Quinoxalinone‐based, endoplasmic reticulum‐targeting photosensitizer nanoparticles for tumor photodynamic therapy
4 affiliations
- 1Department of Pharmacy The Second Qilu Hospital of Shandong University Jinan China
- 2Department of Spinal Surgery People's Hospital of Wudi Binzhou China
- 3Department of Pharmacy Zibo Central Hospital Zibo China
- 4Department of Spinal Surgery The Second Qilu Hospital of Shandong University, Cheeloo College of Medicine, Shandong University Jinan China
Abstract
The endoplasmic reticulum (ER) is an indispensable organelle responsible for the synthesis and transport of proteins and membrane lipids, playing a critical role in numerous physiological and pathological processes. Leveraging the properties of the ER, we developed novel quinoxalinone‐based, ER‐targeting photosensitizer nanoparticles (Qui‐PS NPs) by conjugating an ER‐specific targeting peptide(RACR) and evaluated their photodynamic therapy (PDT) efficacy. The size, morphology, cellular uptake, ER targeting capability, cell viability, biodistribution, and antitumor efficacy were assessed using dynamic light scattering, transmission electron microscopy, confocal microscopy, CCK‐8 assay, ICP‐Mass spectrometry, and tumor volume measurements, respectively. The results demonstrated that the synthesized Qui‐PS NPs possessed an average diameter of 79.74±9.4 nm, a polydispersity index (PDI) of 0.23±0.02, and a Zeta potential of −11.63±2.86 mV. These nanoparticles exhibited near‐infrared fluorescence emission centered at 830 nm and demonstrated superior singlet oxygen (1O2) generation capability. The NPs were readily internalized by MCF‐7 cells, displayed specific ER targeting, and induced cytotoxic effects upon light irradiation, with an IC50 value of 3.2±0.06 μg/mL. In tumor‐bearing mice, Qui‐PS NPs preferentially accumulated in tumor tissue and significantly suppressed tumor progression under light irradiation, with minimal impact on body weight. These findings suggest that these ER‐targeted NPs represent a promising nanoplatform for potential application in tumor PDT.
Related
- PRKACA modulates endoplasmic reticulum stress-associated dysfunction in granulosa cell models relevant to polycystic ovary syndrome
- Polycystin-2 functions as a calcium leak channel under endoplasmic reticulum stress to protect against myocardial ischemia
- Peripheral Axons Form Endoplasmic Reticulum-Rich Conduits With Breast Cancer Cells
- Endoplasmic reticulum and Golgi stress signaling-mediated regulation of protein secretion
- Mechanisms and therapeutic prospects of short-chain fatty acids in neonatal hypoxic–ischemic encephalopathy via modulation of mitochondrial dysfunction and endoplasmic reticulum stress
BibTeX
@article{sun2026quinoxalinonebased,
title = {{Quinoxalinone‐based, endoplasmic reticulum‐targeting photosensitizer nanoparticles for tumor photodynamic therapy}},
author = {Chao Sun and Lici Wang and Tao Li and Lei Duan and Yan Dong and Ji Li},
journal = {Bioengineering \& Translational Medicine},
year = {2026},
month = aug,
doi = {10.1002/btm2.70170},
url = {https://doi.org/10.1002/btm2.70170},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Quinoxalinone‐based, endoplasmic reticulum‐targeting photosensitizer nanoparticles for tumor photodynamic therapy
AU - Chao Sun
AU - Lici Wang
AU - Tao Li
AU - Lei Duan
AU - Yan Dong
AU - Ji Li
PY - 2026
DA - 2026/08/09
JO - Bioengineering & Translational Medicine
DO - 10.1002/btm2.70170
UR - https://doi.org/10.1002/btm2.70170
AB - The endoplasmic reticulum (ER) is an indispensable organelle responsible for the synthesis and transport of proteins and membrane lipids, playing a critical role in numerous physiological and pathological processes. Leveraging the properties of the ER, we developed novel quinoxalinone‐based, ER‐targeting photosensitizer nanoparticles (Qui‐PS NPs) by conjugating an ER‐specific targeting peptide(RACR) and evaluated their photodynamic therapy (PDT) efficacy. The size, morphology, cellular uptake, ER targeting capability, cell viability, biodistribution, and antitumor efficacy were assessed using dynamic light scattering, transmission electron microscopy, confocal microscopy, CCK‐8 assay, ICP‐Mass spectrometry, and tumor volume measurements, respectively. The results demonstrated that the synthesized Qui‐PS NPs possessed an average diameter of 79.74±9.4 nm, a polydispersity index (PDI) of 0.23±0.02, and a Zeta potential of −11.63±2.86 mV. These nanoparticles exhibited near‐infrared fluorescence emission centered at 830 nm and demonstrated superior singlet oxygen (1O2) generation capability. The NPs were readily internalized by MCF‐7 cells, displayed specific ER targeting, and induced cytotoxic effects upon light irradiation, with an IC50 value of 3.2±0.06 μg/mL. In tumor‐bearing mice, Qui‐PS NPs preferentially accumulated in tumor tissue and significantly suppressed tumor progression under light irradiation, with minimal impact on body weight. These findings suggest that these ER‐targeted NPs represent a promising nanoplatform for potential application in tumor PDT.
SN - 2380-6761
ER -