Exploring anticancer efficiency of mitochondria-targeted cyclometalated iridium(III) complexes.

Abstract:

:We prepared and characterized new iridium(III) complexes: [Ir(NC)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.

journal_name

J Inorg Biochem

authors

Gu Y,Wen H,Bai L,Zhou Y,Zhang H,Tian L,Zhang Y,Hao J,Liu Y

doi

10.1016/j.jinorgbio.2020.111215

subject

Has Abstract

pub_date

2020-11-01 00:00:00

pages

111215

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(20)30243-9

journal_volume

212

pub_type

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