PMID: 3754895Jun 1, 1986Paper

Inhibition of renal membrane binding and nephrotoxicity of aminoglycosides

The Journal of Pharmacology and Experimental Therapeutics
P D WilliamsD B Bennett

Abstract

The initial event in the renal tubular reabsorption of nephrotoxic aminoglycosides involves binding to brush border membranes. This primary event was measured in renal brush border membrane vesicles prepared from rat renal cortex utilizing [3H]gentamicin. In order to gain structure-activity information regarding this interaction the effect of substances having chemical similarities to aminoglycosides (sugars, polyamines and amino acids) on gentamicin binding to brush border membranes was determined. Polyamino acids were found to possess the greatest inhibitory potency. In addition to polymers of cationic amino acids (lysine, ornithine, arginine and histidine), polymers of neutral (asparagine) and acidic (aspartic and glutamic acid) amino acids also exhibited inhibition of the membrane binding of gentamicin. Inasmuch as inhibition of renal membrane binding has the potential to decrease aminoglycoside nephrotoxicity, several polyamino acids that inhibited membrane binding were tested in vivo for potential protective activity vs. gentamicin- and amikacin-induced nephrotoxicity. Polyasparagine90 and polyaspartic acid100 inhibited gentamicin and amikacin nephrotoxicity completely when coadministered to rats with the aminoglycosides....Continue Reading

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Aminoglycosides (ASM)

Aminoglycoside is a medicinal and bacteriologic category of traditional Gram-negative antibacterial medications that inhibit protein synthesis and contain as a portion of the molecule an amino-modified glycoside. Discover the latest research on aminoglycoside here.

Aminoglycosides

Aminoglycoside is a medicinal and bacteriologic category of traditional Gram-negative antibacterial medications that inhibit protein synthesis and contain as a portion of the molecule an amino-modified glycoside. Discover the latest research on aminoglycoside here.

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