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Pegylated Phosphotidylethanolamine Inhibiting P-Glycoprotein Expression and Enhancing Retention of Doxorubicin in MCF7/ADR Cells
Wang, Jing1; Qu, Hui1; Jin, Lingtao1; Zeng, Wenfeng1; Qin, Lei1; Zhang, Fayun1; Wei, Xiuli1; Lu, Wanliang2; Zhang, Chunling1; Liang, Wei1
关键词P-glycoprotein Peg-pe Polymeric Drug Carrier Micelle Multidrug Resistance Mdr-1 Sirna Doxorubicin Cancer Chemotherapy
刊名JOURNAL OF PHARMACEUTICAL SCIENCES
2011-06-01
DOI10.1002/jps.22461
100期:6页:2267-2277
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]SENSITIVE POLYMERIC MICELLES ; TUMOR VASCULAR-PERMEABILITY ; FATTY-ACID DIESTERS ; MULTIDRUG-RESISTANCE ; MOLECULAR-MECHANISMS ; CANCER-CELLS ; DRUG ; DELIVERY ; GENE ; TRANSPORTERS
英文摘要

The failure of the clinical treatment of cancer patients is often attributed to drug resistance of the tumor to chemotherapeutic agents. P-glycoprotein (P-gp) contributes to drug resistance via adenosine 5′-triphosphate (ATP)-dependent drug efflux pumps and is widely expressed in many human cancers. Up to date, a few of nanomaterials have shown the effects on P-gp function by different ways. To study the mechanism of the increased cytotoxicity of doxorubicin (DOX) by pegylated phosphotidylethanolamine (PEG-PE) in drug-resistant cancer cells, a series of in vitro cell assays were performed, including identification of P-gp function, quantitative studies on uptake and efflux of DOX, inhibitory effects of blank PEG-PE micelles on mRNA and protein levels of P-gp, and intracellular ATP content alteration. Finally, combining MDR-1 RNA interference (siRNA) with DOX encapsulated in PEG-PE micelles (M-DOX) to improve cytotoxicity of DOX was also studied. M-DOX showed fivefold lower the concentration that caused 50% killing tumor cellthan that of free DOX in the P-gp-overexpressing MCF-7 breast cancer (MCF-7/ADR) cells. M-DOX enhanced the cellular uptake and retention of DOX in MCF-7/ADR cells. PEG-PE block molecules can inhibit P-gp expression through downregulating MDR-1 gene. Cytotoxicity of M-DOX was further improved by knocking down the MDR-1 gene using siRNA in the multidrug-resistant cells. We conclude that the increased cytotoxicity of DOX encapsulated in PEG-PE micelle is due to the reduced P-gp expression by PEG-PE block molecules, and accordingly enhancing the cellular accumulation of DOX. To overcome drug resistance of tumor cells, the combination of nanotechnology and biotechnology could be an effective strategy such as PEG-PE formed micelles and siRNA. (C) 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:2267-2277, 2011

语种英语
WOS记录号WOS:000289442200023
引用统计
被引频次:24[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/400002259/51017
专题北京大学药学院
作者单位1.Chinese Acad Sci, Natl Lab Biomacromol, Inst Biophys, Prot & Peptide Pharmaceut Lab, Beijing 100101, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
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GB/T 7714
Wang, Jing,Qu, Hui,Jin, Lingtao,et al. Pegylated Phosphotidylethanolamine Inhibiting P-Glycoprotein Expression and Enhancing Retention of Doxorubicin in MCF7/ADR Cells[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2011,100(6):2267-2277.
APA Wang, Jing.,Qu, Hui.,Jin, Lingtao.,Zeng, Wenfeng.,Qin, Lei.,...&Liang, Wei.(2011).Pegylated Phosphotidylethanolamine Inhibiting P-Glycoprotein Expression and Enhancing Retention of Doxorubicin in MCF7/ADR Cells.JOURNAL OF PHARMACEUTICAL SCIENCES,100(6),2267-2277.
MLA Wang, Jing,et al."Pegylated Phosphotidylethanolamine Inhibiting P-Glycoprotein Expression and Enhancing Retention of Doxorubicin in MCF7/ADR Cells".JOURNAL OF PHARMACEUTICAL SCIENCES 100.6(2011):2267-2277.
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