A biheteroaryl-bridged fluorescence probe enables lipid droplets-specific bioimaging and photodynamic therapy in clinical clear cell renal cell carcinoma

Tan, Ping; Li, Chengming; Wang, Yinchan; Zhuang, Weihua; Chen, Mao; Zhou, Linsen; Zhang, Jiapeng; Gong, Qiyong; Wang, Qiang; You, Jingsong

doi:10.1016/j.dyepig.2021.109215

Cited by 17 publications

(4 citation statements)

References 44 publications

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“…After incubation with THTTPy for 40 min at 37 °C, THTTPy first showed a strong green fluorescence in lysosomes and lipid droplets, which was confirmed by costaining with LysoTracker Red and Nile Red (Figure A). The acidic lysosomes (pH ∼5) and hydrophobic LDs-targeted accumulation of THTTPy can be respectively ascribed to its basic tetrahydropyridine group and high hydrophobicity (calculated ClogP = 7.63), which also lead to a turn-on green fluorescence emission based on its high pH and polarity-sensitivity. , Under continuous light irradiation for 5 min, a prominent red fluorescence emission was observed specifically in mitochondria, which was validated through costaining with MitoTracker Green (Figure B). This can be ascribed to the photooxidative dehydrogenation of THTTPy into TTPy with mitochondria-targeted ability and red emission (Scheme S2).…”

Section: Results and Discussionmentioning

confidence: 74%

Photoactivatable Sequential Destruction of Multiorganelles for Cancer Therapy

Pan,

Shao,

et al. 2023

ACS Appl. Mater. Interfaces

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Organelle-targeted therapy guided by fluorescence imaging is promising for precise cancer treatment. However, most current organelle-targeted therapeutics can only destruct single organelles, which suffer from limited therapeutic efficacy. To address this challenge, a photoactivatable probe was developed for sequential photodynamic destruction of multiorganelles in cancer cells, including lysosomes, lipid droplets, and mitochondria. This photoactivatable probe not only exhibits efficient cancer cell eradication in vitro but also can suppress tumor growth in vivo. Simultaneously, the photoactivatable probe enables sequential destruction of multiple organelles in cancer cells, which can be observed in situ through the conversion of green-to-red fluorescence facilitated by a photooxidative dehydrogenation reaction. We believe this photoactivatable probe for sequential destruction of multiple organelles associated with fluorescence color conversion provides a new strategy for cancer treatment with greatly improved efficacy.

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Section: Results and Discussionmentioning

confidence: 74%

Photoactivatable Sequential Destruction of Multiorganelles for Cancer Therapy

Pan,

Shao,

et al. 2023

ACS Appl. Mater. Interfaces

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“…Besides the AIE effect in FL-PDT agents, it is also known that photodynamic theranostics can be improved by promoting the accumulation of the theranostic agent in the cells; therefore, Tabero et al [92] and others [93][94][95] investigated LDs as possible targets for directing photodynamic theranostics. The capability of LDs to serve as sensitive targets for PDT and photodynamic theranostics was investigated using fluorescent BOD-IPYs [85], which were found to specifically accumulate in LDs.…”

Section: Targeting Novel Therapeuticsmentioning

confidence: 99%

Lipid Droplets in Cancer: From Composition and Role to Imaging and Therapeutics

et al. 2022

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Cancer is the second most common cause of death worldwide, having its origin in the abnormal growth of cells. Available chemotherapeutics still present major drawbacks, usually associated with high toxicity and poor distribution, with only a small fraction of drugs reaching the tumour sites. Thus, it is urgent to develop novel therapeutic strategies. Cancer cells can reprogram their lipid metabolism to sustain uncontrolled proliferation, and, therefore, accumulate a higher amount of lipid droplets (LDs). LDs are cytoplasmic organelles that store neutral lipids and are hypothesized to sequester anti-cancer drugs, leading to reduced efficacy. Thus, the increased biogenesis of LDs in neoplastic conditions makes them suitable targets for anticancer therapy and for the development of new dyes for cancer cells imaging. In recent years, cancer nanotherapeutics offered some exciting possibilities, including improvement tumour detection and eradication. In this review we summarize LDs biogenesis, structure and composition, and highlight their role in cancer theranostics.

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“…10,11 LDs function as a vital energy source for the proliferation of tumor cells, underscoring the importance of LD-targeted PS research in PDT. [12][13][14] The endoplasmic reticulum (ER) is a crucial organelle in eukaryotic cells and is primarily responsible for lipid and protein syntheses. 15 As the largest intracellular membrane structure, the ER accounts for over half of the cytoplasmic content of the cell membrane, and any substantial damage to this extensive membrane system can trigger apoptosis.…”

Section: Introductionmentioning

confidence: 99%