Jellum E, Munthe E, Guldal G, Aaseth J
Scand J Rheumatol Suppl. 1979(28):28-36.
Double isotope-labelled auro thiomalate (Au195-C14-thiomalate) has been administered to mice and rats, and the excretory fate and tissue distribution have been studied. The results show that the gold and the thiomalate separate in vivo resulting in protein-bound gold and release of free thiomalate. About half of this thiol is excreted in the urine during the first day and the remaining half is taken up by the tissues. Thiomalate penetrates cellular membranes poorly, but is able to interact slowly with proteins (mixed disulphide formation). Part of the thiomalate which remains in the body is membrane bound. In contrast to penicillamine little thiomalate remains in circulation a few hours after administration. Gas chromatography--mass spectrometry has been used to search for the presence of free thiomalate in rheumatoid arthritis patients on Myocrisin (auro thiomalate) therapy. Thiomalate was found in their urine, but not in serum and synovial fluid 20 hours after administration. As thiomalate is released in the body after administration of Myocrisin. the question arises whether this thiol, like penicillamine, may have a beneficial effect in the treatment of rheumatoid arthritis.
已将双同位素标记的硫代苹果酸金（Au195 - C14 - 硫代苹果酸）给予小鼠和大鼠，并对其排泄去向和组织分布进行了研究。结果表明，金和硫代苹果酸在体内分离，导致形成蛋白质结合金并释放出游离硫代苹果酸。大约一半的这种硫醇在第一天经尿液排出，其余一半被组织摄取。硫代苹果酸穿透细胞膜的能力较差，但能够与蛋白质缓慢相互作用（形成混合二硫键）。体内残留的部分硫代苹果酸与膜结合。与青霉胺不同，给药几小时后，循环中残留的硫代苹果酸很少。已使用气相色谱 - 质谱法来探寻接受硫代苹果酸金治疗的类风湿性关节炎患者体内游离硫代苹果酸的存在情况。给药20小时后，在其尿液中发现了硫代苹果酸，但在血清和滑液中未发现。由于给药后硫代苹果酸在体内释放，因此产生了这样一个问题，即这种硫醇是否像青霉胺一样，可能对类风湿性关节炎的治疗具有有益作用。
