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Helvetica Physiologica Et... 1957
Topics: Animals; Aurothioglucose; Mice; Obesity; Weight Loss
PubMed: 13474592
DOI: No ID Found -
Veterinarni Medicina Feb 1976We investigated the effect of a single application of aurothioglucose on the weight and fat content of mice in the case of a limited feed quantity. In the experiment we...
We investigated the effect of a single application of aurothioglucose on the weight and fat content of mice in the case of a limited feed quantity. In the experiment we used 41 mice -- females of the "H" strain, of which 14 served as controls and 27 were experimental mice to which we applied aurothioglucose in the dose of 1 mg g-1 of liveweight, i. p. We found that, under the conditions of feeding a limited quantity of feeds, there occurs in the animals that had been injected with aurothioglucose a statistically significant increase of the weight gains and of the total quantity of fat compared with the control animals.
Topics: Adipose Tissue; Animal Feed; Animals; Aurothioglucose; Body Composition; Body Weight; Female; Gold; Lipid Metabolism; Mice
PubMed: 820037
DOI: No ID Found -
Fitoterapia Apr 2006Goldthioglucose induces in mice a significant increase in body weight, glucose, insulin and lipid levels. Treatment with 250 mg/kg of methanol and ethyl acetate extracts... (Comparative Study)
Comparative Study
Goldthioglucose induces in mice a significant increase in body weight, glucose, insulin and lipid levels. Treatment with 250 mg/kg of methanol and ethyl acetate extracts of Zingiber officinale for 8 weeks produces significant reduction in body weight, glucose, insulin and lipid levels as compared to obese control mice. The reduction in elevated glucose along with elevated insulin levels indicates that the treatment with Z. officinale improves insulin sensitivity.
Topics: Acetates; Animals; Aurothioglucose; Blood Glucose; Body Weight; Female; Zingiber officinale; Insulin; Lipids; Methanol; Mice; Obesity; Phytotherapy; Plant Extracts
PubMed: 16513292
DOI: 10.1016/j.fitote.2006.01.005 -
The American Journal of Medicine Dec 1983The new oral gold compound auranofin differs pharmacokinetically from the existing injectable gold compounds such as gold sodium thiomalate. Following a standard 50 mg...
The new oral gold compound auranofin differs pharmacokinetically from the existing injectable gold compounds such as gold sodium thiomalate. Following a standard 50 mg intramuscular injection of gold sodium thiomalate, plasma gold levels rise sharply, peak between 400 and 800 micrograms/dl in approximately two hours, then decline to approximately 300 micrograms/dl by seven days. With repeated 50 mg weekly injections, stable plasma concentrations are gradually achieved, although absolute levels vary greatly among individual subjects. On the other hand, auranofin is associated with lower (50 to 70 micrograms/dl) and more predictable plasma concentrations. Single-dose kinetic studies using isotopically labelled gold show that the plasma disappearance half-time for gold sodium thiomalate is relatively rapid (approximately six days) compared with 17 days for auranofin. Both compounds are retained within the body over prolonged periods. Retention of auranofin is much less, about 1 percent of the original tracer dose remaining at 180 days, compared with more than 30 percent retention of gold sodium thiomalate. Excretory pathways are notable different. The majority of gold sodium thiomalate (greater than 70 percent) is excreted by the kidneys, with the remaining fraction appearing erratically in the stool. In contrast, the enteric pathway represents the major excretory route for auranofin, with nearly 85 percent of the dose eventually recoverable in the stool and less than 15 percent in the urine. In human subjects, parenterally administered gold is almost universally dispersed among body tissues, although highest concentrations occur in the organs of the reticuloendothelial system and the adrenal and renal cortices. Comparable studies are not available for auranofin, but animal studies show comparatively less affinity for liver, kidney, and spleen. To date, attempts to correlate the pharmacokinetics of the injectable gold compounds with clinical response and toxicity have been largely unsuccessful. The distinctive pharmacokinetic profile of auranofin, when compared with gold sodium thiomalate, may nonetheless account in part for the clinical and pharmacologic differences between these compounds.
Topics: Animals; Anti-Inflammatory Agents; Auranofin; Aurothioglucose; Gold; Half-Life; Humans; Kinetics; Mice; Protein Binding; Rabbits; Rats; Tissue Distribution
PubMed: 6419592
DOI: 10.1016/0002-9343(83)90483-7 -
Annals of Internal Medicine Oct 1986Ninety patients were entered into a randomized, controlled, double-blind trial lasting 12 months to compare auranofin (6 mg/d), and D-penicillamine (250 mg/d for 4... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Ninety patients were entered into a randomized, controlled, double-blind trial lasting 12 months to compare auranofin (6 mg/d), and D-penicillamine (250 mg/d for 4 weeks, 500 mg/d for 4 weeks, then 750 mg/d thereafter) in the treatment of rheumatoid arthritis. Most patients in both groups completed the trial with significant improvement in all quantitative measures of efficacy. Patients treated with D-penicillamine were more likely to have "important improvement" in physician global assessment, swollen joint count, and score and grip strength. The overall frequency of side effects was similar between the two groups; however, more patients were withdrawn for adverse effects from the D-penicillamine group, and proteinuria (greater than or equal to 2+) and thrombocytopenia (less than 100 000 mm3) occurred significantly more frequently with D-penicillamine than auranofin (p = 0.028). These results suggest that in the dosage regimen used, auranofin is safer than D-penicillamine but that D-penicillamine tends to show greater clinical effectiveness in patients with rheumatoid arthritis.
Topics: Arthritis, Rheumatoid; Auranofin; Aurothioglucose; Clinical Trials as Topic; Double-Blind Method; Female; Gold; Humans; Joints; Male; Middle Aged; Movement; Penicillamine; Random Allocation
PubMed: 3092712
DOI: 10.7326/0003-4819-105-4-528 -
Wiener Klinische Wochenschrift.... 1984Parenterally administered gold compounds have been used for decades for treatment of rheumatoid arthritis. The new gold compound triethylphosphine gold (auranofin) can... (Review)
Review
Parenterally administered gold compounds have been used for decades for treatment of rheumatoid arthritis. The new gold compound triethylphosphine gold (auranofin) can be partially absorbed in the gut following oral administration due to its higher lipophilic nature. This is probably also the main cause for the differences in kinetic properties versus the parenteral gold compounds. Following administration of auranofin, there are lower concentrations of gold in blood and organs; 95% of the gold is excreted in feces whereas 70% of gold, following gold sodium thiomalate, is excreted in the urine. These differences have consequences for the mode of adverse reactions. A common property of all gold compounds, however, is the relative distribution in organs. The highest concentrations of gold were found in the reticuloendothelial system, in liver, kidney and spleen, followed by joints. The mode of action of gold compounds is still unexplained. They inhibit some types of experimental inflammation and the activity of various cells involved in inflammatory processes. In some cases auranofin exerts a higher influence. Following incorporation of gold in lysosomes, the impairment of macrophage function appears to be most important. This effect probably influences (indirectly) the immune system since macrophages interact with T- and B-lymphocytes. The significance of these findings for the therapeutic effect of gold compounds is, however, not known. The rate of undesirable effects of gold compounds is very high requiring exact supervision during chrysotherapy. Mucosal and cutaneous reactions are very frequent, followed by proteinuria, diarrhea and thrombocytopenia. Bone marrow aplasia is most serious but relatively rare.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Animals; Anti-Inflammatory Agents; Arthritis, Rheumatoid; Auranofin; Aurothioglucose; Gold; Gold Sodium Thiomalate; Humans; Kinetics; Macrophages
PubMed: 6442062
DOI: No ID Found -
Angewandte Chemie (International Ed. in... 2008
Topics: Antibodies, Monoclonal; Aurothioglucose; Cell Line, Tumor; ErbB Receptors; Ferrosoferric Oxide; Humans; Magnetic Resonance Imaging; Magnetics; Microscopy, Electron, Transmission; Nanoparticles; Particle Size; Surface Properties
PubMed: 17992677
DOI: 10.1002/anie.200704392 -
Journal of Inorganic Biochemistry May 1992The effects of the antiarthritic drugs aurothiomalate (AuTm), aurothioglucose (AuTg), auranofin, its metabolite triethylphosphinegold(I)thioglucose (Et3PAuTg), and... (Comparative Study)
Comparative Study
The effects of the antiarthritic drugs aurothiomalate (AuTm), aurothioglucose (AuTg), auranofin, its metabolite triethylphosphinegold(I)thioglucose (Et3PAuTg), and several related complexes on the growth of Pseudomonas putida were studied. Two strains were used, one of which (BK135) was more sensitive to Et3PAuTg (tolerant up to 4 microM) than the other (BK403; tolerant to at least 500 microM). Gold thiolate complexes and thiolate ligands alone had little effect on growth. Gold phosphine complexes increased the length of the lag phase of growth and reduced oxygen uptake. Marked changes in cellular morphology were determined by electron microscopy. Copper(II) compounds and aurothiomalate were synergistic in their growth inhibitory effects towards these bacteria. Experiments with 195Au suggested that a mechanism does not exist for the short term (minutes) uptake of gold by sensitive or resistant bacteria, but the resistant strain appeared to limit gold uptake over a longer term (hours).
Topics: Antirheumatic Agents; Auranofin; Aurothioglucose; Gold Radioisotopes; Gold Sodium Thiomalate; Hydrogen-Ion Concentration; Microscopy, Electron; Oxygen Consumption; Pseudomonas putida
PubMed: 1355789
DOI: 10.1016/0162-0134(92)80016-o -
Deutsche Medizinische Wochenschrift... Jan 1986
Topics: Abnormalities, Drug-Induced; Adult; Animals; Arthritis, Rheumatoid; Aurothioglucose; Breast Feeding; Female; Gold; Humans; Infant, Newborn; Maternal-Fetal Exchange; Pregnancy; Pregnancy Complications; Rats; Teratogens
PubMed: 3079697
DOI: 10.1055/s-2008-1068397 -
Microbiology Spectrum Feb 2024Auranofin, an FDA-approved drug for rheumatoid arthritis, has emerged as a promising antiparasitic medication in recent years. The gold(I) ion in auranofin is postulated...
Auranofin, an FDA-approved drug for rheumatoid arthritis, has emerged as a promising antiparasitic medication in recent years. The gold(I) ion in auranofin is postulated to be responsible for its antiparasitic activity. Notably aurothiomalate and aurothioglucose also contain gold(I), and, like auranofin, they were previously used to treat rheumatoid arthritis. Whether they have antiparasitic activity remains to be elucidated. Herein, we demonstrated that auranofin and similar derivatives, but not aurothiomalate and aurothioglucose, inhibited the growth of . We found that auranofin affected the biological cycle (lytic cycle) by inhibiting invasion and triggering its egress from the host cell. However, auranofin could not prevent parasite replication once resided within the host. Auranofin treatment induced apoptosis in parasites as demonstrated by its reduced size and elevated phosphatidylserine externalization (PS). Notably, the gold from auranofin enters the cytoplasm of as demonstrated by scanning transmission electron microscopy-energy dispersive X-ray spectroscopy (STEM-EDS) and Inductively Coupled Plasma-Mass Spectrometry (ICP-MS).IMPORTANCEToxoplasmosis, caused by , is a devastating disease affecting the brain and the eyes, frequently affecting immunocompromised individuals. Approximately 60 million people in the United States are already infected with , representing a population at-risk of developing toxoplasmosis. Recent advances in treating cancer, autoimmune diseases, and organ transplants have contributed to this at-risk population's exponential growth. Paradoxically, treatments for toxoplasmosis have remained the same for more than 60 years, relying on medications well-known for their bone marrow toxicity and allergic reactions. Discovering new therapies is a priority, and repurposing FDA-approved drugs is an alternative approach to speed up drug discovery. Herein, we report the effect of auranofin, an FDA-approved drug, on the biological cycle of and how both the phosphine ligand and the gold molecule determine the anti-parasitic activity of auranofin and other gold compounds. Our studies would contribute to the pipeline of candidate anti- agents.
Topics: Humans; Auranofin; Gold; Toxoplasma; Ligands; Aurothioglucose; Arthritis, Rheumatoid; Gold Sodium Thiomalate; Toxoplasmosis; Antiparasitic Agents; Phosphines
PubMed: 38206030
DOI: 10.1128/spectrum.02968-23