^(131)I-fulvestrant的合成与鉴定

Synthesis and identification of ^(131)I-fulvestrant

目的:建立氟维司群(fulvestrant)放射性碘(^(131)I)标记技术。方法:采用改良氯胺-T法对氟维司群进行放射性碘标记,纸层析法测定标记率及标记物稳定性,柱层析法分离及纯化,质谱法鉴定标记化合物,细胞结合实验及MTT实验检测标记化合物对MCF-7(ER+)细胞的结合及抑制能力。结果:在pH 7.5,室温反应5 min的条件下,碘化氟维司群标记率为(62.34±1.80)%,放化纯度为(98.6±3.4)%,48 h半数抑制浓度(IC50)为35μCi,标记化合物具有良好的稳定性且保留了与人乳腺癌细胞MCF-7(ER+)的结合能力。结论:成功利用放射性碘标记氟维司群,为今后开发新型乳腺癌药物提供可能。

Objective ：To label the fulvestrant （an endocrine therapy drug for breast cancer） with the radioiodine. Methods ：The fulvestrant was radioiodine labeled by improved chloramine T method. The paper chromatography was used to detect the labeling rate and the stability of the labeled compound. The column chromatography was used to detect the separation and purification of labeled compound. The changes in physicochemical property of the 131I-fulvestrant was detected by mass-spectrography;the combining ability and inhibiting ability of labeled compound to human breast cancer ceils MCF-7（ER＋） was detected by cell binding assay and MTr assay. Results：When the reaction lasted for 5 min at room temperature at the pH value of 7.5,the radiochemical yield of the radioiodine labeling to fulvestrant was （62.34 ± 1.80）% ,radiochemical purity was （98.6 ± 3.4）% ,the half maximal inhibitory concentration （IC50） of 48 h was 35 uCi. The labeled compound was stable and its combining ability to human breast cancer cells MCF-7（ER＋） was also retained. Conclusion：The radioiodine labeling to the fulvestrant is successful, and it may be used to develop a new drug for breast cancer.