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Updated: Aug 3, 2026
Anticancer Efficacy of Photodynamic Therapy with Lung Cancer-Targeted Nanoparticles
Published on: December 1, 2016
Golgi apparatus-targeted aggregation-induced emission luminogens for effective cancer photodynamic therapy
Minglun Liu1, Yuncong Chen2,3, Yan Guo1
1State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Chemistry and Biomedicine Innovation Center (ChemBIC), Nanjing University, Nanjing, 210023, China.
Abstract:
Golgi apparatus (GA) oxidative stress induced by in situ reactive oxygen species (ROS) could severely damage the morphology and function of GA, which may open up an avenue for effective photodynamic therapy (PDT). However, due to the lack of effective design strategy, photosensitizers (PSs) with specific GA targeting ability are in high demand and yet quite challenging. Herein, we report an aggregation-induced emission luminogen (AIEgen) based PS (TPE-PyT-CPS) that can effectively target the GA via caveolin/raft mediated endocytosis with a Pearson correlation coefficient up to 0.98. Additionally, the introduction of pyrene into TPE-PyT-CPS can reduce the energy gap between the lowest singlet state (S1) and the lowest triplet state (T1) (ΔEST) and exhibits enhanced singlet oxygen generation capability. GA fragmentation and cleavage of GA proteins (p115/GM130) are observed upon light irradiation. Meanwhile, the apoptotic pathway is activated through a crosstalk between GA oxidative stress and mitochondria in HeLa cells. More importantly, GA targeting TPE-T-CPS show better PDT effect than its non-GA-targeting counterpart TPE-PyT-PS, even though they possess very close ROS generation rate. This work provides a strategy for the development of PSs with specific GA targeting ability, which is of great importance for precise and effective PDT.
Insights
This study developed a novel photosensitizer that targets the Golgi apparatus (GA), enhancing photodynamic therapy (PDT) effectiveness. The targeted approach causes significant GA damage and cell death, offering a promising strategy for precise cancer treatment.
Area of Science:
- Biochemistry
- Cell Biology
- Photochemistry
Background:
- Oxidative stress in the Golgi apparatus (GA) can impair its function and morphology.
- Developing targeted photosensitizers (PSs) for specific organelle delivery, like the GA, is crucial for effective photodynamic therapy (PDT).
- Current PS design strategies lack specificity for GA targeting, presenting a significant challenge.
Purpose of the Study:
- To design and synthesize an aggregation-induced emission luminogen (AIEgen) based PS (TPE-PyT-CPS) with specific Golgi apparatus targeting ability.
- To investigate the mechanism of GA targeting and the subsequent effects on cellular structures and pathways.
- To evaluate the enhanced PDT efficacy of the GA-targeting PS compared to its non-targeting counterpart.
Main Methods:
- Synthesis of an AIEgen-based PS (TPE-PyT-CPS) incorporating pyrene for enhanced singlet oxygen generation.
- Utilizing caveolin/raft mediated endocytosis for specific GA targeting, quantified by Pearson correlation coefficient.
- Irradiation of cells with the PS to induce GA fragmentation, protein cleavage, and apoptosis via crosstalk with mitochondria.
- Comparative analysis of PDT effects between GA-targeting and non-GA-targeting PSs.
Main Results:
- TPE-PyT-CPS demonstrated effective GA targeting with a high Pearson correlation coefficient (0.98).
- The pyrene moiety enhanced singlet oxygen generation by reducing the S1-T1 energy gap.
- Light irradiation induced GA fragmentation, cleavage of p115/GM130 proteins, and activated apoptosis through GA-mitochondria crosstalk.
- The GA-targeting PS exhibited superior PDT efficacy compared to the non-targeting PS, despite similar reactive oxygen species (ROS) generation rates.
Conclusions:
- A novel AIEgen-based PS (TPE-PyT-CPS) was successfully developed for specific Golgi apparatus targeting.
- Targeting the GA with this PS leads to significant cellular damage and apoptosis, demonstrating an effective PDT strategy.
- This research provides a valuable approach for designing targeted PSs, improving the precision and efficacy of photodynamic therapy.
