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At least 973 records · Page 54Linked to original sources
PubMed1982

Reduced pyridine nucleotides and cytochrome b5 as electron donors for prostaglandin synthetase reconstituted in dimyristyl phosphatidylcholine vesicles.

Prostaglandin synthetase has been reconstituted in dimyristyl phosphatidylcholine vesicles. These vesicles in either 80 or 2 microM flufenamate utilized NADH or NADPH as electron donor in the reductive peroxidative step of prostaglandin H2 formation. Vesicles containing bound cytochrome b5 reductase and cytochrome b5 in order to complete an NADH cytochrome b5 reductase system also utilized reduced cytochrome b5 as the electron donor for this peroxidative step. In systems containing cytochrome and reductase, the rate of NADH oxidation exceeded that of NADPH oxidation, indicating that reduced cytochrome b5 is an effective electron donor for prostaglandin H2 formation, enhancing both the initial rate and the extent of the reaction. The concentrations of reduced pyridine nucleotides and cytochrome b5 employed in these experiments to provide reductants for prostaglandin synthetase are within the concentration ranges that obtain under physiological conditions.

Chemical Phenomena↗
PubMed1981

[Gas-liquid chromatographic determination of etofenamate/ Determination, method and use in biological material (author's transl)].

Etofenamate in biological specimen can be determined by gas-liquid chromatography with etofenamate benzyl ether as internal standard. Determination in urine is done directly after extraction and concentration, whereas plasma and homogenates from organs have to be prepurified by thin-layer chromatography. Unchanged etofenamate is found in small amounts in human urine (0--4, 6--6, 6--8 h p. appl.). Inflamed rat paws after local application contain up to 75 microgram etofenamate/g in comparison to only 2 microgram flufenamic acid/g tissue. Both compounds are also found in non-inflamed paws, contents being only 3--4% as compared to the inflamed tissue. Elimination of etofenamate from the inflamed area occurs with a half-life of approx. 8.5 h. These results from gas-liquid chromatography correspond to results from t.l.c./fluorescence measurements.

Animals↗
PubMed1981

A morphological study of the effects of indomethacin, flufenamate, salicylate and calcium ions on rabbit peritoneal neutrophil polymorphs.

Rabbit peritoneal neutrophil polymorphs have been examined by transmission electron microscopy to determine the effects of removing and replacing extracellular calcium. Degranulation, disruption of the cell membrane and vesiculation are all more marked in the presence of calcium than in its absence. Cooling the cells to 4 degrees has a protective effect. The addition of indomethacin, flufenamate or salicylate to a calcium-free incubating medium decreases degranulation, protects the membrane and reduces vesiculation, particularly at 4 degrees. When extracellular calcium is replaced at 37 degrees indomethacin and salicylate slightly reduce the amount of degranulation; flufenamate and salicylate significantly reduce the signs of damage. Higher concentrations of indomethacin and flufenamate cause considerable degranulation and damage. When extracellular calcium is present in the incubating medium throughout, the addition of indomethacin, flufenamate or salicylate shows varying effects. High concentrations of all these drugs, however, cause extensive degranulation and damage.

Animals↗
PubMed1994

A simple microassay for computing the hemolytic potency of drugs.

A simple microassay and computer program are described for determining the erythrocyte hemolytic potency of drugs in vitro. This microassay is sensitive for both micro as well as macro ranges of hemoglobin concentration. An ELISA reader has been adapted to read erythrocyte lysis (hemolysis), which reduces the number and culture of replicates. A computer program was developed that calculates parameters such as C50 (concentration of drug causing 50% hemolysis), C100 (concentration of drug causing 100% hemolysis) and beta (slope of the curve) and graphically expresses the hemolytic patterns of various drugs simultaneously. The program can obtain optical densities directly from a 96-well plate ELISA reader by interfacing the microplate reader to the computer or by using a keyboard. This method is useful for screening a large number of hemolytic drugs and requires lower amounts of test compounds. It may also be applicable to quantitative functional assays, such as complement-mediated hemolysis and enumeration of antibody-secreting cells. The program can be obtained from the authors on request.

Animals↗
PubMed1975

The significance of inhibition of prostaglandin synthesis in the selection of non-steroidal anti-inflammatory agents.

A statistically significant correlation can be shown to exist between the concentrations in which established non-steroidal anti-inflammatory agents inhibit prostaglandin synthesis in vitro and the doses in which they exert anti-inflammatory and antipyretic effects in animals. With regard to their antinociceptive activity, this relation is less distinct. Derivatives of clinically effective non-steroidal anti-inflammatory agents can interfere with prostaglandin synthesis in vitro without displaying any activity in vivo. Moreover, the capacity to inhibit this enzyme system is not a property exclusive to non-steroidal anti-inflammatory agents; tricyclic psychotropic drugs exert a similar action. The fact that a substance affects prostaglandin synthetase in vitro is consequently not a reliable indication that it possesses anti-inflammatory properties. On the other hand, the demonstration of effects of this type is important in elucidating the mechanism of action of a drug.

Analgesia↗
PubMed1979

Purification and properties of an antiactivator fraction from bovine serum.

A method is described for the purification of antiactivator from bovine euglobulin-free serum by means of gelfiltration and ion exchange chromatography. The purified antiactivator has no antifibrinolytic activity. It has a molecular weight of about 115,000 and it appears to be a gamma globulin. The dissociation constant of its complex with urokinase is 1.6 x 10(-9) M and the maximum urokinase binding is close to 2000 CTA units per mg. Its concentration in bovine serum is 0.37%. Flufenamate displaces urokinase from the antiactivator at very low concentrations, about 10(-4) M. Cysteine restores its activity if lost by standing. Also an antifibrinolysin fraction is obtained free of antiactivator activity.

Animals↗