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用于原位癌症选择性标记-成像-靶向的抗癌发光金量子团簇。

Anticancer luminescent gold quantum clusters for in situ cancer-selective marking-imaging-targeting.

机构信息

Cardiovascular Research Institute, Yokohama City University, Graduate School of Medicine, Yokohama 236-0004, Japan.

出版信息

Nanoscale. 2017 Jul 6;9(26):9071-9082. doi: 10.1039/c7nr02229h.

DOI:10.1039/c7nr02229h
PMID:28639680
Abstract

Ultrafine Au quantum clusters (QCs) were synthesized by etching host Au nanoparticles in the presence of ethylenediamine (en) and exhibited both strong photoluminescence (PL) and specific anticancer activity. The cutting-edge feature of this QC compound comprises subnanometer-size rhombohedral Au, which consists of 8 units of the anticancer motif, namely, an Au(en) complex (Au(en)QCs), which contributes to photo- and physicochemical stability as well as subcellular theranostic activity in intracellular PL imaging and in situ targeting. Moreover, the Au(en)QCs can be surface-encapsulated by transferrins (Tf) to create TfAu(en)QCs as a multipurpose drug carrier owing to numerous merits, which include cancer-selective biolabeling, high loading/release efficiency, high activity against drug-resistant tumor cells, low toxicity to normal cells, and physiological stability against biothiols, e.g., glutathiones. These versatile features, which are due to intrinsic optical and anticancer properties, provide potential as a single-drug delivery PL probe for preclinical applications, which has yet to be achieved using conventional nanoclusters.

摘要

超精细金量子团簇(QCs)在乙二胺(en)的存在下通过刻蚀主体金纳米颗粒而合成,并表现出强的光致发光(PL)和特定的抗癌活性。该 QC 化合物的最先进特征包括亚纳米尺寸的菱面体金,它由 8 个抗癌基序组成,即金(en)配合物(Au(en)QCs),这有助于光物理化学稳定性以及细胞内 PL 成像和原位靶向的亚细胞治疗活性。此外,由于具有多种优点,例如癌症选择性生物标记、高载药量/释放效率、对耐药肿瘤细胞的高活性、对正常细胞的低毒性以及对生物硫醇(例如谷胱甘肽)的生理稳定性,Au(en)QCs 可以被转铁蛋白(Tf)表面包裹,从而形成 TfAu(en)QCs 作为多用途药物载体。这些多功能特性归因于内在的光学和抗癌特性,为临床前应用提供了作为单一药物递送 PL 探针的潜力,而这是使用传统纳米簇尚未实现的。

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