Details

Autor(en) / Beteiligte

• Qi, Sujie
• Kwon, Nahyun
• Yim, Yubin
• Nguyen, Van-Nghia
• Yoon, Juyoung

Titel

Fine-tuning the electronic structure of heavy-atom-free BODIPY photosensitizers for fluorescence imaging and mitochondria-targeted photodynamic therapy

Ist Teil von

• Chemical science (Cambridge), 2020-03, Vol.11 (25), p.6479-6484

Ort / Verlag

England: Royal Society of Chemistry

Erscheinungsjahr

2020

Link zum Volltext

Quelle

EZB Electronic Journals Library

Beschreibungen/Notizen

• Theranostics that combines both diagnosis and therapy into a single platform has recently emerged as a promising biomedical approach for cancer treatment; however, the development of efficient theranostic agents with excellent optical properties remains a challenge. Here, we report novel mitochondria-targeting photosensitizers ( s) that possess considerable singlet oxygen generation capabilities and good fluorescence properties for imaging-guided photodynamic therapy (PDT). The incorporation of sulfur atoms into the π-conjugated skeleton of along with the introduction of different functional groups at the -position of the core is essential for tuning the photophysical and photosensitizing properties. Notably, the MeOPh-substituted thiophene-fused ( , R = -methoxyphenyl) displayed the highest singlet oxygen generation capability ( ≈ 0.85 in air-saturated acetonitrile) and a moderate fluorescence quantum yield ( = 17.11). Furthermore, showed good biocompatibility, low dark toxicity and superior fluorescence imaging properties in living cells. More importantly, the PDT efficacy of mitochondria-specific anchoring of was remarkably amplified with an extremely low half-maximal inhibitory concentration (IC ) value of 95 nM. We believe that the incorporation of an electron-donating group at the -position of the thiophene-fused platform may be an effective approach for developing theranostic agents for precision cancer therapy.