A Near-Infrared II Luminogen with a Photothermal Effect toward Tumor Drug Resistance Reversal
Kaihong Du1,2, Guiquan Zhang1,2, Dong He3
1State Key Laboratory of Luminescent Materials and Devices, Guangdong Provincial Key Laboratory of Luminescence from Molecular Aggregates, South China University of Technology, Guangzhou 510640, China.
Abstract:
Multidrug resistance of tumor cells has greatly limited the chemotherapy effect. The development of reliable strategies to deal with tumor multidrug resistance is highly desirable for tumor therapy. In this work, a near-infrared II (NIR II) luminogen was rationally designed and prepared, which could act as a photothermal reagent to reverse the drug resistance of tumor cells by reducing the related protein expression, achieving a high inhibition efficiency with the synergistic effect of chemotherapeutic drugs. By the selection of a strong electron-withdrawing unit, the emission peak of the luminogen could reach 973 nm. Moreover, this luminogen shows outstanding photothermal conversion ability and improved thermal stability compared to ICG. Notably, after the photothermal treatment of drug-resistant tumor cells by the NIR II luminogen, the antitumor efficiency of chemotherapeutic drugs, including paclitaxel, cis-platinum, and doxorubicin, was significantly enhanced. The mechanism exploration revealed that drug resistance-related proteins were remarkably reduced, making the cells more sensitive toward drugs. Thus, this strategy demonstrated a promising and reliable approach to reverse the drug resistance of tumor cells for efficient tumor inhibition in the clinic.
Insights
Researchers developed a near-infrared II (NIR II) luminogen to overcome tumor multidrug resistance. This photothermal agent enhances chemotherapy effectiveness by reducing drug resistance proteins, offering a promising strategy for efficient tumor inhibition.
Area of Science:
- Biomedical Engineering
- Materials Science
- Oncology
Background:
- Multidrug resistance (MDR) in tumor cells significantly compromises chemotherapy efficacy.
- Developing effective strategies to overcome MDR is crucial for improving cancer treatment outcomes.
Purpose of the Study:
- To design and synthesize a near-infrared II (NIR II) luminogen capable of reversing tumor cell drug resistance.
- To investigate the synergistic effect of the NIR II luminogen with chemotherapeutic drugs for enhanced tumor inhibition.
Main Methods:
- Rational design and synthesis of a novel NIR II luminogen with an emission peak at 973 nm.
- Evaluation of the luminogen's photothermal conversion efficiency and thermal stability.
- Assessment of the enhanced antitumor efficacy of combined photothermal treatment and chemotherapy on drug-resistant tumor cells.
Main Results:
- The synthesized NIR II luminogen exhibited excellent photothermal conversion ability and superior thermal stability.
- Photothermal treatment using the NIR II luminogen significantly enhanced the efficacy of paclitaxel, cis-platinum, and doxorubicin against drug-resistant tumor cells.
- Mechanism studies revealed a notable reduction in drug resistance-related proteins, restoring tumor cell sensitivity to chemotherapeutic agents.
Conclusions:
- The developed NIR II luminogen effectively reverses multidrug resistance in tumor cells via photothermal therapy.
- This strategy offers a promising approach to enhance chemotherapy by synergizing photothermal treatment with conventional drugs.
- The findings present a reliable method for improving tumor inhibition and clinical outcomes in patients with resistant cancers.


