Cytotoxicity of a transferrin-adriamycin conjugate to anthracycline-resistant cells.
Conjugates of adriamycin coupled to transferrin by glutaraldehyde are cytotoxic to human promyelocytic (HL-60) and erythroleukemic (K562) cells. Growth inhibition of adriamycin-sensitive cells, as evaluated by thymidine incorporation and the MTT-assay, was higher for conjugates than for free adriamycin. The cytotoxicity toward adriamycin-resistant K562 and HL-60 cells was 3-fold and more than 10-fold higher, respectively, for the transferrin-adriamycin conjugate than for the free drug. The effect of the conjugate was dependent on its adriamycin content, i.e., on its conjugation number.
Fritzer
M
M
Institut für Medizinische Chemie, University of Vienna, Austria.
Barabas
K
K
Szüts
V
V
Berczi
A
A
Szekeres
T
T
Faulk
W P
WP
Goldenberg
H
H
D004317:Doxorubicin / Q000008:administration & dosage* / Q000494:pharmacology; D004351:Drug Resistance; D006801:Humans; D004915:Leukemia, Erythroblastic, Acute / Q000473:pathology; D015473:Leukemia, Promyelocytic, Acute / Q000473:pathology; D014168:Transferrin / Q000008:administration & dosage* / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D014168:Transferrin; D004317:Doxorubicin