In vitro and in vivo anti-tumor activity of two gold(III) complexes with isoquinoline derivatives as ligands.

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In vitro and in vivo anti-tumor activity of two gold(III) complexes with isoquinoline derivatives as ligands.

Eur J Med Chem. 2019 Feb 01;163:333-343

Authors: Khan TM, Gul NS, Lu X, Wei JH, Liu YC, Sun H, Liang H, Orvig C, Chen ZF

Abstract
Two gold(III) complexes of isoquinoline derivatives: [Au(L1)Cl2] (Au1) and [Au(L2)Cl2] (Au2) have been prepared and characterized. Au1 and Au2 exhibited greater cytotoxicity than their corresponding ligands and cisplatin against T-24 cells. Both complexes arrested cell cycle at S-phase by upregulation of p53, p27, and p21, and downregulation of cyclin A and cyclin E. The depolarization of the mitochondrial membrane potential, generation of ROS, and stimulated Ca2+ release activated the caspase cascade and ultimately caused apoptosis by increasing the levels of Bax and Bak, and decreasing the levels of Bcl-2 and Bcl-xl. Cell apoptosis was achieved via mitochondria mediated pathways. The in vivo studies of Au1 and Au2 demonstrated that they were safer than cisplatin and could effectively inhibit tumor growth.

PMID: 30529636 [PubMed - indexed for MEDLINE]

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