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Cellular kinetics of prednimustine versus chlorambucil plus prednisolone in vitro

  • Original Articles
  • Prednimustine, Chlorambucil, Prednisolone, Cellular Kinetics, Cytotoxicity
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Summary

Intracellular concentrations of prednimustine (PM), chlorambucil (CLB), phenylacetic acid mustard (PAAM) and prednisolone (P) were measured in different experimental tumor cell lines that had been incubated with either PM or CLB+P. For intracellular analytical determination, we modified a high-pressure liquid chromatographic method for the detection of these substances in plasma. Intact PM could be detected in the intracellular compartment of the incubated tumor cells. PM-incubated cells from PM-injected rats exhibited a higher intracellular concentration-time integral (PAAM) and longer concentration-time profiles for drugs with alkylating capacity than did cells exposed to the CLB+P mixture or to CLB. PAAM was not detectable after incubation of cells with PM, whereas in CLB-incubated cells the AUC of PAAM exceeded that of the parent drug CLB. Our in vitro results therefore favour the concept of a facilitated intracellular uptake and an increased antiproliferative effect for PM versus CLB and CLB+P.

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Authors and Affiliations

  1. Department of Internal Medicine, Mary's Hospital Bottrop, FRG

    Eugen Musch

  2. Department of Internal Medicine, University of Bonn, Sigmund-Freud-Str. 25, D-5300, Bonn 1, Federal Republic of Germany

    Mouhamad Malek

  3. Institute for Physiological Chemistry, University of Bonn, FRG

    Jasna Peter-Katalinic & Heinz Egge

  4. Institute for Radiobiology, University of Bonn, FRG

    Hermann Rink

  5. Department of Internal Medicine, University of Cologne, FRG

    Bernd Lathan

  6. Institute for Biochemistry, University of Berlin, FRG

    Eberhard Riedel

Authors
  1. Eugen Musch
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  2. Mouhamad Malek
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  3. Jasna Peter-Katalinic
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  4. Heinz Egge
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  5. Hermann Rink
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  6. Bernd Lathan
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  7. Eberhard Riedel
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Dedicated to Prof. Dr. H. J. Dengler on the occasion of his 65th birthday. This study was supported by the Ministry of Science and Research of Nordrhein-Westfalen

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Musch, E., Malek, M., Peter-Katalinic, J. et al. Cellular kinetics of prednimustine versus chlorambucil plus prednisolone in vitro. Cancer Chemother. Pharmacol. 29, 297–304 (1992). https://doi.org/10.1007/BF00685948

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  • DOI: https://doi.org/10.1007/BF00685948

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