Red AIE conjugated polyelectrolytes for long-term tracing and image-guided photodynamic therapy of tumors

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d AIE conjugated polyelectrolytes for long-term tracing and image-guided photodynamic therapy of tumors 1†

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Hongming Yao , Jun Dai , Zeyan Zhuang , Jinya Yao , Zixuan Wu , Shixuan Wang , 4 1* 4* 2* Fan Xia , Jian Zhou , Xiaoding Lou & Zujin Zhao 1

College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou 311121, China; State Key Laboratory of Luminescent Materials and Devices, Guangdong Provincial Key Laboratory of Luminescence from Molecular Aggregates, South China University of Technology, Guangzhou 510640, China; 3 Department of Obstetrics and Gynecology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430074, China; 4 Engineering Research Center of Nano-Geomaterials of Ministry of Education, Faculty of Materials Science and Chemistry, China University of Geosciences, Wuhan 430074, China

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Received June 12, 2020; accepted July 11, 2020; published online October 10, 2020

Robust photosensitizers with strong red/NIR fluorescence, efficient reactive oxygen species (ROS) generation and high photostability are highly desired for photodynamic therapy (PDT). Herein, three novel red conjugated polyelectrolytes (CPEs) with tetraphenylethene and 2,1,3-benzothiadiazole on the main chains and triphenylphosphonium on the side chains are developed. These CPEs display apparent aggregation-induced emission feature and high fluorescence quantum yields in the aggregated state. They can target lysosome in HeLa cells for fluorescence bioimaging. By virtue of the good retention effect and high photostability, these CPEs show ultralong-term tracing performance of subcutaneous tumors, and the tumor site can still be visualized for 20 days after injection. Owing to their good biocompatibility and strong ROS generation ability, the image-guided PDT based on these CPEs can effectively inhibit the growth of subcutaneous tumor and significantly prolong the survival of tumor bearing mice. The H&E and IHC staining reveal that the PDT of these CPEs depress the proliferation of tumor cells, and promote apoptosis and necrosis process. These new CPEs may be employed both as fluorescent probes for in vitro and in vivo long-term tracing and as photosensitizers for image-guided PDT of tumors. conjugated polyelectrolytes, aggregation-induced emission, long-term tracing, fluorescence imaging, photodynamic therapy Citation:

Yao H, Dai J, Zhuang Z, Yao J, Wu Z, Wang S, Xia F, Zhou J, Lou X, Zhao Z. Red AIE conjugated polyelectrolytes for long-term tracing and imageguided photodynamic therapy of tumors. Sci China Chem, 2020, 63, https://doi.org/10.1007/s11426-020-9824-2

1 Introduction Fluorescence imaging has emerged as a powerful tool for biomedical studies owing to its high sensitivity, excellent spatial and temporal resolution, noninvasiveness, real-time wide-field image acquisition, simple operation and low cost †These authors contributed equally to this work. *Corresponding authors (email: [email protected]; [email protected]; mszjzhao@scut