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

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. Heterocikličke strukture osnovne su gradivne jedinice mnogih prirodnih organskih spojeva ključnih za odvijanje životnih funkcija u biljnom i životinjskom svijetu kao što su ugljikohidrati i vitamini, a nije strana niti njihova uloga kao sirovina za proizvodnju lijekova. U ovom su radu ispitana antiproliferativna svojstva triju odabranih liganada iz skupine benzopirona (kromon-2-karboksilna kiselina) i hidroksipirona (maltol i kumalična kiselina) kao i novog kompleksnog spoja pripravljenog iz bakrova(II) nitrata s maltolom kao ligandom. Za potrebe istraživanja pripravljene su serije otopina ispitivanih tvari različitih finalnih koncentracija (10 –5 mol dm –3 , 10 –6 mol dm –3 i 10 –7 mol dm –3 ), koje su potom aplicirane na ukupno 7 odabranih humanih staničnih linija od kojih je jedna bila zdrava, a ostale tumorske stanične linije. Rezultati MTT testa citotoksičnosti na odabranim 2D staničnim modelima pokazali su da niti jedan od testiranih liganada ne pokazuje an