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Design,Synthesis,and Anticancer Effect Studies of Iridium(Ⅲ...

Design,Synthesis,and Anticancer Effect Studies of Iridium(Ⅲ) Polypyridyl Complexes against HeLa Cells

作     者:Yi-Ying Gu Lan Bai Wen-Yao Zhang Fan Du Miao He Yun-Jun Liu 

作者单位:School of PharmacyGuangdong Pharmaceutical University 

会议名称:《第十一届全国化学生物学学术会议》

会议日期:2019年

学科分类:1007[医学-药学(可授医学、理学学位)] 10[医学] 100701[医学-药物化学] 

关 键 词:Iridium complex antitumor activity mitochondrial dysfunction DNA damage 

摘      要:An iridium(Ⅲ) complex([Ir(PTTP)2(ppy)](PF)(Ir-1) were synthesized and characterized. The cytotoxicity of Ir-1 against cancer cell lines SGC-7901, A549, HeLa, HepG2 and BEL-7402 was investigated using the MTT method. The results showed that the iridium(Ⅲ) complex had moderate in vitro anti-tumor activity toward HeLa cells. Further studies showed that the complex induce cell apoptosis through DNA damage, cell cycle arrest at the G0/G1 phase, ROS elevation, increased levels of Ca, high mitochondrial membrane depolarization, and cellular ATP depletion. Transwell and Colony-Forming assays revealed that Ir-1 can also effectively inhibit the metastasis and proliferation of tumor cells. These results demonstrate that Ir-1 induce apoptosis in HeLa cells through ROS-mediated mitochondrial damage and DNA damage pathways, as well as by inhibiting cell invasion, thereby exerting anti-tumor cell proliferation activity in vitro.

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