A Simple Route toward Next-Generation Thiobase-Based Photosensitizers for Cancer Theranostics.
Van-Nghia NguyenSeonye HeoChang Woo KohJeongsun HaGyoungmi KimSungnam ParkJuyoung YoonPublished in: ACS sensors (2021)
Sulfur-substituted biocompatible carbonyl fluorophores have been recognized as effective heavy-atom-free photosensitizers (PSs) for cancer therapy due to their remarkable phototherapeutic properties. However, guidelines on their molecular design are still a substantial challenge. Most of the existing thiocarbonyl-based PSs are nonemissive in both the solution and restricted states, which hinders their further biomedical applications. Herein, we report the interesting finding that sulfur-substituted coumarins exhibit an uncommon phenomenon, aggregation-induced emission. More intriguingly, we also found that the introduction of a strong electron-accepting trifluoromethyl group is crucial to facilitate the mitochondrial-targeting ability of neutral coumarin fluorophores. The resulting CMS-2 PS displayed selective imaging of mitochondria and exhibited much higher photodynamic therapy efficiency toward cancer cells than that of the commercial PS erythrosine B. This work provides deep insight into the molecular design of heavy-atom-free thiobase-based PSs and simultaneously offers a great opportunity to develop novel mitochondrial-targeting fluorescent indicators with neutral bioinspired platforms.
Keyphrases
- photodynamic therapy
- cancer therapy
- fluorescence imaging
- drug delivery
- oxidative stress
- molecular docking
- molecular dynamics
- papillary thyroid
- electron transfer
- high resolution
- drug release
- quantum dots
- squamous cell
- cell death
- ionic liquid
- clinical practice
- solid state
- young adults
- squamous cell carcinoma
- mass spectrometry
- living cells
- label free
- childhood cancer