Pyridine-Embedded Phenothiazinium Dyes as Lysosome-Targeted Photosensitizers for Highly Efficient Photodynamic Antitumor Therapy
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AbstractDevelopment of new photosensitizers (PSs) with high photodynamic efficacy and minimal side effects is of great interest in photodynamic therapy (PDT). In this work, we reported several pyridine-embedded phenothiazinium (pyridophenothiazinium) dyes, which could be conveniently synthesized in a few short steps and acted as highly efficient and potent PSs to selectively localize to lysosomes and photosensitively kill cancer cells. Among them, compound 5, which possessed the ability of promoting intracellular reactive oxygen species (ROS) upon light irradiation by almost 40-fold higher than that of methylene blue (MB, a general phenothiazinium-based PS), exhibited a remarkable phototherapeutic index (PI = 53.8) against HT29 cancer cells, leading to eradication of large solid tumors (∼300 mm3) in a xenograft mouse model without apparent side effects. These results suggest that the pyridophenothiazinium dyes developed herein, especially compound 5, may serve as promising lysosome-targeted PSs for efficient photodynamic antitumor therapy.
All Author(s) ListQicai Xiao, Huirong Lin, Juan Wu, Xin Pang, Quanming Zhou, Yue Jiang, Pan Wang, Wing Nang Leung, Hung Kay Lee, Sheng Jiang, Shao Q. Yao, Liqian Gao, Gang Liu, Chuanshan Xu
Journal nameJournal of Medicinal Chemistry
Volume Number63
Issue Number9
PublisherAmerican Chemical Society
Pages4896 - 4907
LanguagesEnglish-United States

Last updated on 2021-18-09 at 00:03