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本文报道用葡聚糖为中间体制备鼠抗人胃癌单克隆抗体MGb_2与平阳霉素的结合物。经测算结合物中MGb_2:葡聚糖:平阳霉素的克分子比为1:3:65±5。任制备过程中结合物中抗体活性无损失,结合物对靶细胞具有较强的选择性细胞毒作用(IC_(50)为86μg/ml),优干游离平阳霉素及无关机体结合物(IC_(50)>600μg/ml)。对非靶细胞则毒性很弱(IC_(50)>600μg/ml)。在荷瘤裸鼠体内放射免疫显像及生物学分布研究表明,该结合物能选择性地定位于肿瘤部位,在局部达到较高浓度。提示该结合物是一种较好的导向药物。
In this paper, the conjugates of mouse anti-human gastric cancer monoclonal antibody MGb 2 and pingyangmycin are prepared using dextran as an intermediate. The molar ratio of MGb_2: glucan to pingyangmycin in the conjugate was measured to be 1:3:65±5. In the preparation process, there was no loss of antibody activity in the conjugate, the conjugate had a strong selective cytotoxic effect on the target cells (IC_(50) was 86 μg/ml), excellent dry free pingyangmycin and irrelevant body conjugates (IC_ (50)> 600 μg/ml). The toxicity is weak for non-target cells (IC_(50) > 600 μg/ml). The radioimmunoscintigraphy and biodistribution studies in tumor-bearing nude mice indicate that the conjugate can be selectively localized in the tumor site and reach a higher concentration locally. It is suggested that the conjugate is a better directed drug.