Zhou Si-Han, Liao Wen-Hui, Yang Yun, Li Wei, Wu Yuan-Yuan, Wu Tian-Tian, Deng Shi-Hui, Zhou Jie, Li Zhe, Zhao Qi-Hua, Xu Jing-Yuan, Chen Ceshi, Xie Ming-Jin
School of Chemical Science and Technology, Yunnan University, Kunming 650091, Yunnan, China.
Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650201, Yunnan, China.
ACS Omega. 2023 Feb 8;8(7):6945-6958. doi: 10.1021/acsomega.2c07742. eCollection 2023 Feb 21.
A series of (8-hydroxyquinoline) gallium(III) complexes (CP--) was synthesized and characterized by single X-ray crystallography and density functional theory (DFT) calculation. The cytotoxicity of the four gallium complexes toward a human nonsmall cell lung cancer cell line (A549), human colon cancer cell line (HCT116), and human normal hepatocyte cell line (LO2) was evaluated using MTT assays. CP- exhibited excellent cytotoxicity against HCT116 cancer cells (IC = 1.2 ± 0.3 μM) and lower toxicity than cisplatin and oxaliplatin. We also evaluated the anticancer mechanism studies in cell uptake, reactive oxygen species analysis, cell cycle, wound-healing, and Western blotting assays. The results showed that CP- affected the expression of DNA-related proteins, which led to the apoptosis of cancer cells. Moreover, molecular docking tests of CP- were performed to predict other binding sites and to confirm its higher binding force to disulfide isomerase (PDI) proteins. The emissive properties of CP- suggest that this complex can be used for colon cancer diagnosis and treatment, as well as imaging. These results also provide a foundation for the development of gallium complexes as potent anticancer agents.
合成了一系列（8-羟基喹啉）镓（III）配合物（CP--），并通过单晶X射线晶体学和密度泛函理论（DFT）计算对其进行了表征。使用MTT法评估了四种镓配合物对人非小细胞肺癌细胞系（A549）、人结肠癌细胞系（HCT116）和人正常肝细胞系（LO2）的细胞毒性。CP-对HCT116癌细胞表现出优异的细胞毒性（IC = 1.2±0.3 μM），且毒性低于顺铂和奥沙利铂。我们还在细胞摄取、活性氧分析、细胞周期、伤口愈合和蛋白质印迹分析中评估了抗癌机制研究。结果表明，CP-影响了与DNA相关蛋白的表达，从而导致癌细胞凋亡。此外，进行了CP-的分子对接测试，以预测其他结合位点并确认其与二硫键异构酶（PDI）蛋白的更高结合力。CP-的发光特性表明该配合物可用于结肠癌的诊断、治疗以及成像。这些结果也为开发作为强效抗癌剂的镓配合物奠定了基础。
Zotero 插件
