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学科主题临床医学
A novel indirubin derivative PHII-7 potentiates adriamycin cytotoxicity via inhibiting P-glycoprotein expression in human breast cancer MCF-7/ADR cells
Shi, Ruizan2,3,4; Li, Wei2,3,5; Zhang, Xiuli2,3; Zhang, Yanjun1,2,3; Peng, Hongwei2,3; Xie, Yinliang2,3; Fan, Dongmei2,3; Liu, Rong2,3; Liu, Xuyi6; Xiong, Dongsheng2,3
关键词Phii-7 Mdr (Multidrug Resistance) P-gp (P-glycoprotein) Reversal Effect
刊名EUROPEAN JOURNAL OF PHARMACOLOGY
2011-11-01
DOI10.1016/j.ejphar.2011.07.047
669期:1-3页:38-44
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]MEDIATED MULTIDRUG-RESISTANCE ; MULTIPLE-DRUG RESISTANCE ; LEUKEMIA-CELLS ; APOPTOSIS ; MECHANISMS ; STRATEGIES ; CHEMOTHERAPY ; DOXORUBICIN ; CARCINOMA ; REVERSAL
英文摘要

Multidrug resistance (MDR) is a major impediment to the effective chemotherapy of many human malignancies, and novel MDR reversal agents are desirable for combination therapy to reduce MDR, enhance anti-tumor activity and reduce side effects. Overexpression of P-glycoprotein (P-gp) is the most prevalent cause of MDR in cancer tissues, and resistance to apoptosis is a common characteristic for the multidrug resistant cancer cells. Our group has synthesized a novel potent anti-tumor indirubin derivative, PHII-7. In this study, MCF-7/ADR cells, an adriamycin (ADR)-selected human breast tumor cell line with the MDR phenotype, were used to investigate the anticancer properties of this novel indirubin derivative. Cytotoxicity and apoptosis assays showed that PHII-7 significantly inhibited cell growth, induced apoptosis, potentiated ADR cytotoxicity and restored chemotherapy sensitivity in the MDR cancer cells. Further studies indicated that by down-regulation of P-gp expression, PHII-7 partially inhibited P-gp efflux pump function and increased intracellular accumulation of Rhodamine 123, a P-gp substrate. These results provide a biochemical basis for possible clinical application of PHII-7 alone or in combination with conventional antineoplastic agents in the treatment MDR tumors. (C) 2011 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000296989500006
引用统计
被引频次:16[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/54930
专题北京大学临床肿瘤学院
作者单位1.Chinese Acad Med Sci, Dept Pharmacol, State Key Lab Expt Hematol, Inst Hematol, Tianjin 300020, Peoples R China
2.Chinese Acad Med Sci, Hosp Blood Dis, Tianjin 300020, Peoples R China
3.Peking Union Med Coll, Tianjin 300020, Peoples R China
4.Shanxi Med Univ, Dept Pharmacol, Taiyuan 030001, Shanxi, Peoples R China
5.Tianjin Med Univ, Canc Inst & Hosp, Tianjin, Peoples R China
6.Beijing Univ, Sch Oncol, Beijing Canc Hosp, Beijing 100036, Peoples R China
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Shi, Ruizan,Li, Wei,Zhang, Xiuli,et al. A novel indirubin derivative PHII-7 potentiates adriamycin cytotoxicity via inhibiting P-glycoprotein expression in human breast cancer MCF-7/ADR cells[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2011,669(1-3):38-44.
APA Shi, Ruizan.,Li, Wei.,Zhang, Xiuli.,Zhang, Yanjun.,Peng, Hongwei.,...&Xiong, Dongsheng.(2011).A novel indirubin derivative PHII-7 potentiates adriamycin cytotoxicity via inhibiting P-glycoprotein expression in human breast cancer MCF-7/ADR cells.EUROPEAN JOURNAL OF PHARMACOLOGY,669(1-3),38-44.
MLA Shi, Ruizan,et al."A novel indirubin derivative PHII-7 potentiates adriamycin cytotoxicity via inhibiting P-glycoprotein expression in human breast cancer MCF-7/ADR cells".EUROPEAN JOURNAL OF PHARMACOLOGY 669.1-3(2011):38-44.
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