Tuning Organelle Specificity and Photodynamic Therapy Efficiency by Molecular Function Design
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Abstract
Efficient organic photosensitizers (PSs) have attracted much attention because of their promising applications in photodynamic therapy (PDT). However, guidelines on their molecular design are rarely reported. In this work, a series of PSs are designed and synthesized based on a triphenylamine-azafluorenone core. Their structure-property-application relationships are systematically studied. Cationization is an effective strategy to enhance the PDT efficiency of PSs by targeting mitochondria. From the molecularly dispersed state to the aggregate state, the fluorescence and the reactive oxygen species generation efficiency of PSs with aggregation-induced emission (AIE) increase due to the restriction of the intramolecular motions and enhancement of intersystem crossing. Cationized mitochondrion-targeting PSs show higher PDT efficiency than that of nonionized ones targeting lipid droplets. The ability of AIE PSs to kill cancer cells can be further enhanced by combination of PDT with radiotherapy. Such results should trigger research enthusiasm for designing and synthesizing AIE PSs with better PDT efficiency and properties.
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- Authors
- Liu, Z., Zou, H., Zhao, Z., Zhang, P., Shan, G.-G., Kwok, R. T. K., Lam, J. W. Y., Zheng, L., & Tang, B. Z.
- Affiliations
- Hong Kong University of Science and Technology (HK)
- Nanfang Hospital (CN)
- Chinese Academy of Sciences (CN)
- Corresponding author
- Zheng, Lei
- Tang, Ben Zhong
- ORCID
- Venue
- ACS Nano
- Publisher
- American Chemical Society (ACS)
- Published
- 2019-09-17
- Volume
- 13
- Issue
- 10
- Pages
- 11283-11293
- ISSN
- 1936-0851 (ISSN-L)
- 1936-086X
- OpenAlex
- W2973403573
- Cited by
- 260
- References
- 56
- Citations by year
- 2026: 17 · 2025: 19 · 2024: 32 · 2023: 43 · 2022: 67 · 2021: 47 · 2020: 35
- FWCI
- 27.37
- Type
- journal article
- Language
- en
- Open access
- green
- doi.org
- Licence
- Locations
- ACS Nano (publishedVersion)
- ChemRxiv (acceptedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- Rare & Special e-Zone (The Hong Kong University of Science and Technology) (submittedVersion)
- Figshare (submittedVersion, cc-by-nc-nd)
- Funders
- Research Grants Council, University Grants Committee (16308016, AHKUST605/16, C6009-17G)
- Ministry of Science and Technology of the People's Republic of China (2018YFE0190200)
- Innovation and Technology Commission (ITCPD/17-9, ITS/254/17, ITC-CNERC14SC01)
- University Grants Committee (AIE/P03/08)
- National Natural Science Foundation of China (21788102)
- Science and Technology Plan of Shenzhen (JCYJ20170818113602462, JCYJ20170818113530705)
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Photodynamic Therapy Research Studies
- Physical Sciences › Materials Science › Materials Chemistry › Luminescence and Fluorescent Materials
- Physical Sciences › Engineering › Biomedical Engineering › Nanoplatforms for cancer theranostics
- Keywords
- organic photosensitizers, photodynamic therapy, aggregation-induced emission, cationization, mitochondrial targeting, lipid droplet targeting, reactive oxygen species generation, intersystem crossing, structure-property relationships, tumor cell killing
- MeSH terms
- Fluorescence, Free Radicals, HeLa Cells, Humans, Photochemotherapy, Organelles, Photosensitizing Agents, Reactive Oxygen Species, Cell Line, Tumor
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