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单克隆抗体与链黑菌素偶联物的抗肝癌BEL-7402细胞活性
引用本文:刘亚萍,吴剑波. 单克隆抗体与链黑菌素偶联物的抗肝癌BEL-7402细胞活性[J]. 中国医学科学院学报, 1993, 0(3)
作者姓名:刘亚萍  吴剑波
作者单位:中国医学科学院医药生物技术研究所 北京(刘亚萍),中国医学科学院医药生物技术研究所 北京(吴剑波)
摘    要:采用活化酯法制备链黑菌素与抗人肝癌单克隆抗体(McAb)3A5的免疫偶联物,该偶联物兼有二者的生物活性和紫外吸收特征。抗体与链黑菌素偶联分子比为1:2~6,蛋白回收率为76%,链黑菌素保留原活性的12.5%,抗体活性基本上完全保持。但随着药物分子偶联数目的增加,抗体活性减小。偶联物在体外细胞克隆生成试验中,对肝癌BEL-7402细胞的抑制作用为游离链黑菌素的63倍,而对与抗原性无关的人咽上皮癌KB细胞的作用则较游离的链黑菌素弱11倍。以上结果表明,该免疫偶联物对靶细胞显示选择性杀伤作用。

关 键 词:抗体  单克隆  链黑菌素  免疫偶联物  细胞毒性  肝癌细胞

Cytotoxicity to Hepatoma BEL-7402 Cells of an Antitumor Monoclonal Antibody-Streptonigrin Conjugate
Liu Yaping and Wu Jianbo. Cytotoxicity to Hepatoma BEL-7402 Cells of an Antitumor Monoclonal Antibody-Streptonigrin Conjugate[J]. Acta Academiae Medicinae Sinicae, 1993, 0(3)
Authors:Liu Yaping and Wu Jianbo
Abstract:Streptonigrin, a highly active antitumor antibiotic, was covalently conjugated to anti-human heptoma monoclonal antibody 3A5 via the active ester method. The conjugate showed biological activities and UV spectra characteristics of Streptonigrin and McAb 3A5. The molar ratio of Streptonigrin to 3A5 was 2~6:1, with protein recovery of 76%. The conjugate retained 12.5% of drug activity and nearly full antibody activity, though as the number of Streptonigrin molecules in the conjugate increased, the antibody activity of the conjugate decreased. As determined by clonogenic assay with human heptoma BEL-7402 cells in vitro, the inhibitory poteney of the conjugate was 63-fold stronger than that of free Streptonigrin. For KB cells (which react weakly with 3A5) the cytotoxicity was 11-fold weaker. The results indicate that the McAb 3A5-streptonigrin conjugate is selective for target cells.
Keywords:antibodies   monoclonal streptonigrin immunoconjugate cytotoxicity heptoma cell
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