The aim of the present study was to investigate the immune-modulatory and antioxidant effects of the synbiotic product "NАR," a probiotic beverage.Methods: The presence of IL-2, IL-4, IL-6, IL-8, IL-10, αTNF, γIFN, Ig A, Ig M, and Ig E was studied in vitro using a solid immunosorbent analysis. The total antioxidant activities of superoxide dismutase and glutathione reductase were determined by a spectrophotometry using the Sigma-Aldrich sets.Results: Studies of the immune-modulatory properties of the synbiotic product NAR showed 1.7 fold increase of γINF levels (p<0.01) in blood after consumption of the synbiotic product “NAR” in comparison to control values, whereas the concentrations of IL-4 and Ig E decreased 2.0 times (treatment: 9.3; control: 18.7; p<0.01) and 1.3 times (p<0.1), respectively. The consumption of the synbiotic product “NAR” caused an increase in the proportion of γINF/IL 4 (treatment: 15.4; control: 4.4; p<0.01), which indicates a reduction in functional activity of Th2-type lymphocytes in comparison with the function of Th1 cells.Our study showed a high level of the total antioxidant activity of the synbiotic product (67.4 mmol/ml). The antioxidant activity of the intact cells of consortium (15.3 mM/ml), which was the basis for the preparation of the symbiotic product, is several times lower than the activity observed in the symbiotic samples.Expression of SOD is one of the mechanisms of antioxidant stress radicals inactivation by bacteria. The analysis identified a superoxide dismutase activity of synbiotic product (1.42 U/mg protein). A glutathione reductase activity of the synbiotic product was elevated (0.06 U/ml). Conclusion: The majority of the inflammatory mediators found in the blood after the consumption of symbiotic product NAR were inflammatory mediators that activate a cellular component of the resistance. Moreover, the symbiotic product has a high antioxidant activity. 

Aktywność przeciwutleniająca ekstraktów z wybranych roślin należących do rodziny Rosaceae

2018 ◽  
Vol 19 (3) ◽  
Author(s):  
Anna Muzykiewicz ◽  
Joanna Zielonka-Brzezicka ◽  
Adam Klimowicz
Keyword(s):  
Antioxidant Activity ◽  
Extraction Method ◽  
Extraction Methods ◽  
Biologically Active ◽  
Sorbus Aucuparia ◽  
Cydonia Oblonga ◽  
Leaf Extracts ◽  
Soxhlet Apparatus ◽  
Rosaceae Family

Introduction. Plants are a valuable source of biologically active compounds, including antioxidants, which could prevent the development of oxidative stress. The members of Rosaceae family such as Sorbus aucuparia L. and Cydonia oblonga Mill. are the examples of plants contained antioxidants. Aim. The aim of the study was to evaluate the antioxidant potential of leaves and fruits extracts of rowan and quince, taking into account influence of the extrahent as well as extraction method on this activity. Material and methods. The extracts were obtained by classic extraction methods – shaking and extraction in Soxhlet apparatus. Methanol, acetone as well as 70 and 96% (v/v) ethanol were used as solvents. Antioxidant activity was estimated by DPPH, FRAP, Folin-Ciocalteu (F-C) and ABTS methods. Results. The highest antioxidant activity was found in leaf extracts of both plants. In most cases, rowan extracts showed higher potential than appropriate extracts of quince. The most effective extraction method was extraction in Soxhlet apparatus using methanol (in case of rowan and quince) as well as 96% (v/v) ethanol (quince) and 70% (v/v) ethanol (rowan). The highest results were obtained with FRAP method, whereas the lowest – with DPPH. Conclusions. The presented in vitro results confirmed, that the leaves and fruits extracts of selected plants belonging to the Rosaceae family showed antioxidant activity and could be applied in various industry branches.

Evaluation of antioxidant activity of Melothria maderaspatana in vitro

2010 ◽  
Vol 5 (2) ◽  
pp. 224-230 ◽  
Author(s):  
Boobalan Raja ◽  
Kodukkur Pugalendi
Keyword(s):  
Hydrogen Peroxide ◽  
Antioxidant Activity ◽  
Free Radical ◽  
Hydroxyl Radical ◽  
Superoxide Anion ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Free Radical Scavenging ◽  
Melothria Maderaspatana

AbstractIn this study, an aqueous extract of leaves from Melothria maderaspatana was tested for in vitro antioxidant activity. Free radical scavenging assays, such as hydroxyl radical, hydrogen peroxide, superoxide anion radical and 2,2-diphenyl-1-picryl hydrazyl (DPPH), 2,2’-azinobis-(3-ethyl-enzothiazoline-6-sulfonic acid) (ABTS) radical scavenging, and reducing power assay, were studied. The extract effectively scavenged hydroxyl radical, hydrogen peroxide and superoxide anion radicals. It also scavenged DPPH and ABTS radicals. Furthermore, it was found to have reducing power. All concentrations of leaf extract exhibited free radical scavenging and antioxidant power, and the preventive effects were in a dose-dependent manner. The antioxidant activities of the above were compared to standard antioxidants such as butylated hydroxytoluene (BHT), ascorbic acid, and α-tocopherol. The results obtained in the present study indicate that the M. maderaspatana extract could be considered a potential source of natural antioxidant.

scholarly journals The Nutritional Value of Non-Traditional Gluten-Free Flakes and Their Antioxidant Activity

Antioxidants ◽  
2019 ◽  
Vol 8 (11) ◽  
pp. 565
Author(s):  
Kristýna Šťastná ◽  
Martina Mrázková ◽  
Daniela Sumczynski ◽  
Betül Cındık ◽  
Erkan Yalçın
Keyword(s):  
Antioxidant Activity ◽  
High Performance ◽  
Sugar Content ◽  
Chenopodium Quinoa ◽  
Biologically Active ◽  
Eragrostis Tef ◽  
Total Phenolic ◽  
Phenolic Antioxidants ◽  
In Vitro Digestibility

Nowadays, there is a growing interest for foods with a lower sugar content and rich in fiber and biologically active substances. The main purpose of this study was to prepare flakes from non-traditional pigmented cereals (Oryza sativa, Chenopodium quinoa, and Eragrostis tef) and to analyze their fibre, sugar, and in vitro digestibility values. Regarding phenolic antioxidants (soluble, soluble conjugated, and insoluble bound fractions), their content and antioxidant activity were measured using spectrophotometry and high performance liquid chromatography (HPLC) methods. Hydrothermally treated grains resulted in flakes with higher total dietary fibre contents (11.1–24.4%), quinoa and teff flakes were rich in maltose (up to 42.0 mg/g). Non-traditional flakes had lower in vitro digestibility, but conversely, they exhibited the highest phenolic contents corresponding with the highest antioxidant activity values (up to 2.33 mg Gallic acid equivalent/g of total phenolic content and 1.59 mg Trolox equivalent/g for 2,2-diphenyl-1-picrylhydrazyl (DPPH) in case of brown teff). Among free phenolics, the main contributors to an antioxidant activity were p-coumaric, o-coumaric, and gallic acids (r > 0.8186); among the soluble conjugated fractions, they were epigallocatechin, epicatechin, caffeic, and vanillic acids (r > 0.5935); while caffeic, protocatechuic, and ferulic acids (r > 0.5751) were the main contributors among the insoluble bound phenolics.

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