Related Experiment Video
Updated: Jan 6, 2026
Author Spotlight: Advancing Mitochondrial Research - mtHyper7 Biosensor for Subcellular Analysis
Published on: June 2, 2023
Mitochondrial targeting ratiometric theranostic probe activated by hydrogen peroxide toward tracking pH variations in
Yan Zhang1, Huifeng Zhang2, Jing He1
1College of Chemistry, Jilin University, Changchun, 130012, China.
Background:
At present, cancer remains one of the most devastating health challenges worldwide. Its high mortality rate, metastatic potential, and resistance to conventional treatments make it particularly lethal. Under these circumstances, developing comprehensive theranostic probe that can combine precise tumor detection with efficient treatment has become an urgent priority. Particularly, activatable theranostic probe that can dynamically monitor the changes of cells during the treatment intervention process has become a new research hotspot, bringing hope for more accurate diagnosis and effective treatment.
Results:
In this work, we constructed an activatable theranostic probe RF-HPQ-HP using delocalized lipophilic cations as mitochondrial targeting groups, boric ester (H2O2 recognition group) as a "switch" for diagnosis and treatment of tumor cells, and insoluble group HPQ which can cause cellular oxidative stress as a toxic motif. The probe RF-HPQ-HP can enter tumor cells by targeting mitochondria through mitochondrial membrane potential, and then high H2O2 content will change the fluorescence and simultaneously release insoluble dye RF-HPQ in the cells, thereby triggering subsequent reactions. Cell experiments have shown that the insoluble dye RF-HPQ can not only exploit the selective high toxicity to tumor cells through oxidative stress, but also track pH fluctuations of mitochondrial, meaning that it has the potential to track changes in cell state.
Significance:
This study not only provides a new strategy for the design of activatable theranostic probe with organelle-targeting capabilities, but also establishes a novel method for monitoring dynamic cellular state changes during tumor treatment. The proposed approach shows potential to cancer diagnosis and treatment by enabling simultaneous imaging and therapeutic monitoring.
Insights
Researchers developed an activatable theranostic probe for cancer. This probe targets mitochondria, detects hydrogen peroxide (H2O2), and releases a toxin for simultaneous imaging and treatment monitoring.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Molecular Imaging
Background:
- Cancer is a major global health challenge with high mortality and treatment resistance.
- There is an urgent need for theranostic probes that combine tumor detection and treatment.
- Activatable probes that monitor cellular changes during treatment are a key research area.
Purpose of the Study:
- To construct an activatable theranostic probe for cancer diagnosis and treatment.
- To develop a probe that targets mitochondria and responds to hydrogen peroxide.
- To create a system for monitoring dynamic cellular state changes during tumor therapy.
Main Methods:
- Constructed an activatable theranostic probe (RF-HPQ-HP) using lipophilic cations, a boric ester switch, and an insoluble toxic dye (HPQ).
- Utilized mitochondrial membrane potential for targeting tumor cell mitochondria.
- Investigated the probe's ability to detect H2O2, release the dye, and induce oxidative stress.
Main Results:
- The probe successfully targeted tumor cell mitochondria.
- Hydrogen peroxide triggered fluorescence changes and released the insoluble dye RF-HPQ.
- The released dye exhibited selective toxicity to tumor cells via oxidative stress and tracked mitochondrial pH fluctuations.
Conclusions:
- Developed a novel strategy for designing organelle-targeting activatable theranostic probes.
- Established a new method for monitoring dynamic cellular state changes during cancer treatment.
- The probe demonstrates potential for simultaneous cancer imaging and therapeutic monitoring.
