Probes allowing high-contrast discrimination of cancer cells and effective retention are powerful tools for the early diagnosis and treatment of cancer. However, conventional small-molecule probes often show limited performance in both aspects. Herein, we report an ingenious molecular engineering strategy for tuning the cellular uptake and retention of rhodamine dyes. Introduction of polar aminoethyl leads to the increased brightness and reduced cellular uptake of dyes, and this change can be reversed by amino acetylation. Moreover, these modifications allow cancer cells to take up more dyes than normal cells (16-fold) through active transport. Specifically, we further improve the signal contrast (56-fold) between cancer and normal cells by constructing activatable probes and confirm that the released fluorophore can remain in cancer cells with extended time, enabling long-term and specific tumor imaging.
Bacterial infections can easily occur when patients mishandle
wounds
or eat moldy food. The prompt diagnosis of a bacterial infection could
effectively reduce the risk of possible anatomical damage. However,
non-invasive early detection of bacterial infections is difficult
to achieve due to the lack of favorable tools. Here, we designed two
hNQO1 fluorescent probes (RX2 and RX3) to
visualize bacterial infection after deep learning on the pathogenesis
of bacterial infection. RX2 and RX3 enable
early detection of bacterial infection and are verified to be, respectively,
suitable for fluorescence imaging (FLI) and photoacoustic imaging
(PAI) by comparing the signal-to-background ratio of both probes in
a mouse model of myositis caused by Escherichia coli infection. In view of the difference in penetration depth between
the two imaging modalities, we further applied RX2 for
FLI of E. coli-infected wounds and RX3 for PAI of E. coli-infected
inflammatory bowel disease, suggesting the great potential of both
probes for early diagnosis of bacterial infections.
Probes allowing high‐contrast discrimination of cancer cells and effective retention are powerful tools for the early diagnosis and treatment of cancer. However, conventional small‐molecule probes often show limited performance in both aspects. Herein, we report an ingenious molecular engineering strategy for tuning the cellular uptake and retention of rhodamine dyes. Introduction of polar aminoethyl leads to the increased brightness and reduced cellular uptake of dyes, and this change can be reversed by amino acetylation. Moreover, these modifications allow cancer cells to take up more dyes than normal cells (16‐fold) through active transport. Specifically, we further improve the signal contrast (56‐fold) between cancer and normal cells by constructing activatable probes and confirm that the released fluorophore can remain in cancer cells with extended time, enabling long‐term and specific tumor imaging.
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