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目的：制备抗表皮生长因子受体单克隆抗体（ＥＱ７５）与化疗药物阿霉素（ＡＤＲ）、免疫偶联物（ＥＱ７５－ＡＤＲ），研究该偶联物对人表皮癌Ａ４３１的抑癌作用和小鼠的副作用，为最终应用于临床打下基础。方法：用改进的戊二醛方法制备ＥＱ７５－ＡＤＲ，ＭＴＴ法检测ＥＱ７５－ＡＤＲ对人表皮癌细胞Ａ４３１和对照细胞人羊膜细胞Ｗｉｓｈ的４８ｈ和２ｈ细胞毒作用，建立荷人表皮癌裸鼠模型和Ｃ５７ＢＬ／６Ｊ小鼠模型，观察ＥＱ７５－ＡＤＲ的抑瘤作用，比较ＥＱ７５－ＡＤＲ和ＡＤＲ对Ｃ５７ＢＬ／６Ｊ的副作用。结果：ＥＱ７５－ＡＤＲ对Ａ４３１细胞有明显的细胞毒作用，体外作用４８ｈ，ＥＱ７５－ＡＤＲ对Ａ４３１细胞的杀伤分别是ＥＱ７５，ＡＤＲ和ＥＱ７５与ＡＤＲ混合物（ＥＱ７５＋ＡＤＲ）的５０倍，１４倍和１０倍，而ＥＱ７５－ＡＤＲ对Ｗｉｓｈ细胞的杀伤只有ＡＤＲ和ＥＱ７５＋ＡＤＲ的１／１０，对Ｗｉｓｈ细胞的杀伤只有对Ａ４３１细胞的１／３００，２ｈ作用得到类似结果。ＥＱ７５－ＡＤＲ显著抑制裸鼠体内肿瘤的生长，抑制率高达９２．２％（Ｐ＜０．０１），对Ｃ５７ＢＬ／６Ｊ小鼠的副作用明显低ＡＤＲ。结论：ＥＱ７５－ＡＤＲ具有选择性杀伤作用，在体外和体内对表皮癌均?
Objective: To prepare a monoclonal antibody against epidermal growth factor receptor (EQ75) and chemotherapeutic drugs adriamycin (ADR) and immunoconjugate (EQ75-ADR) to study the anti-cancer effect of this conjugate on human epidermal carcinoma A431. The side effects of mice lay the foundation for the final application to the clinic. METHODS: EQ75-ADR was prepared by modified glutaraldehyde method. 48h and 2h cytotoxicity of EQ75-ADR on human epidermal cancer cell line A431 and control human amniotic cells Wish was detected by MTT assay, and a mouse model of human epidermal carcinoma was established. In C57BL/6J mouse model, the antitumor effect of EQ75-ADR was observed and the side effects of EQ75-ADR and ADR on C57BL/6J were compared. RESULTS: EQ75-ADR had obvious cytotoxicity on A431 cells, and 48 h in vitro. The killing of A431 cells by EQ75-ADR was 50, 14 and 10 times that of EQ75, ADR and EQ75 and ADR mixture (EQ75+ADR), respectively. The killing of Wish cells by EQ75-ADR was only 1/10 of that of ADR and EQ75+ADR. The killing of Wish cells resulted in similar results for only 1/300, 2 h of A431 cells. EQ75-ADR significantly inhibited the growth of tumor in nude mice, and the inhibition rate was as high as 92.2% (P<0.01). The side effects on C57BL/6J mice were significantly lower than that of ADR. Conclusion: EQ75-ADR has a selective killing effect on epidermal cancer both in vitro and in vivo.