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以７５％、５０％、３０％和２５％氧化程度的葡聚糖为偶联剂，制备阿霉素与转铁蛋白受体单抗的偶联物Ｃ７５、Ｃ５０、Ｃ３０和Ｃ２５，并对其各方面参数作了比较，结果表明，其偶联度分别为１６２、１０３、７２与５２Ｍｏｌｅｓ／每个抗体分子，即葡聚糖的氧化程度越高，其偶联度越高。然而，以１３１Ｉ－ＳｐＡ为二抗的细胞结合分析结果表明，Ｃ７５、Ｃ５０均丧失大部分的抗体活性。３Ｈ－ＴｄＲ掺入细胞抑制实验也表明，Ｃ７５与Ｃ５０丧失大部分药物活性，而Ｃ３０均保持大部分的抗体活性与药物活性，认为３０％氧化葡聚糖为最佳偶联方案。实验还表明，Ｃ３０对体外靶细胞的杀伤具有高度的选择性。而且，其分药物活性的丧失，可以通过延长与靶细胞的孵育时间而得到补偿。号。就Ａｄｒ－Ｄｅｘ－ＷｕＴ９偶联物而言，同样孵育４ｈ，对肝癌细胞和正常肝细胞却有不同和杀伤率，（ｐ＜０．０１，见表中的▲号）。说明偶联物Ｃ３０对肝癌细胞的杀伤作用具有高度的选择性。与此相反，孵育４ｈ，Ａｄｒ不但对肝癌细胞，而且对正常肝细胞也产生明显的细胞毒作用（ｐ＞０．０５，见表中的△△号），说明游离的Ａｄｒ无明显的选择性。而且Ａｄｒ与ＷｕＴ９偶联之后，所产生的部分药物活性的丧失（约丧失２?
The conjugates C75, C50, C30 and C25 of doxorubicin and transferrin receptor monoclonal antibody were prepared with dextran of 75%, 50%, 30% and 25% All parameters were compared, the results showed that the degree of coupling were 162,103,72 and 52Moles / each antibody molecule, that is, the higher the degree of oxidation of dextran, the higher the degree of coupling. However, the cell binding assay with 131I-SpA as a secondary antibody showed that most of the antibody activity was lost by both C75 and C50. 3H-TdR incorporation in cell inhibition experiments also showed that C75 and C50 lost the majority of drug activity, while C30 maintained most of the antibody activity and drug activity, that 30% dextran is the best coupling protocol. Experiments also show that C30 is highly selective for killing target cells in vitro. Moreover, the loss of its pharmacological activity can be compensated for by prolonging the incubation time with the target cells. number. For the Adr-Dex-WuT9 conjugate, the same incubation for 4 h resulted in different rates of killing of hepatoma cells and normal liver cells (p <0.01, see ▲ in the table). This shows that the conjugate C30 has a high selectivity for the killing of hepatoma cells. On the contrary, Adr not only had obvious cytotoxic effect on hepatoma cells but also on normal hepatocytes (p> 0.05, see △△ in the table), indicating that there was no obvious selectivity for free Adr . And after Adr and WuT9 coupling, the resulting loss of part of the drug activity (about loss of 2?