18 November 2014 Synthesis of folate receptor-targeted photosensitizers for photodynamic therapy
Author Affiliations +
A series of amphiphilic benzylidene cycloalkanes ketone photosensitizers C1-C4 with or without folate receptor-targeted agent were designed and synthesized. Their photophysical properties and in vitro photodynamic therapy (PDT) effects were studied. The results showed that all compounds exhibited appropriate lipid-water partition coefficients and high reactive oxygen yields. The introduction of the folate receptor-targeted agent had no obvious influence on the basic photophysical & photochemical properties of C2 and C4 compared to those of their corresponding prototype compounds (C1 and C3). In vitro studies were carried out using MCF-7 cells (FR+), Hela cells (FR+) and A549 cells (FR-), which represented different levels of folate receptor (FR) expression. All of C1-C4 showed low dark toxicity and superior PDT effects compared with the clinical drug PSD-007 (a mixture of porphyrins). What’s more, folate receptor-targeted photosensitizers (C2 and C4) achieved higher accumulation and more excellent PDT effects in MCF-7 cells (FR+) and Hela cells (FR+) than photosensitizers (C1 and C3) without folate receptor-targeted agent and PSD-007. The photocytotoxicity of these photosensitizers showed no obvious differences in A549 cells (FR-).
© (2014) COPYRIGHT Society of Photo-Optical Instrumentation Engineers (SPIE). Downloading of the abstract is permitted for personal use only.
Yanyan Fang, Yanyan Fang, Xiaopu Wang, Xiaopu Wang, Qianli Zou, Qianli Zou, Yuxia Zhao, Yuxia Zhao, Feipeng Wu, Feipeng Wu, "Synthesis of folate receptor-targeted photosensitizers for photodynamic therapy", Proc. SPIE 9268, Optics in Health Care and Biomedical Optics VI, 92680O (18 November 2014); doi: 10.1117/12.2071756; https://doi.org/10.1117/12.2071756

Back to Top