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Updated: Aug 9, 2025
High-throughput Screening and Biosensing with Fluorescent C. elegans Strains
Published on: May 19, 2011
GSH-specific fluorescent probe for sensing, bioimaging, rapid screening of natural inhibitor Celastrol and ccRCC
Chanjuan Zhang1, Yan Qin2, Changfeng Deng3
1Laboratory of Stem Cell Regulation with Chinese Medicine and Its Application, School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, PR China; TCM and Ethnomedicine Innovation & Development International Laboratory, School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, PR China.
Abstract:
High level of intracellular glutathione (GSH) has been identified as a major barrier for cancer therapy. Therefore, effective regulation of GSH can be regarded as a novel approach for cancer therapy. In this study, an off-on fluorescent probe (NBD-P) is developed for selective and sensitive sensing GSH. NBD-P has a good cell membrane permeability that can be applied in bioimaging endogenous GSH in living cells. Moreover, the NBD-P probe is used to visualize GSH in animal models. In addition, a rapid drug screening method is successfully established using the fluorescent probe NBD-P. A potent natural inhibitor of GSH is identified as Celastrol from Tripterygium wilfordii Hook F, which effectively triggers mitochondrial apoptosis in clear cell renal cell carcinoma (ccRCC). More importantly, NBD-P can selectively respond to GSH fluctuations to distinguish cancer tissues from normal tissues. Thus, the present study provides insights into fluorescence probes for the screening GSH inhibitors and cancer diagnosis, as well as in-depth exploration of the anti-cancer effects of Traditional Chinese Medicine (TCM).
Insights
Researchers developed a fluorescent probe (NBD-P) to detect glutathione (GSH) in cells and animals. This probe identified Celastrol as a natural compound that inhibits GSH, offering a new approach for clear cell renal cell carcinoma (ccRCC) therapy.
Area of Science:
- Biomedical Engineering
- Molecular Biology
- Cancer Research
Background:
- Elevated intracellular glutathione (GSH) levels impede cancer treatment efficacy.
- Targeting GSH offers a promising strategy for novel cancer therapies.
Purpose of the Study:
- To develop a selective and sensitive fluorescent probe (NBD-P) for sensing intracellular GSH.
- To establish a drug screening platform utilizing the NBD-P probe.
- To investigate the anti-cancer effects of natural compounds on GSH regulation in ccRCC.
Main Methods:
- Synthesis and characterization of the NBD-P off-on fluorescent probe.
- Bioimaging of endogenous GSH in living cells and animal models using NBD-P.
- High-throughput drug screening to identify GSH inhibitors.
- Evaluation of Celastrol's efficacy in inducing apoptosis in ccRCC cells.
Main Results:
- NBD-P demonstrated excellent cell membrane permeability for bioimaging GSH in living systems.
- A rapid drug screening method identified Celastrol from Tripterygium wilfordii Hook F as a potent GSH inhibitor.
- Celastrol effectively induced mitochondrial apoptosis in clear cell renal cell carcinoma (ccRCC).
- NBD-P distinguished cancer tissues from normal tissues by responding to GSH fluctuations.
Conclusions:
- The NBD-P probe is a valuable tool for sensing GSH, facilitating drug screening and cancer diagnosis.
- Celastrol exhibits significant anti-cancer potential against ccRCC by inhibiting GSH and triggering apoptosis.
- This study highlights the therapeutic promise of targeting GSH and explores the anti-cancer properties of Traditional Chinese Medicine (TCM).
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