新型肿瘤治疗药物.pdf

CNIC-01919 CAEP-0204 131 I BGTP 的研究 新型肿瘤治疗药物 何佳恒蒋树斌王关全 (中囡工程物理研究院核物理与化学研究所，绵阳，621900) 摘要 成功合成了一种二肤分子一叔丁基氧二肤胶磷酸对破苯盼醋;采 用封管法进行了二肤的131 I 标记，标记率可达 85% ;采用细胞结合实 验对配合物体外生物活性进行了评价，标记抗原保持了原来的亲和 力，在标记等操作过程中未受到明显损伤;并对配合物进行了稳定 性、亲脂性、急性毒性的考察。结果表明，配合物亲脂性高、毒性低、 结构和性能比较稳定?三天后的脱破率约为 12% ;成功建立了肿瘤动 物模型，得到了配合物在正常小鼠和肿瘤大白兔体内的分布结果。 关键词:肤 131 I 活性 111 A New Anticancer Agent一一_131 I BGTP (In Chinese) HE Jiaheng JIANG Shubin WANG GuanQuan (Institute of N udear Physics and Chemistry , CAEP，如1ianyang ， 621900) ABSTRACT A new anticancer precursor , di-peptide[p-Boc-Gly-Tyr-NH (CH )2 NH--PO 2 (ONH )-O-PhI 长 J ， was synthesized and labelled with 131 I using enveloped- tube 4 techniq肘，the labelling yield could reach 85 %. lJ sing cell coalescent method , the biological activity in vitro of the labelled compounds was evaluated , show- ing that the primary appetency was kept and not damaged obviously during la- belling. Rεsults on judgεment of their stability , lipophilicity and toxicity dem- onstrated lower toxicity , higher lipophilicity and lower iodium disassociation percentage « 12 % after 72 h); furthermore , a tumour-bearing animal model , was establishd successfully , on which , the biological properties of the labelled agent was studied. Key words: Peptide , I:Jl 1, Activity 112 引 口 一 一 午 放射性棋标记的单克隆抗体作为一种靶向药物具有许多优点，但是由于单克隆抗体作 为诊断和治疗癌症的载体的