@article{832392c7287044728e4d644730cfb08e,
title = "A red-light-activated sulfonamide porphycene for highly efficient photodynamic therapy against hypoxic tumor",
abstract = "Photodynamic therapy (PDT) is an emerging alternative cancer treatment modality that utilizes photo-sensitivity to cause cell death upon photo-irradiation. However, PDT efficiency has been hampered by tumor hypoxia, blue-shifted excitation wavelengths, and the high dark toxicity of photo-sensitizers. We designed and synthesized two novel porphycene-based photosensitizers (TBPoS-OH and TBPoS-2OH) with potent photo-cytotoxicity and a LD50 in the nM range under both normoxic and hypoxic conditions in a variety of cell types after photo-irradiation (λ = 640 ± 15 nm). Further studies showed fast-cellular uptake for TBPoS-OH that localized lysosomes and subsequently induced cell apoptosis via the lysosomal-mitochondrial pathway. Moreover, TBPoS-OH significantly reduced tumor growth in two xenografted mouse models bearing melanoma A375 and B16 cells. Finally, TBPoS-OH exhibited no obvious immunogenicity and toxicity to blood cells and major organs in mice. These data demonstrated that these two porphycene-based photosensitizers, especially TBPoS-OH, could be developed as a potential PDT modality.",
keywords = "Hypoxic, Melanoma, Photodynamic therapy, Porphycene, Tumor",
author = "Yuzhi Wang and Zhaohai Pan and Cheng, \{Xiao Lan\} and Kai Zhang and Xin Zhang and Yao Qin and Jiaojiao Fan and Ting Yan and Tao Han and Shiu, \{Kwok Keung\} and Hau, \{Sam Chun-Kit\} and Mak, \{Nai Ki\} and Kwong, \{Daniel W J\} and Xiaona Liu and Minjing Li and Guowei Deng and Qiusheng Zheng and Jun Lu and Defang Li",
note = "Funding Information: We acknowledge the financial support from the National Natural Science Foundation of China (Grant Nos. 81872162 and 81602556 to Defang Li, Grant No. 81803374 to Jun Lu, and Grant No. 31870338 to Qiusheng Zheng), Shandong Provincial Natural Science Foundation of China (Grant No. ZR2017JL030 to Defang Li), the Hong Kong Research Grants Council General Research Fund (GRF-HKBU 201312), Shenzhen science and technology innovation fund (Grant No. JCYJ20180302174121208 to Jun Lu), Key Research and Development Program of Shandong Province of China (Grant No. GG201809270118 to Qiusheng Zheng), HKBU Inter-institutional Collaborative Research Scheme (RC-ICRS/15?16/02D), Taishan Scholars Construction Engineering of Shandong Province (to Defang Li), Yantai High-End Talent Introduction Plan ?Double Hundred? (to Defang Li), the Scientific Research Foundation of Binzhou Medical University (Grant no. BY2016KYQD01 to Defang Li), and the Dominant Disciplines? Talent Team Development Scheme of Higher Education of Shandong Province (to Defang Li). Funding Information: We acknowledge the financial support from the National Natural Science Foundation of China (Grant Nos. 81872162 and 81602556 to Defang Li , Grant No. 81803374 to Jun Lu , and Grant No. 31870338 to Qiusheng Zheng), Shandong Provincial Natural Science Foundation of China (Grant No. ZR2017JL030 to Defang Li), the Hong Kong Research Grants Council General Research Fund ( GRF-HKBU 201312 ), Shenzhen science and technology innovation fund (Grant No. JCYJ20180302174121208 to Jun Lu), Key Research and Development Program of Shandong Province of China (Grant No. GG201809270118 to Qiusheng Zheng), HKBU Inter-institutional Collaborative Research Scheme ( RC-ICRS/15–16/02D ), Taishan Scholars Construction Engineering of Shandong Province (to Defang Li), Yantai High-End Talent Introduction Plan “Double Hundred” (to Defang Li), the Scientific Research Foundation of Binzhou Medical University (Grant no. BY2016KYQD01 to Defang Li), and the Dominant Disciplines{\textquoteright} Talent Team Development Scheme of Higher Education of Shandong Province (to Defang Li). Copyright {\textcopyright} 2020 Elsevier Masson SAS. All rights reserved.",
year = "2021",
month = jan,
day = "1",
doi = "10.1016/j.ejmech.2020.112867",
language = "English",
volume = "209",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "Elsevier Masson s.r.l.",
}
