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基于金簇的多功能近红外发射纳米复合物用于肿瘤成像和治疗。

Multifunctional near-infrared-emitting nano-conjugates based on gold clusters for tumor imaging and therapy.

机构信息

Department of Biomedical Engineering, School of Life Science and Technology, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Gulou District, Nanjing 210009, China.

出版信息

Biomaterials. 2012 Nov;33(33):8461-76. doi: 10.1016/j.biomaterials.2012.08.034. Epub 2012 Aug 28.

Abstract

Gold nanoclusters (NCs) were functionalized as a fluorescent probe and a pro-drug intended for tumor diagnosis and therapy. Firstly, Au NCs were conjugated with methionine (Met) and MPA, a near-infrared (NIR) fluorescent dye, giving a probe, Au-Met-MPA. The tumor targeting capability endowed by Met as well as low cytotoxicity of this contrast agent and its clinical potential for tumor targeting imaging were demonstrated in vitro and in vivo. Secondly, Doxorubicin (DOX), a widely used clinical anti-cancer drug, was immobilized on the methionine modified Au NCs to form a pro-drug, Au-Met-DOX. The enhanced tumor affinity and improved anti-tumor activity of this pro-drug were demonstrated. Results in this study suggest not only the prospect of non-toxic Au NCs modified with functional ligands for tumor-targeted imaging, but also confirm the promising future of Au NCs as a core for the design of pro-drug in the field of cancer therapy.

摘要

金纳米簇 (NCs) 被功能化为荧光探针和前药,用于肿瘤的诊断和治疗。首先,将 Au NCs 与蛋氨酸 (Met) 和 MPA 缀合,MPA 是一种近红外 (NIR) 荧光染料,得到探针 Au-Met-MPA。Met 赋予的肿瘤靶向能力以及该对比剂的低细胞毒性及其在肿瘤靶向成像方面的临床应用潜力在体外和体内得到了证明。其次,将阿霉素 (DOX),一种广泛应用于临床的抗癌药物,固定在蛋氨酸修饰的 Au NCs 上形成前药 Au-Met-DOX。证明了该前药具有增强的肿瘤亲和力和提高的抗肿瘤活性。本研究结果不仅表明了用功能配体修饰的无毒 Au NCs 用于肿瘤靶向成像的前景,还证实了 Au NCs 作为癌症治疗领域前药设计核心的广阔前景。

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