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Issue 5, 2021
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All-in-one mitochondria-targeted NIR-II fluorophores for cancer therapy and imaging

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Abstract

Small-molecule subcellular organelle-targeting theranostic probes are crucial for early disease diagnosis and treatment. The imaging window of these molecules is mainly focused on the visible and near-infrared region (below ∼900 nm) which limits the tissue penetration depth and therapeutic effects. Herein, a novel NIR-II small-molecule probe H4–PEG-Glu with a thiopyrylium cation was synthesized. H4–PEG-Glu not only can quickly and effectively image mitochondria in acute myeloid leukemia (AML) cells, and induce G0/G1 phase arrest by the intrinsic mitochondrial apoptosis pathway w/o irradiation, but also exhibit moderate cytotoxicity against AML cancer cells in a dose dependent-manner without laser irradiation. The THP-1 cells treated with H4–PEG-Glu upon NIR laser irradiation showed enhanced chemo- and photothermal therapy (CPTT) with 93.07% ± 6.43 apoptosis by Annexin V staining. Meanwhile, H4–PEG-Glu displayed high synergistic CPTT effects in vivo, as well as specific NIR-II tumor imaging in AML patient derived PDX mouse models for the first time. Our work lays down a solid foundation for designing small-molecule NIR-II mitochondria-selective theranostic probes.

Graphical abstract: All-in-one mitochondria-targeted NIR-II fluorophores for cancer therapy and imaging

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Supplementary files

Article information


Submitted
27 Aug 2020
Accepted
26 Nov 2020
First published
27 Nov 2020

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2021,12, 1843-1850
Article type
Edge Article

All-in-one mitochondria-targeted NIR-II fluorophores for cancer therapy and imaging

Y. Zheng, Q. Li, J. Wu, Z. Luo, W. Zhou, A. Li, Y. Chen, T. Rouzi, T. Tian, H. Zhou, X. Zeng, Y. Li, X. Cheng, Y. Wei, Z. Deng, F. Zhou and X. Hong, Chem. Sci., 2021, 12, 1843
DOI: 10.1039/D0SC04727A

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