Rugstad H E, Glennås A
Division of Clinical Pharmacology, Rikshospitalet, Oslo, Norway.
Scand J Rheumatol. 1988;17(3):175-81. doi: 10.3109/03009748809098780.
Cross-resistance between auranofin and sodium aurothiomalate was tested in two substrains of cultured human epithelial cells. The HEAF cells were previously made resistant to the otherwise lethal concentration of 2 mumol auranofin per litre of culture medium. The HEmyo cells were made resistant to the otherwise lethal effect of 300 mumol sodium aurothiomalate/l. After 4 days of continuous treatment with 2 mumol auranofin/l, 4.6% of the parent HE cells, 55.7% of the HEAF cells and 51.7% of the HEMyo cells continued to grow, compared with controls grown without drug supplement. After 4 days on 300 mumol sodium aurothiomalate/l, 17.6% of the HE cells, 101.0% of the HEMyo cells and 45.3% of the HEAF cells continued to grow. Thus, there was an almost complete cross-resistance to auranofin in the HEMyo cells, and a relative cross-resistance to sodium aurothiomalate in the HEAF cells. The cross-resistance was not found to be related to decreased cytosolic concentration of total gold in the cross-resistant lines.
在两株培养的人上皮细胞亚株中测试了金诺芬与硫代苹果酸金钠之间的交叉耐药性。HEAF细胞先前已对每升培养基中2 μmol金诺芬的致死浓度产生抗性。HEmyo细胞已对300 μmol硫代苹果酸金钠/升的致死效应产生抗性。与未添加药物培养的对照相比,用2 μmol金诺芬/升连续处理4天后,亲代HE细胞的4.6%、HEAF细胞的55.7%和HEmyo细胞的51.7%继续生长。在用300 μmol硫代苹果酸金钠/升处理4天后,HE细胞的17.6%、HEmyo细胞的101.0%和HEAF细胞的45.3%继续生长。因此,HEmyo细胞对金诺芬几乎完全交叉耐药,而HEAF细胞对硫代苹果酸金钠存在相对交叉耐药。未发现交叉耐药与交叉耐药细胞系中总金的胞质浓度降低有关。