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基于抗癌药物的多功能纳米凝胶:通过葡聚糖-姜黄素共轭物自组装实现癌症诊疗

Anticancer drug-based multifunctional nanogels through self-assembly of dextran-curcumin conjugates toward cancer theranostics.

作者信息

Nagahama Koji, Sano Yoshinori, Kumano Takayuki

机构信息

Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology (FIRST), Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.

Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology (FIRST), Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.

出版信息

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2519-22. doi: 10.1016/j.bmcl.2015.04.062. Epub 2015 Apr 25.

DOI:10.1016/j.bmcl.2015.04.062
PMID:25958243
Abstract

Curcumin (CCM) has been received much attention in cancer theranostics because CCM exhibits both anticancer activity and strong fluorescence available for bio-imaging. However, CCM has never been utilized in clinical mainly due to its extremely low water solubility and its low cellular uptake into cancer cells. We fabricated novel CCM-based biodegradable nanoparticles through self-assembly of amphiphilic dextran-CCM conjugates. Significantly high CCM loading contents in the nanoparticles and the high water solubility were achieved. Importantly, the dextran-CCMs nanoparticles were effectively delivered into HeLa cells and exhibited strong fluorescence available for live-cell imaging, although the nanoparticles were not delivered into normal cells. Thus, the dextran-CCMs nanoparticles could be a promising for creation of novel CCM-based cancer theranostics with high efficacy.

摘要

姜黄素(CCM)在癌症诊疗领域备受关注,因为它既具有抗癌活性,又有可用于生物成像的强荧光特性。然而,CCM从未被应用于临床,主要原因是其极低的水溶性以及对癌细胞的低细胞摄取率。我们通过两亲性葡聚糖-CCM共轭物的自组装制备了新型的基于CCM的可生物降解纳米颗粒。纳米颗粒中实现了显著高的CCM负载量和高水溶性。重要的是,葡聚糖-CCM纳米颗粒能够有效地递送至HeLa细胞,并表现出可用于活细胞成像的强荧光,尽管这些纳米颗粒并未递送至正常细胞。因此,葡聚糖-CCM纳米颗粒有望用于创建高效的新型基于CCM的癌症诊疗方法。

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