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. 2006 Sep;50(9):3173-4.
doi: 10.1128/AAC.00427-06.

Intracellular penetration and activity of DX-619 in human polymorphonuclear leukocytes

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Intracellular penetration and activity of DX-619 in human polymorphonuclear leukocytes

Isabel García et al. Antimicrob Agents Chemother. 2006 Sep.

Abstract

The intracellular penetration and activity of DX-619 in human polymorphonuclear leukocytes have been evaluated. DX-619 reached intracellular concentrations 10 times higher than the extracellular concentrations reached. Uptake was rapid, reversible, nonsaturable, and affected by environmental temperature, some metabolic inhibitors, and a soluble membrane activator. DX-619 showed intracellular activity against Staphylococcus aureus.

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Figures

FIG. 1.
FIG. 1.
DX-619 uptake by human PMNs and efflux of PMN-associated DX-619 after removal of the extracellular drug (n = 4). The extracellular concentration was 2 μg/ml. Error bars indicate standard deviations.
FIG. 2.
FIG. 2.
Activities of DX-619 and ciprofloxacin against intracellular S. aureus in human PMNs (n = 4). Data are expressed as percentages of surviving bacteria after 3 h of incubation relative to controls without antimicrobial agents (means ± standard deviations [error bars]). *, P was <0.05 relative to ciprofloxacin.

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