| Autor: |
Zhong, Qishuo, Cao, Yin, Xie, Xiaopan, Wu, Yuhang, Chen, Zhiqing, Zhang, Qiuping, Jia, Chunyan, Wu, Zhen, Xin, Pengyang, Yan, Xiaosheng, Zeng, Zhiping, Ren, Changliang |
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| Zdroj: |
Angewandte Chemie International Edition; Jan2024, Vol. 63 Issue 3, p1-12, 12p |
| Abstrakt: |
The development of stimuli‐responsive artificial H+/Cl− ion channels, capable of specifically disturbing the intracellular ion homeostasis of cancer cells, presents an intriguing opportunity for achieving high selectivity in cancer therapy. Herein, we describe a novel family of non‐covalently stapled self‐assembled artificial channels activatable by biocompatible visible light at 442 nm, which enables the co‐transport of H+/Cl− across the membrane with H+/Cl− transport selectivity of 6.0. Upon photoirradiation of the caged C4F‐L for 10 min, 90 % of ion transport efficiency can be restored, giving rise to a 10.5‐fold enhancement in cytotoxicity against human colorectal cancer cells (IC50=8.5 μM). The mechanism underlying cancer cell death mediated by the H+/Cl− channels involves the activation of the caspase 9 apoptosis pathway as well as the scarcely reported disruption of the autophagic processes. In the absence of photoirradiation, C4F‐L exhibits minimal toxicity towards normal intestine cells, even at a concentration of 200 μM. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
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