Binding of gentamicin to subcellular fractions of rabbit kidney: inhibition by spermine and other polyamines

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Abstract
The accumulation and persistence of gentamicin and other aminoglycoside antibiotics in kidney is often associated with renal damage. To learn more about possible sites and modes of binding, radioactive gentamicin and subcellular fractions from rabbit kidney were examined in vitro. Gentamicin bound avidly to mitochondria, microsomal and brush border vesicles, and, to a lesser extent, to macromolecules present in cytosol. Binding to mitochondria was not associated with inhibition of oxygen consumption. Polyamines such as spermine, spermidine, polymyxin B, polylysine and other aminoglycosides markedly diminished gentamicin binding. The divalent cations, Ca + + and Mg + +, inhibited gentamicin binding slightly, whereas monoamines and diamines had no effect. Many of the polyamines have been reported to have nephrotoxic potential. These data indicate that gentamicin and other nephrotoxic amines have similar binding sites. This may be useful in the identification of specific macromolecules which are responsible for binding and in the search for nontoxic inhibitors.

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