Fukushima T, Kawai Y, Urasaki Y, Yoshida A, Ueda T, Nakamura T
First Department of Internal Medicine, Fukui Medical School, Japan.
Leuk Res. 1994 Dec;18(12):943-7. doi: 10.1016/0145-2126(94)90106-6.
We investigated the antileukemic potency of idarubicinol (IDAol), a 13-dihydro (13-OH) metabolite of idarubicin (IDA), on the HL60 line of human leukemia cells. In contrast to daunorubicinol (DNRol) and to doxorubicinol (DOXol), IDAol showed an extensive accumulation in HL60 cells. The high affinity for DNA and the strong DNA cleavage activity of IDAol were comparable to values for IDA; consequently, IDAol was strongly cytotoxic against HL60 cells. IDAol may play an important role in the clinical efficacy of IDA in patients with acute leukemia, particularly since it persists in the blood for prolonged periods after the administration of IDA.
我们研究了伊达比星醇(IDAol),即伊达比星(IDA)的13-二氢(13-OH)代谢产物,对人白血病HL60细胞系的抗白血病效力。与柔红霉素醇(DNRol)和多柔比星醇(DOXol)不同,IDAol在HL60细胞中大量蓄积。IDAol对DNA的高亲和力和强大的DNA切割活性与IDA相当;因此,IDAol对HL60细胞具有很强的细胞毒性。IDAol可能在IDA治疗急性白血病患者的临床疗效中发挥重要作用,特别是因为在给予IDA后,它在血液中持续存在较长时间。