与柔红霉素相比，伊达比星和伊达比星醇受拓扑异构酶II相关多药耐药性的影响较小。

Idarubicin and idarubicinol are less affected by topoisomerase II-related multidrug resistance than is daunorubicin.

作者信息

Fukushima T, Inoue H, Takemura H, Kishi S, Yamauchi T, Inai K, Nakayama T, Imamura S, Urasaki Y, Nakamura T, Ueda T

机构信息

First Department of Internal Medicine, Fukui Medical University, Matsuoka, Japan.

出版信息

Leuk Res. 1998 Jul;22(7):625-9. doi: 10.1016/s0145-2126(98)00060-5.

DOI:10.1016/s0145-2126(98)00060-5

PMID:9680113

Abstract

We investigated the cytotoxicity and cellular pharmacology of idarubicin (IDA), idarubicinol (IDAol) and daunorubicin (DNR) in K562/VP-H2 cells, which show topoisomerase II-related multidrug resistance but do not overexpress P-glycoprotein. K562/VP-H2 cells were less resistant to IDA and IDAol than to DNR. There was no significant difference in the accumulation of each drug between K562 and K562/VP-H2 cells. The cleavage of DNA induced by each drug was decreased in K562/VP-H2 cells, however, the decrease in cleavage in K562/VP-H2 cells was less with IDA and IDAol than with DNR. These results suggest that IDA and IDAol have more cytotoxic potency than DNR in topoisomerase II-related multidrug-resistant leukemia cells.

摘要

我们研究了伊达比星（IDA）、伊达比星醇（IDAol）和柔红霉素（DNR）对K562/VP-H2细胞的细胞毒性和细胞药理学特性，该细胞表现出拓扑异构酶II相关的多药耐药性，但不高表达P-糖蛋白。K562/VP-H2细胞对IDA和IDAol的耐药性低于对DNR的耐药性。K562细胞和K562/VP-H2细胞之间每种药物的蓄积没有显著差异。每种药物诱导的DNA裂解在K562/VP-H2细胞中减少，然而，与DNR相比，IDA和IDAol在K562/VP-H2细胞中引起的裂解减少较少。这些结果表明，在拓扑异构酶II相关的多药耐药白血病细胞中，IDA和IDAol比DNR具有更强的细胞毒性效力。