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一种用于包载姜黄素的脂-聚乙二醇-聚醚酰亚胺复合物,可增强其对姜黄素敏感和耐药细胞的抗肿瘤作用。

A Lipo-PEG-PEI complex for encapsulating curcumin that enhances its antitumor effects on curcumin-sensitive and curcumin-resistance cells.

机构信息

Institute of Molecular Medicine and Bioengineering, National Chiao Tung University, Hsinchu, Taiwan.

出版信息

Nanomedicine. 2012 Apr;8(3):318-27. doi: 10.1016/j.nano.2011.06.011. Epub 2011 Jun 24.

DOI:10.1016/j.nano.2011.06.011
PMID:21704596
Abstract

A cationic liposome-PEG-PEI complex (LPPC) was used as a carrier for the encapsulation of hydrophobic curcumin to give curcumin/LPPC. Curcumin/LPPC had an average size less than 270 nm and a zeta potential of approximately 40 mV. The LPPC encapsulation efficiency for curcumin was about 45%. The authors found it surprising that the cytotoxic activity of the curcumin/LPPC was fivefold higher than curcumin when tested on curcumin-sensitive cells and 20-fold more active against curcumin-resistant cells. Curcumin/LPPC treatment caused a cell cycle arrest at G2/M phase, which rapidly resulted in apoptosis. The increased cytotoxic activity of curcumin/LPPC is likely attributable to its rapid accumulation in the cell. In vivo, administration of curcumin/LPPC inhibited about 60 - 90% of tumor growth in mice bearing CT-26 or B16F10 cells. These results demonstrate LPPC encapsulation technology is able to enhance the effects of antitumor drugs. Use of this technology may provide a new tool for cancer therapy, especially for drug-resistant cancer. From the Clinical Editor: This team of investigators used a cationic liposome-PEG-PEI complex (LPPC) to encapsulate curcumin. The different delivery method resulted in the five-fold increase of cytotoxic activity against curcumin-sensitive cells and twenty-fold against curcumin-resistant cells.

摘要

阳离子脂质体-PEG-PEI 复合物 (LPPC) 被用作包裹疏水性姜黄素的载体,得到姜黄素/LPPC。姜黄素/LPPC 的平均粒径小于 270nm,zeta 电位约为 40mV。LPPC 对姜黄素的包封效率约为 45%。作者惊讶地发现,在测试姜黄素敏感细胞时,姜黄素/LPPC 的细胞毒性活性比姜黄素高五倍,而对姜黄素耐药细胞的活性则高 20 倍。姜黄素/LPPC 处理导致细胞周期停滞在 G2/M 期,迅速导致细胞凋亡。姜黄素/LPPC 的细胞毒性活性增加可能归因于其在细胞内的快速积累。在体内,给予姜黄素/LPPC 抑制了携带 CT-26 或 B16F10 细胞的小鼠约 60-90%的肿瘤生长。这些结果表明 LPPC 包封技术能够增强抗肿瘤药物的疗效。该技术的应用可能为癌症治疗提供一种新的工具,特别是对于耐药性癌症。来自临床编辑:该研究小组使用阳离子脂质体-PEG-PEI 复合物 (LPPC) 包裹姜黄素。不同的给药方法导致对姜黄素敏感细胞的细胞毒性活性增加五倍,对姜黄素耐药细胞的细胞毒性活性增加二十倍。

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