scholarly journals Adenosine Derivates as Antioxidant Agents: Synthesis, Characterization, in Vitro Activity, and Theoretical Insights

Antioxidants ◽  
2019 ◽  
Vol 8 (10) ◽  
pp. 468 ◽  
Author(s):  
Francisco Valdes ◽  
Nelson Brown ◽  
Alejandro Morales-Bayuelo ◽  
Luis Prent-Peñaloza ◽  
Margarita Gutierrez
Keyword(s):  
Antioxidant Properties ◽  
Free Radical Scavengers ◽  
Pharmacokinetic Parameters ◽  
Quantum Similarity ◽  
Antioxidant Agents ◽  
Molecular Quantum Similarity ◽  
Adenosine Derivatives ◽  
Oxidative Processes ◽  
Theoretical Analyses

In this work, we present results about the synthesis and the antioxidant properties of seven adenosine derivatives. Four of these compounds were synthesized by substituting the N6-position of adenosine with aliphatic amines, and three were obtained by modification of the ribose ring. All compounds were obtained in pure form using column chromatography, and their structures were elucidated by infrared spectroscopy (IR) and Nuclear Magnetic Resonance (NMR). All adenosine derivatives were further evaluated in vitro as free radical scavengers. Our results show that compounds 1c, 3, and 5 display a potent antioxidant effect compared with the reference compound ascorbic acid. In addition, the absorption, distribution, metabolism and excretion (ADME) calculations show favorable pharmacokinetic parameters for the set of compounds analyzed, which guarantees their suitability as potential antioxidant drugs. Furthermore, theoretical analyses using Molecular Quantum Similarity and reactivity indices were performed in order to discriminate the different reactive sites involved in oxidative processes.

Plant polyphenols: free radical scavengers or chain-breaking antioxidants?

1995 ◽  
Vol 61 ◽  
pp. 103-116 ◽  
Author(s):  
Catherine Rice-Evans
Keyword(s):  
Biological Effects ◽  
Relative Effectiveness ◽  
Antioxidant Properties ◽  
Peroxyl Radicals ◽  
Free Radical Scavengers ◽  
Dietary Polyphenols ◽  
Chain Breaking ◽  
Lipid Peroxyl Radicals

There is increasing interest in the biological effects of tea- and wine-derived polyphenols and many studies in vitro and in vivo are demonstrating their antioxidant properties. Tea is a major source of dietary polyphenols and an even richer source of the flavanols, the catechins and catechin/gallate esters. Although there are limited studies on the bioavailability of the polyphenols, the absorption of flavanols in humans has been shown. The studies described in this chapter discuss the relative antioxidant potentials of the polyphenolic flavonoids in vitro against radicals generated in the aqueous phase in comparison with their relative effectiveness as antioxidants against propagating lipid peroxyl radicals, and how their activity influences that of α-tocopherol in low-density lipoproteins exposed to oxidative stress.

scholarly journals The Effect of Ten Essential Oils on Several Cutaneous Drug-Resistant Microorganisms and Their Cyto/Genotoxic and Antioxidant Properties

Molecules ◽  
2019 ◽  
Vol 24 (24) ◽  
pp. 4570 ◽  
Author(s):  
Katarína Kozics ◽  
Mária Bučková ◽  
Andrea Puškárová ◽  
Viktória Kalászová ◽  
Terézia Cabicarová ◽  
...  
Keyword(s):  
Essential Oils ◽  
Antioxidant Properties ◽  
Total Antioxidant Status ◽  
Human Keratinocytes ◽  
Drug Resistant ◽  
Healthy Human ◽  
Antioxidant Agents ◽  
Total Antioxidant ◽  
Antibacterial And Antifungal

In this study, we determined the antimicrobial activity of ten essential oils (EOs)—oregano, thyme, clove, arborvitae, cassia, lemongrass, melaleuca, eucalyptus, lavender, and clary sage—against drug-resistant microorganisms previously isolated from patients with skin infections. The essential oil compositions were determined using gas chromatography coupled to mass spectrometry (GC/MS). The assayed bacteria included Pseudomonas aeruginosa, Proteus vulgaris, Citrobacter koseri, and Klebsiella pneumoniae. Two drug-resistant yeasts (Candida albicans and Candida parapsilosis) were also involved in our survey. Oregano, thyme, cassia, lemongrass and arborvitae showed very strong antibacterial and antifungal activity against all tested strains. These results show that these essential oils may be effective in preventing the growth of the drug-resistant microorganisms responsible for wound infections. In this study, the genotoxic effects of tested essential oils on healthy human keratinocytes HaCaT were evaluated using the comet assay for the first time. These results revealed that none of the essential oils induced significant DNA damage in vitro after 24 h. Moreover, the treatment of HaCaT cells with essential oils increased the total antioxidant status (TAS) level. The obtained results indicate that EOs could be used as a potential source of safe and potent natural antimicrobial and antioxidant agents in the pharmaceutical and food industries.

scholarly journals Ocoxin Modulates Cancer Stem Cells and M2 Macrophage Polarization in Glioblastoma

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Esther Hernández-SanMiguel ◽  
Ricardo Gargini ◽  
Teresa Cejalvo ◽  
Berta Segura-Collar ◽  
Paula Núñez-Hervada ◽  
...  
Keyword(s):  
Stem Cells ◽  
Cancer Stem Cells ◽  
Macrophage Polarization ◽  
Antioxidant Properties ◽  
Therapy Resistance ◽  
Oral Solution ◽  
M2 Macrophage ◽  
Antioxidant Agents

Glioblastoma (GBM) is the most common and devastating primary brain tumor. The presence of cancer stem cells (CSCs) has been linked to their therapy resistance. Molecular and cellular components of the tumor microenvironment also play a fundamental role in the aggressiveness of these tumors. In particular, high levels of hypoxia and reactive oxygen species participate in several aspects of GBM biology. Moreover, GBM contains a large number of macrophages, which normally behave as immunosuppressive tumor-supportive cells. In fact, the presence of both, hypoxia and M2-like macrophages, correlates with malignancy and poor prognosis in gliomas. Antioxidant agents, as nutritional supplements, might have antitumor activity. Ocoxin® oral solution (OOS), in particular, has anti-inflammatory and antioxidant properties, as well as antitumor properties in several neoplasia, without known side effects. Here, we describe how OOS affects stem cell properties in certain GBMs, slowing down their tumor growth. In parallel, OOS has a direct effect on macrophage polarization in vitro and in vivo, inhibiting the protumoral features of M2 macrophages. Therefore, OOS could be a feasible candidate to be used in combination therapies during GBM treatment because it can target the highly resilient CSCs as well as their supportive immune microenvironment, without adding toxicity to conventional treatments.

Anti-inflammatory, Antinociceptive, and Antioxidant Potentials of Algerian Zizyphus jujuba Mill. Fruits and Leaves In Vivo and In Vitro in Different Experimental Models

2019 ◽  
Author(s):  
N. Gadiri ◽  
C. Tigrine ◽  
Z. Lakache ◽  
A. Kameli
Keyword(s):  
Antioxidant Properties ◽  
Experimental Models ◽  
Protective Capacity ◽  
Aerial Parts ◽  
Antioxidant Agents ◽  
Zizyphus Jujuba ◽  
Anti Inflammatory ◽  
Dpph Scavenging

The ethanolic extracts of the aerial parts, leaves, and fruits, of Zizyphus jujuba Mill. were studied in vivo and in vitro for their anti-inflammatory, analgesic, and antioxidant properties, respectively. A preliminary phytochemical screening was carried out. It revealed the presence of several phytoconstituents such as flavonoids, phenols, and alkaloids. The acute toxicity study was conducted using a limit dose of 2,000mg/kg. The extracts studied showed no signs of toxicity or mortality. Anti-inflammatory activity, assessed by carrageenan-induced paw edema, and antinociceptive activity, assessed by pain-induced acetic acid in mice, were significantly reduced (P < 0.001). Moreover, both extracts showed considerable DPPH scavenging activity and β-carotene protective capacity. The present study suggests that leaf and fruit extracts from Zizyphus jujuba have a pharmacological interest probably related to the presence of some bioactive compounds and could be a potential source of antiinflammatory, antinociceptive, and antioxidant agents that should be further investigated.

Endothelium-Dependent Relaxation Effects of Actinidia arguta Extracts in Coronary Artery: Involvement of eNOS/Akt Pathway

2020 ◽  
Vol 20 (9) ◽  
pp. 5381-5384 ◽  
Author(s):  
Dal-Seong Gong ◽  
Kushal Sharma ◽  
Ki-Woon Kang ◽  
Dong-Wook Kim ◽  
Min-Ho Oak
Keyword(s):  
Nitric Oxide ◽  
Coronary Artery ◽  
Cardiovascular Diseases ◽  
Vascular Reactivity ◽  
Antioxidant Properties ◽  
Vascular Effect ◽  
Porcine Coronary Artery ◽  
Actinidia Arguta ◽  
Antioxidant Agents

Cardiovascular diseases (CVD) are the major cause of death globally. Bioavailability of nitric oxide, antioxidative activity, and regulation of ionic homeostasis are the key targets for prevention of CVD. Actinidia arguta (AA) has shown promising effect for anticancer, anti-hypercholesterolemia, and antioxidant agents. However, the vascular effect of AA remains unclear. Therefore, we investigated the vascular relaxation of AA extract as well as the underlying mechanisms. Vascular reactivity was assessed in organ baths using porcine coronary arteries and antioxidant properties were assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH). Methanol extract of AA stem (AASE) induced significantly vasorelaxation of porcine coronary artery and its effects is endothelium-dependent without cytotoxicity effects. In addition, ASSE scavenged reactive oxygen species (ROS) in vitro and strongly inhibited NADPH-oxidase activity, which is major source of ROS in vasculature. AASE strongly and dose-dependently activate endothelial nitric oxide synthase (eNOS), the major vascular protective enzyme, and Akt, the upstream signaling protein of eNOS, in porcine coronary artery endothelial cell. Altogether, these results have demonstrated that AASE is a potent endotheliumdependent vasodilator and this effect was involved in, at least in part, Akt/eNOS/NO pathway with strong anti-oxidant properties. The present findings indicate that AA stem could be a valuable candidate of herbal medicine for cardiovascular diseases associated with endothelial dysfunction and atherosclerosis.

scholarly journals Computational and In Vitro Investigation of (-)-Epicatechin and Proanthocyanidin B2 as Inhibitors of Human Matrix Metalloproteinase 1

Biomolecules ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 1379 ◽  
Author(s):  
Kyung Eun Lee ◽  
Shiv Bharadwaj ◽  
Umesh Yadava ◽  
Sang Gu Kang
Keyword(s):  
Binding Free Energy ◽  
Antioxidant Properties ◽  
Epigallocatechin Gallate ◽  
Free Energy Calculations ◽  
Free Radical Scavengers ◽  
Strong Inhibitor ◽  
Docking Simulations ◽  
Matrix Metalloproteinase 1 ◽  
In Vitro Investigation

Matrix metalloproteinases 1 (MMP-1) energetically triggers the enzymatic proteolysis of extracellular matrix collagenase (ECM), resulting in progressive skin aging. Natural flavonoids are well known for their antioxidant properties and have been evaluated for inhibition of matrix metalloproteins in human. Recently, (-)-epicatechin and proanthocyanidin B2 were reported as essential flavanols from various natural reservoirs as potential anti-inflammatory and free radical scavengers. However, their molecular interactions and inhibitory potential against MMP-1 are not yet well studied. In this study, sequential absorption, distribution, metabolism, and excretion (ADME) profiling, quantum mechanics calculations, and molecular docking simulations by extra precision Glide protocol predicted the drug-likeness of (-)-epicatechin (−7.862 kcal/mol) and proanthocyanidin B2 (−8.145 kcal/mol) with the least reactivity and substantial binding affinity in the catalytic pocket of human MMP-1 by comparison to reference bioactive compound epigallocatechin gallate (−6.488 kcal/mol). These flavanols in docked complexes with MMP-1 were further studied by 500 ns molecular dynamics simulations that revealed substantial stability and intermolecular interactions, viz. hydrogen and ionic interactions, with essential residues, i.e., His218, Glu219, His222, and His228, in the active pocket of MMP-1. In addition, binding free energy calculations using the Molecular Mechanics Generalized Born Surface Area (MM/GBSA) method suggested the significant role of Coulomb interactions and van der Waals forces in the stability of respective docked MMP-1-flavonol complexes by comparison to MMP-1-epigallocatechin gallate; these observations were further supported by MMP-1 inhibition assay using zymography. Altogether with computational and MMP-1–zymography results, our findings support (-)-epicatechin as a comparatively strong inhibitor of human MMP-1 with considerable drug-likeness against proanthocyanidin B2 in reference to epigallocatechin gallate.

scholarly journals Synthesis of Novel Nitric Oxide Releasing Furoxan Hybrids from Biologically Active Bicyclic Amine and their Antioxidant Activity

2019 ◽  
Vol 31 (8) ◽  
pp. 1724-1728
Author(s):  
P.M. Swami ◽  
P.K. Zubaidha ◽  
G.B. Tiwari
Keyword(s):  
Nitric Oxide ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Biologically Active ◽  
Scavenging Effect ◽  
Antioxidant Agents ◽  
Radical Scavenging Effect ◽  
Nitric Oxide Releasing

The present paper describes the synthesis of novel nitric oxide hybrids obtained by linking bioactive bicyclic amine to substituted furoxans. The antioxidant activities were studied in vitro based on the radical scavenging effect of stable DPPH free radical using ascorbic acid as a standard. The nitric oxide hybrids showed remarkable antioxidant properties and hence, can be employed as potential antioxidant agents.

scholarly journals Chemical, enzymatic and cellular antioxidant activity studies of Agaricus blazei Murrill

2013 ◽  
Vol 85 (3) ◽  
pp. 1073-1082 ◽  
Author(s):  
RICARDO A. HAKIME-SILVA ◽  
JOSE C.R. VELLOSA ◽  
NAJEH M. KHALIL ◽  
OMAR A.K. KHALIL ◽  
IGUATEMY L. BRUNETTI ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Direct Action ◽  
Antioxidant Properties ◽  
Polymorphonuclear Neutrophils ◽  
Free Radical Scavengers ◽  
Agaricus Blazei ◽  
Resistance To Oxidation ◽  
Medicinal Properties ◽  
Agaricus Blazei Murill

Mushrooms possess nutritional and medicinal properties that have long been used for human health preservation and that have been considered by researchers as possible sources of free radical scavengers. In this work, the antioxidant properties of water extracts from Agaricus blazei Murill, produced by maceration and decoction, are demonstrated in vitro. Resistance to oxidation is demonstrated through three mechanisms: i) inhibition of enzymatic oxidative process, with 100% inhibition of HRP (horseradish peroxidase) and MPO (myeloperoxidase); ii) inhibition of cellular oxidative stress, with 80% inhibition of the oxidative burst of polymorphonuclear neutrophils (PMNs); and iii) direct action over reactive species, with 62% and 87% suppression of HOCl and superoxide anion radical (O2• –), respectively. From the data, it was concluded that the aqueous extract of A. blazei has significant antioxidant activity, indicating its possible application for nutraceutical and medicinal purposes.

Effect of antioxidants on preimplantation embryo development in vitro: a review

Zygote ◽  
2021 ◽  
pp. 1-15
Author(s):  
Sam Zarbakhsh
Keyword(s):  
Embryo Development ◽  
Antioxidant System ◽  
Culture Medium ◽  
Free Radical Scavengers ◽  
Preimplantation Embryo Development ◽  
Oxidative Stresses ◽  
Embryo Culture Medium ◽  
Oxidative Processes ◽  
Development In Vitro

Summary In vitro culture of the embryo is a useful method to treat infertility that shows embryo potential for selecting the best one to transfer and successfully implantation. However, embryo development in vitro is affected by oxidative stresses such as reactive oxygen species that may damage embryo development. Antioxidants are molecules found in fruits, vegetables, and fish that play an important role in reducing oxidative processes. In the natural environment, there is a physiological antioxidant system that protects embryos against oxidative damage. This antioxidant system does not exist in vitro. Antioxidants act as free radical scavengers and protect cells or repair damage done by free radicals. Various studies have shown that adding antioxidants into embryo culture medium improves embryo development in vitro. This review article emphasizes different aspects of various antioxidants, including types, functions and mechanisms, on the growth improvement of different species of embryos in vitro.

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