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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.
Keywords: Ionophore antibiotics, monensin, salinomycin, bioconjugation, hybrid compounds, anticancer activity, antibacterial activity.
Mini-Reviews in Organic Chemistry
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.
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Antoszczak Michal*, Huczyński Adam, Bioconjugation of Ionophore Antibiotics: A Way to Obtain Hybrids with Potent Biological Activity, Mini-Reviews in Organic Chemistry 2017; 14 (4) . https://dx.doi.org/10.2174/1570193X14666170518112608
DOI https://dx.doi.org/10.2174/1570193X14666170518112608 |
Print ISSN 1570-193X |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6298 |
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