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PubMedDate not supplied

[Criteria of pharmacologic effectiveness of antioxidant and membrane-stabilizing drugs in various disorders of cerebral circulation].

The criteria of the effectiveness of preparations possessing the antioxidative and membrane reparative properties in 135 patients with different clinical forms of disorders of the cerebral circulation were developed. It was found that the effectiveness of antioxidative and membrane stabilizing drugs in relieving consequences of free radical aggression as compared with traditional means varied and manifested itself in such an order: essenciale----alpha-tocopherol----unithiol. The presented methods of therapy and appropriate drugs may be recommended for the introduction in the complex of therapeutic and rehabilitative measures.

Cerebrovascular Disorders↗
PubMed1988

Oleic acid-induced pulmonary injury in rats: potential role of sulfidopeptide leukotrienes.

Lung injury following intravenous oleic acid is characterized by pulmonary edema, leukopenia and hypoxemia. Because leukotrienes can increase permeability and cause leukocyte adherence, we evaluated their potential role in oleic acid-induced lung injury in the anesthetized rat using a selective LTD4/E4 antagonist, LY171883. 99mTc-albumin and 99mTc-red blood cells (99mTc-RBC) were used to measure changes in the pulmonary permeability index and intravascular space by non-invasive scintigraphy. Intravenous oleic acid (0.06 ml/kg) increased the pulmonary permeability index 11 (P less than 0.01) and 5.8 fold (P less than 0.01) at 5 and 50 min after its injection compared to baseline, but had no effect on mean pulmonary arterial pressure or pulmonary distribution of 99mTc-RBC. Oleic acid also induced arterial hypoxemia, and increased bronchoalveolar lavage-fluid levels of immunoreactive (i) leukotriene LTC4 from 0.40 +/- 0.14 ng/ml to 2.27 +/- 0.55 ng/ml (mean +/- S.E.M., n = 4, P less than 0.05) and iLTB4 (from 0.42 +/- 0.05 ng/ml to 1.91 +/- 0.63 ng/ml, n = 5-7, P less than 0.01). LY171883 attenuated the elevated permeability by 24% and 68% at 5 (P less than 0.05) and 50 min (P less than 0.01), but did not alter the hypoxemia. These results support the hypothesis that oleic acid elevates leukotriene levels which may increase pulmonary vascular permeability. Furthermore, they suggest that the prevention of elevated pulmonary vascular permeability and edema may be necessary, but are clearly not sufficient to prevent arterial hypoxemia following oleic acid injury in the rat.

Acetophenones↗
PubMedDate not supplied

In vivo renal tubular secretion and metabolism of the disulfide of 2,3-dimercaptopropane-1-sulfonate.

The in vivo renal tubular secretion and metabolism of the disulfide of the heavy metal-complexing agent 2,3-dimercaptopropane-1-sulfonate (DMPS) was examined in the Sperber preparation. DMPS was readily oxidized to DMPS disulfide when incubated with chicken plasma, with whole blood or with urine in the presence of transition metals. Net reduction of the disulfide was not detected when the disulfide was incubated with chicken blood. When the disulfide was infused into the saphenous vein of chickens at a rate of 1 mumol of DMPS equivalents.min-1.kg of body weight-1, 62% of the DMPS disulfide that entered the renal portal circulation of the ipsilateral kidney was excreted in the urine unchanged during a single pass through the peritubular capillaries, 28% was excreted as DMPS, and 9% as an unidentified mixed disulfide. Net reduction of DMPS disulfide to DMPS occurred in vitro in rat kidney cytosol (pH 7.4) supplemented with 0.5 or 5.0 mM reduced glutathione. Reduction of DMPS disulfide to DMPS also occurred in EDTA-Tris HCl (pH 9) containing glutathione disulfide and glutathione reductase. Intracellular reduction of DMPS disulfide to DMPS in the kidney, involving a glutathione-disulfide exchange reaction, may be important for the in vivo activity of DMPS as a complexing agent for mercury.

Animals↗
PubMed1988

[Effect of phosphaden and unithiol on the cyclase system of the small intestine mucosa in rabbits in experimental salmonellosis].

The study was made on 59 chinchilla rabbits. S. typhimurium 1847 live culture was introduced into the lumen of an isolated loop of the thin intestine. The activity of adenylate cyclase (AC), guanylate cyclase (GC), the levels of cyclic adenosine 3,5-monophosphate (cAMP), cyclic guanosine 3,5-monophosphate (cGMP), the activity of cAMP- and cGMP-phosphodiesterases were determined in the mucous membrane of the ligated part of the intestine. Considerable fluid accumulation in the loop, activation of AC and cGMP-phosphodiesterase, a rise in the level of cAMP and a drop in the level of cGMP in the mucosa of the ligated part of the intestine were registered. In one group of the animals phosphadene and in the other group unitiol were introduced into the infected intestinal loop; as a result, a decrease in the accumulation of fluid in the loop, on the average, by 40% and a tendency to an increase in the level of cAMP and a drop in the level of cGMP in the mucous membrane of the ligated part of the intestine were observed. Changes in the level of cGMP play, seemingly, a more important role in the development of diarrhea in salmonellosis.

Adenosine Monophosphate↗
PubMedDate not supplied

Determination and metabolism of dithiol chelating agents. III. Formation of oxidized metabolites of 2,3-dimercaptopropane-1-sulfonic acid in rabbit.

Disulfide metabolites of 2,3-dimercaptopropane-1-sulfonic acid (DMPS), a heavy metal chelating agent, have been found in the urine of catheterized rabbits after a single dose of DMPS. After treating the urine with a reducing agent such as NaBH4, a 20-fold increase in DMPS was observed within 6 hr after administration. This suggested the presence of disulfide metabolites of DMPS. The disulfide metabolites were isolated from urine by extraction and were further purified by ion-interaction reverse phase HPLC. Upon reduction with NaBH4 or dithiothreitol, the isolated disulfides converted to DMPS. The isolated metabolites were not chelates of copper or zinc as determined by atomic absorption. Negative ion fast atom bombardment mass spectra indicated that the isolated metabolites were cyclic and acyclic polymeric disulfides of DMPS. The cyclic polymeric disulfides consisted of dimeric and trimeric forms of DMPS. One of the acyclic polymeric disulfides was identified as a DMPS dimer. Urinary excretion profiles of rabbits revealed that the majority of the altered DMPS consisted of cyclic and acyclic polymeric disulfides of DMPS. The cyclic disulfides increased with time while the acyclic disulfides decreased with time, suggesting that the acyclic forms are intermediates and oxidize to the cyclic forms. The rapid formation of stable 8-membered cyclic dimeric and 12-membered cyclic trimeric disulfides of DMPS strongly suggests that oxidation-reduction reactions are occurring. Both spontaneous and enzymatic oxidation mechanisms appear to be involved.

Animals↗
PubMed1985

[Comparative analysis of the effectiveness and tolerance of chrysanol and myochrysine in patients with rheumatoid arthritis (preliminary report)].

Fifty patients with a significant rheumatoid arthritis (RA) were treated with gold salts for 6 months to 4 years. Patients with highly active conditions (stages II-III) and with erosive arthritis (stages IIb-IV) prevailed. Extraarticular manifestations were recognized in 76% of the patients. The efficacy of chrisanol given in a dose of 1.5 ml of a 5% solution was compared to that of myocrisin in a dose of 50 mg, i. e. 25 mg metallic gold once a week. The efficacy of the drugs was evaluated from their effects on the disease activity (clinical manifestations of the articular syndrome, ESR, morphological signs of rheumatoid synovitis) and progression (the rate of the development of erosive arthritis in hand and foot joints, the time course of serum RF content, and systemic disease manifestations). These characteristics were examined with the aid of modern ultrasonic and radionuclide research methods. The evaluations were made by the treatment onset and by months 3, 6, 12 and 18 of the treatment. Analysis of the data obtained attests to a high clinical efficacy of both the drugs exhibiting basic activity which is confirmed by a decrease in the degree of the morphological manifestations of synovitis and extraarticular signs of RA, particularly of myocarditis. A method for following up outpatients to prevent grave complications of chrysotherapy is offered.

Adolescent↗
PubMed1987

Traditional remedies and lead intoxication.

Three Saudi children suffered from lead intoxication as a result of ingestion of a preparation prescribed by a traditional practitioner. Two of them showed no symptoms of lead intoxication while the third child gave a history of symptomatic intoxication in the form of convulsions. The blood lead levels were increased in all patients and radiographic lead bands were seen in the long bones of the three children. The blood lead concentration was decreased by Na-Ca-EDTA and BAL treatment in the three patients.

Bone and Bones↗