Meng Xiaoqing, Yang Yueting, Zhou Lihua, Zhang Li, Lv Yalin, Li Sanpeng, Wu Yayun, Zheng Mingbin, Li Wenjun, Gao Guanhui, Deng Guanjun, Jiang Tao, Ni Dapeng, Gong Ping, Cai Lintao
Guangdong Key Laboratory of Nanomedicine, CAS Key Lab of Health Informatics, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
Theranostics. 2017 Apr 10;7(7):1781-1794. doi: 10.7150/thno.18437. eCollection 2017.
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. 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 and . Such versatile small-molecule theranostic probe may be promising for tumor targeted imaging and precision therapy.
精准肿瘤学在很大程度上依赖于多功能试剂的开发，以整合肿瘤靶向、成像和治疗。在本研究中，首个小分子诊疗探针RhoSSCy通过使用可还原二硫键连接子和pH可调氨基将5'-羧基罗丹明（Rho）与七甲川花菁IR765（Cy）共轭构建而成，以实现硫醇/pH双传感。实验证实，RhoSSCy对细胞内pH梯度和生物硫醇的定量分析和成像具有高度敏感性。此外，RhoSSCy通过近红外荧光（NIRF）和光声（PA）显示出卓越的肿瘤靶向双模态成像。重要的是，RhoSSCy还能诱导产生强活性氧用于肿瘤光动力疗法（PDT），在体内和体外均具有强大的抗肿瘤活性。这种多功能小分子诊疗探针可能在肿瘤靶向成像和精准治疗方面具有广阔前景。
