Comparative intracellular uptake of adriamycin and 4'-deoxydoxorubicin by non-small cell lung tumor cells in culture and its relationship to cell survival.

  title={Comparative intracellular uptake of adriamycin and 4'-deoxydoxorubicin by non-small cell lung tumor cells in culture and its relationship to cell survival.},
  author={David J Kerr and A. M. Kerr and R. Ian Freshney and Stanley B. Kaye},
  journal={Biochemical pharmacology},
  volume={35 16},
The effect of adriamycin and 4'-deoxydoxorubicin on cell survival of human lung tumour cells grown in monolayer and as spheroids.
Using growth delay and clonogenic cell survival as end points, we have shown that the 3-dimensional structure of human lung tumour spheroids confers a degree of resistance to the anthracyclines
Cytotoxic drug penetration studies in multicellular tumour spheroids.
The spheroid model demonstrated that penetration is an important aspect of resistance to anthracycline drugs, and this approach may represent a better in vitro system for testing lipophilic analogues of cytotoxic drugs.
Accumulation of anthracenyl-amino acid topoisomerase I and II inhibitors in drug-sensitive and drug-resistant human ovarian cancer cell lines determined by high-performance liquid chromatography
A high-performance liquid chromatography method is described for simultaneous determination of five compounds that exhibit novel mechanisms of action as topoisomerase I and II inhibitors, correlated to the chemosensitivity of the two cell lines to the three compounds.
A Flow Cytometric Clonogenic Assay Reveals the Single-Cell Potency of Doxorubicin.
A flow cytometric clonogenic assay to correlate the amount of drug in a single cell with the cell's ability to proliferate using a cell tracing dye and doxorubicin, a naturally fluorescent chemotherapeutic drug is developed and can be used for any fluorescent or fluorescently labeled drug, including nanoparticles or antibody-drug conjugates.
P-glycoprotein inhibitors enhance saturable uptake of idarubicin in rat heart: pharmacokinetic/pharmacodynamic modeling.
  • M. Weiss, W. Kang
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 2002
Results indicate the existence of a saturable, Michaelis-Menten type uptake process into the heart of idarubicin, which is transported by P-glycoprotein directly out of the membrane before it gets into the cell.
Two-mechanism peak concentration model for cellular pharmacodynamics of Doxorubicin.
The model provides a unified framework for analyzing doxorubicin cellular pharmacokinetic and pharmacodynamic data, and can be applied in mathematical models for tumor response and treatment optimization.
Sensitization of multidrug-resistant colon cancer cells to doxorubicin encapsulated in liposomes
The results suggest that the enhanced cytotoxicity of liposomal doxorubicin to colon cancer cells was due to some secondary non-DNA target and may have clinical applications.


Intracellular uptake of 7-con-o-methylnogarol and adriamycin by cells in culture and its relationship to cell survival.
7-con-O-Methylnogarol is a new anthracycline antitumor agent with significant activity in vivo against murine P388 and L1210 leukemia and B16 melanoma and, even at similar intracellular concentration, more exponentially growing than plateau-phase cells were killed.
A differential interaction of daunomycin, adriamycin, and N-trifluoroacetyladriamycin 14-valerate with mouse peritoneal macrophages.
The interaction of three anthracycline drugs, daunomycin, Adriamycin, and N-trifluoroacetyladriamyin 14-valerate, with mouse peritoneal macrophages was explored and cytoplasmic inclusions were vacuoles containing some amorphous material and not the classical autophagic vacuole containing organelles and membrane lamellae.
Characteristics of doxorubicin transport in human red blood cells.
  • M. Dalmark
  • Biology, Chemistry
    Scandinavian journal of clinical and laboratory investigation
  • 1981
It appears that doxorubicin transport in human erythrocytes takes place by free diffusion of the electrically uncharged (unprotonated) doxorbicin molecule through the lipid domain of the cell membrane.
Cytofluorescence localization of anthracycline antibiotics.
Modification of specific sites on the anthracycline molecule are correlated with intracellular drug localization as defined by fluorescence microscopy, but the effects of these modifications on other aspects of drug accumulation and cell macromolecular biosynthesis are much less predictable.
A Fickian diffusion transport process with features of transport catalysis. Doxorubicin transport in human red blood cells
The hypothesis is proposed that doxorubicin transport across cell membranes takes place by simple Fickian diffusion.
New antitumor anthracyclines.