MITOXANTRONE AFFECTS TOPOISOMERASE ACTIVITIES IN HUMAN-BREAST CANCER-CELLS
MITOXANTRONE AFFECTS TOPOISOMERASE ACTIVITIES IN HUMAN-BREAST CANCER-CELLS
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DOI：
10.1016/0006-291x(86)90471-7
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发表时间：
1986-04-29
影响因子：
3.1
通讯作者：
BALDI, A
中科院分区：
文献类型：
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作者：
CRESPI, MD;IVANIER, SE;BALDI, A
在两种人乳腺癌细胞系中研究了抗肿瘤DNA插入剂米托蒽醌对拓扑异构酶I和II的影响。当细胞暴露于不同剂量的米托蒽醌时，发现拓扑异构酶I活性大幅增加。在T47D和MCF-7细胞中，分别以20和40 ng/ml的剂量达到最大效果。拓扑异构酶I活性的增强似乎是可逆的，依赖于暴露于药物的时间和需要细胞完整性。10 ng/mL米托蒽醌作用1小时后，T47D细胞ⅱ型拓扑异构酶被抑制，更高剂量（40 ng/mL）时酶活性无法检测。除非插入物的浓度增加到400-500 ng/mL，否则这种抑制作用不会在体外发生。
The effects of mitoxantrone, an antineoplastic DNA intercalator, on topoisomerase I and II were studied in two human breast cancer cell lines. A large increase of topoisomerase I activity was found when cells were exosed to various doses of mitoxantrone. Maximal effect was achieved with 20 and 40 ng/ml, in T47D and MCF-7 cells respectively. The enhancement on topoisomerase I activity seemed to be reversible, to be dependent on time of exposure to the drug and to require cellular integrity. Type II topoisomerase was inhibited in T47D cells after treatment for one hour with 10 ng/mL of mitoxantrone and enzyme activity was undetectable at higher doses (40 ng/mL). This inhibitory effect did not take place in vitro unless the concentration of the intercalator was increased to 400-500 ng/mL.