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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。
The immunoconjugates of streptavidin and anti-human hepatoma monoclonal antibody (McAb) 3A5 were prepared by the activated ester method. The conjugate has both biological activity and ultraviolet absorption characteristics. The ratio of antibody to streptavidin-coupled molecules was 1:2 to 6, the protein recovery was 76%, streptavidin retained 12.5% of the original activity, and antibody activity was substantially completely maintained. However, as the number of coupled drug molecules increases, the antibody activity decreases. The conjugates showed a 63-fold inhibition of hepatocellular carcinoma BEL-7402 cells in the in vitro cell clone generation assay, which was 63 times greater than that of free streptavidin, whereas the role of KB cells in human pharyngeal epithelial cancer cells that were not related to antigenicity was greater than that of free strands. Melanin is 11 times weaker. The above results indicate that the immunoconjugate exhibits a selective killing effect on the target cells.