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Updated: Oct 19, 2025
Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
Near-infrared frequency upconversion probe for revealing the relationship between glutathione S-transferase and
Wenchao Zhu1, Hui Yu2, Xiaoli Qian2
1School of Mechanical Engineering, Southeast University, Nanjing, 211189, China; School of Engineering, China Pharmaceutical University, Nanjing, 211198, China.
Abstract:
Drug resistance poses an enormous challenge for successful chemotherapy. Glutathione S-transferase (GST) has been confirmed to be involved in the progression of drug resistance to some anticancer drugs, thus revealing that the role of GST in anticancer drug resistance is necessary. Herein, by taking advantage of frequency upconversion luminescence (FUCL) technology, we reported an FUCL probe (NRh-NDs) that can detect GST based on a rhodamine derivative structure decorated with a 2,4-dinitrobenzenesulfonyl group (NDs). The NRh-NDs showed excellent sensitivity and high selectivity for GST and released the emissive dye NRh-NH2, which showed emission and excitation wavelengths in vitro of 820 nm and 850 nm, respectively. The NRh-NDs probe successfully tested endogenic GST in U87, MCF-7 and A549 cells. The cell data showed that the increased levels of GST were positively related to cisplatin resistance but not to 5-fluorouracil resistance. These results suggested that the probe could be used as a visual tool to reveal the cause of drug resistance for cisplatin resistance in cancer treatment. Furthermore, it may serve as an effective tool to confirm the mechanism of antitumor drug resistance.
Insights
A new frequency upconversion luminescence probe detects Glutathione S-transferase (GST), an enzyme linked to chemotherapy drug resistance. This tool helps identify cisplatin resistance mechanisms in cancer cells.
Area of Science:
- Biochemistry
- Biomedical Engineering
- Analytical Chemistry
Background:
- Drug resistance is a major obstacle in cancer chemotherapy.
- Glutathione S-transferase (GST) plays a role in the development of resistance to certain anticancer drugs.
Purpose of the Study:
- To develop a novel frequency upconversion luminescence (FUCL) probe for sensitive and selective detection of GST.
- To investigate the correlation between GST levels and resistance to cisplatin and 5-fluorouracil in cancer cells.
Main Methods:
- Utilized frequency upconversion luminescence (FUCL) technology to create a probe (NRh-NDs) based on a rhodamine derivative.
- The probe detects GST by releasing an emissive dye (NRh-NH2) with specific emission and excitation wavelengths (820 nm and 850 nm).
- Tested the probe's efficacy in detecting endogenous GST in U87, MCF-7, and A549 cancer cell lines.
Main Results:
- The NRh-NDs probe demonstrated high sensitivity and selectivity for GST detection.
- Successfully detected endogenous GST in various human cancer cell lines.
- Found a positive correlation between elevated GST levels and cisplatin resistance.
- No significant correlation was observed between GST levels and 5-fluorouracil resistance.
Conclusions:
- The developed FUCL probe serves as a visual tool for identifying GST, a key factor in cisplatin resistance.
- This probe can aid in understanding and confirming the mechanisms underlying anticancer drug resistance.
- Offers potential for personalized cancer treatment strategies by assessing drug resistance profiles.
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