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At least 901 records · Page 50Linked to original sources
PubMed1978

Chemical structure and biodegradability of halogenated aromatic compounds. Substituent effects on dehydrogenation of 3,5-cyclohexadiene-1,2-diol-1-carboxylic acid.

The dehydrogenation of substituted 3,5-cyclohexadiene-1,2-diol-1-carboxylic acids by dihydrodihydroxybenzoic acid dehydrogenases from benzoate grown cells of Alcaligenes eutrophus and Pseudomonas sp. B 13 and 3-chlorobenzoate grown cells of the latter organism was examined. No significant differences (Km and Vrel values) were detected for the enzymes from both organisms. The same dihydrodihydroxybenzoic acid dehydrogenase is formed in Pseudomonas sp. B13 during growth on benzoate as well as on 3-chlorobenzoate. The lower turnover rates of 3- and 5-chlorodrodihydroxybenzoic acid compared to dihydrodihydroxybenzoic acid are counterbalanced by an increase in specific activity. With the exception of 4-substituted dihydrodihydroxybenzoic acids exhibiting relative high Km values, only slight sterical and electronic substituent effects are evident. Reaction rates were never reduced to a critical level.

Alcaligenes↗
PubMed1985

Non-hereditary angioedema treated with tranexamic acid. A 6-month placebo controlled trial with follow-up 4 years later.

Ten patients with frequent attacks of non-hereditary angioedema were treated with tranexamic acid or placebo in a double blind manner, each period lasting 3 months. During the tranexamic acid period nine patients became symptom-free, or substantially improved, while one was unaffected (P less than 0.05). In four patients itching was a major accompanying complaint which was relieved in three. Diarrhoea and abdominal discomfort were more pronounced during tranexamic acid treatment (P less than 0.05), but only necessitated dose reduction in one patient. Four years later contact was obtained with eight of the nine responders and six were still taking tranexamic acid regularly, while in two patients the attacks were so infrequent that the drug was not taken regularly.

Adult↗
PubMed1976

Tranexamic acid (AMCA) and late hyphaema. A double blind study in cataract surgery.

A double blind study of the effect of tranexamic acid (AMCA) on late hyphaema after cataract surgery is reported. A total of 244 patients were included in the study after strict selection. It was shown that the incidence of late hyphaema in the treated group was significantly lower at the 5% level than that in the placebo group. The conclusion is made that the fibrinolytic inhibitor tranexamic acid can be used therapeutically or prophylactically to decrease the risk for re-bleeding after ocular surgery.

Administration, Oral↗
PubMed1970

Trisporic acid synthesis in Blakeslea trispora.

Cultures of the (-) strain of Blakeslea trispora synthesize trisporic acid C, a sex hormone, from precursors made by cultures of the (+) strain. The precursors are nonacidic compounds isolated from the culture medium of the (+) strain by chloroform extraction. Actidione does not inhibit trisporic acid synthesis from isolated precursors, suggesting that the enzymes involved in the synthesis in cultures of the (-) strain are constitutive.

Carbon Isotopes↗
PubMed1989

Effects of fibrinolytic inhibitors on mortality from upper gastrointestinal haemorrhage.

OBJECTIVE: To see whether fibrinolytic inhibitors are of value when given to patients with upper gastrointestinal haemorrhage. DESIGN: Meta-analysis of six randomised double blind placebo controlled trials. Two methods used for obtaining an overall estimate of effect, including a random effects model incorporating any heterogeneity of outcome in the estimate of the overall treatment effect. SETTING: Inpatient care in hospitals in the United Kingdom, Sweden, and Australia. PATIENTS: 1267 Patients admitted to hospital with primary diagnosis of acute upper gastrointestinal haemorrhage. Five of the six trials included a high proportion of elderly patients. Most patients were bleeding from peptic ulcers in the stomach and duodenum (43-88%) or gastric erosions (4-23%). A variable proportion had a degree of clinical shock at entry. INTERVENTIONS: Tranexamic acid 3-6 g/day given intravenously for two or three days followed by 3-6 g/day by mouth for a further three to five days (four trials) or 4.5-12 g/day by mouth for two to seven days (two trials). END POINTS: Frequency of recurrent haemorrhage, need for surgery, and death. MAIN RESULTS: Treatment with tranexamic acid was associated with a 20-30% reduction in the rate of rebleeding, a 30-40% reduction (95% confidence interval 10% to 60%) in mortality. CONCLUSIONS: Treatment with tranexamic acid may be of value to patients considered to be at risk of dying after an upper gastrointestinal haemorrhage.

Clinical Trials as Topic↗
PubMed1982

Effects of tranexamic acid on the coagulation and fibrinolytic systems in pregnancy complicated by placental bleeding.

Treatment with the fibrinolytic inhibitor tranexamic acid was investigated in 12 women with vaginal bleeding in the second half of pregnancy. The aim of the therapy was to accelerate haemostasis in the uteroplacental circulation and to prevent further bleeding at the placental site. Tranexamic acid 1 g 8-hourly was given for 7 days. Serial investigations of coagulation and fibrinolysis were carried out. Plasma fibrinolytic activity, plasminogen, antiplasmin and platelet count significantly decreased during treatment, while antithrombin III and factor VIII related antigen showed a significant increase. Plasma tranexamic acid levels ranged from 5 mg/l to 17 mg/l. Two patients on treatment at the time of delivery had plasma tranexamic acid levels of 9 mg/l and 12 mg/l detected in the umbilical cord venous blood. No adverse effects were detected in any of the mothers and all 12 were delivered of live born infants. Tranexamic acid may have a therapeutic role in accelerating haemostasis in the uteroplacental circulation and thereby reducing the adverse effects of bleeding at the placental site.

Blood Coagulation↗
PubMed1993

Gabapentin actions on ligand- and voltage-gated responses in cultured rodent neurons.

Gabapentin (GBP) is a cyclic gamma-aminobutyric acid (GABA) analog and investigational antiepileptic drug which is effective in the treatment of a variety of human and experimental seizures. GBP's antiepileptic mechanism of action is not known. The present studies tested for effects of GBP on inhibitory (GABA and glycine) and excitatory (N-methyl-D-aspartate (NMDA) and non-NMDA) amino acid neurotransmitter receptors, on repetitive firing of sodium (Na+) action potentials, and on voltage-dependent calcium (Ca2+) channel currents in cultured rodent neurons using intracellular, whole cell, or single channel recording techniques. GBP did not have a significant effect in any experiment when tested at or above concentrations that are therapeutic in humans except for a variable enhancement of NMDA-evoked depolarizations. These results suggest that the antiepileptic activity of GBP is not due to direct effects at receptors for inhibitory or excitatory amino acids or on voltage-dependent Na+ or Ca2+ channels.

Acetates↗
PubMed1996

Nidulal, a novel inducer of differentiation of human promyelocytic leukemia cells from Nidula candida.

Nidulal (1), a novel inducer of differentiation of human HL-60 promyelocytic leukemia cells, was isolated from fermentations of the basidiomycete Nidula candida together with low amounts of niduloic acid (2). Both compounds are bisabolane sesquiterpenes. Their structures were elucidated by spectroscopic methods. In reporter gene assays nidulal (1) preferentially activated the transcription factor complex AP-1-mediated expression of secreted alkaline phosphatase in COS-7 cells. In addition nidulal (1) and niduloic acid (2) exhibited weak cytotoxic and antibiotic activities.

Alkaline Phosphatase↗
PubMed1981

Inhibition of tumour vascularization by tranexamic acid. Experimental studies on possible mechanisms.

The vascularization of an intramuscularly transplanted rat sarcoma was studied by microangiography. Administration of tranexamic acid as well as of indomethacin reduced the vascular connections between tumour and surrounding normal muscle. These drugs also reduced tumour growth rate irrespective of whether they were administered early or late during tumour growth. An electron microscopy study of tumour specimens from animals given tranexamic acid did not reveal any degenerative vascular changes. One explanation of the inhibition of tumour growth and vascularization by tranexamic acid and by indomethacin may be reduction of a local inflammatory reaction induced by tumour transplantation and stimulating tumour vascularization.

Angiography↗
PubMed1976

4-hydroxycyclohexane-1-carboxylic acid: an unusual compound isolated from the urine of children with suspected disorders of metabolism.

1. An unknown compound has been isolated in the acidic fraction of urine samples taken from several children suspected of having metabolic disorders. 2. This unknown has been characterized using a gas chromatograph/mass spectrometer/computer system. Both the high and low resolution mass spectra have been determined and a structure proposed. 3. Authentic samples were synthesized and compared to the unknown and a final proof of structure is presented. The compound, 4-hydroxycyclohexane-1-carboxylic acid, is suspected to come from a dietary source but the actual genesis will be determined in future work.

Child↗
PubMed1986

The inhibitory effect of tranexamic acid on human ovarian carcinoma cell grown in vitro and in vivo.

Effects of tranexamic acid on tumor growth were examined by using five kinds of human cultured cell lines derived from ovarian malignant tissues. An optimum inhibitory effect on cell proliferation was observed at a concentration of 10 mg/ml tranexamic acid, while replication of a clear cell carcinoma cell line (OK) was not inhibited by any concentration of tranexamic acid used in the present study. Exposure of a cystadenocarcinoma cell line (HR) to 10 mg/ml tranexamic acid for 2 hr resulted in significant growth retardation of tumors formed in nude mice. Further, tranexamic acid seemed to change the morphology of the ovarian carcinoma cells to enlarged cells with abundant cytoplasm. These results suggest that fibrinolytic factors are associated with growth of the tumor and tranexamic acid is useful as an adjuvant therapy for ovarian carcinoma.

Adenocarcinoma↗
PubMedDate not supplied

[A method for determining arsenic in biological material].

Method of extraction-atomic absorption detection of arsenic in biologic material using naphthenic acid was developed and tested. Method can be used for arsenic detection in postmortem material. It differs from the known method by its accuracy, reliability and simple use.

Arsenic↗
PubMed1990

[Synthesis and inhibition on beta-lactamase of 4-(3-amido-4-substituted phenyl-2-oxo-azetidinonyl-1)methyl-cyclohexane carboxylic acids and -benzoic acids].

Eleven title compounds have been synthesized from trans-4-amino-methyl-cyclohexylic acid and 4-aminomethyl-benzoic acid, and were identified via elemental analysis, IR, 1HMNR and MS. Their beta-lactamase inhibition activity was determined and contrasted with penicillanic acid S-dioxide. The results of the preliminary test show that all the products have beta-lactamase inhibition activity to some extent.

Azetidines↗
PubMed1978

The effect of tranexamic acid on the fibrinolytic activity of vein walls.

16 patients were treated with the fibrinolytic inhibitor tranexamic acid in an initial i.v. dose of 1 g followed by an oral dose of 4 g a day for one week and 3 g a day for two weeks. Biopsy specimens of superficial veins were obtained before and on the last day of treatment and examined histochemically for their fibrinolytic activity. Tranexamic acid did not suppress the fibrinolytic activity in the vessel walls, which is the most important link in the fibrinolytic defence system against thrombosis.

Administration, Oral↗
PubMed1981

The chemical labeling of glutamate decarboxylase in vivo.

Mouse brain glutamate decarboxylase(s) was specifically titrated in vivo and in crude brain homogenates by a combination of gabaculine and [alpha-3H]acetylenic gamma-aminobutyric acid. This specific titration is based on the differential spectra of action of these two mechanism-based enzyme inactivators. The specificity of the titration in vitro was demonstrated by showing that the time course of radioactivity incorporation exactly paralleled the time course for glutamate of decarboxylase inactivation. Furthermore, pretreatment of the crude homogenate with aminooxyacetic acid and alpha-methyl-trans-3-dehydroglutamate, two inactivators of glutamate decarboxylase which function by entirely different mechanisms, decreased count incorporation ([alpha-3H]acetylenic gamma-aminobutyric acid) to the same extent as the activity was decreased. Injection of [alpha-3H]acetylenic gamma-aminobutyric acid intraperitoneally after gabaculine injection led to incorporation of 0.46 nmol of inactivator/mouse brain, when approximatley 70% of the enzyme was inactivated. This means that there is approximately 0.66 nmol of glutamate decarboxylase/0.5 g of mouse brain, assuming the stoichiometry of inactivator bound to enzyme is one. This value is similar to the one (0.646 nmol) obtained from a calculation based on the enzyme purification data (Wu, J.-Y. (1974) in gamma-Aminobutyric Acid in Nervous System Function (Roberts, E., Chase, E. N., and Tower, D. B., eds) pp. 7-55, Raven Press, New York).

Alkynes↗
PubMedDate not supplied

[The mechanism of action of trisportic acids on the carotene-synthesizing enzymes of the (-) strain of Blakeslea trispora].

Trisporic acids were found to increase the content of carotene, protein, and RNA in the (-)strain of Blakeslea trispora. Trisporic acids are inductors of the synthesis of carotenogenous enzymes as was found in experiments with the inhibitor of transcription (cycloheximide) and translation (actinomycin D). Trisporic acids stimulate the formation of neutral fractions of the sex hormone, the process being regulated presumably at the level of posttranscription control.

Carotenoids↗
PubMed1996

Probing pH and pressure effects on the apomyoglobin heme pocket with the 2'-(N,N-dimethylamino)-6-naphthoyl-4-trans-cyclohexanoic acid fluorophore.

The environmentally sensitive fluorophore 2'-(N,N-dimethylamino)-6-naphthoyl-4-trans-cyclohexanoic acid (DANCA) has been used to probe the apomyoglobin heme pocket. The unexpected polarity of this domain is generally interpreted as arising from dynamic dipolar relaxation of the peptide dipoles surrounding the heme pocket. In the present work we reexamine the photophysical properties of DANCA in a variety of solvents and complexed with apomyoglobin (apoMb) to further probe the heme pocket environment as a function of external solvent conditions. Absorption and excitation spectra in a number of solvents are consistent with the well-known pi*<--pi (LE) and pi*<--n (CT) electronic absorption transitions observed for naphthylamine derivatives. Dual emission is also a well-documented property of such derivatives. Based on the time scale of the heterogeneity in the decay of the DANCA fluorophore observed in a series of solvents, we propose that the emission properties of DANCA in apoMb are not uniquely attributable to dynamic relaxation events, but also reflect dual emission from both a long-lived, red CT state and the shorter-lived, blue LE state. The pH studies in the range of pH 5-9 of the emission properties of DANCA in apoMb support this hypothesis. They also suggest a specific interaction of DANCA with one or both of the pocket histidyl residues, which leads to a drastic static quenching and red shift of the bound DANCA fluorescence upon protonation. Similar effects are observed with increasing pressure, indicating that these two perturbations alter the DANCA-apoMb complex in a similar fashion. The pressure-induced form of the protein is distinct both energetically and structurally from the previously characterized acid intermediate, in that it is populated above pH 5 and retains a significant degree of integrity of the heme pocket.

Animals↗