TY - JOUR
T1 - Multifunctional Organelle‐Targeting Probes for Intracellular Imaging and Enhanced Cancer Phototherapy
AU - Ma, Weijun
AU - Xie, Chen
AU - Li, Xiaomin
AU - Tam, Ka Bo Leo
AU - Wu, Yue
AU - Wang, Rui
AU - Lam, Pak-Lun
AU - Chau, Ho-Fai
AU - Wong, Ka-Leung
N1 - K.-L. W. gratefully acknowledges the financial assistance from the Hong Kong Research Grants Council Grant No. 12300021, and NSFC/RGC Joint Research Scheme (N_PolyU209/21).
Publisher Copyright
© 2025 The Author(s).
PY - 2025/6/10
Y1 - 2025/6/10
N2 - Photodynamic therapy (PDT) represents a promising modality for cancer treatment; however, its clinical application is hindered by challenges such as glutathione (GSH)-mediated quenching of reactive oxygen species (ROS) and autofluorescence interference during visible light imaging. This study introduces Cy-NBD-5F, a photosensitizer engineered to address these limitations. Upon activation by GSH, Cy-NBD-5F exhibits 5.5-fold fluorescence enhancement at 701 nm, producing its reduced form, Cy-OH-5F, which demonstrates enhanced ROS generation, including a 1.4-fold increase in singlet oxygen and 1.2-fold increase in superoxide anion radicals. Under light irradiation, Cy-OH-5F induces significant cytotoxicity (IC50 < 3 μM). Additionally, the molecule predominantly localizes within lysosomes and the endoplasmic reticulum, showing organelle-specific effects to improve therapeutic efficacy. These findings show the potential of Cy-NBD-5F as a precise and effective tool for cancer theranostics.
AB - Photodynamic therapy (PDT) represents a promising modality for cancer treatment; however, its clinical application is hindered by challenges such as glutathione (GSH)-mediated quenching of reactive oxygen species (ROS) and autofluorescence interference during visible light imaging. This study introduces Cy-NBD-5F, a photosensitizer engineered to address these limitations. Upon activation by GSH, Cy-NBD-5F exhibits 5.5-fold fluorescence enhancement at 701 nm, producing its reduced form, Cy-OH-5F, which demonstrates enhanced ROS generation, including a 1.4-fold increase in singlet oxygen and 1.2-fold increase in superoxide anion radicals. Under light irradiation, Cy-OH-5F induces significant cytotoxicity (IC50 < 3 μM). Additionally, the molecule predominantly localizes within lysosomes and the endoplasmic reticulum, showing organelle-specific effects to improve therapeutic efficacy. These findings show the potential of Cy-NBD-5F as a precise and effective tool for cancer theranostics.
KW - activatable fluorescence
KW - dual-targeting
KW - hemicyanine dye
KW - nir emission
KW - photodynamic therapy
UR - http://www.scopus.com/inward/record.url?scp=105008537329&partnerID=8YFLogxK
U2 - 10.1002/chem.202500831
DO - 10.1002/chem.202500831
M3 - Journal article
SN - 0947-6539
JO - Chemistry - A European Journal
JF - Chemistry - A European Journal
M1 - e202500831
ER -
