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含喹啉衍生物配体的新型半夹心钌配合物的抗肿瘤活性

and antitumor activity of novel half-sandwich ruthenium complexes containing quinoline derivative ligands.

作者信息

He Xiangdong, Chen Jun, Kandawa-Shultz Martha, Shao Guoqiang, Wang Yihong

机构信息

School of Chemistry and Chemical Engineering, Southeast University, Nanjing, 211189, China.

Department of Nuclear Medicine, Nanjing First Hospital, Nanjing Medical University, Nanjing 211166, China.

出版信息

Dalton Trans. 2023 Apr 11;52(15):4728-4736. doi: 10.1039/d2dt03317h.

Abstract

A series of half-sandwich ruthenium complexes containing quinoline derivative ligands was synthesized, which had excellent antitumor toxicity toward a variety of cell lines and could localize lysosomes. The damage of lysosomes promotes the release of cathepsin B and initiates downstream apoptotic cascade signals. The increase in reactive oxygen species (ROS) caused by the decrease in mitochondrial membrane potential (Δ) synergistically amplified the damage degree of lysosomes. In addition, the complex could inhibit cell transfer and clone formation. results showed that the complex had excellent biological effects in tested mouse samples as the body weight of mice did not change much during the treatment, and the mean tumor volume was significantly lower than the control group.

摘要

合成了一系列含喹啉衍生物配体的半夹心钌配合物,其对多种细胞系具有优异的抗肿瘤毒性,且能定位于溶酶体。溶酶体的损伤促进组织蛋白酶B的释放并启动下游凋亡级联信号。线粒体膜电位(Δ)降低导致的活性氧(ROS)增加协同放大了溶酶体的损伤程度。此外,该配合物可抑制细胞转移和克隆形成。结果表明,该配合物在受试小鼠样本中具有优异的生物学效应,因为在治疗期间小鼠体重变化不大,且平均肿瘤体积显著低于对照组。

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