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一种具有内在癌症靶向、成像和光动力特性的近红外七甲川染料。

A NIR heptamethine dye with intrinsic cancer targeting, imaging and photosensitizing properties.

机构信息

Institute of Combined Injury, State Key Laboratory of Trauma, Burns and Combined Injury, Chongqing Engineering Research Center for Nanomedicine, College of Preventive Medicine, Third Military Medical University, 30 Gaotanyan Road, Chongqing 400038, China.

出版信息

Biomaterials. 2012 Mar;33(7):2230-9. doi: 10.1016/j.biomaterials.2011.11.081. Epub 2011 Dec 17.

DOI:10.1016/j.biomaterials.2011.11.081
PMID:22182749
Abstract

The future personalized oncology significantly relies on the development of multifunctional agents to integrate tumor targeting, imaging, and cytotoxic activities. In our recent study, we have recently identified a near infrared fluorescent heptamethine dye, IR-780, with unexpected preferential accumulation in a broad spectra of tumor cells for in vivo tumor targeting and imaging. On the basis of this foregoing work, in this study, we describe here the chemical synthesis and biological characterization of an analog of IR-780, termed as IR-808, which not only possesses similar tumor targeting and imaging properties of IR-780, but also has unique photodependent cytotoxic activity. In addition, IR-808 also exhibits favorable optical and pharmacokinetic properties, as well as good biocompatibility. This dye may hold promise as a candidate multifunctional theranostic agent for future tumor targeted imaging and photodynamic therapy.

摘要

未来的个性化肿瘤学在很大程度上依赖于多功能试剂的发展,以整合肿瘤靶向、成像和细胞毒性作用。在我们最近的研究中,我们最近发现了一种近红外荧光七甲川染料 IR-780,它具有出乎意料的广谱肿瘤细胞优先积累,可用于体内肿瘤靶向和成像。基于这项前期工作,在本研究中,我们描述了 IR-780 的一种类似物,称为 IR-808 的化学合成和生物学特性,它不仅具有与 IR-780 相似的肿瘤靶向和成像特性,而且具有独特的光依赖性细胞毒性活性。此外,IR-808 还表现出良好的光学和药代动力学特性以及良好的生物相容性。这种染料可能有望成为未来肿瘤靶向成像和光动力治疗的候选多功能治疗剂。

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