Eco-Friendly Approach for the Synthesis of Thiophene Linked Benzothiazepines as Biocompatible Free Radical Scavengers

2021 ◽  
Vol 6 (1) ◽  
pp. 1-6
Author(s):  
P. Sudeep ◽  
K.R. Raghavendra ◽  
R. Sowmya ◽  
K. Ajay Kumar
Keyword(s):  
Free Radical ◽  
Hydroxyl Radical ◽  
Phase Transfer ◽  
Tetrabutylammonium Bromide ◽  
Radical Scavenging ◽  
Phase Transfer Catalyst ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Citrus Juice

A series of new thiophene tethered benzothiazepines (5a-h) were synthesized through citrus juice mediated (4+3) annulations of thienyl chalcones with 2-aminobenzenethiol in the presence of tetrabutylammonium bromide as phase transfer catalyst under reflux conditions. The synthesized compounds were characterized by spectroscopic and CHN analysis. To check the antioxidant potentials of the synthesized compounds, in vitro DPPH and hydroxyl radical scavenging assays were conducted. The results shows that amongst the series, compounds 5b with (21.44-49.72%) and (16.88-42.60%); 5c with (24.88-56.00%) and (22.33-53.12%); and 5h with (22.80-47.10%) and (15.33-44.12%) excellent DPPH and hydroxyl radical potencies comparable with the respective standards used in the experiments.

scholarly journals Biological Activity of the Methanol and Water Extracts of the Fruits of Anthocyanin-Rich Plants Grown in South-West Poland

2015 ◽  
Vol 10 (3) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Paulina Strugala ◽  
Anna Dudra ◽  
Alicja Z. Kucharska ◽  
Anna Sokół-Łętowska ◽  
Dorota Wojnicz ◽  
...  
Keyword(s):  
Free Radical ◽  
Biological Effects ◽  
Radical Scavenging ◽  
Antibacterial Properties ◽  
Bacterial Biofilm ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Water Extracts ◽  
South West ◽  
Anti Inflammatory

In this study we focused on the chemical composition, antioxidant, anti-inflammatory and antibacterial properties of methanol and water extracts of fruits of six species grown in south-west Poland: blackberry, blackcurrant, chokeberry, cherry, gooseberry and raspberry. No general correlation could be drawn between extract chemical properties (i.e. antioxidant and free radical scavenging) and observed biological effects. However, blackcurrant and blackberry extracts (both methanol and water) appeared to be good antioxidants and free radical scavengers, as well as effective inhibitors of E. coli adhesion to the uroepithelial cells. On the other hand, the poorest antioxidants and free radical scavengers, cherry and gooseberry extracts, also poorly affected bacterial growth, swimming ability and adhesion to epithelial cells. Surprisingly, gooseberry extracts, which showed generally weak effects, appeared to be the most effective inhibitor of bacterial biofilm formation. Additionally, most of the studied extracts showed reasonably strong anti-inflammatory properties.

scholarly journals Polyphenols in human nutrition: from the in vitro antioxidant capacity to the beneficial effects on cardiometabolic health and related inter-individual variability – an overview and perspective

2019 ◽  
Vol 123 (3) ◽  
pp. 241-254 ◽  
Author(s):  
T. Ruskovska ◽  
V. Maksimova ◽  
D. Milenkovic
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging ◽  
Individual Variability ◽  
Free Radical Scavengers ◽  
Cardiometabolic Health ◽  
Dietary Recommendations ◽  
Beneficial Effects

AbstractOxidative damage of cells and tissues is broadly implicated in human pathophysiology, including cardiometabolic diseases. Polyphenols, as important constituents of the human diet and potent in vitro free radical scavengers, have been extensively studied for their beneficial effects on cardiometabolic health. However, it has been demonstrated that the in vivo antioxidant activity of polyphenols is distinct from their in vitro free radical-scavenging capacity. Indeed, bioavailability of nutritional polyphenols is low and conditioned by complex mechanisms of absorption, distribution, metabolism and excretion. Nowadays, it is commonly accepted that the cellular antioxidant activity of polyphenols is mainly carried out via modification of transcription of genes involved in antioxidant defence. Importantly, polyphenols also contribute to cardiometabolic health by modulation of a plethora of cellular processes that are not directly associated with antioxidant enzymes, through nutri(epi)genomic mechanisms. Numerous human intervention studies have demonstrated beneficial effects of polyphenols on the key cardiometabolic risk factors. However, inconsistency of the results of some studies led to identification of the inter-individual variability in response to consumption of polyphenols. In perspective, a detailed investigation of the determinants of this inter-individual variability will potentially lead us towards personalised dietary recommendations. The phenomenon of inter-individual variability is also of relevance for supplementation with antioxidant (pro)vitamins.

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.

Target Size Analysis by Radiation Inactivation: The Use of Free Radical Scavengers

2005 ◽  
Vol 230 (7) ◽  
pp. 455-463 ◽  
Author(s):  
Gene C. Ness ◽  
Laura C. Pendleton ◽  
Michael J. McCreery
Keyword(s):  
Enzyme Activity ◽  
Free Radical ◽  
Functional Unit ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Target Size ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Radiation Inactivation ◽  
Glucose 6 Phosphate Dehydrogenase

Several model systems were employed to assess indirect effects that occur in the process of using radiation inactivation analysis to determine protein target sizes. In the absence of free radical scavengers, such as mannitol and benzoic acid, protein functional unit sizes can be drastically overestimated. In the case of glutamate dehydrogenase, inclusion of free radical scavengers reduced the apparent target size from that of a hexamer to that of a trimer based on enzyme activity determinations. For glucose-6-phosphate dehydrogenase, the apparent target size was reduced from a dimer to a monomer. The target sizes for both glutamate dehydrogenase and glucose-6-phosphate dehydrogenase in the presence of free radical scavengers corresponded to subunit sizes when determinations of protein by sodium dodecyl sulfate–polyacrylamide gel electrophoresis or immunoblotting were done rather than enzyme activity. The free radical scavengers appear to compete with proteins for damage by secondary radiation products, since irradiation of these compounds can result in production of inhibitory species. Addition of benzoic acid/mannitol to samples undergoing irradiation was more effective in eliminating secondary damage than were 11 other potential free radical scavenging systems. Addition of a free radical scavenging system enables more accurate functional unit size determinations to be made using radiation inactivation analysis.

Discovery of New N-hydrazinecarbothioamide Indazole Hybrids: As Potential Radical (ABTS and DPPH) Scavengers

2020 ◽  
Vol 17 (9) ◽  
pp. 1177-1185
Author(s):  
Rafaila Rafique ◽  
Arshia ◽  
Kanwal ◽  
Khalid Mohammed Khan ◽  
Sridevi Chigurupati ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Free Radicals ◽  
Free Radical ◽  
Radical Scavenging ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Synthetic Compounds ◽  
Free Radical Generation ◽  
Radical Generation

Background: Free radicals are the main cause of numerous diseases. Their overproduction needs to be controlled in order to combat several ailments. The current study deals with the discovery of new free radical scavengers. Methods: Substituted N-hydrazinecarbothioamide indazoles 1-18 were evaluated for DPPH and ABTS radical scavenging activities. Results: All synthetic compounds possess good radical DPPH and ABTS scavenging potential in the ranges of IC50 = 2.11 ± 0.17 - 5.3 ± 0.11 μM and IC50 = 2.31 ± 0.06 - 5.5 ± 0.07 μM, respectively, as compared to standard ascorbic acid having IC50 = 2.02 ± 0.11 μM for DPPH and IC50 = 2.1 ± 0.07 μM for ABTS. Conclusion: These compounds could serve as leads for antioxidant activity that have the ability to control free radical generation and ward off free radical-induced disorders.

scholarly journals Studies on free radical scavenging substances from microorganisms. II. Neocarazostatins A, B and C, novel free radical scavengers.

1991 ◽  
Vol 44 (8) ◽  
pp. 903-907 ◽  
Author(s):  
SHINICHIRO KATO ◽  
KAZUTOSHI SHINDO ◽  
YOKO KATAOKA ◽  
YUJI YAMAGISHI ◽  
JUNICHIRO MOCHIZUKI
Keyword(s):  
Free Radical ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Free Radical Scavengers ◽  
Radical Scavengers
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