Key Laboratory of Pesticides and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, 430079 Wuhan, China.
International Joint Research Center for Intelligent Biosensor Technology and Health, Chemical Biology Center, College of Chemistry, Central China Normal University, 430079 Wuhan, China.
Proc Natl Acad Sci U S A. 2019 Feb 5;116(6):1968-1973. doi: 10.1073/pnas.1817021116. Epub 2019 Jan 22.
Fluorescent theranostics probes at the second near-IR region (NIR-II; 1.0-1.7 µm) are in high demand for precise theranostics that minimize autofluorescence, reduce photon scattering, and improve the penetration depth. Herein, we designed and synthesized an NIR-II theranostic nanoprobe 1 that incorporates a Pt(II) metallacycle 2 and an organic molecular dye 3 into DSPE-mPEG5000 (1,2-distearoyl-sn-glycero-3-phosphoethanolamine--[methoxy(polyethylene glycol)-5000]). This design endows 1 with good photostability and passive targeting ability. Our studies show that 1 accurately diagnoses cancer with high resolution and selectively delivers the Pt(II) metallacycle to tumor regions via an enhanced permeability and retention effect. In vivo studies reveal that 1 efficiently inhibits the growth of tumor with minimal side effects. At the same time, improved fluorescent imaging quality and signal-to-noise ratios are shown due to the long emission wavelengths. These studies demonstrate that 1 is a potential theranostic platform for tumor diagnosis and treatment in the NIR-II region.
近红外二区（NIR-II；1.0-1.7 µm）的荧光诊疗探针在精准诊疗方面的需求很高，因为这种探针能够最小化自发荧光、减少光子散射，并提高穿透深度。在此，我们设计并合成了一种将 Pt(II) 金属络合物 2 和一种有机分子染料 3 整合到 DSPE-mPEG5000（1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-甲氧基聚乙二醇 5000）中的 NIR-II 诊疗纳米探针 1。这种设计使 1 具有良好的光稳定性和被动靶向能力。我们的研究表明，1 可以通过高分辨率准确诊断癌症，并通过增强的通透性和保留效应选择性地将 Pt(II) 金属络合物递送到肿瘤区域。体内研究表明，1 能够有效地抑制肿瘤生长，且副作用极小。同时，由于发射波长较长，荧光成像质量和信噪比也得到了提高。这些研究表明，1 是一种用于肿瘤诊断和 NIR-II 区域治疗的潜在诊疗平台。
