Upconversion NIR-II fluorophores for mitochondria-targeted cancer imaging and photothermal therapy

Hui Zhou, Xiaodong Zeng, Anguo Li, Wenyi Zhou, Lin Tang, Wenbo Hu, Quli Fan, Xianli Meng, Hai Deng, Lian Duan, Yanqin Li, Zixin Deng, Xuechuan Hong () and Yuling Xiao ()
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Hui Zhou: Wuhan University School of Pharmaceutical Sciences
Xiaodong Zeng: Wuhan University School of Pharmaceutical Sciences
Anguo Li: Wuhan University School of Pharmaceutical Sciences
Wenyi Zhou: Wuhan University School of Pharmaceutical Sciences
Lin Tang: Wuhan University School of Pharmaceutical Sciences
Wenbo Hu: Nanjing University of Posts and Telecommunications
Quli Fan: Nanjing University of Posts and Telecommunications
Xianli Meng: Chengdu University of Traditional Chinese Medicine, Wenjiang
Hai Deng: University of Aberdeen
Lian Duan: Wuhan University School of Pharmaceutical Sciences
Yanqin Li: Wuhan University School of Pharmaceutical Sciences
Zixin Deng: Wuhan University School of Pharmaceutical Sciences
Xuechuan Hong: Wuhan University School of Pharmaceutical Sciences
Yuling Xiao: Wuhan University School of Pharmaceutical Sciences

Nature Communications, 2020, vol. 11, issue 1, 1-14

Abstract: Abstract NIR-II fluorophores have shown great promise for biomedical applications with superior in vivo optical properties. To date, few small-molecule NIR-II fluorophores have been discovered with donor-acceptor-donor (D-A-D) or symmetrical structures, and upconversion-mitochondria-targeted NIR-II dyes have not been reported. Herein, we report development of D-A type thiopyrylium-based NIR-II fluorophores with frequency upconversion luminescence (FUCL) at ~580 nm upon excitation at ~850 nm. H4-PEG-PT can not only quickly and effectively image mitochondria in live or fixed osteosarcoma cells with subcellular resolution at 1 nM, but also efficiently convert optical energy into heat, achieving mitochondria-targeted photothermal cancer therapy without ROS effects. H4-PEG-PT has been further evaluated in vivo and exhibited strong tumor uptake, specific NIR-II signals with high spatial and temporal resolution, and remarkable NIR-II image-guided photothermal therapy. This report presents the first D-A type thiopyrylium NIR-II theranostics for synchronous upconversion-mitochondria-targeted cell imaging, in vivo NIR-II osteosarcoma imaging and excellent photothermal efficiency.

Date: 2020
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DOI: 10.1038/s41467-020-19945-w

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