Abstract :
[en] A series of novel Pt(II) complexes [cis- and trans-Pt(II)(salicylaldimine)(DMSO)Cl (C-1), trans-Pt(II)(salicylaldimine)(
4-picoline)Cl (C-2), Pt(II)(salicylaldimine)Cl (C-3), trans- and cis/trans-Pt2(II)(salicylaldimine)
(DMSO)2Cl2 (C-4), trans-Pt2(II)(salicylaldimine)(4-picoline)2Cl2 (C-5) was synthesized and characterized.
The structures of C-1-cis, C-1-trans and C-3 were determined using a single crystal X-ray analysis. This
class of Pt(II) complexes has been studied for their in vitro cytotoxicity in multiple human cancer cell lines,
including breast (MCF-7), liver (HepG2), lung (A549), colon (HCT116) and cervical (Hela) cancers. C-1-
trans, C-2 and C-4-trans showed significant cytotoxicity to these cancer cells comparable to cisplatin.
A time- and dose-dependent MTT assay revealed that these complexes can suppress cell viability and cell
proliferation. Mechanistically these complexes induced pro-apoptotic gene expression such as BAX,
PUMA and NOXA and thereby enhanced apoptosis. Moreover, PARP cleavage in a dose-dependent
manner indicated their cytotoxic effect against cancer cells. Apoptosis of cancer cells occurred through
apoptotic pathways as explained by the cytometry analysis. The DNA unwinding properties of these active
Pt(II) complexes were studied by gel electrophoresis using pBR322 plasmid DNA as a target. Changes in
the morphology of cancer cells were also observed upon the addition of C-1-trans, C-2 and C-4-trans.
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