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Chelating Activity (chelating + activity)

Distribution by Scientific Domains

Medical Sciences	50%
Chemistry	30%

Kinds of Chelating Activity

iron chelating activity

Selected Abstracts

Combined therapy of silymarin and desferrioxamine in patients with ,-thalassemia major: a randomized double-blind clinical trial

FUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 3 2009
Marjan Gharagozloo
Abstract Silymarin, a flavonolignan complex isolated from Silybum marianum, has a strong antioxidant, hepatoprotective, and iron chelating activities. The present study was designed to investigate the therapeutic activity of orally administered silymarin in patients with thalassemia major under conventional iron chelation therapy. A 3-month randomized, double-blind, clinical trial was conducted in 59 ,-thalassemia major patients in two well-matched groups. Patients were randomized to receive a silymarin tablet (140 mg) three times a day plus conventional desferrioxamine therapy. The second group received the same therapy but a placebo tablet instead of silymarin. Clinical laboratory tests were assessed at the beginning and the end of the trial, except for serum ferritin level that was assessed at the middle of the trial as well. Results of this study revealed that the combined therapy was well tolerated and more effective than desferrioxamine in reducing serum ferritin level. Significant improvement in liver alkaline phosphatase and glutathione levels of red blood cells was also observed in silymarin-treated ,-thalassemia patients. However, no significant difference in serum ferritin levels was detected between silymarin and placebo groups after 1.5 and 3 months treatment, probably because of insufficient sample size to detect subtle changes in ferritin levels between groups. This is the first report showing the beneficial effects of silymarin in thalassemia patients and suggests that silymarin in combination with desferrioxamine can be safely and effectively used in the treatment of iron-loaded patients. [source]

Oak leaf extract as topical antioxidant: Free radical scavenging and iron chelating activities and in vivo skin irritation potential

BIOFACTORS, Issue 4 2008
Isabel F. Almeida
Abstract The topical application of antioxidants may be beneficial for the protection of the skin against UV damage. An extract of Quercus robur leaves was prepared and evaluated considering its putative application as topical antioxidant. The solvent and extractive method selection was monitored by 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging activity and polyphenols extraction (measured by the Folin Ciocalteu assay). Iron chelating activity and the phenolic composition (HPLC/DAD) were assessed on the extract obtained under optimized conditions. Skin irritation potential was investigated by performing an in vivo patch test in 19 volunteers. The extraction solvent which resulted in the highest activity was ethanol:water (4:6) and thus it was selected for further preparation of this extract. The IC50a for the iron chelation and DPPH scavenging assays were 153.8 ± 26.3 ,g.mL,1 and 7.53 ± 0.71 ,g.mL,1 (mean ± SD), respectively. The total phenolic content was found to be 346.3 ± 6.7 mg gallic acid equivalents (GAE)/g extract (mean ± SD). Three phenolic compounds were identified in the extract namely: ellagic acid, rutin and hyperoside. The major identified component was ellagic acid. The patch test carried out showed that the extract can be regarded as safe for topical application. [source]

Calcium-independent cytoskeleton disassembly induced by BAPTA

FEBS JOURNAL, Issue 15 2004
Yasmina Saoudi
In living organisms, Ca2+ signalling is central to cell physiology. The Ca2+ chelator 1,2-bis(2-aminophenoxy)ethane- N,N,N,,N,-tetraacetic acid (BAPTA) has been widely used as a probe to test the role of calcium in a large variety of cell functions. Here we show that in most cell types BAPTA has a potent actin and microtubule depolymerizing activity and that this activity is completely independent of Ca2+ chelation. Thus, the depolymerizing effect of BAPTA is shared by a derivative (D-BAPTA) showing a dramatically reduced calcium chelating activity. Because the extraordinary depolymerizing activity of BAPTA could be due to a general depletion of cell fuel molecules such as ATP, we tested the effects of BAPTA on cellular ATP levels and on mitochondrial function. We find that BAPTA depletes ATP pools and affects mitochondrial respiration in vitro as well as mitochondrial shape and distribution in cells. However, these effects are unrelated to the Ca2+ chelating properties of BAPTA and do not account for the depolymerizing effect of BAPTA on the cell cytoskeleton. We propose that D-BAPTA should be systematically introduced in calcium signalling experiments, as controls for the known and unknown calcium independent effects of BAPTA. Additionally, the concomitant depolymerizing effect of BAPTA on both tubulin and actin assemblies is intriguing and may lead to the identification of a new control mechanism for cytoskeleton assembly. [source]

Antioxidant activities of red pepper (Capsicum annuum) pericarp and seed extracts

INTERNATIONAL JOURNAL OF FOOD SCIENCE & TECHNOLOGY, Issue 10 2008
Ki Hyeon Sim
Summary In this study, we examined the antioxidant activities of red pepper (Capsicum annuum, L.) pericarp and red pepper seed extracts. The extracts were evaluated by various antioxidant assays, including 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, superoxide anion radical scavenging, hydroxyl radical scavenging, [2,2,-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid)] (ABTS) radical scavenging, ferrous chelating activity, superoxide dismutase (SOD) activity and reducing power, along with the determination of total phenolic and flavonoid contents. All the extracts showed strong antioxidant activity by the testing methods. The red pepper pericarp extract exhibited strong ferrous chelating activity and high scavenging activity against free radicals, including both the hydroxyl and DPPH radicals, but it exhibited weaker scavenging activity for the superoxide anion radical and for SOD. In contrast, the red pepper seed extract exhibited strong SOD activity and high scavenging activity against the superoxide anion radical, but showed weaker ferrous chelating activity, hydroxyl radical scavenging, and DPPH radical scavenging. We observed that the reducing power level and ABTS radical scavenging activity of the red pepper seed were higher than those of the red pepper pericarp at the highest tested concentration. Most of the test results for the red pepper seed and red pepper pericarp extracts increased markedly with increasing concentration; however, the metal chelating, SOD and ABTS radical scavenging activities did not increase with the concentration. Highest total phenolic and flavonoid contents were obtained from the red pepper pericarp extracts. Overall, the red pepper seed and red pepper pericarp extracts were highly effective for the antioxidant properties assayed, with the exceptions of ferrous chelating activity, hydroxyl radical scavenging and SOD activity. [source]

GRAPE SEED PROANTHOCYANIDIN EXTRACT CHELATES IRON AND ATTENUATES THE TOXIC EFFECTS OF 6-HYDROXYDOPAMINE: IMPLICATIONS FOR PARKINSON'S DISEASE

JOURNAL OF FOOD BIOCHEMISTRY, Issue 2 2010
TZU-HUA WU
ABSTRACT Proanthocyanidins are potent antioxidants associated with protection against diseases. We tested the reducing capacity, iron chelating activity, and anti-auto-oxidation ability of grape seed proanthocyanidin extract (GSPE). The mechanisms underlying GSPE attenuation of oxidative processes induced by 6-hydroxydopamine (6-OHDA), a neurotoxin used to induce Parkinson's disease, were investigated in cell-based systems. At high concentrations, GSPE (50 µg/µL) was a mild pro-oxidant in a Fenton-type reaction. GSPE (300 µg/mL) was as potent as 30 µM deferoxamine in its iron-chelating capacity, and as efficient as 5 mM ascorbic acid in delaying 6-OHDA auto-oxidation. In PC-12 cell cultures, 100 and 300 µg/mL GSPE significantly protected (P < 0.05) cells from 6-OHDA-induced (400 µM) toxicity. GSPE-induced cytoprotection is enhanced by a nitric oxide synthase inhibitor (NOSI), implying that the cytoprotective effect of GSPE does not require NOS activation. In conclusion, the iron-chelating activity of GSPE minimizes its pro-oxidant activity and delays 6-OHDA auto-oxidation to provide cytoprotection. PRACTICAL APPLICATIONS Parkinson's disease is a neurodegenerative disorder characterized by the degeneration of dopaminergic neurons. The recognized pharmacological strategies to prevent or treat Parkinson's disease include the minimization of oxidative stress, iron release and excitotoxicity resulting from excess nitric oxide formation. One of the best ways to delay or prevent the onset of the disease is to improve the biological antioxidant status by providing additional radical scavengers that are not pro-oxidants. The pro-oxidant activity, such as that of the antioxidant ascorbic acid, enhances radical cycling under certain conditions, and therefore may be detrimental. Grape seed proanthocyanidin extracts (GSPEs) are used as a dietary supplement in food products in several countries. Our current report provides evidence that GSPE has limited pro-oxidant activity, presumably because of its iron-chelating abilities, and protects cells from neurotoxic insults. GSPE may be effective as a dietary supplement for prophylactic use against the progressive neurodegeneration seen in Parkinson's disease. [source]

Antiparkinson drug , Mucuna pruriens shows antioxidant and metal chelating activity

PHYTOTHERAPY RESEARCH, Issue 1 2008
Muralikrishnan Dhanasekaran
Abstract Parkinson's disease is a neurodegenerative disorder for which no neurorestorative therapeutic treatment is currently available. Oxidative stress plays an important role in the pathophysiology of Parkinson's disease. The ancient Indian medical system, Ayurveda, traditionally uses Mucuna pruriens to treat Parkinson's disease. In our earlier studies, Mucuna pruriens has been shown to possess antiparkinson and neuroprotective effects in animal models of Parkinson's disease. The antioxidant activity of Mucuna pruriens was demonstrated by its ability to scavenge DPPH radicals, ABTS radicals and reactive oxygen species. Mucuna pruriens significantly inhibited the oxidation of lipids and deoxyribose sugar. Mucuna pruriens exhibited divalent iron chelating activity and did not show any genotoxic/mutagenic effect on the plasmid DNA. These results suggest that the neuroprotective and neurorestorative effect of Mucuna pruriens may be related to its antioxidant activity independent of the symptomatic effect. In addition, the drug appears to be therapeutically safe in the treatment of patients with Parkinson's disease. Copyright © 2007 John Wiley & Sons, Ltd. [source]

Reduction of oxidative changes in human spermatozoa by exogenous gangliosides

ANDROLOGIA, Issue 1 2005
M. Gavella
Summary The effect of exogenous gangliosides, the sialic acid-containing glycosphingolipids, on oxidative changes in human spermatozoa was investigated. The incorporation of disialogangliosides or trisialogangliosides (GD1b and GT1b, respectively) into the iron/ascorbate promoter system for induction of lipid peroxidation decreased the release of malondialdehyde (MDA) from peroxidizing spermatozoa. The application of monosialogangliosides and disialogangliosides (GM1 and GD1a, respectively) did not have any effect under identical experimental conditions. GT1b, at a micromolar concentration, significantly inhibited the production of MDA, a breakdown product of lipid peroxide decomposition in spermatozoa of normozoospermic infertile men (P < 0.001; n = 51). An enhanced generation of MDA exhibited by the sperm population from the low-density Percoll fraction containing defective and/or immature spermatozoa was significantly reduced in the presence of GT1b. These results and the experiments on the influence of iron-chelating agent ethylenediamine tetraacetic acid (EDTA) as well as ferrous ion concentration itself on lipid peroxidation support the hypothesis that the protective effect of ganglioside against MDA generation could be the result of its chelating activity. Furthermore, superoxide anion release of phorbol myristate acetate-stimulated spermatozoa was significantly reduced in the presence of 50 and 100 ,mol l,1 GD1b (P < 0.05) and GT1b (P < 0.005). The inhibitory effect of 100 ,mol l,1 GT1b on spermatozoa from infertile normozoospermic men was statistically significant (P < 0.001; n = 21) and did not depend on the initial superoxide anion production. In conclusion, the protective action of GD1b and GT1b could be related to both scavenging of free radicals and metal-chelating properties, which might have relevance in the protection against oxidation-induced processes in human spermatozoa. [source]

Hepatoprotective Activity of Polyherbal Formulation (Normeta®) in Oxidative Stress Induced by Alcohol, Polyunsaturated Fatty Acids and Iron in Rats

BASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 3 2009
Shilpa N. Patere
The present study was carried out to evaluate the effects of oral treatment with polyherbal formulation Normeta® (2 ml and 4 ml/kg) on hepatic damage induced by alcohol 10,30% (blood alcohol was maintained at levels between 150 and 350 mg/dl), thermally oxidized oil (polyunsaturated fatty acids) (15% of diet) and carbonyl iron (1.5,2% of diet) for 30 days in rats. In vitro studies with 1, 1-Diphenyl, 2-Picrylhydrazyl (DPPH), Nitric oxide and Ferric chloride (Fe+3 ions) showed that Normeta® possesses antioxidant and metal chelating activity. Alcohol, polyunsaturated fatty acids and iron feeding produced an increase in serum levels of iron, serum glutamate pyruvate transaminase and decrease in serum proteins. It was also associated with elevated lipid peroxidation (thiobarbituric acid reactive substances) and disruption of antioxidant defence mechanism in liver, decreased body weight and increased liver to body weight ratio. Oral administration of Normeta® along with alcohol, polyunsaturated fatty acids and iron decreased the serum iron, serum glutamate pyruvate transaminase levels and increased serum protein levels. The levels of liver thiobarbituric acid reactive substances were decreased and the activities of antioxidant enzymes superoxide dismutase and catalase were increased. Improvement in body weight and liver to body weight ratio was also observed. The effects of Normeta® on physico-metabolic parameters were comparable with silymarin. This indicates that Normeta® has favourable effect in bringing down the severity of hepatotoxicity. [source]