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Mitochondial Uncoupler, 2,4-Dinitrofon, уменьшает парализ спинальной коры и потерю ячеек сетчатки в экспериментальной аутоиммунной модели склероза.

Оптический неврит является воспалительным демиелинизирующим заболеванием зрительного нерва, которое часто встречается у пациентов с множественным склерозом (MS). Шестьдесят процентов пациентов имеют определенный уровень постоянной потери зрения из-за повреждения ячеек сетчатки после оптического неврата, при этом не известно, каким образом они могли бы предотвратить эту потерю. Проведенные ранее исследования показали, что MP201 - лекарство в виде 2,4 динозема (DNP), применяемое в экспериментальной модели мышью аутоиммунного энцефалита (EAE) MS-смягченного оптического невралита с сохранением зре

Совпадение в аннотации оригинала
Optic neuritis is an inflammatory demyelinating disease of the optic nerve that often occurs in multiple sclerosis (MS) patients. Sixty perc … uritis, with no known treatment to prevent this loss. Prior studies showed that MP201, a prodrug of 2,4-dinitrophenol (DNP) administered in the experimental autoimmune encephalitis (EAE) mouse model of MS attenuated optic neuritis with preserved vision, increased retinal ganglion cell (RGC) survival, decreased axon loss, and reduced demyelination. Oral administrati …

Effects of 2,4-dinitrophenol amylobarbitone and certain other drugs on the rate of oxygen consumption and force of contraction of isolated curarized diaphragm muscle of the rat.

1 A technique has been developed for studying over periods of 10 min or longer the effects of drugs on both the force of electrically-induced contractions and the oxygen consumption of an isolated, curarized, mammalian, skeletal muscle preparation.2 The resting oxygen consumption of the muscle was increased substantially by 2,4-dinitrophenol in concentrations (0.02 mM and higher) that eventually produced contracture. Two other uncoupling agents, 4,6-dinitro-o-cresol and carbonylcyanide-p-trifluoromethoxyphenylhydrazone, behaved similarly.3 The oxygen consumption over 10 min of the stimulated m…

In vitro synthesis of 1,N6-etheno-2'-deoxyadenosine and 1,N2-etheno-2'-deoxyguanosine by 2,4-dinitrophenol and 1,3-dinitropyrene in presence of a bacterial nitroreductase.

The formation of covalent nitro-PAH DNA adducts and nitro-PAH mediated oxidative lesions are two possible mechanisms for the initiation of nitro-PAH carcinogenesis. Sixty-minute incubation of 1,3-dinitropyrene (100 microM) or 1,4-dinitrophenol (100 microM) with a mixture of 150 microM NADH, 0.5 units of E. coli nitroreductase, 100 microM linoleic acid, 0.5 mM ferrous iron, and 100 microM 2'-deoxyadenosine (2'-dA) or 100 microM 2'-deoxyguanosine (2'-dG) were analyzed by liquid chromatography multistage mass spectrometry. Mixtures of 1,N(6)-etheno-2'-deoxyadenosine (epsilondA) plus 4-oxo-2-nonen

Mitochondrial uncoupler 2,4-dinitrophenol (DNP) confers protection from the acute effect of ionizing radiation by regulating redox homeostasis in radio-sensitive organs of C57BL/6 mice.

PURPOSE: The development of radiation countermeasures is an unmet need. Several cytoprotective approaches have been demonstrated to minimize ionizing radiation-induced tissue toxicity. Previously, our research indicated that mild mitochondrial uncoupling by 2,4-dinitrophenol (DNP) potentially counteract the IR-induced cell death. Herein, our investigation delves into the radio-protective efficacy of DNP following total-body irradiation (TBI) in C57BL/6 mice. METHOD: DNP was administered orally 2 h prior to TBI (7.6 Gy gamma (γ)-radiation) as a prophylactic approach against acute radiation syn…

Effect of organic toxicants on the activity of denitrifying granular sludge.

Denitrification plays a key role in the biological nitrogen removal from the wastewater using granular sludge as the integral part of a high-rate denitrification technology. It is helpful to evaluate the effect of typical organic toxicants on the activity of denitrifying granular sludge for the application of denitrification technology. In this study, four typical organic toxicants, namely, penicillin, chloramphenicol, 2,4-dinitrophenol and polymyxin B sulphate were used to assess the effect of organic toxicants on the activity of denitrifying granular sludge. The results of individual toxicit…

Halide salts induced the photodegradation of a fat-burning compound 2, 4-dinitrophenol by iron-montmorillonite.

Natural montmorillonite clay and anthropogenic organic pollutants frequently coexist in the estuarine environment where freshwater from rivers mixes with saltwater from the ocean. In this environment, the sharply changed aqueous chemistry especially salt content could significantly alter the photochemical behaviors of pollutants. However, this process was rarely investigated. In this study, the photodegradation of a representative anthropogenic weight-loss compound 2,4-dinitrophenol in the presence of Fe3+-montmorillonite and different halide salts was systematically investigated. Results show…

Quenching of tryptophan fluorescence in the presence of 2,4-DNP, 2,6-DNP, 2,4-DNA and DNOC and their mechanism of toxicity.

Although they are widely used as insecticides, acaricides and fungicides in the agriculture or as raw materials in the dye industry, dinitro … ir toxicity. Fluorescence quenching of tryptophan was tested using different dinitrophenols such as 2,4-dinitrophenol (2,4-DNP), 4,6-dinitro-orthocresol (DNOC), 2-[(2,4-dinitrophenyl)amino]acetic acid (GlyDNP), 2-(1-methyl-heptyl)-4.6-dinitrophenyl crotonate (Karathan), 2-amino-5-[(1-((carboxymethyl)amino)-3-((2,4-dinitrophenyl)thio)-1-oxopropan-2-yl)amino]-5-oxope …

Side reactions in peptide synthesis. IX. Suppression of the formation of aminosuccinyl peptides with additives.

The base-catalyzed ring closure of beta-benzylaspartyl peptides was efficiently suppressed by the addition of phenols (with electron-withdrawing substituents) to the reaction mixtures. From a series of compounds tested, 2,4-dinitrophenol and pentachlorophenol were the most effective. No direct relationship was found between the acidity of the additives and their ability to suppress the formation of aminosuccinyl peptides. The applicability of 2,4-dinitrophenol and pentachlorophenol in practical syntheses was also examined.

Glucose transport in Salmonella typhimurium and Escherichia coli.

We have investigated the claim by Schweiger and coworkers [Eur. J. Biochem. 102(1979)231-236] that glucose transport in Escherichia coli is catalyzed mainly by an ATP-dependent transport system instead of the phosphoenolpyruvate:sugar phosphotransferase system. A major argument was the differential effect of 2,4-dinitrophenol on glucose uptake and the transport of its non-metabolizable analogue, methyl alpha-glucoside. Whereas the first was inhibited, the second was stimulated. When subsequent glucose metabolism is prevented by introducing mutations that eliminate glucose 6-phosphate metabolis…

Biodegradation of the pesticide 4,6-dinitro-ortho-cresol by microorganisms in batch cultures and in fixed-bed column reactors.

A mixed culture of microorganisms able to utilize 4,6-dinitro-ortho-cresol (DNOC) as the sole source of carbon, nitrogen and energy was isolated from soil contaminated with pesticides and from activated sludge. DNOC was decomposed aerobically in batch cultures as well as in fixed-bed column reactors. Between 65% and 84% of the substrate nitrogen was released as nitrate into the medium, and 61% of the carbon from uniformly 14C-labelled DNOC was recovered as 14CO2. The mixed microbial culture also decomposed 4-nitrophenol and 2,4-dinitrophenol but not 2,3-dinitrophenol, 2,6-dinitrophenol, 2,4-di…

Degradation of 2-sec-butyl-4,6-dinitrophenol (dinoseb) by Clostridium bifermentans KMR-1.

A strain of Clostridium bifermentans, KMR-1, degraded 2-sec-butyl-4,6-dinitrophenol (dinoseb) to a level below the limit of detection by high-performance liquid chromatography (0.5 mg/liter) within 96 h, with no accumulation of aromatic intermediates. KMR-1 could not utilize dinoseb as a sole carbon or energy source, and degradation occurred via cometabolism in the presence of a fermentable carbon source. KMR-1 mineralized some dinoseb in anaerobic cultures, evolving 7.2% of the radioactive label in U-ring 14C-labeled dinoseb as 14CO2. The remaining anaerobic degradation products were incubate

Dinitrophenol poisoning: a diagnosis to consider in undiagnosed fever.

A 32-year-old farmer had signs and symptoms of dinitrophenol poisoning after crop spraying with a herbicide containing derivatives of 2,4-dinitrophenol. Dinitrophenol causes toxicity by the uncoupling of oxidative phosphorylation in the mitochondria of cells throughout the body. In man the classic syndrome consists of lassitude, malaise, headache, increased perspiration, thirst, and dyspnea which may progress to hyperpyrexia, profound weight loss, respiratory failure, and death. Because dinitrophenol compounds are widely used, it is likely that some patients with unexplained fever have unrecog…

Effect of uncoupler on "downhill" substrate efflux of Escherichia coli is dependent on (Mg2+, Ca2+). Adenosine triphosphatase.

Previous studies have shown that mutations in the unc gene of Escherichia coli K12 cause defects in energy transduction as well as a membrane-bound (Mg2+, Ca2+)-adenosine triphosphatase. We studied the effect of this mutation on the "downhill" efflux of methyl-beta-D-galactopyranoside, a suboli K12 did not show significant differences in substrate influx of efflux, a differential effect of an uncoupler, 2,4-dinitrophenol was demonstrated. In contrast to the unc+, dinitrophenol failed to inhibit significantly the rate coefficient of efflux in the unc- strain. Analysis of spontaneous unc+ revert…

Influence of chromium on some physiological variables of Anabaena doliolum: interaction with metabolic inhibitors.

The impact of 2,4-dinitrophenol and chlorophenyl dimethylurea on ATP content, carbon fixation, O2 evolution, nitrogenase activity and Cr uptake of Anabaena doliolum has been studied. 2,4-Dinitrophenol has been found to be more toxic than chlorophenyldimethylurea for all these processes. However, when Cr toxicity to above variables was assessed in their presence the interaction was less than additive. An initial (10-15 min) concentration-dependent rapid Cr uptake, followed by a slow one, indicates a biphasic uptake. A significant inhibition of Cr uptake in the presence of both these metabolic i…

Bivascular liver perfusion in the anterograde and retrograde modes: zonation of the response to inhibitors of oxidative phosphorylation.

The action of cyanide (500 microM), 2,4-dinitrophenol (50 microM) and atractyloside (100 microM) on glycogen catabolism and oxygen uptake was investigated in the bivascularly perfused liver of fed rats. Cyanide, 2,4-dinitrophenol and attractyloside were infused at identical rates into the hepatic artery in either the anterograde or retrograde perfusion. The accessible aqueous cell spaces were determined by means of the multiple-indicator dilution technique. Glucose release, oxygen uptake and glycolysis were measured as metabolic parameters. Oxygen uptake changes per unit cell space caused by a…

2,4-Dichlorophenoxyacetic acid influx is mediated by an active transport system in Chinese hamster ovary cells.

The influx of 2,4-dichlorophenoxyacetic acid (2,4-D) into Chinese hamster ovary (CHO) cells was studied. The cells mainly took up but did not metabolize the undissociated form of the herbicide. The uptake of 2,4-D was carried out against a concentration gradient and was inhibited by sodium azide and dinitrophenol. The results presented here show that the herbicide influx was an active, energy dependent process. (Na+ + K+)ATPase does not seem to be involved because ouabain, an inhibitor of the enzyme, did not affect the 2,4-D uptake.

Blockade of adenosine triphosphate-sensitive potassium channels by thiamylal in rat ventricular myocytes.

BACKGROUND: The adenosine triphosphate (ATP)-sensitive potassium (KATP) channels protect myocytes during ischemia and reperfusion. This stud … onfiguration, KATP channel currents were assessed before and during activation of these channels by 2,4-dinitrophenol and after administration of 25, 50, and 100 mg/l thiamylal. The open probability was determined from current-amplitude histograms. In the inside-out configuration, the current-voltage relation was obtained before and after the application of thiamyl …