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.

Synthesis, Characterization and Antioxidant Activity of Cooper-Quercetin Complex and Iron-Quercetin Complex

2018 ◽  
Vol 69 (10) ◽  
pp. 2621-2624
Author(s):  
Svetlana Trifunschi ◽  
Melania Florina Munteanu
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging ◽  
Free Radical Scavengers ◽  
Spectroscopic Techniques ◽  
Dpph Radical ◽  
Radical Scavengers ◽  
Therapeutic Applications ◽  
Flavonoid Quercetin ◽  
Dpph Radical Scavenging

Complexes of cooper (II) and iron (II) with flavonoid quercetin have been synthesized. The structure of compounds has been confirmed by means of UV-Vis and FTIR spectroscopic techniques. The antioxidant activity of the flavonoid complexes has been evaluated by using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. These complexes of flavonoids are much more effective free radical scavengers than the free flavonoids, an aspect which recommends them for further studies on possible therapeutic applications.

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 Has Oxidative Stress any Role on Mechanisms of Aminophylline – Induced Seizures? An Animal Study

2015 ◽  
Vol 12 (4) ◽  
pp. 269-274 ◽  
Author(s):  
UK Roy ◽  
M Pal ◽  
S Datta ◽  
S Harlalka
Keyword(s):  
Oxidative Stress ◽  
Free Radicals ◽  
Free Radical ◽  
Molecular Mechanisms ◽  
Clinical History ◽  
Antioxidant Vitamin ◽  
Dependent Manner ◽  
Free Radical Generation ◽  
Radical Generation ◽  
Pre Treatment

Background Aminophylline can trigger seizures in patients without known underlying epilepsy or added risk factor for seizure exacerbation in epilepsy. Most of these seizures are difficult to control and are underappreciated compared to other drug toxicities. Despite a long clinical history of aminophylline-induced seizures, relatively little is known about the underlying molecular mechanisms that contribute to methylxanthine-induced seizure generation.Objective The present study evaluated the possible involvement of free radicals in aminophylline induced seizures in rat.Method The rats were divided into two groups. The first group graded single doses of aminophylline from 100 to 300 mg/kg were administered intraperitoneally. On the basis of the results Aminophylline, a dose (300 mg/kg) producing tonic-clonic seizures and mortality in 100% animals was selected as control in the study. The second group were subjected to single antioxidant (Vitamin E or Vitamin C) or in combination for 45 days then single doses of aminophylline 300 mg/kg administered intraperitoneally to rats.Result Aminophylline induced convulsions in rats in a dose-dependent manner, and both incidence of seizure and mortality were maximum at 300 mg/kg and there was significant increase of free radical generation. But though pre-treatment with antioxidants showed differential attenuating effects on aminophylline induced free radical generation as we all known but they were very much ineffective in antagonizing aminophylline induced seizures and post-seizure mortality by any appreciable extent.Conclusion Though Aminophylline induces oxidative stress the results are suggestive that at least free radicals is not only cause of convulsiogenic effects and post-seizure mortality of aminophylline.Kathmandu University Medical Journal Vol.12(4) 2014; 269-274

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.

Diaphragmatic free radical generation increases in an animal model of heart failure

2005 ◽  
Vol 99 (3) ◽  
pp. 1078-1084 ◽  
Author(s):  
Gerald S. Supinski ◽  
Leigh A. Callahan
Keyword(s):  
Heart Failure ◽  
Free Radicals ◽  
Free Radical ◽  
Protein Carbonyl ◽  
Protein Carbonyls ◽  
Force Frequency ◽  
Free Radical Generation ◽  
Coronary Ligation ◽  
Radical Generation ◽  
Frequency Relationship

Heart failure evokes diaphragm weakness, but the mechanism(s) by which this occurs are not known. We postulated that heart failure increases diaphragm free radical generation and that free radicals trigger diaphragm dysfunction in this condition. The purpose of the present study was to test this hypothesis. Experiments were performed using halothane-anesthetized sham-operated control rats and rats in which myocardial infarction was induced by ligation of the left anterior descending coronary artery. Animals were killed 6 wk after surgery, the diaphragms were removed, and the following were assessed: 1) mitochondrial hydrogen peroxide (H2O2) generation, 2) free radical generation in resting and contracting intact diaphragm using a fluorescent-indicator technique, 3) 8-isoprostane and protein carbonyls (indexes of free radical-induced lipid and protein oxidation), and 4) the diaphragm force-frequency relationship. In additional experiments, a group of coronary ligation animals were treated with polyethylene glycol-superoxide dismutase (PEG-SOD, 2,000 units·kg−1·day−1) for 4 wk. We found that coronary ligation evoked an increase in free radical formation by the intact diaphragm, increased diaphragm mitochondrial H2O2 generation, increased diaphragm protein carbonyl levels, and increased diaphragm 8-isoprostane levels compared with controls ( P < 0.001 for the first 3 comparisons, P < 0.05 for 8-isoprostane levels). Force generated in response to 20-Hz stimulation was reduced by coronary ligation ( P < 0.05); PEG-SOD administration restored force to control levels ( P < 0.03). These findings indicate that cardiac dysfunction due to coronary ligation increases diaphragm free radical generation and that free radicals evoke reductions in diaphragm force generation.

Effects of free radical generation on mouse pial arterioles: probable role of hydroxyl radicals

1983 ◽  
Vol 245 (1) ◽  
pp. H139-H142 ◽  
Author(s):  
W. I. Rosenblum
Keyword(s):  
Free Radical ◽  
Xanthine Oxidase ◽  
Hydroxyl Radicals ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Pial Arterioles ◽  
Probable Role ◽  
Radical Generation ◽  
Superoxide Scavenger

Mouse pial arterioles were exposed to the free radical-generating reactants acetaldehyde and xanthine oxidase. Concentrations of 0.5 mM acetaldehyde and 0.1 U/ml xanthine oxidase caused reversible dilations, whereas higher concentrations produced initial constrictions followed by reversible dilations. The following free radical scavengers inhibited the dilation when added to the lower concentrations of reactants: superoxide dismutase, a superoxide scavenger; catalase, an H2O2 scavenger; and mannitol, a hydroxyl scavenger. In addition, pretreatment of the animal with dimethyl sulfoxide, a hydroxyl scavenger, also inhibited the response. The scavengers were also tested against either the dilation produced by increased inspired CO2 or against the dilation produced by local application of 10(-3) M papaverine. No significant effect was observed. The data support the hypothesis that hydroxyl radicals can dilate pial arterioles, since all the scavengers can ultimately reduce levels of hydroxyl generated by acetaldehyde plus xanthine oxidase.

Free Radical Scavenging and Antioxidant Activity of Ascorbigen Versus Ascorbic Acid: Studies in Vitro and in Cultured Human Keratinocytes

2008 ◽  
Vol 56 (24) ◽  
pp. 11694-11699 ◽  
Author(s):  
Anika E. Wagner ◽  
Patricia Huebbe ◽  
Tetsuya Konishi ◽  
M. Mamunur Rahman ◽  
Meiko Nakahara ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Free Radical ◽  
Radical Scavenging ◽  
Human Keratinocytes ◽  
Free Radical Scavenging

Free radicals as potential mediators of metal-allergy: Ni2+- and Co2+-mediated free radical generation

1998 ◽  
Vol 6 (4) ◽  
pp. 279-286 ◽  
Author(s):  
Leon T Van den Broeke ◽  
Astrid Gräslund ◽  
J.Lars G Nilsson ◽  
Jan E. Wahlberg ◽  
Annika Scheynius ◽  
...  
Keyword(s):  
Free Radicals ◽  
Free Radical ◽  
Metal Allergy ◽  
Free Radical Generation ◽  
Radical Generation

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.

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