Phospholipase aminoglycosides

Tab. 4.39 Binding of aminoglycosides to phospholipids, energy of aminoglycoside-phospholipid interaction, and inhibition of phospholipase A, activity. (Reprinted from Tab. 1 of ref. 138 with permission from Elsevier Science)...

Drug Aminoglycoside-phospolipid (molar ratio)9 Energy of interaction6 Phospholipase A1 inhibition (%)c... 

Carher MB, Laurent G, Claes PJ, Vanderhaeghe HJ, Tulkens PM. Inhibition of lysosomal phospholipases by aminoglycoside antibiotics in vitro comparative studies. Antimicrob Agents Chemother 1983 23(3) 440-9. 

Hostetler KY, Hall LB, Inhibition of kidney lysosomal phospholipases A and C by aminoglycoside antibiotics possible mechanism of aminoglycoside toxicity, Proc Nat Acad Sci, 1982,79 1663-67. 

Schwertz DW, Kreisberg Jl, Venkatachalam, Effects of aminoglycosides on proximal tubule brush border membrane phosphati-dylinositol-specific phospholipase C, J Pharmac and ExpTherap, 1984,231(1) 48-55. 

E. coli. Phospholipase C, also a metalloenzyme, can also be inhibited by aminoglycosides. Inhibition of dopamine regulating P-type Ca channels by neomycin can also be considered a toxic pathway. Lastly, aminoglycosides have been shown to bind triple-helical DNA, which are known to exist in biological systems as potential regulators of gene expression. ... 

C2iH39NtO,2 581.579 Aminoglycoside antibiotic. Isol. from Streptomyces griseus. Clinically used broad spectrum antibacterial (tuberculostatic) agent. Neuromuscular blocking agent. Phospholipase D inhibitor. Sol. H2O fairly sol. MeOH poorly sol. butanol, hexane. Log P -7.17 (uncertain value) (calc). Indefinite Mp. 

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