State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmacy, Guangxi Normal University, Guilin 541004, China.
International Center for Chemical and Biological Sciences, University of Karachi, Karachi-74270, Pakistan.
Dalton Trans. 2019 Aug 14;48(30):11469-11479. doi: 10.1039/c9dt01951k. Epub 2019 Jul 10.
Two rhodium complexes Rh1 and Rh2 with isoquinoline derivatives were synthesized and characterized. Both complexes displayed strong anticancer activity against various cancer cells and low cytotoxicity against non-cancer cells. These complexes triggered apoptosis via mitochondrial dysfunction that increased the levels of ROS and Ca and released cytochrome C which ultimately activated caspases and the apoptosis pathway. The different biological activities of Rh1 and Rh2 could be associated with the presence of methoxy substituents on the ligands. In vivo studies showed that Rh1 effectively inhibited tumor growth in a T-24 xenograft mouse model with a less adverse effect than cisplatin. Overall, Rh1 and Rh2 induced apoptosis via mitochondrial pathways and could be developed as effective anticancer agents.
合成并表征了两个带有异喹啉衍生物的铑配合物 Rh1 和 Rh2。这两个配合物对多种癌细胞表现出强烈的抗癌活性，对非癌细胞的细胞毒性低。这些配合物通过线粒体功能障碍引发细胞凋亡，增加 ROS 和 Ca 的水平，并释放细胞色素 C，最终激活半胱天冬酶和凋亡途径。Rh1 和 Rh2 的不同生物学活性可能与配体上甲氧基取代基的存在有关。体内研究表明，Rh1 能有效抑制 T-24 异种移植小鼠模型中的肿瘤生长，其不良反应小于顺铂。总之，Rh1 和 Rh2 通过线粒体途径诱导细胞凋亡，可开发为有效的抗癌药物。
