期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 145, 期 -, 页码 338-349出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.11.091
关键词
Iridium(III) complex; Ca2+ levels assay; Apoptosis; In vivo; Autophagy; PI3K/AKT/mTOR
资金
- Natural Science Foundation of Guangdong Province [2016A030313728]
- Project of Innovation for Enhancing Guangdong Pharmaceutical University, Provincial Experimental Teaching Demonstration Center of Chemistry & Chemical Engineering
An iridium (III) complex [lr(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 mu M 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. (C) 2017 Elsevier Masson SAS. All rights reserved.
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