免疫导向药物B_（159）－Dex－EPI与B_（159）－Dex－ADR抗肿瘤活性研究

作者应用氧化葡聚糖Ｔ_（１０）作为交联剂，将抗Ｂ淋巴细胞白血病单抗Ｂ_（１５９）分别与抗癌药物表阿霉素（ＥＰＩ）和阿霉素（ＡＤＲ）连接，制成免疫导向药物Ｂ_（１５９）－Ｄｅｘ－ＥＰＩ和Ｂ_（１５９）－Ｄｅｘ－ＡＤＲ，Ｂ_（１５９）与ＥＰＩ或ＡＤＲ的克分子比均为１：１２～１４。经活细胞免疫荧光法和细胞ＥＬＩＳＡ法测定，免疫导向药物保持了抗体活性。ＭＴＴ试验证实，两种免疫导向药物均具有明显的选择性杀伤作用，对非靶细胞毒性小；两种免疫导向药物对靶细胞的杀伤作用明显强于游离药物和正常鼠抗体结合物；Ｂ_（１５９）－Ｄｅｘ－ＥＰＩ的靶细胞毒性作用强于Ｂ_（１５９）－Ｄｅｘ－ＡＤＲ。

Study of Antitumor Activity of B_(159)-Dex-EPI and B_(159)-Dex- ADR Immunoconjugates in Vitro

An anti-human B lymphocytic leukemia monoclonal antibody B_(159) was selected to conjugate respectively with epirubicin (EPI) and adriamycin (ADR) via oxidative dextran T_(10) as linker to construct B_(159)-Dex-EPI and B_(159)-Dex-ADR.The molar ratios of B_(159) to the drugs were all 1 to l2-14 in these conjugates.The conjugates were proven keeping the original immunological activity with living cell immunofluorescence test and cell ELISA.MTT test indicated that the conjugates had stronger selective cytotoxicity against the target cell and less cytotoxicity against non-target cells than free drugs and normal mice IgG conjugates.B_(159)-Dex-EPI had stronger antitumor activity than B_(159)-Dex-ADR.