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Antimicrobial activities of N-chloramines and diazolidinyl urea.

A combination of MICs of an N-chloramine, a simple chlorinated amino acid, and diazolidinyl urea gave synergistic activity against bacteria, but not fungi. The two compounds at a higher concentration, 0.1 and 0.3%, respectively, gave synergistic inhibition of fungi; kill times were 1 h for Trichophyton tonsurans, 3 h for Aspergillus niger and Fusarium moniliforme, and 6 h for Aspergillus fumigatus.

Anti-Infective Agents, Local↗

Bacterial nitrification in chloraminated water supplies.

Nitrifying bacteria were detected in 64% of samples collected from five chloraminated water supplies in South Australia and in 20.7% of samples that contained more than 5.0 mg of monochloramine per liter. Laboratory experiments confirmed that nitrifying bacteria are relatively resistant to the disinfectant. Increased numbers of the bacteria were associated with accelerated decays of monochloramine within distribution systems. The combination of increased concentrations of oxidized nitrogen with decreased total chlorine residuals can be used as a rapid indicator of bacterial nitrification.

Chloramines↗

Hypochlorous acid and chloramines increase endothelial permeability: possible involvement of cellular zinc.

The migration of neutrophils through the endothelium at sites of inflammation may be facilitated by oxidant-mediated disruption of cellular junctions. The present study examined the effects of noncytotoxic concentrations of the membrane-penetrating neutrophil oxidants hypochlorous acid (HOCI) and monochloramine (NH2Cl), or the membrane-impermeant taurine chloramine (taurine NCl), on cultured bovine aorta endothelial monolayers. HOCl (25 microM) or NH2Cl (10 microM), but not taurine NCl (100 microM), caused a reversible shortening of the cytoskeletal actin microfilaments, cell retraction, and increased permeability within 2 min. These effects were accompanied by an increase in intracellular zinc concentration as well as the oxidation of intracellular glutathione and protein sulfhydryls. The zinc ionophore pyrithione also increased permeability. HOCl or NH2Cl, but not taurine NCl, also rapidly increased microvascular permeability in isolated perfused rat lungs. The data suggest that HOCl and NH2Cl can increase endothelial permeability by causing very rapid cytoskeletal shortening and cell retraction, possibly as a result of the oxidation of intracellular sulfhydryls and mobilization of zinc.

Actin Cytoskeleton↗

Comparison of Bolton-Hunter and chloramine-T techniques for the radioiodination of prostatic acid phosphatase.

A double antibody, semi-automated radioimmunoassay for serum prostatic acid phosphatase (PAP) is described, which uses the 125I-labelled N-succinimidyl-3-(4-hydroxyphenyl) propionate ester of PAP. This type of label has substantially higher immunoreactivity than that prepared using the chloramine-T method of radioiodination. Chromatographic purification of either label on Ultrogel ACA44 further improved immunoreactivity. The lowest detection limit (0 . 35 micrograms/l) was achieved with the chromatographically purified ester label.

Acid Phosphatase↗

Iodination of mono- and heteroclonal immunoglobulin G with lactoperoxidase and chloramine T.

The difference in the reactivity of tyrosine and histidine residues in mono- and heteroclonal IgG protein toward enzyme catalyzed and chemical iodination has been studied. One heteroclonal and four monoclonal IgG proteins were iodinated using lactoperoxidase or chloramine T. The ratio of the degrees of substitution of the light and the heavy chains varied from IgG to IgG. One of the monoclonal IgG proteins, IgG-Dam, could only be modified in the gamma-chain. The lack of reactivity was attributed to steric hindrance and other local peculiarities. This interpretation is supported by spectrophotometric titration studies.

Amino Acids↗

A highly sensitive spectrophotometric method for the determination of some phenothiazine antipsychotics using chloramine-T and indigocarmine.

A new simple, accurate and precise spectrophotometric method for the determination of six phenothiazine drugs in pure form and in dosage forms is described. The method is based on the oxidation of the studied drugs by a known excess of Chloramine-T in hydrochloric acid medium and subsequent determination of the unreacted oxidant by reacting it with indigocarmine in the same acid medium. The reacted oxidant corresponds to the drug content. The colored species exhibits maximum absorption at 610 nm. The apparent molar absorptivity values and Sandell sensitivity values are in the range 1.53 x 10(4)-2.96 x 10(4) l mol-1 cm-1 and 13.75-37.15 ng cm-2, respectively. The method is highly sensitive and suitable for 1-15 micrograms ml-1 concentrations with the detection limits being in the range, 0.0651-0.1724 microgram ml-1. The method was successfully applied to the studied drugs in their dosage forms. The results are reproducible within +/- 1% and compare favorably with those obtained by the procedures of the British Pharmacopeia.

Antipsychotic Agents↗

The effect of the oxidizing agents chloramine-T and cigarette smoke on dog serum proteinase inhibitor(s).

Dog serum treated with the oxidant chloramine-T is rapidly and selectively depleted of its ability to inhibit porcine pancreatic elastase or dog neutrophil elastase. Trypsin inhibitory capacity of serum is not affected. Purified dog alpha-1-proteinase inhibitor (alpha-1-PI) is similarly oxidized with an apparent rate constant of 1.1 x 10(3) M-1 sec-1. Reversal of the oxidative inactivation using dithiothreitol was demonstrated. Cigarette smoke also directly affects the inhibitory capacity of both serum and pure alpha-1-PI. These studies form a basis for developing a model of functionally deficient alpha-1-PI by taking advantage of oxidative inactivation of normal proteinase inhibitor levels.

Animals↗

Heinz-body haemolysis in haemodialysed patients caused by chloramines in Sydney tap water.

In August 1981, there was an outbreak of Heinz-body-positive haemolytic anaemia among patients who were undergoing dialysis in Sydney Hospital. This appeared to be due to excessive chloramines in and inadequate carbon filtration of, the water used for haemodialysis. After improvement of the carbon filtration system, there have been no further cases of anaemia.

Anemia, Hemolytic↗

[The subcellular mechanisms of the action of disinfectants. The effect of iodine and chloramine-B on bacterial ribosomes].

The composition of ribosomal material in bacterial cells of 5 families, subjected to the minimal bactericidal action of iodine and chloramine-B, was studied with the use of electrophoresis in polyacrylamide gel. The study demonstrated that under these conditions protein-synthesizing organelles of vibrios and bifidobacteria did not undergo perceptible changes, while Escherichia, Pseudomonas and bacilli essential ribosomal degradation was found to occur, which was manifested by a decrease in the intensity of bands 23S and 16S of ribosomal RNA. The conclusion was made that the in vivo destruction of ribosomes was not the direct result of the action of disinfectants, but mediated by some cellular mechanisms.

Chloramines↗

[Peculiarities of the development of chloramine induced pulmonary edema in rabbits in various age periods].

Rabbits under three weeks of age were found to be less tolerant to chloramine (CA) than adult rabbits. For them the lethal dose of CA was 40--50 mg/kg. They perished from intoxication with the symptoms of protracted collapse without any manifestations of edema. For older rabbits the lethal dose of CA was 60--70 mg/kg. Death occurred with phenomena of acute and sharp edema of the lungs. In young rabbits atypical edema of the lungs occurred only with the administration of very high doses of CA--200--250 mg/kg. Edematous fluid is present in small amount only; there is a prevalence of hemorrhage, this being possibly caused by a direct alterating action of the CA excreted through the lungs on the walls of the arterioles and capillaries of the vascular system of the lungs.

Age Factors↗

Satisfactory radioiodination of rabbit fibrinogen using chloramine-T.

A method for radioiodination of fibrinogen using chloramine-T is described. Samples of greater than 90 per cent clottable counts were obtained. Electrophoretic mobility and immunodiffusion showed that the entire radioactivity was present in the fibrinogen band. In vivo studies on the turnover of this labeled product in rabbits showed a half-life of 52.8 to 61.7 hours in two batches of animals. The results compare very well with the reported results obtained from fibrinogen labeled with radioactive iodine by the iodine-monochloride method. The advantages of the new method are indicated.

Animals↗

[Determination of trace iodine based on kinetic-spectrophotometry with malachite green-chloramine T system].

In this paper, a new kinetic-spectrophotometric method for the determination of trace amount of iodine has been proposed. It is based on the iodine catalysed the reaction of malachite green oxidized by chloramine T in hydrochloric acid medium. The method is sensitive, simple and with good selectivity. The linear range of determination of iodine is 0-48 micrograms.L-1, the detection limit is 4.9 x 10(-10) g.mL-1. The method has been used for the determination of trace amount of iodine in food with satisfactory results.

Chloramines↗

Some properties of sodium channels in neuroblastoma cells modified with scorpion toxin and chloramine-T. Single channel measurements.

Currents through sodium channels of neuroblastoma cells were measured using patch technique in outside-out configuration. Scorpion toxin (ScTX) produced 3 to 4 fold prolongation of mean open time and increased number of reopenings. The mean open times showed slow fluctuations around some average values. The distribution of channel open times for ScTX-modified channels required more than one exponential to be fitted. Chloramine-T (ChT) produced qualitatively similar, though weaker, prolongation of open times.

Animals↗

Effect of chloramine-T and N-bromsuccinimide on intracellular and extracellular action potentials from unmyelinated axons.

The change in intracellular (ICAPs) and extracellular (ECAPs) potentials of unmyelinated axons of Lumbricus terrestris under the effect of Chloramine-T (CT) and N-Bromsuccinimide (NBS), applied extracellularly, is studied. Delay of the repolarization phase of ICAPs was found under the effect of NBS, as well as slight decrease of the amplitude of ICAPs and ECAPs, with an insignificant decrease in the propagation velocity of the excitation. The first (V') and second (V") time derivatives and the total ionic current (Ii) are calculated from the intracellular action potential in norm and under the effect of NBS. A delay of the inactivation phase of the inward sodium current and a decrease of the amplitude of the total ionic current, calculated from ICAP, were found. Under the effect of CT there was a decrease in the amplitude of the action potentials, without a delay in the repolarization phase and the propagation velocity of the excitation decreases. CT leads to lasting inhibition of the excitability of the axon under prolonged impact (20 min).

Action Potentials↗

Use-dependent blockade of sodium channels by local anaesthetics and antiarrhythmic drugs. Effects of chloramine-T and calcium ions.

Voltage clamp studies were carried out of the effects of chloramine-T(CT) and external Ca++ on the blocking interactions of local anaesthetics (LAs) and antiarrhythmic drugs (lidocaine, tetracaine, N-propyl ajmaline, compound KC 3791) with Na+ channels in frog Ranvier nodes. The results obtained provided direct evidence for the notion that: LAs interact preferentially with inactivated Na+ channels and stabilize their inactivated conformation ("drug-induced slow inactivation": SI); and SI underlies the cumulative inhibition of INa during repetitive membrane stimulation. Normal inactivation is not indispensable, but plays an auxiliary role in the mechanism of cumulative inhibition of INa by drugs interacting with open Na+ channels. This block results mainly from accumulation of the channels in the resting blocked state (due to the inability of charged drugs to leave the channel via a "hydrophobic pathway"). The contribution of the blockade-inactivated state to this type of block may depend on some properties of the drug and the holding membrane potential. The problem of the location of the binding site responsible for LA-induced SI requires further investigation in view of the fact that in the myocardium, along with LA, the lipid-insoluble tetrodotoxin (TTX) induces a pronounced SI.

Amines↗