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PubMed1979

Relationship between lactate and glutamine metabolism in vitro by the kidney: differences between dog and rat and importance of alanine synthesis in the dog.

Interaction between lactate (1 or 5 mM) and glutamine (1 or 5 mM) metabolism was studied with renal cortical slices incubated at a pH of 7.0 and obtained from acidotic (ammonium chloride) dogs and rats. The effect of aminooxyacetate (0.2 mM), dichloroacetate (3 mM), and fluoroacetate (0.05 mM) was also studied. Significant differences were observed between dog and rat. In the dog, lactate had no effect on glutamine uptake and vice versa, but gluconeogenesis increased. Ammonia production, however, decreased by 13 to 21%, whereas a significant increase in alanine production was noted. In the rat, glutamine extraction and ammonia production dropped by 33% with 5 mM lactate. In contrast to the observation in the dog, no production of alanine was noted, but significant accumulation of glutamate took place. Amino-oxyacetate inhibited alanine production in the dog and reestablished ammoniagenesis, and it led to a marked decrement in the uptake of lactate and glucose production in both species. Dichloroacetate in the dog resulted in a reduction in pyruvate, alanine, glucose, and ammonia production while glutamate accumulation was observed. In both species, fluoroacetate stimulated glutamine uptake and ammonia production. With lactate alone, fluoroacetate decreased lactate uptake and glucose production. With both lactate and glutamine in the medium, fluoroacetate prevented any effect of lactate on ammoniagenesis. The present study demonstrates that lactate has a modest depressing effect on renal ammonia production by dog slices through increased synthesis of alanine and redistribution of nitrogen from glutamine. In the rat, the depressing effect of lactate on ammonia production in the alanine amino-transferase deficient kidney occurs through accumulation of glutamate. The data also reveal that oxidation of lactate to carbon dioxide is greater in the dog than it is in the rat, but that gluconeogenesis from lactate is more important in the rat.

Acidosis↗
PubMed1968

The utilization of some halogenated aromatic acids by Nocardia. Oxidation and metabolism.

1. Halogen analogues of p-nitrobenzoate and benzoate were oxidized by washed cells of Nocardia erythropolis. 2. The oxidation of 2-fluoro-4-nitrobenzoate ceased at the level of acetate, and fluoroacetate was found in the incubation medium and particularly in hot-ethanolic extracts of the cells. 3. Several fluorine-containing intermediates were detected and 2-fluoroprotocatechuate was identified as one of them. 4. The nitro group was also reduced by the organism, as evidenced by the formation of 4-amino-2-fluorobenzoate. 5. Extracts of N. erythropolis activated fluoroacetate and condensed the resulting fluoroacetyl-CoA with oxaloacetate to form fluorocitrate. This product was a very powerful inhibitor of citrate metabolism by guinea-pig kidney homogenates and of the aconitase also present in the bacterial extracts. The inhibitions effected by synthetic fluorocitrate and the natural product were comparable. 6. 2-Fluoro-4-nitrobenzoate had negligible mammalian toxicity. 7. The isolation of fluoroacetate as a product of 2-fluoro-4-nitrobenzoate oxidation implies that the aromatic ring in this bacterium must be degraded via a gamma-carboxymuconolactone; fluoroacetate cannot arise by metabolism through the isomeric beta-carboxymuconolactone.

Acetates↗
PubMed1995

Biosynthesis of fluorinated secondary metabolites by Streptomyces cattleya.

The biosynthesis of organofluorine compounds by Streptomyces cattleya NRRL 8057 was examined using 19F NMR spectroscopy. The organism produced 1.2 mM fluoroacetate and 0.5 mM 4-fluorothreonine as secondary metabolites when cultured for 28 d on a chemically defined medium containing 2 mM fluoride. Cell suspensions from batch cultures harvested at the growth maximum of 4 d were not capable of fluoride uptake or fluorometabolite biosynthesis, but by 6 d had developed an efficient fluoride-uptake system and biosynthesized the two fluorometabolites in almost equal proportions. As the harvest age increased, the proportion of fluoroacetate to 4-fluorothreonine formed by cell suspensions rose progressively so that 16-d-old cells showed a ratio of 76:26 for the two compounds. Fluoride uptake and fluorometabolite production by cell suspensions were highly dependent on pH, with both processes showing a maximum rate at pH 6.0 but declining rapidly at higher pH values. This decrease was particularly marked in the case of fluoroacetate biosynthesis which was barely detectable at pH 7.5. Fluoroacetate and 4-fluorothreonine showed only low levels of interconversion by cell suspensions, suggesting that the carbon skeleton of neither was derived by metabolism of the other. The limited interconversion observed is explicable in terms of a small degree of biological defluorination occurring with each compound, followed by reincorporation of the resulting fluoride ion into the organic form by the active fluorinating system, a phenomenon also noted on incubation of cell suspensions with a number of other fluorinated biochemical intermediates.(ABSTRACT TRUNCATED AT 250 WORDS)

Culture Media↗
PubMed1967

Effects of metabolic poisons on rice: the comparative sensitivity of aerobic and anaerobic modes of germination.

Rice germinates equally well when incubated in air and in nitrogen. It was therefore chosen for a comparative study of the effect of oxygen status in a single organism upon the activity of conventional metabolic poisons. Inhibitor activity was based upon the concentration required for 50% inhibition of germination. The inhibitors were: AgNO(3), HgCl(2), phenylmercuric acetate, iodoacetamide, KCN, NaN(3), NaF, fluoroacetate, 2,4-dinitrophenol, Na(2)HAsO(4) and CO. Only 5 inhibitors out of 11 differed significantly in their effects on aerobic and anaerobic germination. These included phenylmercuric acetate (N(2)), sodium fluoroacetate (air), NaN(3) (air), and 2,4-dinitrophenol (N(2)). CO activity was manifest only in air and it was photo-reversible. The effects of CO, NaN(3), and fluoroacetate were consistent with their conventional role in aerobic metabolism. The failure of KCN to discriminate was attributed to its relative non-specificity. 2,4-Dinitrophenol behaved anomalously, requiring a 20-fold lower concentration for inhibition under nitrogen than under air. Among sulfhydryl poisons, only phenylmercuric acetate differentiated between germination in air and nitrogen and was nearly 8 times more active under nitrogen. Uptake measurements using phenylmercuric acetate and arsenate showed both compounds to be in greater concentration under aerobic conditions, thereby rendering unlikely any explanation based upon greater permeability under nitrogen. In addition to other anomalies, the fact that NaN(3), fluoroacetate and CO inhibited anaerobic germination at any concentration requires explanation. It was concluded that the general significance and utility of metabolic inhibitor studies in vivo required further evaluation.

Journal Article↗
PubMed1981

Ammonia and disinhibition in cat motor cortex by ammonium acetate, monofluoroacetate and insulin-induced hypoglycemia.

Ammonia intoxication abolished the suppression of action potential generation by cortical postsynaptic inhibition due to the inactivation of neuronal Cl- extrusion. The disinhibition by ammonia intoxication occurred when ammonia concentrations in the cerebral cortex were increased to 320% of normal. Fluoroacetate poisoning and insulin-induced hypoglycemia, which are known to increase ammonia concentrations in the CNS and previously have been shown to inactivate Cl- extrusion in spinal motoneurons, abolished the suppression of action potential generation by cortical postsynaptic inhibition like ammonia intoxication. This disinhibition occurred at unchanged cerebral ammonia concentrations. The effect of fluoroacetate and insulin induced hypoglycemia on cortical postsynaptic inhibition is either due to a direct, i.e. not ammonia mediated, inactivation of neuronal Cl- extrusion or due to a disturbance of the synaptic mechanisms mediated by the transmitter of cortical inhibition, GABA. Toxic-metabolic encephalopathies which increase cerebral ammonia concentrations beyond 320% of normal may produce a dysfunction of the CNS due to inactivation of neuronal Cl- extrusion leading to ineffective cortical inhibition. However, in fluoroacetate poisoning and insulin-induced hypoglycemia increased ammonia concentrations in the CNS have only a secondary role in initiating a dysfunction of the CNS since disinhibition occurs before ammonia concentrations increase.

Acetates↗
PubMed2002

In vitro uptake of [1-14C]Octanoate in brain slices of rats: basic studies for assessing [1-11C]Octanoate as a PET tracer of glial functions.

To clarify the contribution of glial cells to octanoate uptake into the brain, we determined the effects of fluoroacetate, a selective inhibitor of glial metabolism, on in vitro brain uptake of [1-14C]octanoate, using rat brain slices. The [1-14C]octanoate uptake significantly decreased, depending on the concentration of fluoroacetate (p = 0.001). The [1-14C]octanoate uptakes at 5 mM (0.23 +/- 0.05% uptake/mg slice) and 25 mM fluoroacetate (0.12 +/- 0.01% uptake/mg slice) were significantly lower than that at control (0.29 +/- 0.02% uptake/mg slice, p < 0.05 and p < 0.001, respectively). The results demonstrate the contribution of glial cells to octanoate uptake into the brain. The potential of [1-11C]octanoate as a PET tracer for studying glial functions is suggested.

Animals↗
PubMed1972

Locations of amino acids in brain slices from the rat. Tetrodotoxin-sensitive release of amino acids.

1. Amino acids, particularly glutamate, gamma-aminobutyrate, aspartate and glycine, were released from rat brain slices on incubation with protoveratrine (especially in a Ca(2+)-deficient medium) or with ouabain or in the absence of glucose. Release was partially or wholly suppressed by tetrodotoxin. 2. Tetrodotoxin did not affect the release of glutamine under various incubation conditions, nor did protoveratrine accelerate it. 3. Protoveratrine caused an increased rate of formation of glutamine in incubated brain slices. 4. Increased K(+) in the incubation medium caused release of gamma-aminobutyrate, the process being partly suppressed by tetrodotoxin. 5. Incubation of brain slices in a glucose-free medium led to increased production of aspartate and to diminished tissue contents of glutamates, glutamine and glycine. 6. Use of tetrodotoxin to suppress the release of amino acids from neurons in slices caused by the joint action of protoveratrine and ouabain (the latter being added to diminish reuptake of amino acids), it was shown that the major pools of glutamate, aspartate, glycine, serine and probably gamma-aminobutyrate are in the neurons. 7. The major pool of glutamine lies not in the neurons but in the glia. 8. The tricarboxylic cycle inhibitors, fluoroacetate and malonate, exerted different effects on amino acid contents in, and on amino acid release from, brain slices incubated in the presence of protoveratrine. Fluoroacetate (3mm) diminished the content of glutamine, increased that of glutamate and gamma-aminobutyrate and did not affect respiration. Malonate (2mm) diminished aspartate and gamma-aminobutyrate content, suppressed respiration and did not affect glutamine content. It is suggested that malonate acts mainly on the neurons, and that fluoroacetate acts mainly on the glia, at the concentrations quoted. 9. Glutamine was more effective than glutamate as a precursor of gamma-aminobutyrate. 10. It is suggested that glutamate released from neurons is partly taken up by glia and converted there into glutamine. This is returned to the neurons where it is hydrolysed and converted into glutamate and gamma-aminobutyrate.

Amino Acids↗
PubMed1988

Structural beta-cell changes and transient hyperglycemia in mice treated with compounds inducing inhibited citric acid cycle enzyme activity.

An initial transient hyperglycemia was seen in mice injected with asparagine, fluoroacetate, hydroxylamine, or malonate plus methionine, whereas an initial triphasic blood glucose response and a transient "secondary" hyperglycemia were exhibited in those injected with hydroxylamine plus arsenite, and a delayed hypoglycemia was observed in those treated with fluoroacetate or arsenite. The glucose-induced insulin secretion was significantly decreased in isolated pancreatic islets incubated with hydroxylamine plus arsenite. Light and electron microscopy, pyroantimonate technique, and X-ray microanalysis disclosed mitochondrial damage, degeneration, and necrosis among the beta-cells in the islets of mice injected with hydroxylamine plus arsenite. Glycogen depletion and microvesicular fatty change were seen in the liver of mice treated with fluoroacetate, arsenite, or hydroxylamine plus arsenite. These observations support the view that inhibition of the activity of citric acid cycle enzymes and associated reactions in the beta-cells play a role in the induction of diabetic features.

Animals↗
PubMed2005

Role of different additives and metallic micro minerals on the enhanced citric acid production by Aspergillus niger MNNG-115 using different carbohydrate materials.

The present investigation deals with the promotry effect of different additives and metallic micro minerals on citric acid production by Aspergillus niger MNNG-115 using different carbohydrate materials. For this, sugar cane bagasse was fortified with sucrose salt medium. Ethanol and coconut oil at 3.0% (v/w) level increased citric acid productivity. Fluoroacetate at a concentration of 1.0 mg/ml bagasse enhanced the yield of citric acid significantly. However, the addition of ethanol and fluoroacetate after 6 h of growth gave the maximum conversion of available sugar to citric acid. In another study, influence of some metallic micro-minerals viz. copper sulphate, molybdenum sulphate, zinc sulphate and cobalt sulphate on microbial synthesis of citric acid using molasses medium was also carried out. It was found that copper sulphate and molybdenum sulphate remarkably enhanced the production of citric acid while zinc sulphate was not so effective. However, cobalt sulphate was the least effective for microbial biosynthesis of citric acid under the same experimental conditions. In case of CuSO(4), the strain of Aspergillus niger MNNG-115 showed enhanced citric productivity with experimental (9.80%) over the control (7.54%). In addition, the specific productivity of the culture at 30 ppm CuSO(4) (Q(p) = 0.012a g/g cells/h) was several folds higher than other all other concentrations. All kinetic parameters including yield coefficients and volumetric rates revealed the hyper productivity of citric acid by CuSO(4) using blackstrap molasses as the basal carbon source.

Alcohols↗
PubMed1982

Development of Aspergillus parasiticus and formation of aflatoxin B1 under the influence of conidiogenesis affecting compounds.

The influence of various inhibitors of hyphal growth, sporulation and biosynthesis of aflatoxin B1 in Aspergillus parasiticus NRRL2999 was studied. 6-Thioguanine, DL-ethionine, fluoroacetic acid and phenylboric acid, inhibitors of maturation of fungal conidiophores and of conidiogenesis, were added at various concentrations to malt extract agar. Lower concentrations of 6-thioguanine and DL-ethionine did not inhibit the growth of hyphae and the sporulation. Phenylboric acid reduced conidiogenesis more than hyphal growth. The yields of aflatoxin B1 were significantly reduced. Additions of fluoroacetic acid did not greatly affect the growth of hyphae but totally inhibited the production of conidia and concurrently significantly reduced the formation of aflatoxin B1. An interrelation between conidiogenesis and onset of secondary metabolism in A. parasiticus is evident.

Aflatoxin B1↗
PubMed1979

The influence of some metabolic inhibitors on phagocytic activity of mouse macrophages in vitro.

The action of different metabolic inhibitors on phagocytosis by macrophages from mouse peritoneal exudate cultured in vitro was studied. The following metabolic inhibitors were tested: sodium iodoacetate, sodium fluoride, sodium fluoroacetate, sodium malonate, 2-4-dinitrophenol, sodium azide, ouabain and cycloheximide, all at the concentration of 10(-3) M. Iodoacetate caused a strong inhibitory effect on phagocytosis; this observation confirms that glycolysis is the main source of energy for the phagocytic process. On the contrary, fluoride, although it is an effective inhibitor of glycolysis, did not exert any effect. This difference may be explained by the fact that sodium fluoride blocks anaerobic glycolysis only in vitro at an unphysiological temperature (0 degrees C). Fluoroacetate and malonate, two compounds which interfere with the Krebs cycle, did not inhibit phagocytosis, but it is known that the Krebs cycle activity is poorly developed in the macrophagic cells. Sodium azide and 2-4-dinitrophenol, two inhibitors of oxidative phosphorylation, showed an effect on phagocytosis only after 3 h of contact with the cell cultures. Ouabain blocks Na+ and K+ transport across the plasma membrane and, probably, it inhibited phagocytosis by interfering with the movements of the cell membrane. Finally, the mode of action of cycloheximide on phagocytosis is uncertain. This compound inhibits the protein synthesis and, perhaps, it can act by preventing the renewal of the cell membrane.

Animals↗
PubMed1993

4-Aminopyridine causes reduction of cytochromes partly originated in glia with enhanced evoked potentials in the olfactory cortex slice.

Enhanced electrical and metabolic activities with addition of 4-aminopyridine (4-AP) were investigated in the olfactory cortex slice by recording evoked potentials, the redox state of cytochromes and the rate of oxygen uptake. During perfusion with 4-AP (0.01-0.1 mM), the late N-wave was dose-relatedly elicited in the evoked potential, concomitant with reduction of cytochromes and acceleration of oxygen uptake. These enhanced responses by 4-AP (0.1 mM) depended on the extracellular Ca2+. When the slice was subject to 2-deoxy-D-glucose (2-DG) (10 mM), initiation of the late N-wave by 4-AP (0.1 mM) was delayed, and both the reduction of cytochromes and the raised oxygen uptake prompted by the same dose of 4-AP were also significantly attenuated. Nevertheless, the presynaptic potential and N-wave, which markedly diminished by 2-DG, became tolerant to glycopenia after addition of 4-AP. By prior exposure to fluoroacetate (1 mM), the N-wave was gradually increased, but the late N-wave was rapidly decreased in amplitude by adding 4-AP (0.1 mM). The cytochrome reduction and the accelerated oxygen uptake by 4-AP (0.1 mM) were suppressed in the presence of fluoroacetate (1 mM). These results indicate that cytochromes become reduced by 4-AP, concomitant with the enhanced evoked potentials and oxygen uptake in a Ca(2+)-dependent manner, and that glial cells probably contribute to the enhanced electrical and metabolic activities in the olfactory cortex slice.

4-Aminopyridine↗
PubMed1995

Engineering gut flora of ruminant livestock to reduce forage toxicity: progress and problems.

The rumen bacterium Butyrivibrio fibrosolvens has been genetically modified to detoxify fluoroacetate (a poisonous component of trees and shrubs in Australia, Africa and Central America) and has been shown to persist when it is returned to the rumen. Such bacteria may save animals from poisoning and, therefore, reduce economic losses for livestock industries in those countries. The ability to make genetic changes to rumen bacteria raises important questions about their practicality, and about the environmental factors that must be considered before releasing modified strains. The fluoroacetate-detoxifying bacterium provides an important model by which these issues can be examined.

Animals↗
PubMed1978

The energy metabolism of adult Haemonchus contortus, in vitro.

A comparison was made of the major excretory products when adult Haemonchus contortus worms were incubated with D-[U-14C]glucose under aerobic and anaerobic conditions. Catabolites measured were propan-1-ol, acetate, n-propionate and CO2 and the only major difference was that nearly twice as much CO2 both in terms of quantity and radioactivity was excreted under aerobic than anaerobic conditions. The worms were also much more physically active under aerobic conditions. When worms were incubated under aerobic conditions with increasing amounts of fluoroacetate their CO2 production was progressively reduced to the anaerobic level. Their movement and their ability to clump together was also progressively reduced. After aerobic incubation with fluoroacetate and D-[U-14C]glucose the quantity and radioactivity of citrate within worms increased greatly. When worms were similarly incubated anaerobically no increase in citrate occurred, no radioactivity was associated with the citrate and the worms appeared physically unaffected. When worms were incubated aerobically with fluoro[1(-14)C]acetate they produced radioactive fluorocitrate.

Acetates↗
PubMed1970

Carbon dioxide fixation in green sulphur bacteria.

1. About one-third of the CO(2) fixed during photosynthesis by washed suspensions of Chlorobium thiosulfatophilum strain 8346 gave rise to alpha-oxoglutarate and branched-chain oxo acids, mainly beta-methyl-alpha-oxovalerate. Another one-third to one-half gave rise to a polyglucose. 2. The fixation of CO(2) was inhibited by fluoroacetate, increasing concentrations up to 1mm stimulating the accumulation of alpha-oxoglutarate and causing a decrease in the formation of the branched-chain oxo acids and polyglucose. 3. Acetate was converted into the same products as was CO(2). 4. Fluoroacetate (1mm) had a negligible effect on the formation of polyglucose from acetate and caused a slight inhibition of the formation of the branched-chain oxo acids and increased accumulation of alpha-oxoglutarate. 5. Iodoacetate (1mm) strongly inhibited polyglucose formation from acetate and caused accumulation of pyruvate. The formation of the branched-chain oxo acids from acetate was only slightly affected by this inhibitor. 6. Pyruvate can be metabolized by this organism in the presence of a suitable electron donor whether CO(2) is present or not. In the absence of CO(2) pyruvate is converted into polyglucose. 7. The accumulation of oxo acids during CO(2) fixation is completely inhibited by NH(4) (+) ions. The formation of the branched-chain oxo acids is considerably decreased by the presence of isoleucine, leucine or valine, or a mixture of these. 8. CO(2) fixation in two other strains of Chlorobium appears to exhibit a similar pattern to that in C. thiosulfatophilum strain 8346. 9. It is concluded that in washed suspensions, CO(2) is fixed mainly by a mechanism involving the reductive carboxylic acid cycle. Acetate, the product of the cycle, is converted into polyglucose via pyruvate synthase and a reversal of glycolysis or into branched-chain oxo acids by an unknown mechanism.

Acetates↗
PubMed1992

The development of cleanup criteria for an acutely toxic pesticide at a contaminated industrial facility.

Sodium fluoroacetate, a restricted-use rodenticide, was improperly applied to kill rats in a South American steel mill. As a result of this application, several workers were seriously injured. During plant decontamination, cleanup levels were developed to ensure that any residual material remaining at the plant did not pose a health risk. Cleanup levels were developed to prevent significant exposure of workers, who could inhale contaminated dust, contact dust, or soil dust in outdoor areas or on plant floors and who could contact contaminated surfaces. On the basis of a health risk analysis, the following cleanup levels for sodium fluoroacetate were developed--air cleanup levels, 0.05 mg/m3; soil/dust cleanup levels, 100 mg/kg; and wipe sample cleanup levels, 0.2 mg/100 cm2. These risk-based cleanup levels were ultimately used to assist the regulatory agencies in reaching a decision to reopen the plant.

Air Pollutants, Occupational↗
PubMed1965

K fluxes in frog skin.

A method has been developed for measuring K influx into the epithelial cells of frog skin from the inside solution. Diffusion delay in the connective tissue has been taken into account. Ninety-four per cent of skin K was found to exchange with K(42) in the inside solution with a single time constant. K influx showed saturation with increasing K concentration, was not altered by imposing a potential difference of +/-200 mv across the skin, and was inhibited by dinitrophenol, fluoroacetate, and ouabain. Relatively low concentrations of dinitrophenol (5 x 10(-5)M) and fluoroacetate (10(-10)M) had no effect on k influx but caused a 40 per cent decrease in net Na flux. There was no correlation between the rate of K uptake at the "inner barrier" and the rate of net Na transport. Reduction of net Na transport by lowering Na concentration in the outside solution caused little change in K uptake. These observations indicate that there is not a significant Na-K exchange involved in active transport of Na across the skin. K influx was found, however, to require Na in the inside bathing solution.

Animals↗