Fritzer M, Barabas K, Szüts V, Berczi A, Szekeres T, Faulk W P, Goldenberg H
Institut für Medizinische Chemie, University of Vienna, Austria.
Int J Cancer. 1992 Oct 21;52(4):619-23. doi: 10.1002/ijc.2910520421.
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.
通过戊二醛将阿霉素与转铁蛋白偶联而成的结合物对人早幼粒细胞（HL - 60）和红白血病细胞（K562）具有细胞毒性。通过胸腺嘧啶核苷掺入法和MTT法评估，结合物对阿霉素敏感细胞的生长抑制作用比对游离阿霉素更强。转铁蛋白 - 阿霉素结合物对阿霉素耐药的K562和HL - 60细胞的细胞毒性分别比游离药物高3倍和10倍以上。结合物的作用取决于其阿霉素含量，即其偶联数。
