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卤化镓叶啉:DNA 相互作用和光动力抗肿瘤活性。

Halogenated Gallium Corroles:DNA Interaction and Photodynamic Antitumor Activity.

机构信息

School of Chemistry and Chemical Engineering, Key Laboratory of Functional Molecular Engineering of Guangdong Province, South China University of Technology, Guangzhou 510641, China.

Molecular Diagnosis and Treatment Center for Infectious Diseases, Dermatology Hospital, Southern Medical University, Guangzhou 510091, China.

出版信息

Inorg Chem. 2021 Feb 15;60(4):2234-2245. doi: 10.1021/acs.inorgchem.0c03016. Epub 2021 Jan 22.

DOI:10.1021/acs.inorgchem.0c03016
PMID:33480681
Abstract

A series of halogenated gallium corroles were synthesized and characterized by UV-vis, HRMS, NMR, and FT-IR. The interaction between these gallium corroles and calf thymus DNA had been investigated by spectroscopic methods. These gallium corroles would interact with CT-DNA via an outside binding mode. The photodynamic antitumor activity in vitro of these gallium corroles toward different cell lines had also been tested. displayed low cytotoxicity to normal cells under both light and dark conditions but high phototoxicity to liver cancer cells HepG2. The vitro experiment results showed that could be efficiently absorbed by tumor cells. After light illumination, it may induce reactive oxygen species (ROS) and cause destruction of the mitochondrial membrane potential, which may finally trigger tumor cell apoptosis. Flow cytometry results showed that HepG2 cells were mainly distributed in the sub-G0 phase, which corresponds to cells with highly fragmented DNA or dead cells generally. This suggests that could lead to tumor cell apoptosis after light illumination.

摘要

一系列卤化镓卟啉被合成并通过紫外可见光谱、高分辨率质谱、核磁共振和傅里叶变换红外光谱进行了表征。通过光谱法研究了这些镓卟啉与小牛胸腺 DNA 的相互作用。这些镓卟啉通过外部结合模式与 CT-DNA 相互作用。还测试了这些镓卟啉对不同细胞系的体外光动力抗肿瘤活性。在光照和黑暗条件下,均显示出对正常细胞的低细胞毒性,但对肝癌细胞 HepG2 具有高的光毒性。体外实验结果表明,能够被肿瘤细胞有效吸收。光照后,可能会诱导活性氧(ROS)并导致线粒体膜电位破坏,最终可能引发肿瘤细胞凋亡。流式细胞术结果表明,HepG2 细胞主要分布在亚 G0 期,这对应于通常具有高度碎片化 DNA 或死亡的细胞。这表明光照后 可能会导致肿瘤细胞凋亡。

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