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- Title
Mitochondria are the primary target in the induction of apoptosis by chiral ruthenium(II) polypyridyl complexes in cancer cells.
- Authors
Wang, Jin-Quan; Zhang, Ping-Yu; Qian, Chen; Hou, Xiao-Juan; Ji, Liang-Nian; Chao, Hui
- Abstract
A series of novel chiral ruthenium(II) polypyridyl complexes ( Δ-Ru1, Λ-Ru1, Δ-Ru2, Λ-Ru2, Δ-Ru3, Λ-Ru3) were synthesized and evaluated to determine their antiproliferative activities. Colocalization, inductively coupled plasma mass spectrometry, and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay studies showed that these ruthenium(II) complexes accumulated preferentially in the mitochondria and exhibited cytotoxicity against various cancer cells in vitro. The complex Δ-Ru1 is of particular interest because it was found to have half-maximal inhibitory concentrations comparable to those of cisplatin and better activity than cisplatin against a cisplatin-resistant cell line, A549-CP/R. Δ-Ru1 induced alterations in the mitochondrial membrane potential and triggered intrinsic mitochondria-mediated apoptosis in HeLa cells, which involved the regulation of Bcl-2 family members and the activation of caspases. Taken together, these data suggest that Δ-Ru1 may be a novel mitochondria-targeting anticancer agent. Graphical abstract: A series of novel chiral ruthenium(II) complexes were found to accumulate preferentially in the mitochondria of HeLa cells and exerted their toxicity through the intrinsic mitochondria-mediated apoptotic pathway. [Figure not available: see fulltext.]
- Subjects
MITOCHONDRIA; APOPTOSIS; RUTHENIUM pyridyls; CANCER cells; INDUCTIVELY coupled plasma mass spectrometry; CELL-mediated cytotoxicity; CISPLATIN
- Publication
Journal of Biological Inorganic Chemistry (JBIC), 2014, Vol 19, Issue 3, p335
- ISSN
0949-8257
- Publication type
Article
- DOI
10.1007/s00775-013-1069-2