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  3. Lysosome-targeting phenalenones as efficient type I/II photosensitizers for anticancer photodynamic therapy

Lysosome-targeting phenalenones as efficient type I/II photosensitizers for anticancer photodynamic therapy

  • Eur J Med Chem. 2023 Jul 5;255:115418. doi: 10.1016/j.ejmech.2023.115418.
Qiaoyun Jiang 1,  Peixia Li 1,  Jingru Qiu 1,  Donghai Li 2,  Guiling Li 3,  Gang Shan 4
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 Wenhuaxi Road, Jinan, Shandong Province, 250012, PR China.
  • 2 Advanced Medical Research Institute, Meili Lake Translational Research Park, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, PR China.
  • 3 Advanced Medical Research Institute, Meili Lake Translational Research Park, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, PR China. Electronic address: liguiling@sdu.edu.cn.
  • 4 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 Wenhuaxi Road, Jinan, Shandong Province, 250012, PR China. Electronic address: gangshan@sdu.edu.cn.
PMID: 37119664 DOI: 10.1016/j.ejmech.2023.115418
Abstract

Development of safe and effective photosensitizers is important for enhancing the efficacy of photodynamic Cancer therapy. Phenalenone is a type II photosensitizer with a high singlet oxygen quantum yield; however, its short UV absorption wavelength hinders its application in Cancer imaging and in vivo photodynamic therapy. In this study, we report a new redshift phenalenone derivative, 6-amino-5-iodo-1H-phenalen-1-one (SDU Red [SR]), as a lysosome-targeting photosensitizer for triple-negative breast Cancer therapy. SDU Red produced singlet oxygen (Type II Reactive Oxygen Species [ROS]) and superoxide anion radicals (Type I ROS) upon LIGHT irradiation. It also exhibited good photostability and a remarkable phototherapeutic index (PI > 76) against triple-negative breast Cancer MDA-MB-231 Cancer cells. Additionally, we designed two amide derivatives, SRE-I and SRE-II, with decreased fluorescence and photosensitizing capabilities based on SDU Red as activatable photosensitizers for photodynamic Cancer therapy. SRE-I and SRE-II could be further converted into the active photosensitizer SDU Red via carboxylesterase-catalyzed amide bond cleavage. Moreover, SDU Red and SRE-II induced DNA damage and cell Apoptosis in the presence of LIGHT. Therefore, SRE-II can act as a promising theranostic agent for triple-negative breast Cancer.

Keywords

Anticancer; Phenalenone; Photodynamic therapy; Photosensitizer; Theranostic.

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