Collation of Anticancer Activities for Benzo/Hydroxypyrone Ligands and Copper(II) Complex with Maltol on 2D Cell Models In Vitro

Abstract

Heterocyclic structures are the basic building blocks of many naturally occurring organic compounds that are important for the development of essential biological processes in plants and animals, including carbohydrates and vitamins. They are also widely used as raw material sources to produce pharmaceuticals. In this study, three ligands from the groups of benzopyrones (chromone-2-carboxylic acid) and hydroxypyrones (maltol and coumalic acid), and a newly prepared complex of copper(II) nitrate with maltol as a ligand were investigated for their ability to inhibit cell proliferation. For research purposes, a series of solutions of the tested materials were prepared at different final concentrations (10–5 mol dm–3, 10–6 mol dm–3, and 10–7 mol dm–3), and then applied to a total of 7 selected cell lines, including one healthy cell line, while the others were tumour cell lines. The results of MTT cytotoxicity assay on the selected 2D cell models showed that none of the selected ligands exhibited antiproliferative activity at any concentration on any of the tested cell lines. The complex of copper(II) nitrate and maltol, in contrast to the tested ligands at the 10–5 mol dm–3 concentration, exhibited significant cytotoxicity as follows: KATO III > HT-29 > Hep G2 > NCI-H358 > MDA-MB-231 > Caco-2 > MRC-5. The healthy cell line (MRC-5) had a survival rate higher than 90.0 % at all tested concentrations, which led to the conclusion of the selectivity of the compound towards tumour cell lines.

Keywords

• maltol
• chromone-2-carboxylic acid
• coumalic acid
• copper(ii) complex
• cell proliferation
• mtt assay
• cell lines
• tumour