2. Academic Validation
  3. Hydroxy-corrole and its gallium(III) complex as new photosensitizer for photodynamic therapy against breast carcinoma

Hydroxy-corrole and its gallium(III) complex as new photosensitizer for photodynamic therapy against breast carcinoma

  • Eur J Med Chem. 2020 Dec 15:208:112794. doi: 10.1016/j.ejmech.2020.112794.
Yan-Mei Sun 1,  Xiao Jiang 1,  Ze-Yu Liu 1,  Ling-Gui Liu 1,  Yu-Hui Liao 2,  Lei Zeng 3,  Yong Ye 1,  Hai-Yang Liu 4
Affiliations

Affiliations

  • 1 School of Chemistry and Chemical Engineering, Key Laboratory of Functional Molecular Engineering of Guangdong Province, South China University of Technology, Guangzhou, 510641, China.
  • 2 Molecular Diagnosis & Treatment of Central Infectious Diseases, Dermatology Hospital, Southern Medical University, Guangzhou, 510091, China.
  • 3 Foresea Life Insurance Guangzhou General Hospital, Guangzhou, 511300, China.
  • 4 School of Chemistry and Chemical Engineering, Key Laboratory of Functional Molecular Engineering of Guangdong Province, South China University of Technology, Guangzhou, 510641, China. Electronic address: chhyliu@scut.edu.cn.
PMID: 32916313 DOI: 10.1016/j.ejmech.2020.112794
Abstract

Three mono-hydroxy corroles 1-3 and their gallium(III) complexes Ga1-3 were synthesized, and their photodynamic antitumour activities towards breast Cancer cells were investigated. All corroles showed excellent cytotoxicity against the MDA-MB-231 and 4T1 cell lines upon light irradiation at 625 nm. Ga3 exhibited excellent phototoxicity and selectivity against MDA-MB-231 cells, with an IC50 of 0.06 ± 0.03 μM and a selective index value of 1338.83 (relative to human normal Huvec cells). The performance of Ga3 was even better than that of the clinical photodynamic therapy drug m-THPC. A preliminary mechanistic investigation revealed that corrole 3 and Ga3 were mainly located in the cytoplasm. Upon irradiation, they could generate intracellular reactive oxygen to destroy the mitochondrial membrane potential and arrest the cell cycle at the sub-G1 phase. Flow cytometry revealed that corrole 3 and Ga3 induced Cancer cell Apoptosis after photodynamic treatment. Corrole 3 and Ga3 displayed negligible cytotoxicity in the dark. These results suggest that corrole 3 and Ga3 are promising candidates for use in the photodynamic therapy of breast Cancer.

Keywords

Breast carcinoma; Corrole; Gallium(III) complex; Photodynamic therapy; Photosensitizer.

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