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Cromolyn sodium in seasonal allergic conjunctivitis.

A formulation of 2% cromolyn sodium (CS) ophthalmic solution without the preservative, 2-phenylethanol, was compared with placebo in 58 patients with seasonal allergic conjunctivitis. Selection was based on history and positive skin tests. Neither immunotherapy nor use of antihistamines was allowed. This study was double-blinded and stratified by RAST scores to assure comparable groups. Either CS or placebo was used six times daily. Patients were observed weekly for 5 weeks during the peak of the fall weed-pollen exposure. Nasal symptoms were treated as required with beclomethasone nasal spray, and uncontrolled ocular symptoms were treated with boric acid and ephedrine solution. Nasal and ocular symptoms were recorded. There was a significant suppression of eye symptoms in the group receiving CS ophthalmic solution (p less than 0.02) during weeks 2, 4, and 5. There was a trend for nasal symptoms and the requirement for nasal beclomethasone to be less in patients receiving CS.

Adolescent↗

Borate and molybdate inhibition of catechol estrogen and pyrocatechol methylation by catechol-O-methyltransferase.

The possibility that boron and molybdenum anions can influence sex steroid metabolism by forming complexes with catechol estrogens has been studied in vitro. The formation of 2-methoxyestrone (2-OHE1 2-Me) from 2-hydroxyestrone (2-OHE1) by catechol-O-methyltransferase (COMT) was followed by measuring the transfer of the radiolabeled methyl group from S-adenosylmethionine. In the presence of both sodium tetraborate and sodium molybdate using a phosphate buffer medium, the formation of 2-OHE1 2-Me decreased as the anion:2-OHE1 molar ratio was increased. However, the reverse effect was observed when using a tris buffer medium and further investigation showed that phosphate and sulphate also enhanced COMT activity in a tris buffer medium. Boric acid affinity medium, used as a substitute for borate salt, also showed a negative relationship with enzyme activity in a phosphate buffer medium, and inhibition of methylation was more marked than with the free anion. Erythrocytes contain appreciable amounts of COMT, which is mostly responsible for the rapid O-methylation of catechol estrogens in blood. The methylation of a simple catechol compound, 1,2-dihydroxybenzene (pyrocatechol) was therefore studied using rat red blood cell lysates. Methylation was inhibited in a concentration-related manner by borate, as found in the studies of 2-OHE1. It is possible that high dietary intakes of boron or molybdenum could regulate the rate of catabolism, or even the metabolic fate of the major estrogens.

Animals↗

Improved separation of modified nucleosides from tRNA hydrolysates: the patterns of tRNA methylation in rat tissues.

A sensitive and reproducible method for the isolation of minor nucleosides derived from tRNA is described. The nucleosides obtained from enzymatic digestion of tRNA are separated into several groups using a QAE Sephadex column and increasing concentrations of boric acid in a step-wise manner. The nucleosides in each group are separated by isocratic elution from a preparative Partisil 10-SCX column and high-performance liquid chromatography at ambient temperature. With this method we have determined the patterns of tRNA methylation in vitro with extracts from rat bone, liver, kidney and adrenal glands. Although different tissues appear to contain the same tRNA methyltransferases, the patterns of methylated nucleosides are different.

Adrenal Glands↗

Inhibition of staphylococcal alpha-toxin by covalent modification of an arginine residue.

The effects of 1,2-cyclohexanedione and phenylglyoxal on staphylococcal alpha-toxin were studied. Modification of one arginine residue in alpha-toxin was sufficient to render the toxin nonhemolytic with no conformational change. Modified alpha-toxin did not protect cells from hemolysis by native alpha-toxin. An arginine residue is therefore at or near the binding site of alpha-toxin. Trypsin digestion of modified alpha-toxin generated a 20 kDa fragment which was isolated using a boric acid gel column. Upon regeneration, this 20 kDa fragment was not recognized by a population of antibodies which prevented alpha-toxin binding. The fragment was recognized by antibodies directed against post-binding events. However, the antibinding antibodies recognized the intact modified toxin. This leads us to conclude that antibinding determinants are not found directly in the binding site or are conformationally masked.

Animals↗

Separation and sensitive determination of i-urobilin and 1-stercobilin by high-performance liquid chromatography with fluorimetric detection.

i-Urobilin and 1-stercobilin were separated by high-performance liquid chromatography on a reversed-phase octadecylsilane-bonded column and detected fluorimetrically through formation of phosphor with zinc ions in the eluent. The separation and the intensity of the fluorescence response were affected by concentrations of zinc acetate and sodium borate buffer, pH and methanol content in the eluent. The optimal eluent used consisted of 0.1% zinc acetate in 75 mM boric acid buffer (pH 6.0)-methanol (25:75). The detection limit was 0.2 microgram/l for both i-urobilin and 1-stercobilin (signal-to-noise ratio 2), which makes the method 250-2500 times more sensitive than conventional methods.

Bile Pigments↗

Separation of serum bilirubin species by micellar electrokinetic chromatography with direct sample injection.

Four major bilirubin species in serum were separated by micellar electrokinetic chromatography with 25 mM sodium dodecyl sulfate (SDS) and 20 mM sodium tetraborate-boric acid buffer at pH 8.5. Due to the solubilization of the serum proteins by the SDS micelles, serum samples were injected directly into a 50 cm x 75 microns I.D. fused-silica capillary and complete separation of the four bilirubin species was accomplished within ca. 10 min without extensive sample pretreatment. Detection was performed by absorbance at 450 nm and average limit of detection was in the 6.0 microM concentration range. The usefulness of this method was demonstrated for the separation and detection of a number of bilirubin species present in pathological human serum samples.

Animals↗

Spectrofluorimetric determination of paracetamol in pharmaceuticals and biological fluids.

A spectrofluorimetric method for the determination of paracetamol is presented, based on the oxidation of the analyte to give the fluorophore 2,2'-dihydroxy-5,5'-diacetyldiaminebiphenyl. Sodium hypochlorite was used as an oxidizing reagent and the optimum pH was found to be 10.0 (sodium carbonate-boric acid buffer solution). The linear concentration range of application was 0.1-100.0 micrograms ml-1 of paracetamol, the detection limit 0.01 micrograms ml-1 and the relative standard deviation 1.2%. The method has been satisfactorily applied to the determination of paracetamol in pharmaceutical formulations and biological fluids.

Acetaminophen↗

Endpoints of spermatotoxicity in the rat after short duration exposures to fourteen reproductive toxicants.

Multiple endpoints of spermatotoxicity in short duration tests (1-5 days exposure; 2.5-week assay interval) were investigated in a number of chemicals reported to produce minimal to severe reproductive effects when administered subchronically. Six of these chemicals (boric acid, dinoseb, 2,5-hexanedione, methoxychlor, metronidazole, ornidazole) produced substantial spermatotoxicity after 1 to 5 doses. Spermatotoxic effects of chlordimeform were equivocal while p,p'-DDT, n-hexane, and sodium chlorite were judged negative. Four chemicals with known acute effects (benomyl, busulfan, ethylene glycol monomethyl ether, nitrobenzene) elicited expected histopathologic responses after a single dose. Testicular histology, testicular sperm head counts, cauda sperm counts, sperm morphology, and sperm velocity proved to be the most toxicologically sensitive endpoints in one or more of the studies, but histopathology of the testis and epididymis was the most consistent indicator of reproductive damage. The percentage of motile sperm and sperm concentration in the epididymal fluid were the least sensitive measurements. The data suggested that most chemicals with the potential to produce moderate to severe sperm damage are detectable with a short duration test. Complementary multiple endpoints enhanced the interpretation of results, often identified cellular targets, and provided insight on possible mechanisms. Specific responses were often similar to specific effects reported for subchronic exposures. A short duration test could be of value as a screen in structure-activity studies or to set priorities for chemicals requiring further evaluation. As a supplement to breeding studies, the data generated in the short test could also be used to enhance the design and interpretation of the longer tests.

Animals↗

Mutations of a shuttle vector plasmid, pZ189, in Escherichia coli induced by boron neutron captured beam (BNCB) containing alpha-particles.

A shuttle vector, pZ189, carrying a bacterial suppressor tRNA marker gene (supF) was dissolved in Tris-EDTA buffer containing 0.3 M 10B-enriched boric acid and then irradiated with boron neutron captured beam (BNCB) produced by the nuclear reaction 10B (n,alpha) 7Li with thermal neutrons. A DNA repair-deficient mutant, KS46 (uvrA-), of Escherichia coli was transformed with the plasmid DNA, and the transformants carrying mutations on the supF gene were selected as nalidixic acid-resistant colonies. The mutation frequency (2.4 x 10(-4)) of pZ189 at the D10 dose was about 70 times greater than the spontaneous rate (3.5 x 10(-6)). The plasmid mutations were analyzed using DNA sequencers; 88% of them were base substitutions. A few minus-one frameshifts (7%) and deletions (5%) were detected. Among these base substitutions, transversions of G:C to T:A (42%) and G:C to C:G (29%) predominated. Twenty-seven percent of the base substitutions were G:C to A:T transitions; no A:T to G:C transitions were detected.

Alpha Particles↗

Boron neutron capture irradiation: setting up a clinical programme in Nice.

Neutron capture irradiation aims to selectively destroy tumor cells using 10B(n,alpha)7Li nuclear reactions produced within themselves. Following the capture reaction, an alpha particle and a, 7Li ion are emitted. Carrying an energy of 2.79 MeV, they destroy all molecular structures along their path close to 10 microns. These captures, used exclusively with a 'slow' neutron irradiation, provide a neutron capture therapy (BNCT). If they are used in addition to a fast neutron beam irradiation, they provide a neutron capture potentiation (NCP). The Centre Antoine-Lacassagne in Nice is actively involved in the European Demonstration Project for BNCT of grade IV glioblastomas (GBM) after surgical excision and BSH administration. Taking into account the preliminary results obtained in Japan, work on an 'epithermal' neutron target compatible with various cyclotron beams is in progress to facilitate further developments of this technique. For NCP, thermalized neutron yield has been measured in phantoms irradiated in the fast neutron beam of the biomedical cyclotron in Nice. A thermal peak appears after 5 cm depth in the tissues, delayed after the fast neutron peak at 1.8 cm depth. Thus, a physical overdosage of 10% may be obtained if 100 ppm of 10B are assumed in the tissues. Our results using CAL 58 GBM cell line demonstrate a dose modification factor (DMF) of 1.19 when 100 ppm of boric acid are added to the growth medium. Thus for the particles, issued from neutron capture, a biological efficiency at least twice that of fast neutrons can be derived. These results, compared with historical data on fast neutron irradiation of glioblastoma, suggest that a therapeutic window may be obtained for GBM.

Boron Neutron Capture Therapy↗

Compost biofiltration of ammonia gas from bin composting.

The effects of the manure compost/coconut peels on the ammonia removal efficiency were examined from dairy manure composting mixed with crop residues. The high rapid composting and manure compost biofiltration experiments consisted of three biofilter vessels with one composter. Dairy manure amended with rice hulls and sawdust was composted in 605 L pilot-scale composter using continuous aeration for 19 days. Three pilot-scale manure compost biofilter amended with media bed 500 mm in depth and 300 mm in diameter were built to clean ammonia emission from composter, respectively. The manure compost biofilter media in the three experimental vessels was using a 50:50 by weight mixture of manure compost and coconut peels (MC/CP). The ammonia concentrations at the inlet and outlet biofilter media were measured by boric acid traps as described by Hong et al. [Hong, J.H., Keener, H.M., Elwell, D.L., 1998. Preliminary study of the effect of continuous and intermittent aeration on composting hog manure amended with sawdust. Compost Science and Utilization 6 (3), 74-88]. Results indicated that the mixture of MC/CP performed well as a biofilter media and the ammonia removal efficiency was 100% for the filter depth of 500 mm.

Ammonia↗

Simultaneous determination of six main nucleosides and bases in natural and cultured Cordyceps by capillary electrophoresis.

A simple method is described for simultaneous determination of six main nucleosides and bases including adenine, uracil, adenosine, guanosine, uridine and inosine in Cordyceps by capillary electrophoresis (CE). Chemometric optimization based on central composite design was employed to find the optimum resolution. The optimum factor space was defined by three parameters: buffer concentration, pH and concentration of acetonitrile as organic modifier. Resolution (Rs) was employed to evaluate the response function. A running buffer composed of 500 mM boric acid, adjusted pH to 8.6 with sodium hydroxide and 12.2% acetonitrile as modifier was found to be the most appropriate for the separation. The contents of the six components were determined by using adenosine monophosphate as an internal standard. Furthermore, hierarchical clustering analysis based on characteristics of 32 peaks in CE profiles from the tested 12 samples showed that natural and cultured Cordyceps were in different clusters. Adenosine and inosine were extracted as markers for discrimination of natural Cordyceps. The result of clustering based on the two peaks characteristics was in excellent agreement with that based on 32 peaks'. Thus, adenosine and inosine could be used as markers for quality control of natural and cultured Cordyceps.

Buffers↗

Simultaneous determination of positional isomers of benzenediols by capillary zone electrophoresis with square wave amperometric detection.

A capillary zone electrophoresis method coupling square wave amperometric detection (SWAD) for the simultaneous determination of positional isomers of benzendiols (i.e. o-, m-, p-benzenediols) has been developed. Effects of several factors, such as the composition of the running buffer, the pH value, separation voltage, injection time and the potential applied to the working electrode, were investigated to acquire the optimum conditions. The efficacy of the boric acid and ascorbic acid in the running buffer were discussed. o-, m-, p-Benzendiols can be well separated within 8 min in a 50 cm length of 50 microm diameter fused-silica capillary at a separation voltage of +15 kV. Operated in a wall-jet configuration, a 100 microm Pt-disk electrode used as the working electrode exhibits good response for the analytes. The relation between peak current and analyte concentration was linear over two orders of magnitude with detection limits (S/N = 3) ranging from 0.5 to 1.5 microM for all analytes. The proposed method has been successfully applied to monitor the o-, m-, p-benzendiols contents in the environmental wastewater samples with satisfactory assay results.

Benzene Derivatives↗

Development and validation of a capillary electrophoresis method for the determination of sulfate in effervescent tablets.

A suitable capillary electrophoresis (CE) method was developed and validated for sulfate anion determination in effervescent tablets of Digedryl. The large excess of other ions in the matrix (i.e. excipients) constituted the main difficulty of this method's development. So an original analytical procedure for both the conditioning and rinsing of the capillary was purposed including a running electrolyte constituted by boric acid 20 mM and hexamethonium dibromide 0.75 mM at pH 8.00. Separation was carried out on a 60.2 cm (50 cm to the detector) x 0.75 microm i.d. fused-silica capillary at a potential of -29 kV and 35 degrees C. Indirect UV detection was performed at a wavelength of 254 nm using a background electrolyte containing potassium chromate. Nitrate anion was used as an internal standard for quantification. This CE method was validated in terms of selectivity, linearity, accuracy and precision.

Calibration↗

Factorial design, physicochemical characterisation and activity of ciprofloxacin-PLGA nanoparticles.

Poly(lactide-co-glycolide) nanoparticles incorporating ciprofloxacin HCl were prepared by means of a W/O/W emulsification solvent evaporation method. The stabiliser selected was poly(vinylalcohol). A 2(4) full factorial design based on four independent variables was used to plan the experiments and the variable parameters were the number of homogenisation cycles, addition of boric acid to the inner water phase containing the drug, ciprofloxacin concentration in the inner water phase and oil:outer water phase ratio. The effects of these parameters on the particle size, zeta potential, drug loading efficiency and drug release were investigated. Also the effect of gamma irradiation on the particle size and drug release was evaluated and DSC and XRD analyses of the compounds and the nanoparticles were performed. The activity on two series of microorganisms, Pseudomonas aeruginosa and Staphylococcus aureus, was examined.

Anti-Bacterial Agents↗

Simultaneous determination of catecholamines and polyamines in PC-12 cell extracts by micellar electrokinetic capillary chromatography with ultraviolet absorbance detection.

A method for simultaneous determination of polyamines and catecholamines in cell extracts by micellar electrokinetic capillary chromatography with UV detection at 254 nm was established at the first time. The polyamines (putrescine, spermidine and spermine) and catecholamines (dopamine, serotonin, norepinephrine and epinephrine) were extracted from PC-12 cells and were derivatized with 6-aminoquinolyl-N-hydroxysuccinimidyl carbamate. Different derivatization conditions such as temperature, ratio of derivatization reagents and incubation time were investigated to find the best reaction condition which gave the highest detection sensitivity for polyamines and catecholamines. The influence of running buffer and additives on the separation such as pH, sodium dodecyl sulfate (SDS) concentrations and various additives was also investigated. Separation was achieved within 20 min with good repeatability in a 100mM boric acid buffer containing 10mM SDS and 10mM 18-crown-6 at a pH of 9.5. The detection limit ranged from 1.0 x 10(-7) to 9.0 x 10(-7) M, which is sufficient for determination of polyamines and catecholamines in many cell extracts. This technique can be easily applied to polyamine-related anticancer drug studies or clinical follow-ups after each dosage of these anticancer drugs, since these drugs not only have great inhibition on polyamine levels in blood, but also have a large influence on catecholamine levels in blood.

Animals↗

Kinetic study of the thermal dehydration of borogypsum.

In Turkey, a large amount of borogypsum waste is discharged by the economically important boric acid industry. Calcination of this waste provides a promising technique not only for recovering an economic value but also for reducing its environmental impact. The aim of this work is to study the thermal behavior of borogypsum, which contains gypsum crystals, boron oxide and some impurities under nonisothermal conditions in air atmosphere by using thermogravimetry and differential thermal analysis techniques (TG-DTA). Experiments were carried out at temperatures ranging from ambient to 773 K at different heating rates. The temperatures of conversion from gypsum to hemihydrate and anhydrite states were determined. Various methods were used to analyze the TG and DTA data for determination of reaction kinetics. The activation energy and frequency factor were calculated for dehydration of borogypsum. Activation energy values of the main dehydration reaction of borogypsum were calculated to be approximately 95-114 kJ mol(-1).

Boron↗

Genotoxicity of five food preservatives tested on root tips of Allium cepa L.

The effects of the food preservatives sodium benzoate (SB), boric acid (BA), citric acid (CA), potassium citrate (PC) and sodium citrate (SC) have been studied on root tips of Allium cepa L. Roots of A. cepa were treated with a series of concentrations, ranging from 20 to 100 ppm for 5, 10 and 20 h. The results indicate that these food preservatives reduced mitotic division in A. cepa compared with the respective control. Mitotic index values were generally decreased with increasing concentrations and longer treatment times. Additionally, variations in the percentage of mitotic stages were observed. The total percentage of aberrations generally increased with increasing concentrations of these chemicals and the longer period of treatment. Different abnormal mitotic figures were observed in all mitotic phases. Among these abnormalities were anaphase bridges, C-mitosis, micronuclei, lagging, stickiness, breaks and unequal distribution.

Allium↗