Sahinoglu T, Grootveld M, Stevens C R, Thompson S J, Claxson A W, Blake D R
Inflammation Group, London Hospital Medical College, UK.
Agents Actions Suppl. 1991;32:71-5. doi: 10.1007/978-3-0348-7405-2_9.
The effect of aurothiomalate in modulating the conversion of xanthine dehydrogenase to its superoxide producing oxidase form in rat and human liver cytosolic preparations has been investigated. Low concentrations (10(-8)-10(-5) mol.dm-3) of this second-line agent were found to inhibit the conversion of the dehydrogenase to its corresponding oxidase form. High concentrations (10(-4) mol.dm-3), however, accelerated this conversion. It is possible that the influence of aurothiomalate on the relative proportions of xanthine dehydrogenase and xanthine oxidase is a reflection of the gold(I) blockage of critical thiol(ate) or sulphido ligands present in this enzymatic system. These effects may form the basis of aurothiomalate's anti-proliferative action on endothelial cells.
已对金硫代苹果酸在大鼠和人肝细胞溶质制剂中调节黄嘌呤脱氢酶向其产生超氧化物的氧化酶形式转化的作用进行了研究。发现这种二线药物的低浓度（10^(-8)-10^(-5) mol·dm^(-3)）可抑制脱氢酶向其相应氧化酶形式的转化。然而，高浓度（10^(-4) mol·dm^(-3)）会加速这种转化。金硫代苹果酸对黄嘌呤脱氢酶和黄嘌呤氧化酶相对比例的影响可能反映了该酶系统中关键硫醇（盐）或硫代配体的金（I）阻断作用。这些效应可能构成金硫代苹果酸对内皮细胞抗增殖作用的基础。
