Zhang L
Peking Union Medical College, Beijing.
Zhonghua Fu Chan Ke Za Zhi. 1991 Nov;26(6):346-8, 387.
Using periodate oxidation method adriamycin was linked to monoclonal antibody OC859, and a monoclonal antibody-adriamycin (McAb ADR) conjugate was produced. The molar ratio of ADR:OC859 was 12:1. This drug-antibody conjugate still retained its cytotoxic effects and antibody activities. The cytotoxic effects of McAb-ADR conjugate on the growth of tumor cells CAOV3 was determined by microculture tetrazolium assay. It revealed that when the concentration of the McAb-ADR conjugate was 1 microM more than 50% of CAOV3 cells were inhibited. And for normal endometrial cells no more than 50% inhibition could be shown even with the concentration up to 10 microM. In vivo, the human ovarian epithelial carcinoma transplanted to nude mice was also inhibited with McAb-ADR conjugate. The above results showed that the McAb-ADR conjugate can selectively cause inhibition of tumor cells both in vivo and in vitro, and may be helpful in the treatment of ovarian epithelial carcinoma in the future.
采用高碘酸盐氧化法将阿霉素与单克隆抗体OC859连接,制备出单克隆抗体-阿霉素(McAb ADR)偶联物。阿霉素与OC859的摩尔比为12:1。该药物-抗体偶联物仍保留其细胞毒性作用和抗体活性。采用微量培养四氮唑蓝法测定McAb-ADR偶联物对肿瘤细胞CAOV3生长的细胞毒性作用。结果显示,当McAb-ADR偶联物浓度为1微摩尔时,超过50%的CAOV3细胞受到抑制。而对于正常子宫内膜细胞,即使浓度高达10微摩尔,抑制率也不超过50%。在体内,移植到裸鼠的人卵巢上皮癌也受到McAb-ADR偶联物的抑制。上述结果表明,McAb-ADR偶联物在体内和体外均可选择性地抑制肿瘤细胞,可能对未来卵巢上皮癌的治疗有帮助。