European Journal of Medicinal Chemistry, volume 208, pages 112794
Hydroxy-corrole and its gallium(III) complex as new photosensitizer for photodynamic therapy against breast carcinoma.
Sun Yanmei
1
,
Jiang Xiaochen
1
,
Liu Ze-Yu
1
,
Liu Ling Gui
1
,
Liao Yuhui
2
,
Zeng Lei
3
,
Ye Yong
1
,
Liu Hai-Yang
1
3
Foresea Life Insurance Guangzhou General Hospital, Guangzhou, 511300, China.
|
Publication type: Journal Article
Publication date: 2020-12-01
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor: 6.7
ISSN: 02235234, 17683254
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
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.
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- Statistics recalculated weekly.
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Sun Y. et al. Hydroxy-corrole and its gallium(III) complex as new photosensitizer for photodynamic therapy against breast carcinoma. // European Journal of Medicinal Chemistry. 2020. Vol. 208. p. 112794.
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Sun Y., Jiang X., Liu Z., Liu L. G., Liao Y., Zeng L., Ye Y., Liu H. Hydroxy-corrole and its gallium(III) complex as new photosensitizer for photodynamic therapy against breast carcinoma. // European Journal of Medicinal Chemistry. 2020. Vol. 208. p. 112794.
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TY - JOUR
DO - 10.1016/j.ejmech.2020.112794
UR - https://doi.org/10.1016%2Fj.ejmech.2020.112794
TI - Hydroxy-corrole and its gallium(III) complex as new photosensitizer for photodynamic therapy against breast carcinoma.
T2 - European Journal of Medicinal Chemistry
AU - Sun, Yanmei
AU - Jiang, Xiaochen
AU - Liu, Ze-Yu
AU - Liu, Ling Gui
AU - Liao, Yuhui
AU - Zeng, Lei
AU - Ye, Yong
AU - Liu, Hai-Yang
PY - 2020
DA - 2020/12/01 00:00:00
PB - Elsevier
SP - 112794
VL - 208
SN - 0223-5234
SN - 1768-3254
ER -
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@article{2020_Sun,
author = {Yanmei Sun and Xiaochen Jiang and Ze-Yu Liu and Ling Gui Liu and Yuhui Liao and Lei Zeng and Yong Ye and Hai-Yang Liu},
title = {Hydroxy-corrole and its gallium(III) complex as new photosensitizer for photodynamic therapy against breast carcinoma.},
journal = {European Journal of Medicinal Chemistry},
year = {2020},
volume = {208},
publisher = {Elsevier},
month = {dec},
url = {https://doi.org/10.1016%2Fj.ejmech.2020.112794},
pages = {112794},
doi = {10.1016/j.ejmech.2020.112794}
}