Anti-inflammatory and Antiarthritic Agents

Gold has been used in medicine for many centuries, and since the 1920s several injectable gold compounds have been widely used for the treatment of rheumatoid arthritis. Recent reviews of the medicinal uses of gold compounds have been published (412-414). 

The only oral complex in clinical use is auranofin 92 (Ridaura), containing tetraacetyl-j8-D-thioglucose and triethyl phosphine ligands. Auranofin is a lipophilic complex, a monomer containing linear two-coordinate Au(I). 

A common metabolite found in the urine and plasma of patients treated with gold drugs is [Au(CN)2], an ion which readily enters cells and can inhibit the oxidative burst of white blood cells. It may therefore be an active metabolite of gold drugs. It also exhibits anticancer and anti-HIV activity. The high Au contents of red blood cells of smokers receiving gold therapy has been attributed to the inhalation of HCN in smoke (420). 

Under conditions mimicking red blood cell concentrations, Elder et al. (421) have observed that [Au(CN)2] reacts with GSH to form [Au(SG)2] , which is also very stable. Because of the high concentration of GSH in the cells, the concentration of [Au(SG)2] in cells may be high. 

The radical anion superoxide 02 is a product of activated leukocytes and endothelial cells and has been postulated to be a mediator of isch-emia-reperfusion injury and inflammatory and vascular diseases. Various superoxide dismutase (SOD) enzymes are known Cu,Zn-SOD in the cytoplasm of eukaryotic cells, Mn-SOD in mitochondria, and Fe-SOD and Mn-SOD in prokaryotic cells. They catalyze the conversion of 02 into H202 and 02 

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Scherrer RA. Introduction to the chemistry of anti-inflammatory and antiarthritic agents. In Scherrer RA, Whitehouse MW, eds. Anti-Inflammatory Agents, vol 1. New York Academic Press, 1974 35-55. 

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