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13C NMR of cyanylated flavodoxin from Megasphaera elsdenii and of thiocyanate model compounds.

Both of the thiol groups of Megasphaera elsdenii flavodoxin have been cyanylated using 13C-enriched cyanide. This chemical modification increases the dissociation constant of the apoflavodoxin-flavin mononucleotide (FMN) complex from 0.4 nM to 2 microM. The thiocyanate carbons of the cyanylated cysteine residues in apoflavodoxin had 13C chemical shifts of 109.4 ppm and 112.2 ppm, which were replaced by signals at 115.5 ppm and 109.6 ppm when FMN was bound. The signals at 109.4 ppm and 112.2 ppm due to the cyanylated apoflavodoxin were unstable at 28 degrees C, and they were slowly replaced signals at 114.5 ppm and 115.3 ppm which are attributed to an inactive form of the apoprotein, which does not bind FMN. At alkaline pH values or after prolonged incubation at neutral pH, the signals at 114.5 ppm and 115.3 ppm were replaced by signals at approximately 171 ppm. On the basis of results obtained with model compounds, the signals at 171 ppm are assigned to the 2-imino carbon of the 2-iminothiazolidine ring formed by the cyclization of the appropriate thiocyanate group. After determining the chemical shift of the thiocyanate carbon of model compounds in a range of solvents, we conclude that the thiocyanate carbons will have a minimal chemical shift of approximately 109 ppm in apolar solvents which do not contain hydrogen bond donors. In water, a more polar hydrogen-bonding solvent, the chemical shift increases to approximately 115 ppm. We also conclude that the chemical shift of a thiocyanate carbon can be used as a probe of its molecular environment.(ABSTRACT TRUNCATED AT 250 WORDS)

Chemical Phenomena↗

Human myeloperoxidase: structure of a cyanide complex and its interaction with bromide and thiocyanate substrates at 1.9 A resolution.

The 1.9 A X-ray crystal structure of human myeloperoxidase complexed with cyanide (R = 0.175, R(free) = 0.215) indicates that cyanide binds to the heme iron with a bent Fe-C-N angle of approximately 157 degrees, and binding is accompanied by movement of the iron atom by 0.2 A into the porphyrin plane. The bent orientation of the cyanide allows the formation of three hydrogen bonds between its nitrogen atom and the distal histidine as well as two water molecules in the distal cavity. The 1.85 A X-ray crystal structure of an inhibitory complex with thiocyanate (R = 0.178, R(free) = 0.210) indicates replacement of chloride at a proximal helix halide binding site in addition to binding in the distal cavity in an orientation parallel with the heme. The thiocyanate replaces two water molecules in the distal cavity and is hydrogen bonded to Gln 91. The 1.9 A structures of the complexes formed by bromide (R = 0.215, R(free) = 0.270) and thiocyanate (R = 0.198, R(free) = 0.224) with the cyanide complex of myeloperoxidase show how the presence of bound cyanide alters the binding site for bromide in the distal heme cavity, while having little effect on thiocyanate binding. These results support a model for a single common binding site for halides and thiocyanate as substrates or as inhibitors near the delta-meso carbon of the porphyrin ring in myeloperoxidase.

Binding, Competitive↗

Leaching of concrete admixtures containing thiocyanate and resin acids.

There is an increasing concern about the emission of pollutants during the construction and lifetime of buildings. The leaching of concrete admixtures containing thiocyanate and resin acids was studied using standard leaching tests and chemical analysis. Ecotoxicological risk was assessed for each admixture. Thiocyanate leaching from concrete, with a chlorine-free accelerating admixture, was determined by ion chromatography. Of the total amount of thiocyanate added, 6-8% was emitted within 30 d. The thiocyanate diffusion curve indicates a fast dissolution process from the surface layer, followed by a slower continuous diffusion process. Thiocyanate exhibits both acute and chronic toxicity, which makes it of immediate environmental concern. Resin acid leaching from concrete test specimens containing an admixture of air-entraining agents with tall oil was determined by solid-phase extraction, methylation, and GC/MS. Of added resin acids, 10% was emitted over 143 d. The leaching curves for the resin acids indicate a continuous diffusion that is proportional to the square root of time and follows Fick's first law of diffusion. The chemical composition of the resin acids in the leachate demonstrates degradation and rearrangement of the resin acids during diffusion. Resin acids emitted from concrete are of environmental concern because they are persistent and have the ability to bioaccumulate in aquatic organisms.

Animals↗

Design and synthesis of aryloxyethyl thiocyanate derivatives as potent inhibitors of Trypanosoma cruzi proliferation.

As a part of our project directed at the search of new chemotherapeutic agents against American trypanosomiasis (Chagas' disease), several drugs possessing the 4-phenoxyphenoxy skeleton and other closely related structures employing the thiocyanate moiety as polar end group were designed, synthesized, and evaluated as antiproliferative agents against Trypanosoma cruzi, the parasite responsible for this disease. These thiocyanate analogues were envisioned bearing in mind the potent activity shown by 4-phenoxyphenoxyethyl thiocyanate (compound 8) taken as lead drug. This compound had previously proved to be an extremely active growth inhibitor against T. cruzi with IC(50) values ranging from the very low micromolar level in epimastigotes to the low nanomolar level in the intracellular form of the parasite. Of the designed compounds, the ethyl thiocyanate drugs connected to nonpolar skeletons, namely, arylthio, 2,4-dichlorophenoxy, ortho-substituted aryloxy, and 2-methyl-4-phenoxyphenoxy (compounds 15, 34, 47, 52, 72, respectively), were shown to be very potent antireplicative agents against T. cruzi. On the other hand, conformationally restricted analogues as well as branched derivatives at the aliphatic side chain were shown to be moderately active against T. cruzi growth. The biological activity of drugs bearing the thiocyanate group correlated quite well with the activity exhibited by their normal precursors, the tetrahydropyranyl ether derivatives, when bonded to the same nonpolar skeleton. Compounds having the tetrahydropyranyl moeity as polar end were proportionally much less active than sulfur-containing derivatives in all cases. Drugs 47 and 72 also resulted to be very active against the amastigote form of the parasite growing in myoblasts; however, they were slightly less active than the lead drug 8. On the other hand, compounds 34 and 52 were almost devoid of activity against myoblasts. Surprisingly, the dithio derivative 15 was toxic for myoblasts.

Animals↗

Determination of thiocyanate in human saliva and urine by ion chromatography.

A simple ion-chromatographic method has been developed for the determination of trace amounts of thiocyanate in human saliva and urine. Thiocyanate separation and detection were carried out on an ODS column coated with cetyldimethylamine and by an ultraviolet detector, respectively. Citrate solution (1 mmol l-1) was used as the mobile phase. Thiocyanate was clearly separated from many organic and inorganic anions found in saliva and urine samples. The analytical results obtained by the proposed method agreed with those of the Fe(3+)-thiocyanate spectrophotometric method. Thiocyanate concentrations in the saliva and urine of smokers were found to be significantly higher than those of non-smokers.

Chromatography, Ion Exchange↗

Simultaneous determination of the tobacco smoke uptake parameters nicotine, cotinine and thiocyanate in urine, saliva and hair, using gas chromatography-mass spectrometry for characterisation of smoking status of recently exposed subjects.

A method using gas chromatography (GC)-mass spectrometry (MS) for the simultaneous determination of the smoke uptake parameters thiocyanate, nicotine and cotinine in human tissues is reported. Nicotine, cotinine and thiocyanate, in combination with a phase-transfer catalyst, were extracted from urine, saliva and hair into dichloromethane (DCM). Thiocyanate was alkylated in the DCM-layer to form a pentafluorobenzyl derivative. The biochemical markers in DCM were directly injected into the GC system and separated on a DB-1MS column using a 9.4 min temperature program. The method was validated in urine and saliva between the limits of quantitation (1.0-15 microg ml(-1) thiocyanate, 0.010-3.0 microg ml(-1) nicotine and cotinine in urine, 0.010-1.0 microg ml(-1) nicotine and cotinine in saliva). The calibration curves were found to be linear (r > 0.996), the within- and between-day accuracy's were 83-120%, the repeatability coefficients of variation were 3-20% and the limits of detection were 0.060 ng ml(-1) thiocyanate and 0.60 ng ml(-1) nicotine and cotinine. The results of the analysis of the biomarkers in the urine of 44 volunteers were used to develop a predictive model for smoking status, using discriminant analysis. The classification model correctly classified 93.2% of cross-validated grouped cases. Saliva samples were used to confirm the results of the classification method.

Biomarkers↗

2,4-Dichlorobenzyl thiocyanate, an antimitotic agent that alters microtubule morphology.

A compound of simple structure, 2,4-dichlorobenzyl thiocyanate (DCBT), is an antimitotic agent with a number of unusual properties. The drug causes an extreme reorganization of microtubules in cells in culture. Most normal microtubules disappear, and remaining tubulin-containing structures appear to be bundled or aggregated. DCBT irreversibly inhibits in vitro polymerization of purified tubulin, but only after a prolonged preincubation of the protein with the drug. Binding of radiolabeled DCBT to tubulin similarly requires a long incubation time, with the reaction not being complete even after 6 hr at 37 degrees C. A specific interaction with tubulin is also shown by the crossresistance to DCBT of Colcemid-resistant cells with an altered beta-tubulin. A human KB carcinoma cell line and a Chinese hamster ovary cell line selected for crossresistance to multiple chemotherapeutic agents, including most antimitotic drugs, are sensitive to DCBT. Initial structure-function studies have demonstrated weak antimitotic and antitubulin activity with the parent compound benzyl thiocyanate. Chlorination at either position 2 or position 4 of the phenyl ring produces compounds of intermediate activity (4-chlorobenzyl thiocyanate is more active than 2-chlorobenzyl thiocyanate). The thiocyanate moiety appears to be essential for activity.

Cell Line↗

Role of thiocyanate, bromide and hypobromous acid in hydrogen peroxide-induced apoptosis.

We have previously reported that H2O2-induced apoptosis in HL-60 human leukemia cells takes place in the presence of chloride, requires myeloperoxidase (MPO), and occurs through oxidative reactions involving hypochlorous acid and chloramines. We now report that when chloride is replaced by the pseudohalide thiocyanate, there is little or no H2O2-induced apoptosis. Furthermore, thiocyanate inhibits H2O2-induced apoptosis when chloride is present at physiological concentrations, and this occurs at thiocyanate concentrations that are present in human serum and saliva. In contrast, bromide can substitute for chloride in H2O2-induced apoptosis, but results in a lower percent of the cells induced into apoptosis. Hypobromous acid is likely a short-lived intermediate in this H2O2/MPO/bromide apoptosis, and reagent hypobromous acid and bromamines induce apoptosis in HL-60 cells. We conclude that the physiologic concentrations of thiocyanate found in human plasma could modulate the cytototoxicity of H2O2 and its resulting highly toxic MPO-generated hypochlorous acid by competing with chloride for MPO. Furthermore, the oxidative products of the reaction of thiocyanate with MPO are relatively innocuous for human leukemic cells in culture. In contrast, bromide can support H2O2/MPO/halide apoptosis, but is less potent than chloride and it has no effect in the presence of physiological levels of chloride.

Amines↗

Effects of prolonged cyanide and thiocyanate feeding in rats.

Male weaning rats were fed a semipurified diet containing 10% casein; this diet restricted in methionine, vitamin B12, and iodine; or the complete and restricted diets supplemented with either 1500 ppm potassium cyanide or 2240 ppm potassium thiocyanate for 11.5 mo. There were no deaths or clinical signs of toxicity. Cyanide, but not thiocyanate, caused a consistent reduction in weight gain in the complete and restricted groups. Both cyanide and thiocyanate caused decreased thyroid gland activity in young rats, particularly in the restricted groups. Plasma thyroxine concentrations were maintained in the mature cyanide-treated rats, even though secretion rates were decreased. However, the mature thiocyanate-treated animals showed decreased plasma thyroxine concentrations, despite thyroid gland enlargement. Modest primary myelin degeneration in the spinal cord white matter was found in the restricted group and in rats receiving this diet supplemented with either cyanide or thiocyanate. The lesions did not resemble those of a vitamin B12 deficiency in appearance or those of acute cyanide intoxication in distribution. Because of tissue autolysis, it could not be determined whether these changes resulted from histotoxic anoxia or an alteration of oligodendroglial myelin metabolism.

Animals↗

Are there gender differences in self-reported smoking practices? Correlation with thiocyanate and cotinine levels in smokers and nonsmokers from the Pawtucket Heart Health Program.

OBJECTIVES: This study compared serum cotinine and thiocyanate in assessment of self-reported smoking behavior among 1400 men and 1809 women from two New England communities. METHODS: Serum thiocyanate and serum cotinine levels were analyzed on 2411 and 798 survey respondents, respectively, in an attempt to provide an objective measurement for validation of self-reported smoking behaviors that were obtained through an in-home interviewer-administered questionnaire. Cross-sectional household surveys were conducted with randomly selected men and women, aged 18-65, between 1981 and 1993 as part of the evaluation of the Pawtucket Heart Health Program. RESULTS: Among smokers, the thiocyanate test had similar rates of agreement for women(88.0%) and for men (89.3%). However, among nonsmokers, thiocyanate had higher rates of agreement for women (91.5%) than for men (85.2%). For cotinine, the rates of agreement among smokers were higher for women (91.6%) than for men (89.7%). Similarly, the rates of agreement among nonsmokers were also higher for women (93.9%) than for men (91.9%). Overall,serum cotinine had a higher concordance rate than serum thiocyanate for both men and women. CONCLUSIONS: Although our results suggested that there were some differences in self-reporting of smoking status by gender, results were quite similar between self-reports of smoking and both biochemical tests. The results obtained from this large population-based study from two New England communities lend credibility to the use of self-reports as a low-cost accurate approach to obtaining information on smoking behaviors among both men and women in large population-based health surveys.

Adolescent↗

Intake of thiocyanate by way of milk and its possible effect on thyroid function.

The keeping quality of milk can be improved if the lactoperoxidase system is activated. To make such an activation efficient the thiocyanate concentration has to be increased. Since, however, thiocyanate has a potent antithyroid effect, thyroid function has been studied in 37 healthy individuals during 12 wk of daily intake of 8 mg thiocyanate by way of milk. The thiocyanate increased significantly in serum and reached a maximum value after 4 wk (+3.8 mg/1). The increased serum levels coincided with an increased excretion in urine (+ 4.8 mg/g creatinine). The levels of thyroxine, triiodothyronine, and thyrotropic hormone were all in the normal range at the beginning of the investigation and no significant changes were found during the experimental period. In conclusion, a daily intake of 8 mg thiocyanate by way of milk does not have any apparent effect on the thyroid function.

Adolescent↗

Determination of thiocyanate anion by high-performance liquid chromatography with fluorimetric detection.

A simple and sensitive high-performance liquid chromatographic (HPLC) method was established for the trace determination of thiocyanate anion as a fluorogenic derivative. The method is based on the chemical derivatization of thiocyanate anion with 3-bromomethyl-7-methoxy-1,4-benzoxazin-2-one. The resulting derivative was separated by a Nova-Pak C18 reversed-phase column. Optimization conditions for the derivatization of thiocyanate anion were investigated by HPLC with fluorimetric detection. The linear range for the quantitation of thiocyanate anion was 1-0.05 nmol in 0.1 mL of sample; the detection limit (with a signal-to-noise ratio of 5) of a 20-microL injected aliquot was approximately 3.3 +/- 1.2 fmol. Application of the method to the analysis of thiocyanate anion in saliva and plasma proved to be feasible.

Anions↗

Determination of urine thiocyanate in patients with amyotrophic lateral sclerosis.

It has been reported that amyotrophic lateral sclerosis-Parkinsonism-dementia in Guam might be related to the eating of Cycas seeds, which contain cyanide. Based on this assumption, we determined the urinary thiocyanate excretion level in patients with ALS and compared this with that of other neurological diseases. The assay method was designed to use column chromatography with Amberlite IRA 402. The thiocyanate level was determined using pyridine-barbiturate method. The 24-h thiocyanate level was higher in the ALS patients of the middle stages than in the normal control group (Wilcoxon's test, P less than 0.02). There were no significant differences between the ALS patient groups of the early and terminal stages, Kugelberg-Welander disease group, Duchenne type muscular dystrophy group and control group. From these results, we concluded that ALS patients were contaminated with cyanide or thiocyanate and that, along with rapid muscular atrophy, the thiocyanate excretion levels were high.

Adult↗

Chronic administration of cyanide: urinary excretion of thiocyanate in male and female rats.

The urinary elimination of thiocyanate was investigated in male and female rats following the chronic administration of potassium cyanide. Female rats dosed at the level of 5 mg KCN/kg once a week and twice a week respectively, displayed no significant difference in the excretion of thiocyanate in urine after periods of up to eight weeks of study. Similarly, male rats that were administered 5 mg/KCN/kg twice weekly showed no significant difference in the amount of thiocyanate excreted. The elimination patterns of thiocyanate in male and female rats showed no significant differences. The results suggest that a substrate saturation phenomenon is not operative with cyanide metabolism at the dosage level of potassium cyanide employed in this study. This is contrary to a previously published study which reported that the urinary excretion of thiocyanate decreased after chronic potassium cyanide administration.

Animals↗

Lactoperoxidase and thiocyanate protect bacteria from hydrogen peroxide.

Lactoperoxidase and thiocyanate were shown to protect Escherichia coli and three oral streptococcal species from the bactericidal effect of hydrogen peroxide under aerobic conditions. Lactoperoxidase in the absence of thiocyanate was also protective for two of the bacterial species in a dilution medium but potentiated hydrogen peroxide toxicity for the other two under the same conditions. The products of the reaction between hydrogen peroxide and thiocyanate in the presence of lactoperoxidase were not bactericidal except in the case of E. coli, and then only under special conditions. The results demonstrate the effectiveness of lactoperoxidase and thiocyanate in protecting living cells from hydrogen peroxide toxicity. Although the effect on human cells was not examined in this study, extrapolation of these results to the cells of the oral mucosa would suggest an important protective role of lactoperoxidase and thiocyanate against the toxic effects of hydrogen peroxide in the oral cavity.

Aerobiosis↗

Evidence for thiocyanate-sensitive peroxidase activity in human saliva.

A procedure was developed for determining the relative levels of lactoperoxidase, leukocyte myeloperoxidase, and thiocyanate-sensitive peroxidase in human saliva. With this procedure, most of the peroxidase activity in whole saliva from normal (those without cancer) subjects was found to be associated with lactoperoxidase and thiocyanate-sensitive peroxidase, with only a minor contribution from leukocyte myeloperoxidase. In contrast, thiocyanate-sensitive peroxidase and leukocyte myeloperoxidase were the major peroxidase activities present in the residual salivary secretion obtainable from two xerostomic patients examined, and these enzymes were present at concentrations much higher than those normally occurring in human saliva. The occurrence of thiocyanate-sensitive peroxidase in saliva has not been previously reported and may represent either an additional peroxidase activity of saliva or a form of lactoperoxidase which is particularly sensitive to inhibition by thiocyanate.

Animals↗

Nitrite and thiocyanate in the fasting and secreting stomach and in saliva.

The concentrations of nitrite and thiocyanate in fasting and pentagastrin stimulated gastric juice and in saliva have been examined. Nitrite was found in all of 17 samples of fasting gastric juice, mean 4-9 +/- 1-1 muM. Stimulation of gastric secretion with pentagastrin caused no significant change in nitrite concentration. Thiocyanate was detected in all of 21 samples of fasting gastric juice and the difference in concentration between smokers and non-smokers probably reflects similar differences in saliva. In contrast to the nitrite data there was a significant drop in thiocyanate concentration of gastric juice after pentagastrin from 0-9 +/- 0-1 mM to 0-3 +/- 0-04 mM, suggesting a salivary origin for the thiocyanate in gastric juice. Thiocyanate is a powerful catalyst of nitrosation, which, together with small amounts of nitrite and naturally occurring amines could lead to the intragastric formation of carcinogenic nitrosamines and in certain circumstances be a factor in the aetiology of gastric cancer.

Fasting↗

Thiocyanate as a marker of saliva in gastric juice?

One source of error in gastric secretion studies is swallowed saliva. The possibility that salivary thiocyanate might be used to measure this contamination has been investigated. Thiocyanate concentration was measured in saliva and gastric juice collected simultaneously in 22 duodenal ulcer patients undergoing routine insulin and histamine secretion studies. On stimulation, despite the increase in the rate of gastric secretion this was not matched by an appropriate fall in the concentration of thiocyanate in gastric juice. Moreover, in one-third of the gastric juice specimens, the thiocyanate concentration was greater than in the simultaneous samples of saliva. Thus, contrary to what has been claimed, thiocyanate is present not only in saliva but also in gastric juice. Therefore it cannot be used as a marker of salivary contamination. An adequate marker of this source of error has not yet been found.

Duodenal Ulcer↗