Tapiéro H, Boule D, Trincal G, Fourcade A
Pathol Biol (Paris). 1987 Jan;35(1):20-6.
The rate of the anthracycline uptake and retention differs with the drug structure and with the cell type. Here we present evidence to show that as compared to carcinoma cells, normal epithelial cells are naturally resistant to adriamycin. Moreover, it is shown that uptake of demethoxy-daunorubicin and THP-ADM is a very rapid process as compared to ADM, epi-ADM or DNR. Cytotoxicity correlates with the intracellular concentration. The relevance of these in vitro findings is considered in the in vivo situation. Resistance to anthracyclines is in part related to decrease accumulation and retention. This resistance can be reversed not only by calcium transport and calmodulin inhibitors but also by co-treatment with aclacinomycin. Wether changes which occurred in acquired resistance can be found in cells with natural resistance to adriamycin remain to be determined.
蒽环类药物的摄取和潴留率因药物结构和细胞类型而异。在此我们提供证据表明，与癌细胞相比，正常上皮细胞对阿霉素天然耐药。此外，研究表明，与阿霉素、表阿霉素或柔红霉素相比，去甲氧基柔红霉素和吡柔比星的摄取过程非常迅速。细胞毒性与细胞内浓度相关。这些体外研究结果在体内情况下的相关性也得到了考量。对蒽环类药物的耐药性部分与药物蓄积和潴留减少有关。这种耐药性不仅可以通过钙转运和钙调蛋白抑制剂逆转，还可以通过与阿克拉霉素联合治疗逆转。对阿霉素天然耐药的细胞中是否存在获得性耐药所发生的变化仍有待确定。
