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Exploring anticancer efficiency of mitochondria-targeted cyclometalated iridium(III) complexes.
Journal of Inorganic Biochemistry ( IF 3.9 ) Pub Date : 2020-08-08 , DOI: 10.1016/j.jinorgbio.2020.111215
Yiying Gu 1 , Haoyu Wen 1 , Lan Bai 1 , Yi Zhou 1 , Huiwen Zhang 1 , Li Tian 1 , Yuanyuan Zhang 1 , Jing Hao 1 , Yunjun Liu 1
Affiliation  

We prepared and characterized new iridium(III) complexes: [Ir(Nsingle bondC)2(MPPIP)](PF6) (N-C = 2-phenylpyridine 1; benzo[h]quinolone 2; 1-phenylisoquinolone, 3, MPPIP = 2-(4-(4′-methylpiperazin-yl)phenyl)-1H-imidazo[4,5-f][1,10]phenanthroline). MTT (MTT = 3-(4,5-dimethylthiazole-2-yl)-2,5-biphenyl tetrazolium bromide) method was used to assay anticancer activities of the complexes 1-3 toward SGC-7901, HeLa, A549, BEL-7402, mouse embryonic fibroblast NIH3T3 cell lines. Complexes 1, 2, 3 are sensitive to A549 cells and display a relatively low IC50 value of 5.4 ± 0.3, 4.2 ± 0.03 and 3.8 ± 0.2 μM, respectively. The apoptotic efficiency was investigated and the number of apoptotic cells induced by 1, 2 and 3 is 9.92%, 11.30% and 16.00%. The complexes are able to increase intracellular ROS content and lessen the mitochondrial membrane potential. Besides, anti-tumor activity in vivo reveals that complex 3 exhibits moderate effect on inhibiting the tumor growth, and complex 3 has no influence on liver, brain, kidney, lung and heart.



中文翻译:

探索靶向线粒体的环金属化铱 (III) 配合物的抗癌效率。

我们制备并表征了新的铱 (III) 配合物:[Ir( NC 单键) 2 (MPPIP)](PF 6 ) (NC = 2-苯基吡啶1;苯并 [ h ] 喹诺酮2;1-苯基异喹诺酮,3,MPPIP = 2 -(4-(4'-甲基哌嗪-基)苯基) -1H-咪唑并[4,5- f ][1,10]菲咯啉)。MTT(MTT = 3-(4,5-二甲基吡啶-2-基)-2,5-联苯溴化四唑)法用于测定复合物的抗癌活性1 - 3朝向SGC-7901,HeLa细胞,A549,BEL- 7402,小鼠胚胎成纤维细胞 NIH3T3 细胞系。配合物1 , 2 , 3对 A549 细胞敏感,并显示出相对较低的 IC 50值,分别为 5.4 ± 0.3、4.2 ± 0.03 和 3.8 ± 0.2 μM。凋亡效率进行了研究,并通过诱导的凋亡细胞的数目123是9.92%,11.30%和16.00%。该复合物能够增加细胞内 ROS 含量并降低线粒体膜电位。此外,体内抗肿瘤活性表明复合物3对抑制肿瘤生长具有中等作用,复合物3对肝、脑、肾、肺和心脏没有影响。

更新日期:2020-09-10
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