A Mitochondria-targeted AIEgen Labelled with 18F for Breast Cancer Cell Imaging and Therapy

Kaiwu Yu; Rui Zhou; Yangyang Xu; Yan Zhong; Shufang Qian; Honghai Zhang; Haibin Shi; Qinggang He; Zhengwei Mao; Haoke Zhang; Yen Wei; Hong Zhang; Mei Tian

doi:10.1002/asia.202101029

A Mitochondria-targeted AIEgen Labelled with ¹⁸F for Breast Cancer Cell Imaging and Therapy

Kaiwu Yu, Rui Zhou, Yangyang Xu, Yan Zhong, Shufang Qian, Honghai Zhang, Haibin Shi, Qinggang He, Zhengwei Mao, Haoke Zhang, Yen Wei, Hong Zhang, Mei Tian

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

10 Scopus citations

Abstract

A lack of efficient diagnostic tools for early and noninvasive diagnosis of breast cancer has restricted the clinical treatment effect. This problem might be addressed by the combination of aggregation-induced emission (AIE) fluorescence imaging and positron emission tomography (PET) with the dual advantages of high resolution and easy operation, and unlimited penetration and high sensitivity. Here, a mitochondria-targeted AIE luminogen (AIEgen) radiolabeled with ¹⁸F was developed through a two-step radiochemical reaction by virtue of a prosthetic group. The obtained ^18/19F-Bz-CP imaging probe was examined by in vitro cell uptake and cell proliferation inhibition in two breast cancer cell lines, showing that the probe can efficiently target and locate in the mitochondria through the analysis of fluorescence imaging and PET simultaneously. Additionally, the probe can induce cancer cell apoptosis with the half maximal inhibitory concentration (IC50) of 4.8 μM for MCF-7 cells and 7.2 μM for T47D cells, indicating its potential application for breast cancer therapy.

Original language	English
Pages (from-to)	3963-3969
Number of pages	7
Journal	Chemistry - An Asian Journal
Volume	16
Issue number	23
DOIs	https://doi.org/10.1002/asia.202101029
State	Published - Dec 1 2021
Externally published	Yes

Funding

This work was sponsored by the National Natural Science Foundation of China (NSFC) (21788102, 81761148029, 21978260).

Keywords

aggregation-induced emission
breast cancer
imaging and therapy
mitochondria
positron emission tomography

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1002/asia.202101029

Cite this

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title = "A Mitochondria-targeted AIEgen Labelled with 18F for Breast Cancer Cell Imaging and Therapy",

abstract = "A lack of efficient diagnostic tools for early and noninvasive diagnosis of breast cancer has restricted the clinical treatment effect. This problem might be addressed by the combination of aggregation-induced emission (AIE) fluorescence imaging and positron emission tomography (PET) with the dual advantages of high resolution and easy operation, and unlimited penetration and high sensitivity. Here, a mitochondria-targeted AIE luminogen (AIEgen) radiolabeled with 18F was developed through a two-step radiochemical reaction by virtue of a prosthetic group. The obtained 18/19F-Bz-CP imaging probe was examined by in vitro cell uptake and cell proliferation inhibition in two breast cancer cell lines, showing that the probe can efficiently target and locate in the mitochondria through the analysis of fluorescence imaging and PET simultaneously. Additionally, the probe can induce cancer cell apoptosis with the half maximal inhibitory concentration (IC50) of 4.8 μM for MCF-7 cells and 7.2 μM for T47D cells, indicating its potential application for breast cancer therapy.",

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T1 - A Mitochondria-targeted AIEgen Labelled with 18F for Breast Cancer Cell Imaging and Therapy

AU - Yu, Kaiwu

AU - Zhou, Rui

AU - Xu, Yangyang

AU - Zhong, Yan

AU - Qian, Shufang

AU - Zhang, Honghai

AU - Shi, Haibin

AU - He, Qinggang

AU - Mao, Zhengwei

AU - Zhang, Haoke

AU - Wei, Yen

AU - Zhang, Hong

AU - Tian, Mei

PY - 2021/12/1

Y1 - 2021/12/1

N2 - A lack of efficient diagnostic tools for early and noninvasive diagnosis of breast cancer has restricted the clinical treatment effect. This problem might be addressed by the combination of aggregation-induced emission (AIE) fluorescence imaging and positron emission tomography (PET) with the dual advantages of high resolution and easy operation, and unlimited penetration and high sensitivity. Here, a mitochondria-targeted AIE luminogen (AIEgen) radiolabeled with 18F was developed through a two-step radiochemical reaction by virtue of a prosthetic group. The obtained 18/19F-Bz-CP imaging probe was examined by in vitro cell uptake and cell proliferation inhibition in two breast cancer cell lines, showing that the probe can efficiently target and locate in the mitochondria through the analysis of fluorescence imaging and PET simultaneously. Additionally, the probe can induce cancer cell apoptosis with the half maximal inhibitory concentration (IC50) of 4.8 μM for MCF-7 cells and 7.2 μM for T47D cells, indicating its potential application for breast cancer therapy.

AB - A lack of efficient diagnostic tools for early and noninvasive diagnosis of breast cancer has restricted the clinical treatment effect. This problem might be addressed by the combination of aggregation-induced emission (AIE) fluorescence imaging and positron emission tomography (PET) with the dual advantages of high resolution and easy operation, and unlimited penetration and high sensitivity. Here, a mitochondria-targeted AIE luminogen (AIEgen) radiolabeled with 18F was developed through a two-step radiochemical reaction by virtue of a prosthetic group. The obtained 18/19F-Bz-CP imaging probe was examined by in vitro cell uptake and cell proliferation inhibition in two breast cancer cell lines, showing that the probe can efficiently target and locate in the mitochondria through the analysis of fluorescence imaging and PET simultaneously. Additionally, the probe can induce cancer cell apoptosis with the half maximal inhibitory concentration (IC50) of 4.8 μM for MCF-7 cells and 7.2 μM for T47D cells, indicating its potential application for breast cancer therapy.

KW - aggregation-induced emission

KW - breast cancer

KW - imaging and therapy

KW - mitochondria

KW - positron emission tomography

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