Theranostics 2017; 7(7):1781-1794. doi:10.7150/thno.18437

Research Paper

Dual-Responsive Molecular Probe for Tumor Targeted Imaging and Photodynamic Therapy

Xiaoqing Meng1, 2*, Yueting Yang1*, Lihua Zhou1, 3, li Zhang1, Yalin Lv1, Sanpeng Li1, 2, Yayun Wu1, Mingbin Zheng1,4,5, Wenjun Li1, Guanhui Gao1, Guanjun Deng1,2, Tao Jiang1, Dapeng Ni1, 2, Ping Gong1, 4, 5✉, Lintao Cai1✉

1. Guangdong Key Laboratory of Nanomedicine, CAS Key Lab of Health Informatics, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China;
2. University of Chinese Academy of Sciences, Beijing 100049, China;
3. College of Life Sciences, Hunan Normal University, Changsha 410081, China;
4. Guangdong Key Laboratory for Research and Development of Natural Drugs, Guangdong Medical University, Dongguan 523808, China;
5. State Key Laboratory of Chemo/Biosensing and Chemometrics, Hunan University, Changsha 410082, China.
*Equal contribution

Abstract

The precision oncology significantly relies on the development of multifunctional agents to integrate tumor targeting, imaging and therapeutics. In this study, a first small-molecule theranostic probe, RhoSSCy is constructed by conjugating 5′-carboxyrhodamines (Rho) and heptamethine cyanine IR765 (Cy) using a reducible disulfide linker and pH tunable amino-group to realize thiols/pH dual sensing. In vitro experiments verify that RhoSSCy is highly sensitive for quantitative analysis and imaging intracellular pH gradient and biothiols. Furthermore, RhoSSCy shows superb tumor targeted dual-modal imaging via near-infrared fluorescence (NIRF) and photoacoustic (PA). Importantly, RhoSSCy also induces strongly reactive oxygen species for tumor photodynamic therapy (PDT) with robust antitumor activity both in vitro and in vivo. Such versatile small-molecule theranostic probe may be promising for tumor targeted imaging and precision therapy.

Keywords: Small-molecule theranostic probe, Dual-stimuli sensing, NIRF/PA imaging, tumor targeting, Photodynamic therapy.

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How to cite this article:
Meng X, Yang Y, Zhou L, Zhang l, Lv Y, Li S, Wu Y, Zheng M, Li W, Gao G, Deng G, Jiang T, Ni D, Gong P, Cai L. Dual-Responsive Molecular Probe for Tumor Targeted Imaging and Photodynamic Therapy. Theranostics 2017; 7(7):1781-1794. doi:10.7150/thno.18437. Available from http://www.thno.org/v07p1781.htm