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Article Abstract
A novel nickel(ii) complex of 6-methoxy-1-pyridine-β-carboline () was synthesized and characterized. The cytotoxicities of the complex towards six cancer cell lines, including MGC-803, Hep G2, T24, OS-RC-2, NCI-H460, and SK-OV-3, and human normal liver cell line HL-7702 were investigated. The IC values for MGC-803, Hep G2, T24, OS-RC-2, NCI-H460 and SK-OV-3 were generally in the micromolar range (3.77-15.10 μM), lower than those of ligand and cisplatin. Furthermore, (6 μM) significantly induced cell cycle arrest at the S phase, and caused the down-regulation of p-AKT, cyclin E, cyclin A and CDK2 and the up-regulation of p27. Various experiments showed that induced apoptosis, activated caspase-3, increased the levels of reactive oxygen species (ROS) and enhanced the intracellular [Ca] levels in MGC-803. In addition, the expression of intrinsic apoptotic proteins, including cytochrome c and apaf-1, increased. Further intrinsic apoptosis was triggered executive molecular caspase-9 and caspase-3. In short, exerted its cytotoxic activity primarily through inducing cell cycle arrest at the S phase and intrinsic apoptosis.
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| http://dx.doi.org/10.1039/c7md00428a | DOI Listing |
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