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A β-carboline derivative-based nickel(II) complex as a potential antitumor agent: synthesis, characterization, and cytotoxicity

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Abstract

A novel nickel(II) complex of 6-methoxy-1-pyridine-β-carboline (4a) 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 IC50 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 4 and cisplatin. Furthermore, 4a (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 4a induced apoptosis, activated caspase-3, increased the levels of reactive oxygen species (ROS) and enhanced the intracellular [Ca2+]c levels in MGC-803. In addition, the expression of intrinsic apoptotic proteins, including cytochrome c and apaf-1, increased. Further intrinsic apoptosis was triggered via executive molecular caspase-9 and caspase-3. In short, 4a exerted its cytotoxic activity primarily through inducing cell cycle arrest at the S phase and intrinsic apoptosis.

Graphical abstract: A β-carboline derivative-based nickel(ii) complex as a potential antitumor agent: synthesis, characterization, and cytotoxicity

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Publication details

The article was received on 19 Aug 2017, accepted on 03 Nov 2017 and first published on 24 Nov 2017


Article type: Research Article
DOI: 10.1039/C7MD00428A
Citation: Med. Chem. Commun., 2018, Advance Article
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    A β-carboline derivative-based nickel(II) complex as a potential antitumor agent: synthesis, characterization, and cytotoxicity

    J. Yang, Y. Zhu, S. Chen, X. Lu, Y. Wu, F. Ma, L. Li, Y. Yang, Z. Shi, K. Huang, X. Hong, P. Jiang and Y. Peng, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C7MD00428A

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