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. 1976 Apr;9(4):696–700. doi: 10.1128/aac.9.4.696

Uptake of Metronidazole and Its Effect on Viability in Trichomonads and Entamoeba invadens Under Anaerobic and Aerobic Conditions

MiklÓs MÜller 1, Donald G Lindmark 1
PMCID: PMC429600  PMID: 1083712

Abstract

[14C]metronidazole used at the chemotherapeutic concentration of 10 μg/ml is taken up rapidly by the anaerobic protozoa Tritrichomonas foetus, Trichomonas vaginalis, and Entamoeba invadens kept under anaerobic conditions. It can be calculated that within 30 to 60 min the intracellular concentration of the label is 50 to 100 times higher than in the medium. The presence of air markedly suppresses the uptake in the trichomonads and abolishes it in E. invadens. The suppression disappears after anaerobic conditions are established. The rate of uptake in T. foetus is dependent on the concentration of the drug in the range studied (1 to 200 μg/ml). Analysis of double reciprocal plots suggests that the drug enters the cells predominantly or exclusively by diffusion. The major factor driving the uptake is most likely the intracellular biotransformation of the compound. If less than 3 μg of drug per mg of protein is taken up by T. foetus no decrease in viability is observed. Above this level the cytotoxic activity corresponds roughly to the amount accumulated in the cell, irrespective of whether the conditions are anaerobic or aerobic.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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