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以葡聚糖(Dex)氧化产物多醛基葡聚糖作为中间载体,将氨甲喋呤(MTX)共价偶联于抗小鼠宫颈癌单克隆抗体AU_(14-1)(IgG)上,制得AU_(14-1)-Dex-MTX偶合物;其中IgG与MTX摩尔比为1:20。间接膜免疫荧光试验表明,偶合物中AU_(14-1)对靶肿瘤U_(14)细胞的特异结合活性在3.75×10~(-8)M水平,与未偶合的AU_(14-1),相似。体外抗肿瘤实验表明,偶合物不仅获得了由单克隆抗体导向的选择性药物抗肿瘤作用,且对HeLa细咆的生长抑制作用强于U_(14)细胞,进一步证明了“进化抗原”理论。本研究提示AU_(14-1)-Dex-MTX偶合物具有临床应用的潜在性。
Dextran (Dex) oxidation product polyaldehyde-based dextran was used as an intermediate carrier to covalently couple methotrexate (MTX) to anti-mouse cervical cancer monoclonal antibody AU_(14-1)(IgG). AU_(14-1)-Dex-MTX conjugate; wherein the molar ratio of IgG to MTX is 1:20. The indirect membrane immunofluorescence assay showed that the specific binding activity of AU_(14-1) to target U_(14) cells in the conjugate was 3.75×10~(-8)M and uncoupled AU_(14-1). ,similar. In vitro anti-tumor experiments showed that the conjugate not only obtained the anti-tumor effect of the selective drug directed by the monoclonal antibody, but also had a stronger growth inhibitory effect on HeLa than the U_(14) cells, which further proved the theory of “evolutionary antigen”. This study suggests that AU_(14-1)-Dex-MTX conjugates have the potential for clinical application.