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; Yuling Xiao

doi:10.1038/s41467-020-19945-w

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^* (Corresponding Author), Yuling Xiao^* (Corresponding Author)

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Article number	6183
Number of pages	14
Journal	Nature Communications
Volume	11
DOIs	https://doi.org/10.1038/s41467-020-19945-w
Publication status	Published - 3 Dec 2020

Keywords

fluorescent probes
Imaging studies
Materials chemistry

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Upconversion NIR-II fluorophores for mitochondria-targeted cancer imaging and photothermal therapy. / Zhou, Hui; Zeng, Xiaodong; Li, Anguo ; Zhou, Wenyi ; Tang, Lin; Hu, Wenbo ; Fan, Quli; Meng, Xianli; Deng, Hai; Duan, Lian ; Li, Yanqin; Deng, Zixin; Hong, Xuechuan (Corresponding Author); Xiao, Yuling (Corresponding Author).

In: Nature Communications, Vol. 11, 6183, 03.12.2020.

Research output: Contribution to journal › Article › peer-review

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title = "Upconversion NIR-II fluorophores for mitochondria-targeted cancer imaging and photothermal therapy",

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.",

keywords = "fluorescent probes, Imaging studies, Materials chemistry",

author = "Hui Zhou and Xiaodong Zeng and Anguo Li and Wenyi Zhou and Lin Tang and Wenbo Hu and Quli Fan and Xianli Meng and Hai Deng and Lian Duan and Yanqin Li and Zixin Deng and Xuechuan Hong and Yuling Xiao",

note = "Acknowledgements: The work was supported by the National Key R&D Program of China (2020YFA0908800), NSFC (81773674, 81573383), Shenzhen Science and Technology Research Grant (JCYJ20190808152019182), Hubei Province Scientific and Technical Innovation Key Project, National Natural Science Foundation of Hubei Province (2017CFA024, 2017CFB711), the Applied Basic Research Program of Wuhan Municipal Bureau of Science and Technology (2019020701011429), Tibet Autonomous Region Science and Technology Plan Project Key Project (XZ201901-GB-11), the Local Development Funds of Science and Technology Department of Tibet (XZ202001YD0028C), Project First-Class Disciplines Development Supported by Chengdu University of Traditional Chinese Medicine (CZYJC1903), Health Commission of Hubei Province Scientific Research Project (WJ2019M177, WJ2019M178), the China Scholarship Council, and the Fundamental Research Funds for the Central Universities.",

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AU - Tang, Lin

AU - Hu, Wenbo

AU - Fan, Quli

AU - Meng, Xianli

AU - Deng, Hai

AU - Duan, Lian

AU - Li, Yanqin

AU - Deng, Zixin

AU - Hong, Xuechuan

AU - Xiao, Yuling

N1 - Acknowledgements: The work was supported by the National Key R&D Program of China (2020YFA0908800), NSFC (81773674, 81573383), Shenzhen Science and Technology Research Grant (JCYJ20190808152019182), Hubei Province Scientific and Technical Innovation Key Project, National Natural Science Foundation of Hubei Province (2017CFA024, 2017CFB711), the Applied Basic Research Program of Wuhan Municipal Bureau of Science and Technology (2019020701011429), Tibet Autonomous Region Science and Technology Plan Project Key Project (XZ201901-GB-11), the Local Development Funds of Science and Technology Department of Tibet (XZ202001YD0028C), Project First-Class Disciplines Development Supported by Chengdu University of Traditional Chinese Medicine (CZYJC1903), Health Commission of Hubei Province Scientific Research Project (WJ2019M177, WJ2019M178), the China Scholarship Council, and the Fundamental Research Funds for the Central Universities.

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N2 - 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.

AB - 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.

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