期刊
INTERNATIONAL JOURNAL OF LABORATORY HEMATOLOGY
卷 32, 期 1, 页码 E123-E131出版社
WILEY-BLACKWELL
DOI: 10.1111/j.1751-553X.2009.01145.x
关键词
Proteasome inhibitor; bortezomib; P-gp; leukemia
类别
资金
- Shanghai science and technology [07ZR14146, 064119511]
- National Natural Science Foundation of China [30873042]
The aim of this study is to clarify the efficacy of proteasome inhibitor bortezomib to multidrug resistant (MDR) acute leukemia cells. We observed the effects of bortezomib on a P-glycoprotein (P-gp) positive leukemia line K562/A02. The results showed that bortezomib has significant effects on P-gp positive K562/A02 cells including cytotoxicity (48 h IC50: 171.36 nm), induction of apoptosis (31.71 +/- 1.07% apoptotic cells after 24 h treatment at 100 nm), and inhibition of proteasome chymotrypsin-like activity (relative activity to untreated controls: 20.07 +/- 0.66% at 24 h with 10 nm bortezomib). These effects were lower than those observed in K562 cells (IC50, percentage of apoptotic cells, relative chymotrypsin-like activity to untreated controls were 56.28 nm, 77.95 +/- 0.35%, 5.35 +/- 2.05% after the same treatments, respectively). No synergy between daunorubicin and bortezomib was shown in the killing of K562/A02 cells (synergistic ratios were < 1). P-gp expression levels did not decrease in K562/A02 cells after bortezomib treatment. Pretreatment with bortezomib does not improve the intracellular anthracycline concentration in K562/A02 cells. Bortezomib shows a promising effect for the treatment of refractory/relapsed leukemia, but it does not improve the effect of anthracycline to MDR leukemia cells.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据