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Issue 6, 2014
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Carbohydrate linked organotin(iv) complexes as human topoisomerase Iα inhibitor and their antiproliferative effects against the human carcinoma cell line

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Abstract

Dimethyltin(IV) complexes with ethanolamine (1) and biologically significant N-glycosides (2 and 3) were designed and synthesized. The structural elucidation of complexes 1–3 was done using elemental and spectroscopic methods; in addition, complex 1 was studied by single crystal X-ray diffraction studies. The in vitro DNA binding profile of complexes 2 and 3 was carried out by employing different biophysical methods to ascertain the feasibility of glycosylated complexes. Further, the cleaving ability of 2 and 3 was investigated by the agarose gel electrophoretic mobility assay with supercoiled pBR322 DNA, and demonstrated significantly good nuclease activity. Furthermore, both the complexes exhibited significant inhibitory effects on the catalytic activity of human Topo I at lower concentration than standard drugs. Computer-aided molecular docking techniques were used to ascertain the mode and mechanism of action towards the molecular target DNA and Topo I. The cytotoxicity of 2 and 3 against human hepatoma cancer cells (Huh7) was evaluated, which revealed significant regression in cancerous cells as compared with the standard drug. The antiproliferative activities of 2 and 3 were tested against human hepatoma cancer cells (Huh7), and results showed significantly good activity. Additionally, to validate the remarkable antiproliferative activity of complexes 2 and 3, specific regulatory gene expression (MMP-2 and TGF-β) was obtained by real time PCR.

Graphical abstract: Carbohydrate linked organotin(iv) complexes as human topoisomerase Iα inhibitor and their antiproliferative effects against the human carcinoma cell line

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Supplementary files

Article information


Submitted
20 Jul 2013
Accepted
16 Nov 2013
First published
19 Nov 2013

Dalton Trans., 2014,43, 2534-2548
Article type
Paper
Author version available

Carbohydrate linked organotin(IV) complexes as human topoisomerase Iα inhibitor and their antiproliferative effects against the human carcinoma cell line

R. A. Khan, S. Yadav, Z. Hussain, F. Arjmand and S. Tabassum, Dalton Trans., 2014, 43, 2534
DOI: 10.1039/C3DT51973B

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