| Literature DB >> 24231745 |
Sze Koon Lee1, Kong Wai Tan2, Seik Weng Ng3, Kah Kooi Ooi4, Kok Pian Ang4, Md Akim Abdah4.
Abstract
A cationic Schiff base ligand, TSB (L) and its Zn (II) complex (1) were synthesized and characterized by using CHN, (1)H-NMR, FT-IR, UV, LC-MS, and X-ray methods. Their ability to inhibit topoisomerase I, DNA cleavage activities, and cytotoxicity were studied. X-ray diffraction study shows that the mononuclear complex 1 is four coordinated with distorted tetrahedral geometry. The singly deprotonated Schiff base ligand L acts as a bidentate ON-donor ligand. Complexation of L increases the inhibitory strength on topoisomerase I activity. Complex 1 could fully inhibit topoisomerase I activity at 250 μM, while L did not show any inhibitory effect on topoisomerase I activity. In addition, L and complex 1 could cleave pBR322 DNA in a concentration and time dependent profile. Surprisingly, L has better DNA cleavage activity than complex 1. The cleavage of DNA by complex 1 is altered in the presence of hydrogen peroxide. Furthermore, L and complex 1 are mildly cytotoxic towards human ovarian cancer A2780 and hepatocellular carcinoma HepG2.Entities:
Keywords: Cytotoxicity; DNA cleavage; Schiff base; Topoisomerase I; Zinc
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Year: 2013 PMID: 24231745 DOI: 10.1016/j.saa.2013.10.084
Source DB: PubMed Journal: Spectrochim Acta A Mol Biomol Spectrosc ISSN: 1386-1425 Impact factor: 4.098