Study of the DNA binding mechanism and in vitro activity against cancer cells of iron(iii) and aluminium(iii) kojic acid derivative complexes

Joanna I. Lachowicz*, Anna Mateddu, Pierpaolo Coni, Claudia Caltagirone, Sergio Murgia, Dan Gibson, Gabriele dalla Torre, Xabier Lopez, Federico Meloni, Giuseppina Pichiri*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

Abstract

Metal ions have unique electrochemical and spectroscopical properties that cannot be attained by purely organic compounds. Most of the metal ions are toxic to humans, but paradoxically, metallodrugs are used in medicine as therapeutics and theranostics. Metallodrugs are eliminated in urine and faeces, and therefore release toxic metals and ligands into aquatic ecosystems, thereby raising concerns regarding environmental risks. The use of metallodrugs based on essential metal ions (i.e., iron, copper and zinc), instead of toxic ions, is a new alternative with minor hazards. Kojic acid is an Asperigillus oryzae metabolite of low toxicity used in the food and cosmetics industries. Its derivatives form stable complexes with iron(iii) ions, which bind effectively to DNA and inhibit DNA polymerization. The iron(iii)/S2 ligand complexes reduce in vitro colon carcinoma (Caco2) cell viability and significantly decrease the cell number. The kojic acid derivative complexes with iron(iii) presented here are an alternative to the currently used platinum complexes in cancer therapy.

Original languageEnglish
Pages (from-to)6254-6263
Number of pages10
JournalDalton Transactions
Volume51
Issue number16
DOIs
StatePublished - 4 Apr 2022

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© 2022 The Royal Society of Chemistry.

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