Polyether ionophore antibiotics (ionophores) represent a large group of naturally-
occurring lipid-soluble compounds isolated from actinomycetes strains of
Streptomyces genus. Ionophores are able to form complexes with the metal cations,
especially sodium and potassium, and transport them across the lipid membranes
according to electroneutral or electrogenic transport mechanism. This process
disturbs the intercellular Na+/K+ concentration gradient and intracellular pH, leads
to the mitochondrial injuries, cell swelling, vacuolization and finally to programmed
cell death (apoptosis). For this reason, ionophore antibiotics found commercial
use in veterinary medicine as coccidiostatic agents and non-hormonal growth
promoters.
In addition to the industrial use of ionophores, some of them effectively and
selectively inhibit properties of different cancer cells as well as enhance the anti-cancer
effects of radio- and/or chemotherapy. In this group, particularly interesting is
salinomycin because of its potent anti-microbial and anti-cancer activity, including
efficiency against multi-drug resistant cancer cells and cancer stem cells.
A very interesting direction of research is the chemical modification of ionophore
antibiotics, which can lead to obtaining various derivatives with better biological
activity and lower toxicity than those of the starting substances. Because
biological activity of ionophore antibiotics and their derivatives is strictly connected
with the ability to form characteristic pseudocyclic structures around the complexed
cations (host-guest complex), it is also important to establish the detailed information
on these structures.
In this context, our review article is focused on the possible role of salinomycin
and its derivatives in anti-microbial as well as anti-cancer therapy, and gives an overview
of the properties of this antibiotic.
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