scholarly journals Potential Antioxidant Activity of New Tetracyclic and Pentacyclic Nonlinear Phenothiazine Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Godwill Azeh Engwa ◽  
Eugene Lekem Ayuk ◽  
Benardeth Ujunwa Igbojekwe ◽  
Marcellus Unaegbu
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Free Radical ◽  
Membrane Damage ◽  
The Body ◽  
Phenothiazine Derivatives ◽  
Antioxidant Agents ◽  
Group 3

The global increase in oxidative stress related diseases such as cancer, cardiovascular, and inflammatory diseases caused by overwhelming level of free radicals in the body has encouraged the search for new antioxidant agents. Based on the ability of newly synthesized phenothiazine derivatives (6-chloro-11-azabenzo[a]phenothiazine-5-one and 6-[4-bromophenyl]-10-methyl-11-azabenzo[a]phenothiazine-5-one) to oxidize H2O2, a known free radical to sulfoxide, this study assessed the in vitro and in vivo antioxidant activity. The synthesized phenothiazine derivatives exhibited reducing power potential to convert Fe3+to Fe2+and high ability to scavenge H2O2free radical in vitro. These activities were comparable to ascorbic acid, a standard antioxidant. The catalase activity significantly increased (p<0.05) in groups 1 and 2 animals that received the phenothiazine derivatives compared to the controls (groups 3 and 4) suggesting the ability of the phenothiazine derivatives to scavenge H2O2in vivo. The malondialdehyde level in groups 1 and 2 animals was lower than that in group 3 that received the reference compound (ascorbic acid) and group 4 that received the solvent suggesting the ability of the phenothiazine derivatives to prevent lipid membrane damage. AST and bilirubin levels were higher in group 2 animals which received 6-[4-bromophenyl]-10-methyl-11-azabenzo[a]phenothiazine-5-one compared to group 3, the positive control. The results suggest that phenothiazine derivatives, especially 6-chloro-11-azabenzo[a]phenothiazine-5-one, possess antioxidant activity though 6-[4-bromophenyl]-10-methyl-11-azabenzo[a]phenothiazine-5-one was slightly toxic. This activity may be due to the presence of electron donors such as sulfur as well as the richness of hydrogen in the additional benzene rings for substitution. Further study is needed to identify tolerable doses for possible therapeutic purposes.

scholarly journals Synthesis of some novel 3- (4-ethoxyphenyl) -5- (4-substituted) -4,5-dihydro-1H-pyrazole derivatives as potent antioxidant agents

2020 ◽  
Vol 11 (2) ◽  
pp. 1571-1577
Author(s):  
Lakshminarayanan B ◽  
Kannappan N ◽  
Subburaju T ◽  
Kalaichelvan V K
Keyword(s):  
Hydrogen Peroxide ◽  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Free Radical ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Assay Method ◽  
Antioxidant Agents ◽  
Ic50 Value

Pyrazolines are the most useful heterocyclic moiety in Pharmaceutical and Chemical fields and as the most potential molecules for the design of new chemical entities. Nitrogen-containing heterocyclic compounds, pyrazolines and their derivatives showed a variety of pharmacological activities, including antioxidant properties. In the present study, eleven novel ethoxylated pyrazoline derivatives were synthesized by condensing chalcones with electron releasingethoxy group at one end and different electron-donating, electron-withdrawing groups in another end with hydrazine hydrate andalcohol. The compounds synthesized were structural elucidated by their spectroscopic studies. All the compounds synthesized were evaluated for their in vitro antioxidant potential by 2,2’-diphenyl-1-picrylhydrazyl (DPPH)and hydrogen peroxide free radical scavenging assay methods.Some of these molecules possess moderate to good antioxidant activitywhen compared to standard ascorbic acid. The compound with methoxy group (EH2) exhibits potent antioxidant activity with IC50 value of 9.02 and 9.44µg/ml in DPPH and hydrogen peroxide assay method respectively and the compound with hydroxy group (EH9) also showed potent antioxidant activity with IC50 value of 12.41 and 14.56µg/ml in DPPH and hydrogen peroxide free radical scavengingassay method respectively when compared to standard. The compounds containing electron-donating substituents were found to be good antioxidantswhen compared to standard ascorbic acid.

scholarly journals Melatonin as a powerful antioxidant

2021 ◽  
Vol 71 (3) ◽  
pp. 335-354
Author(s):  
Agnieszka Chrustek ◽  
Dorota Olszewska-Słonina
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Cardiovascular Diseases ◽  
Molecular Biology ◽  
Aging Process ◽  
The Body ◽  
Many Body ◽  
Melatonin Production

AbstractMelatonin is a hormone that has many body functions and, for several decades, its antioxidant potential has been increasingly talked about. There is a relationship between failure in melatonin production in the pineal gland, an insufficient supply of this hormone to the body, and the occurrence of free radical etiology diseases such as neurodegenerative diseases, cardiovascular diseases, diabetes, cancer and others. Despite the development of molecular biology, numerous in vitro and in vivo studies, the exact mechanism of melatonin antioxidant activity is still unknown. Nowadays, the use of melatonin supplementation is more and more common, not only to prevent insomnia, but also to slow down the aging process and provide protection against diseases. The aim of this study is to get acquainted with current reports on melatonin, antioxidative mechanisms and their importance in diseases of free radical etiology.

scholarly journals Supplementation of Superfine Powder Prepared fromChaenomeles speciosaFruit Increases Endurance Capacity in Rats via Antioxidant and Nrf2/ARE Signaling Pathway

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Ka Chen ◽  
Jia You ◽  
Yong Tang ◽  
Yong Zhou ◽  
Peng Liu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Antioxidant Enzymes ◽  
Raw Material ◽  
Endurance Capacity ◽  
Swimming Time ◽  
Pharmaceutical Industries ◽  
Herb Medicine

Chaenomeles speciosafruit is a traditional herb medicine widely used in China. In this study, superfine powder ofC. speciosafruit (SCE), ground by supersonic nitrogen airflow at −140°C, was investigated to assess itsin vitroantioxidant activity andin vivoantiphysical fatigue activity. SCE was homogenous(d<10 μm)and rich in antioxidants like polyphenols, saponins, oleanolic acid, ursolic acid, ascorbic acid, and SOD. According to thein vitroexperiments, SCE displayed promising antioxidant activity with powerful FARP, SC-DPPH, and SC-SAR activities. According to thein vivoexperiments, rats supplemented with SCE had prolonged exhaustive swimming time (57%) compared to the nonsupplemented rats. Meanwhile, compared to the nonsupplemented rats, the SCE-supplemented rats had higher levels of blood glucose and liver and muscular glycogen and lower levels of LA and BUN. Lower MDA, higher antioxidant enzymes (SOD, CAT, and GSH-Px) activities, and upregulated Nrf2/ARE mediated antioxidant enzymes (HO-1, Trx, GCLM, and GCLC) expression were also detected in the supplemented group. This study indicates that SCE is a potent antioxidant and antifatigue agent, and SCE could be a promising raw material for the food and pharmaceutical industries.

Two in one: bifunctional derivatives of trolox acting as antimalarial and antioxidant agents

2020 ◽  
Vol 12 (20) ◽  
pp. 1845-1854
Author(s):  
Florence Souard ◽  
Edwige Nicolle ◽  
Delphine Cressend ◽  
Alexis Valentin ◽  
Ahcène Boumendjel
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
In Vivo Studies ◽  
Chemical Libraries ◽  
Falciparum Strain ◽  
Antioxidant Agents ◽  
One Step ◽  
Set Up ◽  
Derivatives Of

Background: The aim of the present work was to set-up compounds that are able to act simultaneously as antimalarial and antioxidants. Trolox, a known antioxidant was chosen as a core structure to ensure the antioxidant activity and contribute to antiplasmodial effect. Results: Ten compounds were prepared in one step and evaluated on chloroquino-sensitive (3D7) and chloroquino-resistant (FcB1) strains of Plasmodium falciparum. The most active compound (3d) shows antiplasmodial activity in the range of chloroquine against chloroquino-sensitive and chloroquino-resistant P. falciparum strain. The antioxidant activity of (3d) was conducted through four tests and was found to be more potent than trolox itself and L-ascorbic acid. Conclusion: Compound (3d) can be considered as an excellent lead molecule for further in vivo studies. This study paves the way for building large chemical libraries to be investigated in the field of malaria.

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.

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

scholarly journals A REVIEW ON ANTIOXIDANT METHODS

2016 ◽  
pp. 14 ◽  
Author(s):  
Dontha Sunitha
Keyword(s):  
Reactive Oxygen Species ◽  
Lipid Peroxidation ◽  
Antioxidant Activity ◽  
Free Radical ◽  
Oxygen Species ◽  
Antioxidant Assay ◽  
Antioxidant Effects ◽  
In Vitro Antioxidant Activity

<p>ABSTRACT<br />To provide an outlook of the various available methods of antioxidant activity. Various available in vitro and in vivo methods are listed and the<br />procedure to perform the method, its mechanism is also explained in brief. 1,1-diphenyl-2-picrylhydrazyl method was found to be used mostly for the<br />in vitro antioxidant activity evaluation purpose while lipid peroxidation was found as mostly used in vivo antioxidant assay. An ethanol was with the<br />highest frequency as a solvent for extraction purpose. Summarized information on the various methods available provides with reliable information<br />to confirm the benefits of antioxidant effects.<br />Keywords: Antioxidant activity, Reactive oxygen species, Free radical, 1,1-diphenyl-2-picrylhydrazyl, Flavonoid.</p>

scholarly journals Antioxidant Activity of Pigmented Rice and Impact on Health

JURNAL PANGAN ◽  
2019 ◽  
Vol 28 (1) ◽  
pp. 11-22
Author(s):  
Arfina Sukmawati Arifin
Keyword(s):  
Oxidative Stress ◽  
Diabetes Mellitus ◽  
Antioxidant Activity ◽  
Vascular Function ◽  
Healthy Lifestyle ◽  
Cell Damage ◽  
The Body ◽  
Food Sources

The high number of free radicals that are not balanced with the amount of antioxidants in the body triggers oxidative stress. Oxidative stress causes impaired vascular function, damage to proteins and lipids in membrane cell, and nucleic acid (DNA) mutations. Chronic cell damage has a negative effect on tissue that triggers various diseases such as neurodegenerative diseases (Alzheimer's, Parkinson's), cardiovascular diseases (hypertension, arteriosclerosis, and others), cataracts, retinal damage, maculopathy, rheumatoid arthritis, asthma, stroke, diabetes mellitus , immunodepression, cancer, aging, hyperoxia, dermatitis, and others. The application of a healthy lifestyle for example by consuming food sources of bioactive compounds can minimize health risks. Rice is the staple food of the Indonesian people. Some types of rice contain red and black pigments which are known to have high antioxidant activity compared to white rice. The pigment comes from anthocyanin and proanthocyanidin. Various studies in vitro and in vivo prove that anthocyanin and proantocyanidine act as antioxidants and potency as a preventative for various diseases such as cardiovascular, diabetes mellitus, and etc.

scholarly journals The synthesis and the antioxidant activity of 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2a,4a,8a-triazacyclopenta[cd]azulene-3-carboxylic (or carbothionic) acid derivatives

Pharmacia ◽  
2021 ◽  
Vol 68 (1) ◽  
pp. 251-258
Author(s):  
Sergii Demchenko ◽  
Hanna Yeromina ◽  
Yulia Fedchenkova ◽  
Zinaida Ieromina ◽  
Vitaliy Yaremenko ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Carboxylic Acid ◽  
In Silico ◽  
Pharmacokinetic Profile ◽  
High Antioxidant Activity ◽  
Pharmacological Screening

New 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2а,4a,8a-triazacyclopenta[cd]azulene-3-carboxylic (or carbothionic) acid derivatives have been designed, synthesized and evaluated for their in vitro antioxidant activity under conditions of the artificial oxidative stress using ionol, ascorbic acid and α-tocopherol as the reference drugs. It has been found that 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2а,4a,8a-triazacyclopenta[cd]azulene-3-carbothionic acid derivatives 9b, 9c, 9d, 9e, 9f, 9i and 1-phenoxymethyl-4-(41-chlorophenyl)-5,6,7,8-tetrahydro-2,2a,8-triazacyclopenta[cd]azulene-3-carboxylic acid phenylamide 10 reveal a high antioxidant activity and a good in silico pharmacokinetic profile. The data obtained allowed us to select the most promising objects from the substances synthesized for further pharmacological screening for the presence of the antioxidant activity in vivo.

Synergistic antioxidant activity of size controllable chitosan-templated Prussian blue nanoparticle

Nanomedicine ◽  
2019 ◽  
Vol 14 (19) ◽  
pp. 2567-2578 ◽  
Author(s):  
Hyeryeon Oh ◽  
Jin Sil Lee ◽  
Daekyung Sung ◽  
Jin Hyung Lee ◽  
Sang Hyun Moh ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Antioxidant Activity ◽  
Prussian Blue ◽  
Reactive Oxygen Species Generation ◽  
Reactive Oxygen ◽  
Water Soluble ◽  
Oxygen Species ◽  
Antioxidant Agents

Aim: Prussian blue nanoparticles (PB NPs) have been reported as excellent antioxidant agents owing to their ability to scavenge reactive oxygen species. However, their poor stability in vivo limits their use in biomedical applications. Materials & methods: In this study, we developed chitosan-templated PB NPs using water-soluble chitosan samples with molecular weights ranging from 3 to 100 kDa, which stabilized the PB NPs and improved their antioxidant activity. Results & conclusion: The chitosan-templated PB NPs coordinated with the optimal chitosan molecular weight had uniform sphere-like particles, improved stability and effective scavenging activity of in vitro reactive oxygen species generation in murine fibroblast cells stimulated by oxidative stress agents without any cytotoxicity, implying that they could be promising antioxidant agents.

Sign in / Sign up

Export Citation Format

Share Document