Aurothioglucose is an inhibitor of thioredoxin reductase (TrxR; IC50 = 0.065 ?M for the human placental enzyme).1 It is selective for TrxR over glutathione reductase and glutathione peroxidase (GPX; IC50s = >100 and 80 ?M, respectively). Aurothioglucose (100 ?M) inhibits IL-1β-induced production of IL-6 and IL-8 in isolated human rheumatoid synovial fibroblasts.2 It reduces HIV-1 replication induced by TNF-α in OM10.1 cells latently infected with HIV-1 when used at concentrations of 10 and 25 ?M.3 Aurothioglucose (25 mg/kg) improves survival in a mouse model of acute respiratory distress syndrome (ARDS) induced by LPS and hyperoxia.4 It induces obesity and increases food intake and blood glucose levels in genetically diabetic KK mice.5 Formulations containing aurothioglucose have previously been used in the treatment of rheumatoid arthritis.
1.Gromer, S., Arscott, L.D., Williams, C.H., Jr., et al.Human placenta thioredoxin reductase. Isolation of the selenoenzyme, steady kinetics, and inhibition by therapeutic gold compoundsJ. Biol. Chem.273(32)20096-20101(1998) 2.Yoshida, S., Kato, T., Sakurada, S., et al.Inhibition of IL-6 and IL-8 induction from cultured rheumatoid synovial fibroblasts by treatment with aurothioglucoseInt. Immunol.11(2)151-158(1999) 3.Traber, K.E., Okamoto, H., Kurono, C., et al.Anti-rheumatic compound aurothioglucose inhibits tumor necrosis factor-α-induced HIV-1 replication in latently infected OM10.1 and Ach2 cellsInt. Immunol.11(2)143-150(1999) 4.Britt, R.D., Jr., Velten, M., Locy, M.L., et al.The thioredoxin reductase-1 inhibitor aurothioglucose attenuates lung injury and improves survival in a murine model of acute respiratory distress syndromeAntioxid. Redox Signal.20(17)2681-2691(2014) 5.Matsuo, T., and Shino, A.Induction of diabetic alterations by goldthioglucose-obesity in KK,ICR and C57BL miceDiabetologia8(6)391-397(1972)