Synthesis, characterization and anticancer activity in vitro and in vivo evaluation of an iridium (III) polypyridyl complex

• DOI: 10.1016/j.ejmech.2017.11.091
• Publication Date: 2017-12-02T01:15:21Z
• Authors: Qiao-Yan Yi; Dan Wan; Bing Tang; Yang-Jie Wang; Wen-Yao Zhang; Fan Du; Miao He; Yun-Jun Liu
• Keywords: 0301 basic medicine; Dose-Response Relationship, Drug; Molecular Structure; Cell Survival; Pyridines; Antineoplastic Agents; Apoptosis; Mice, Inbred Strains; Cell Cycle Checkpoints; Neoplasms, Experimental; Iridium; 3. Good health; Mice; Structure-Activity Relationship; 03 medical and health sciences; Coordination Complexes; Cell Line, Tumor; Animals; Humans; Drug Screening Assays, Antitumor; Cell Proliferation

An iridium (III) complex [Ir(ppy)2(BDPIP)]PF6 (Ir-1) was reported to show high anticancer activity and may be used as a potent anticancer drug. In the current study, we designed and synthesized a novel iridium (III) complex and evaluated its potential inhibitory effect on the cancer cell growth in vitro and in vivo. This complex was found to display high cytotoxic activity in vitro and in vivo against A549 cell with a low IC50 value of 3.6 ± 0.3 μM and inhibiting percentage of tumor growth is 63.84% compared with the control. The complex also exhibited potencies superior to that of cisplatin toward A549 cell in vitro and in vivo. Further studies revealed that the complex can induce apoptosis and autophagy, enhance the ROS level, cause a decrease in the mitochondrial membrane potential and inhibit the cell invasion. Our findings indicated that the complex induced apoptosis in A549 through mitochondria dysfunction and PI3K/AKT/mTOR signaling pathways.