作　　者： ; ; ; ; ; ; ; ; ;

机构地区： 南方医科大学南方医院

出　　处： 《核技术》 2013年第6期24-28,共5页

摘　　要： 在固相合成小分子肽的过程中完成酪氨酸与cNGQGEQc的连接,采用氯胺-T法进行131I标记,构建肺腺癌NCI-H1975细胞株荷瘤裸鼠模型,随机分成4组,分别为:131I-cNGQGEQc治疗组、131I-cNAQAEQc治疗组、131I治疗组和生理盐水对照组,每组5只。尾静脉注射相应药物后,连续30天观测荷瘤裸鼠肿瘤移植物的大小,计算各组荷瘤裸鼠的肿瘤抑制率。研究结果表明:小分子多肽的131I标记率均大于90%,放化纯度均大于95%。131I-cNGQGEQc对肺腺癌NCI-H1975细胞移植瘤具有明显的抑制作用,治疗后第30天移植瘤肿瘤抑制率为60.93%。阴性多肽131I-cNAQAEQc治疗组的肿瘤抑制率为11.63%。131I治疗组的肿瘤抑制率为10.70%。实验结果表明,131I-cNGQGEQc对肺腺癌NCI-H1975细胞具有良好的亲和力及明显的靶向抑制作用,对非小细胞肺癌的靶向治疗具有潜在应用价值。 Background： Integrin signal transduction pathways provide an important basis for molecular targeting therapy of cancerin tumor growth, infiltration and transfer. Existing research data have shown that small molecular peptide labeled with radionuclide has good clinical application prospects, but the successful researches on lung cancer have not been reported so far. It is considered that the main reason is the lack of small molecule peptide for specific targeting lung cancer. Purpose： Based on the small molecular peptide cNGQGEQc for specifically identifying integrin or3 and [31 found previously, polypeptide cNGQGEQc is selected and radiolabelled with ^131Ⅰ. And the inhibitory effect of ^131Ⅰ-cNGQGEQc in nude mice bearing lung adenocarcinoma is observed. Methods： The coupling of cNGQGEQc and tyrosine was done in the processing of solid phase synthesis of small molecular peptide. Chloramine-T method was used for radiolabelling of cNGQGEQc with 1311. Twenty nude mice bearing NCI-H1975 were built and randomly divided into four groups with five mice in each group, including the group of ^131Ⅰ-cNGQGEQc, the group ofl31I-cNAQAEQc, the group of ^131Ⅰ and the saline control group. The general condition was observed in nude mice beating tumor after tail vein injection of corresponding drugs. And the tumor sizes after grafting were measured per 3 days in 30 days. The inhibitory rate of tumor in each group was calculated. Results： The labeling efficiencies of ^131Ⅰ-cNGQGEQc and 13aI-cNAQAEQc were greater than 90% with the radiochemical purity of more than 95%, and ^131Ⅰ-cNGQGEQc had obvious inhibitory effect for transplantation tumor in nude mice beating NCI-H1975 adenocarcinoma of lung. After a treatment for 30 days the tumor inhibitory rates were 60.93% for the group of ^131Ⅰ-cNGQGEQc, 11.63% for the group of ^131Ⅰ-cNAQAEQ and 10.70% for the group of ^131Ⅰ. Conclusion： ^131Ⅰ-cNGQGEQc has a good affinity and effective inhibit effect for the NCI-H 1975 lung adenocarcinoma. Integrin is a promisin

关 键 词： 肺腺癌 放射治疗 肽类 碘放射性同位素 裸鼠

领　　域： [核科学技术]