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Usage

Uses

Used in Pharmaceutical Industry:
Aurothioglucose is used as a pharmaceutical agent for the adjunctive treatment of adult and juvenile rheumatoid arthritis. It helps manage the symptoms and progression of the disease by reducing inflammation and joint damage.
Used in Research Applications:
Aurothioglucose is used in redox stress survival assays in human cell lines, providing valuable insights into the mechanisms of cellular stress response and survival under oxidative conditions.
Used in Experimental Animal Models:
Aurothioglucose is used to induce an obese phenotype in mice, serving as a valuable tool for studying the effects of obesity on various physiological processes and for testing potential treatments for obesity-related conditions. It is also used to produce obesity in experimental animals, which helps researchers understand the impact of obesity on health and develop potential interventions.

History

In 1927, aurothioglucose was found to relieve joint pain when used to treat bacterial endocarditis. The area of chrysotherapy had begun. Subsequent investigations led to an extensive study of gold compounds in Great Britain by the Empire Rheumatism Council, which reported in 1961 that sodium aurothiomalate was effective in slowing the development of progressive joint diseases. Both aurothioglucose and sodium aurothiomalate are orally ineffective and are administered by IM injection. In 1985, the first orally effective gold compound for arthritis, auranofin, was introduced in the United States. Several other gold compounds have been evaluated clinically but do not appear to offer advantages in terms of efficacy or toxicity.

Biochem/physiol Actions

Aurothioglucose, a gold compound used clinically to treat rheumatoid arthritis, has recently been found to be a potent PKCiota-Par6 interaction inhibitor, with an IC50 approximately 1 μM. Disruption of this interaction disrupts a rac1 signaling pathway that is required for transformed growth in non-small-cell lung cancer.

Clinical Use

Aurothioglucose is highly water soluble, and its aqueous solutions decompose on long standing. It therefore is available as a suspension in sesame oil. Gold content is approximately 50%. Following IM injection, it is highly protein bound (95%), and peak plasma levels are achieved within 2 to 6 hours. Following a single 50-mg dose, the biological half-life ranges from 3 to 27 days, but following successive weekly doses, the half-life increases to 14 to 40 days after the third dose. The therapeutic effect does not correlate with serum plasma gold levels but appears to depend on total accumulated gold. Aurothioglucose is indicated for the adjunctive treatment of adult and juvenile rheumatoid arthritis.

Safety Profile

Confirmed carcinogen with experimental carcinogenic and neoplastigenic data. A deadly human poison by an unspecified route. An experimental poison by intramuscular route. Moderately toxic by subcutaneous and intravenous routes. Human systemic effects: nausea or vomiting, cholestatic jaundlce, and eye effects. An experimental teratogen. Other experimental reproductive effects. See also GOLD COMPOUNDS. When heated to decomposition it emits very toxic fumes of SOx. Used to treat rheumatoid arthritis.

Purification Methods

Purify it by dissolving it in H2O (0.05g in 1mL) and precipitating it by adding EtOH. It yields yellow crystals with a slight mercaptan odour. It decomposes slowly in H2O, and is soluble in propylene glycol but insoluble in EtOH and other common organic solvents. [Caterson & Taylor FEBS Lett 98 351 1979, Cooney et al. Biochem J 259 651 1989.]

InChI:InChI=1/C6H12O5S.Au/c7-1-2-3(8)4(9)5(10)6(12)11-2;/h2-10,12H,1H2;/q;+1/p-1/t2-,3-,4+,5-,6-;/m1./s1/rC6H11AuO5S/c7-13-6-5(11)4(10)3(9)2(1-8)12-6/h2-6,8-11H,1H2/t2-,3-,4+,5-,6-/m1/s1