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[阿霉素与单克隆抗体OC-859的共价结合物的制备及其抗肿瘤活性]

[Production of adriamycin covalent binding to monoclonal antibody OC-859 and its anti-tumor activities].

作者信息

Zhang L

机构信息

Peking Union Medical College, Beijing.

出版信息

Zhonghua Fu Chan Ke Za Zhi. 1991 Nov;26(6):346-8, 387.

PMID:1804604
Abstract

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.

摘要

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。

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