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  3. Azide-modified corrole phosphorus complexes for endoplasmic reticulum-targeted fluorescence bioimaging and effective cancer photodynamic therapy

Azide-modified corrole phosphorus complexes for endoplasmic reticulum-targeted fluorescence bioimaging and effective cancer photodynamic therapy

  • Eur J Med Chem. 2024 Feb 5:265:116102. doi: 10.1016/j.ejmech.2023.116102.
Jing-He Cen 1,  Qi-Hu Xie 2,  Geng-Hong Guo 2,  Long-Jiang Gao 1,  Yu-Hui Liao 3,  Xiao-Ping Zhong 4,  Hai-Yang Liu 5
Affiliations

Affiliations

  • 1 School of Chemistry and Chemical Engineering, The Key Laboratory of Fuel Cell Technology of Guangdong Province, South China University of Technology, Guangzhou, 510641, China.
  • 2 Department of Plastic Surgery and Burns, The Second Affiliated Hospital of Shantou University Medical College, Shantou, 515041, China.
  • 3 Molecular Diagnosis and Treatment Center for Infectious Diseases, Dermatology Hospital, Southern Medical University, Guangzhou, 510091, China. Electronic address: liaoyh8@mail.sysu.edu.cn.
  • 4 Department of Plastic Surgery and Burns, The Second Affiliated Hospital of Shantou University Medical College, Shantou, 515041, China. Electronic address: zhongxiaoping@stu.edu.cn.
  • 5 School of Chemistry and Chemical Engineering, The Key Laboratory of Fuel Cell Technology of Guangdong Province, South China University of Technology, Guangzhou, 510641, China. Electronic address: chhyliu@scut.edu.cn.
PMID: 38176359 DOI: 10.1016/j.ejmech.2023.116102
Abstract

Study on corrole photosensitizers (PSs) for photodynamic therapy (PDT) has made remarkable progress. Targeted delivery of PSs is of great significance for enhancing therapeutic efficiency, decreasing the dosage, and reducing systemic toxicity during PDT. The development of PSs that can be specifically delivered to the subcellular organelle is still an attractive and challenging work. Herein, we synthesize a series of azide-modified corrole phosphorus and gallium complex PSs, in which phosphorus corrole 2-P could not only precisely target the endoplasmic reticulum (ER) with a Pearson correlation coefficient (PCC) up to 0.92 but also possesses the highest singlet oxygen quantum yields (ΦΔ = 0.75). This renders it remarkable PDT activity at a very low dosage (IC50 = 23 nM) towards HepG2 tumor cell line while ablating solid tumors in vivo with excellent biosecurity. Furthermore, 2-P exhibits intense red fluorescence (ΦF = 0.25), outstanding photostability, and a large Stokes shift (190 nm), making it a promising fluorescent probe for ER. This study provides a clinically potential photosensitizer for Cancer photodynamic therapy and a promising ER fluorescent probe for bioimaging.

Keywords

Corrole; ER-targeted; Fluorescent probe; Gallium(III) complex; Phosphorus(V) complex; Photodynamic therapy.

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