[Anthracycline transport in sensitive and resistant leukemia cells].
The in-vitro uptake of four anthracyclines into leukemic cells was investigated. The accumulation was found to be dependent on the extracellular anthracycline concentration in a linear fashion. The steady state intracellular drug level was reached very quickly and was found to be correlated to the extracellular pH-value in the range between 6.4 and 7.4. Intracellular anthracycline accumulation was restricted in a leukemic subline (F 4-6 R), which was found to be 86 times more resistant to doxorubicin compared with its wild tpye (F 4-6). The importance of the initial uptake phase of anthracyclines into leukemic cells raises the question whether long-term "cardioprotective" anthracycline application schedules will retain the same antileukemic effect as conventional bolus injection.
Erttmann
R
R
Abteilung für Hämatologie und Onkologie, Universitätskinderklinik, Hamburg.
Erb
N
N
Forcadell de Dios
P
P
Neurath
C
C
Looft
G
G
Landbeck
G
G
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics* / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects*; D055598:Chemical Phenomena; D002621:Chemistry; D003630:Daunorubicin / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000493:pharmacokinetics; D004351:Drug Resistance; D015251:Epirubicin / Q000493:pharmacokinetics; D006801:Humans; D015255:Idarubicin / Q000493:pharmacokinetics; D007938:Leukemia; D051379:Mice; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000378:metabolism*
D000903:Antibiotics, Antineoplastic; D015251:Epirubicin; D004317:Doxorubicin; D015255:Idarubicin; D003630:Daunorubicin
Anthracyclintransport in sensible und resistente Leukämiezellen.