Title:Bioconjugation of Ionophore Antibiotics: A Way to Obtain Hybrids with Potent Biological Activity
Volume: 14
Issue: 4
Author(s): Michal Antoszczak*Adam Huczyński
Affiliation:
- Department of Bioorganic Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614 Poznań,Poland
Keywords:
Ionophore antibiotics, monensin, salinomycin, bioconjugation, hybrid compounds, anticancer activity, antibacterial
activity.
Abstract: Polyether antibiotics (ionophores) represent a large group of lipophilic compounds which are
able to form complexes with the metal cations and transport them across the lipid membranes. This process
disturbs the intercellular Na+/K+ concentration gradient and intracellular pH and leads to the mitochondrial
injuries, cell swelling, vacuolization and finally to apoptosis process. For this reason, ionophores
are commonly used in veterinary medicine as the non-hormonal growth-promoting and coccidiostatic
agents. In this group, particularly interesting are monensin and salinomycin because of their
proved anti-tumour activity, including efficiency against multidrug-resistant cancer cells and cancer
stem cells. Prompted by the idea that cancer cells may be individually effectively killed by these compounds,
a very interesting direction of research is bioconjugation process of ionophores. This review is
focused on the possible role of hybrids of ionophore antibiotics with other biologically active substances
in anti-cancer and anti-bacterial treatment and gives an overview of their properties.