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Updated: Sep 29, 2025
Computed Tomography-guided Time-domain Diffuse Fluorescence Tomography in Small Animals for Localization of Cancer Biomarkers
Published on: July 17, 2012
A lipid droplet-targetable and biothiol-sensitive fluorescent probe for the diagnosis of cancer cells/tissues
Yuewei Zhang1, Ning Zhang1,2, Shuohang Wang1
1School of Chemistry and Pharmaceutical Engineering, Jilin Institute of Chemical Technology, Jilin, 132022, P. R. China. dongjibinghuayuxue@163.com.
Abstract:
Lipid droplets (LDs) have recently been reported as an attractive target for cancer diagnosis and treatment, owing to their special structure or microenvironment changes in cancer development and resistance. However, the relationship between the biothiol level of LDs and cancer is still poorly understood, partially owing to the absence of effective molecular tools. Herein, we developed a LD-targetable and biothiol-sensitive fluorescent probe, BTDA-RSS, by introducing 2,4-dinitrobenzenesulfonyl (DNBS) as the biothiol reaction group into a benzothiazolyl derivative. BTDA-RSS displayed a marked and rapid fluorescence turn-on response toward biothiols, due to the biothiol-triggered cleavage of DNBS to yield the highly fluorescent benzothiazolyl iminocoumarin BTDA. In addition, the probe shows significant LD-targetable ability, and has been applied for imaging endogenous/exogenous biothiol changes in LDs. Importantly, BTDA-RSS has successfully been utilized to distinguish cancerous cells/tissues from normal cells/tissues with excellent contrast. Surprisingly, we demonstrated for the first time the visualization of LD biothiols in surgical specimens from cancer patients, thereby holding great potential for the application of BTDA-RSS in the clinical diagnosis of human cancers.
Insights
Researchers developed BTDA-RSS, a fluorescent probe that targets lipid droplets (LDs) and detects biothiols. This tool successfully distinguishes cancer cells and tissues, offering potential for clinical cancer diagnosis.
Area of Science:
- Biochemistry
- Molecular Biology
- Cancer Research
Background:
- Lipid droplets (LDs) are increasingly recognized as crucial in cancer development, resistance, and treatment.
- The role of biothiols within LDs in cancer remains largely unexplored due to a lack of suitable detection tools.
Purpose of the Study:
- To develop a novel fluorescent probe for targeting LDs and sensing biothiols.
- To investigate the potential of this probe for cancer diagnosis by imaging biothiol level changes in LDs.
Main Methods:
- Synthesis of a LD-targetable, biothiol-sensitive fluorescent probe (BTDA-RSS) incorporating a 2,4-dinitrobenzenesulfonyl (DNBS) group.
- Evaluation of the probe's fluorescence response to biothiols and its ability to target LDs.
- Application of the probe for imaging biothiol variations in cancer cells, tissues, and patient surgical specimens.
Main Results:
- BTDA-RSS exhibited a rapid, 'turn-on' fluorescence response upon reaction with biothiols via DNBS cleavage.
- The probe demonstrated effective targeting of LDs and successful imaging of endogenous and exogenous biothiol changes.
- BTDA-RSS clearly differentiated cancerous cells and tissues from normal ones, showing high contrast.
Conclusions:
- BTDA-RSS is an effective tool for visualizing biothiol dynamics in LDs.
- The probe's ability to distinguish cancerous from normal samples highlights its potential for clinical cancer diagnosis.
- This study provides the first visualization of LD biothiols in human cancer surgical specimens, paving the way for new diagnostic applications.
