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将羟基喜树碱(HCPT)、鬼臼毒素(PPT)的衍生物分别与胃癌单克隆抗体RSF_9共价交联成免疫结合物。结合物中每分子抗体分别引入10分子 HCPT 和16分子PPT,而抗体活性仍较好保存。体外细胞杀伤试验显示两免疫结合物对胃癌靶细胞的杀伤力明显优于游离的药物和无关抗体结合物,对非靶细胞的毒性则显著低于游离的药物,提示 HCPT PPT 的衍生物偶合后具较高的杀伤活性,两个免疫结合物具有较强的选择性杀伤靶细胞的作用。
Hydroxycamptothecin (HCPT) and podophyllotoxin (PPT) derivatives were covalently cross-linked with gastric cancer monoclonal antibody RSF_9 into immunoconjugates. In the conjugate, 10 molecules of HCPT and 16 molecules of PPT were introduced per molecule of antibody, and the antibody activity was still well preserved. The in vitro cell killing assay showed that the two immune conjugates had a significantly greater lethality to gastric cancer target cells than free drugs and irrelevant antibody conjugates, and the toxicity to non-target cells was significantly lower than that of free drugs, suggesting that the HCPT PPT derivatives were coupled With higher killing activity, the two immune conjugates have a strong selective killing effect on target cells.