scholarly journals Antiradical activity of novel 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol derivatives

2021 ◽  
Vol 14 (2) ◽  
pp. 162-166
Author(s):  
A. A. Safonov ◽  
I. S. Nosulenko
Keyword(s):  
Free Radicals ◽  
Free Radical ◽  
Antiradical Activity ◽  
The Body ◽  
Biologically Active ◽  
Stable Free Radical ◽  
Free Radical Theory ◽  
Radical Theory ◽  
Initial Molecule

The process of studying free radicals began in the middle of the last century (the free radical theory of aging in 1956). Multiple studies have revealed the effect of free radicals on the cells of the body and the development of various diseases, such as diabetes, autoimmune diseases, diseases of the nervous system, and others. As a result, the term antioxidant has emerged, compounds that reduce and prevent the effects of free radicals. Most of the newly synthesized substances are studied for their antiradical properties. 1,2,4-Triazole derivatives are no exception, which has already proven themselves as biologically active compounds. The aim of this work was the investigation antiradical activity among 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol derivatives. Materials and methods. Previously synthesized 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol derivatives were used as test compounds. The research of antiradical activity was based on the interaction between 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol derivatives and 2,2-diphenyl-1-picrylhydrazyl (DPPH) in vitro. DPPH is a stable free radical. The color of its alcoholic solutions were intense purple (λmax = 517 nm). When DPPH interacted with compounds that were capable of scavenging free radicals, it produced products. These products are yellow in color and do not absorb light of the aforementioned wavelength. The study was carried out according to the method. Results. The antiradical activity of 10 new 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol derivatives was studied. Most of the test compounds show antiradical activity against DPPH. Compound 1 was the most active at a concentration of 1 × 10-3 M and the antiradical effect was close to ascorbic acid. Conclusions. The most active compound is 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol, which in a concentration of 1 × 10-3 M has an antiradical effect in 88.89 %. When reducing the concentration to 1 × 10-4 M, also reduces the antiradical activity to 53.78 %. Some conclusions are drawn regarding the “structure – effect” dependence between 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol derivatives: – the introduction of 4-fluorobenzylidene radical (compound 2) into the 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol molecule results in a slight decrease in activity; – the introduction of 2-hydroxybenzylidene radical (compound 3) into initial molecule results a high antiradical effect, which hardly changes with decreasing concentration; – transformation to 2-((5-(thiophen-2-ylmethyl)-4-((R)amino)-4H-1,2,4-triazol-3-yl)thio)acetic acid has almost no effect on antiradical activity, except for compound 9 (the antiradical effect is reduse).

scholarly journals Oxidative stress in ageing

2017 ◽  
Vol 5 (11) ◽  
pp. 4826 ◽  
Author(s):  
Fasna K. A. ◽  
Geetha N. ◽  
Jean Maliekkal
Keyword(s):  
Oxidative Stress ◽  
Lipid Peroxidation ◽  
Free Radicals ◽  
Free Radical ◽  
Age Groups ◽  
The Body ◽  
Antioxidant Systems ◽  
Lipid Peroxidation Product ◽  
Free Radical Theory ◽  
Radical Theory

Background: Ageing is characterized by a gradual decline in body functions and decreased ability to maintain homeostasis. The free radical theory of ageing proposed by Harman D states that ageing is a result of cumulative damage incurred by free radical reactions. Free radicals are highly reactive molecular species with unpaired electrons; generated in the body by several physiological processes. Prime target to free radical attack are the polyunsaturated fatty acids of cell membranes causing lipid peroxidation. The free radicals are neutralized by the exogenous and endogenous antioxidant systems. Oxidative stress occurs when large number of free radicals are produced or the antioxidant activity is impaired. The present study is focused to find out the role of oxidative stress in ageing.Methods: A cross sectional observational study was undertaken to assess the oxidative stress in ageing; by determining the levels of lipid peroxidation product- malondialdehyde (MDA), the antioxidants- superoxide dismutase (SOD) and ceruloplasmin in various age groups. 150 healthy subjects were selected randomly and categorised into three different age groups of 20-30 years, 40-59 years and 60-90 years; with 50 subjects in each group. Results were expressed as mean ± standard deviation.Results: a significant elevation in serum MDA level and a decline in SOD were observed in 40-59 years and 60-90 years age groups. However, an elevated ceruloplasmin level was found in the above age groups.Conclusions: Aforementioned observations are suggestive of an association between oxidative stress and the progression of ageing process.

scholarly journals Root Cause of Diseases – Ama Concept W.S.R to Free Radical Theory

2015 ◽  
Vol 6 (2) ◽  
Author(s):  
Jaideep Sapra
Keyword(s):  
Free Radicals ◽  
Free Radical ◽  
Present Article ◽  
Oxygen Free Radicals ◽  
The Body ◽  
Whole Body ◽  
Free Radical Theory ◽  
Radical Theory ◽  
Root Cause ◽  
Toxic Material

Ayurveda speaks the main cause of diseases is rooted in the impairment of the body's main fire, called Agni, the fire of digestion. Ayurveda views the health of the body as the functioning of a biological fire-governing metabolism. If this essential part is functioning effectively, the whole body will be nourished, full of life and vibrancy. Altered digestive functioning can lead to the production of Ama, a toxic material that initiates and promotes disease processes throughout the body. In the same way, free radicals are also found to be the root cause of many diseases. The majority of free radicals that damage biological systems are oxygen-free radicals, and these are more generally known as “Reactive oxygen Species” (ROS). These are the main byproducts formed in the cells of aerobic organisms, and can initiate autocatalytic reactions so that molecules to which they react are themselves converted into free radicals to propagate the chain of damage. Here we shall discuss about properties of both Ama and Free Radicals. The present article attempts to correlate the concept of Free radical with the concept of Ama. 

The Free Radical Theory of Aging Matures

1998 ◽  
Vol 78 (2) ◽  
pp. 547-581 ◽  
Author(s):  
KENNETH B. BECKMAN ◽  
BRUCE N. AMES
Keyword(s):  
Free Radical ◽  
Epidemiological Studies ◽  
Biological Research ◽  
Free Radical Theory ◽  
Radical Theory ◽  
Transgenic Organisms ◽  
Expanding Circle ◽  
The Status ◽  
Theory Of Aging

Beckman, Kenneth B., and Bruce N. Ames. The Free Radical Theory of Aging Matures. Physiol. Rev. 78: 547–581, 1998. — The free radical theory of aging, conceived in 1956, has turned 40 and is rapidly attracting the interest of the mainstream of biological research. From its origins in radiation biology, through a decade or so of dormancy and two decades of steady phenomenological research, it has attracted an increasing number of scientists from an expanding circle of fields. During the past decade, several lines of evidence have convinced a number of scientists that oxidants play an important role in aging. (For the sake of simplicity, we use the term oxidant to refer to all “reactive oxygen species,” including O−2⋅, H2O2, and ⋅OH, even though the former often acts as a reductant and produces oxidants indirectly.) The pace and scope of research in the last few years have been particularly impressive and diverse. The only disadvantage of the current intellectual ferment is the difficulty in digesting the literature. Therefore, we have systematically reviewed the status of the free radical theory, by categorizing the literature in terms of the various types of experiments that have been performed. These include phenomenological measurements of age-associated oxidative stress, interspecies comparisons, dietary restriction, the manipulation of metabolic activity and oxygen tension, treatment with dietary and pharmacological antioxidants, in vitro senescence, classical and population genetics, molecular genetics, transgenic organisms, the study of human diseases of aging, epidemiological studies, and the ongoing elucidation of the role of active oxygen in biology.

scholarly journals In vitro antileishmanial and antioxidant activities of essential oils from different parts of Murraya paniculata (L.) Jack: a species of Rutaceae that occur in the Cerrado biome in Brazil

2020 ◽  
pp. 347-353
Author(s):  
Flávia Fernanda Alves da Silva ◽  
Cassia Cristina Fernandes ◽  
Gabriel Almeida de Oliveira ◽  
Ana Carolina Bolela Bovo Candido ◽  
Lizandra Guidi Magalhães ◽  
...  
Keyword(s):  
Free Radical ◽  
Essential Oils ◽  
Antioxidant Activities ◽  
Folk Medicine ◽  
Natural Antioxidants ◽  
The Body ◽  
Antioxidant Compounds ◽  
Stable Free Radical ◽  
Murraya Paniculata

In Brazilian folk medicine, Murraya paniculata has been used for treating intestine disorders, rheumatism and cough. This paper aims to investigate the in vitro antileishmanial and antioxidant activities of essential oils (EO) from M. paniculata leaves and fruits (ripe and unripe ones). Natural antioxidants may be very beneficial to improve quality of life, since they are capable of protecting the body against damage caused by free radicals and, consequently, either preventing or postponing many diseases from starting their cycles. One of the techniques which has been widely used for detecting antioxidant compounds is the method based on the elimination of the stable free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH•). It has been considered easy, precise, fast, simple, economical and appropriate to determine antioxidant activity of pure substances and complex mixtures, such as EO. Thus, antioxidant potential of EO was evaluated by using the method of the free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH•). EO from M. paniculata leaves and fruits exhibited weak potential, since EC50 values were above 700 µg/mL. Several reports have stated that volatile oils from plants show promising leishmanicidal activity against promastigote forms of Leishmania amazonensis; in relation to this activity, leaf oil was highly active (IC50 = 7.33±2.07 µg/mL) while ripe and unripe fruit oils were active, with values of IC50 = 30.77±2.07 µg/mL and 13.04±1.64 µg/mL, respectively. Both GC-FID and GC-MS analyses revealed that the major components determined in EO from M. paniculata were sesquithujene (25.0%), trans-β-caryophyllene (23.8%), α-zingiberene (21.0%), α-ylangene (13.3%), germacrene D (13.1%), α-copaene (12.7%), and β-cubebene (10.2%). In vitro antileishmanial and antioxidant activities of EO from M. paniculata have also been described for the first time.

scholarly journals Microwave-Assisted Synthesis, Characterization, Antimicrobial and Antioxidant Activity of Some New Isatin Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
G. Kiran ◽  
T. Maneshwar ◽  
Y. Rajeshwar ◽  
M. Sarangapani
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging ◽  
Microwave Assisted Synthesis ◽  
Stable Free Radical ◽  
Ft Ir ◽  
Antimicrobial And Antioxidant Activity ◽  
New Compounds ◽  
Isatin Derivatives

A series of β-Isatin aldehyde-N,N′-thiocarbohydrazone derivatives were synthesized and assayed for theirin vitroantimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml against the tested microorganisms. Among the compounds3e,3jand3nshow highest significant antimicrobial activity. The free radical scavenging effects of the test compounds against stable free radical DPPH (α,α-diphenyl-β-picryl hydrazyl) and H2O2were measured spectrophotometrically. Compounds3j,3n,3l, and3e, respectively, had the most effective antioxidant activity against DPPH and H2O2scavenging activity.

scholarly journals Effects of Caloric Restriction on Cardiac Oxidative Stress and Mitochondrial Bioenergetics: Potential Role of Cardiac Sirtuins

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Ken Shinmura
Keyword(s):  
Oxidative Stress ◽  
Free Radical ◽  
Oxidative Damage ◽  
Caloric Restriction ◽  
Functional Decline ◽  
Cellular Damage ◽  
Free Radical Theory ◽  
Radical Theory ◽  
Stress Theory

The biology of aging has not been fully clarified, but the free radical theory of aging is one of the strongest aging theories proposed to date. The free radical theory has been expanded to the oxidative stress theory, in which mitochondria play a central role in the development of the aging process because of their critical roles in bioenergetics, oxidant production, and regulation of cell death. A decline in cardiac mitochondrial function associated with the accumulation of oxidative damage might be responsible, at least in part, for the decline in cardiac performance with age. In contrast, lifelong caloric restriction can attenuate functional decline with age, delay the onset of morbidity, and extend lifespan in various species. The effect of caloric restriction appears to be related to a reduction in cellular damage induced by reactive oxygen species. There is increasing evidence that sirtuins play an essential role in the reduction of mitochondrial oxidative stress during caloric restriction. We speculate that cardiac sirtuins attenuate the accumulation of oxidative damage associated with age by modifying specific mitochondrial proteins posttranscriptionally. Therefore, the distinct role of each sirtuin in the heart subjected to caloric restriction should be clarified to translate sirtuin biology into clinical practice.

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