Bennis S, Garcia C, Robert J
Foundation Bergonié, Bordeaux, France.
Biochem Pharmacol. 1993 May 5;45(9):1929-31. doi: 10.1016/0006-2952(93)90453-4.
We have compared the cytotoxicity, incorporation and metabolism of doxorubicin (dox) and N-l-leucyldoxorubicin (leu-dox) in two human tumor cell lines in culture, the MCF-7 breast cancer line and the K562 leukemia line, and their dox-resistant counterparts. Dox was 3-4-fold more cytotoxic than leu-dox in the MCF-7 lines, and 7-10-fold in the K562 lines. This could be explained by differences in cell incorporation of the drugs, which differs by the same proportion as the cytotoxicities in the various cell lines, rather than by differences in biotransformation of leu-dox into dox, which is similar in all of the cell lines.
我们比较了阿霉素（dox）和N-1-亮氨酰阿霉素（leu-dox）在两种培养的人类肿瘤细胞系（MCF-7乳腺癌细胞系和K562白血病细胞系）及其阿霉素耐药对应细胞系中的细胞毒性、摄取和代谢情况。在MCF-7细胞系中，阿霉素的细胞毒性比亮氨酰阿霉素高3至4倍，在K562细胞系中则高7至10倍。这可以通过药物在细胞摄取方面的差异来解释，其差异比例与各细胞系中的细胞毒性相同，而非亮氨酰阿霉素向阿霉素生物转化的差异，因为在所有细胞系中这种转化都是相似的。
