Abstract
A novel Pt(II) complex of [PtII(MPP)(OPD)]Cl⋅H2O (MPP-Pt) (OPD = o-phenylenediamine) with 2-(2,5-methoxy-phenyl) imidazo [4,5-f]-[1, 10] phenanthrolin (H-MPP) was synthesized and fully characterized. In MPP-Pt complex, the Pt(II) ion adopts a four-coordinated square planar geometry. MPP-Pt exhibited selective cytotoxicity against human carcinoma (A549), hepatoblastoma (Hep-G2), ovarian (SK-OV-3), cervical (HeLa) and gastric adenocarcinoma (MGC80–3) cell lines with IC50 values in the micromolar range (0.31–9.48 μM), but low cytotoxicity toward HL-7702 normal cells. Various experiments showed that MPP-Pt complex caused cell apoptosis via mitochondrial dysfunction in HeLa cells, as shown by the up-regulation expression of p27, apaf-1, p21, cytochrome c (cyc c) and p53 levels, loss of mitochondrial membrane potential (MMP) and the down-regulation expression of bcl-2 protein level.
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