氯米芬的碘-125标记及生物分布研究，以探讨其作为乳腺癌成像模型的潜在用途。

(125)I labeling of clomiphene and biodistribution studies for possible use as a model in breast cancer imaging.

作者信息

Ibrahim I T, El-Kolaly M T, Aboumanei M H, Abdelbary A

机构信息

Labeled Compound Department, Hot Lab Center, Egyptian Atomic Energy Authority, Cairo 11371, Egypt; Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Appl Radiat Isot. 2016 Sep;115:37-44. doi: 10.1016/j.apradiso.2016.06.004. Epub 2016 Jun 13.

DOI:10.1016/j.apradiso.2016.06.004

PMID:27337647

Abstract

Clomiphene has growth-inhibitory effects of breast cancer cells, clomiphene was successfully labeled with (125)I via direct electrophilic substitution reaction with labeling yield 97%. It was obtained at optimum substrate amount of 0.5mg, Chloramine-T was used as an oxidizing agent at optimum amount of 25µg. Labeling reactions was done at pH 5 at ambient temperature. This study showed good in vitro and in vivo stability of the (125)I-clomiphene. The radiolabeled compound showed high ascetic fluid uptake of 18.12±0.27% at 30min post-injection. Solid tumor uptake of (125)I-clomiphene was 12.48±0.32% at 30min post-injection. This data revealed the localization of tracer in tumor tissue with high percent sufficient to use (125)I-clomiphene as a promising tool for the diagnosis of breast cancer.

摘要

克罗米芬对乳腺癌细胞有生长抑制作用，通过直接亲电取代反应成功将克罗米芬用（125）I标记，标记产率为97%。在最佳底物量0.5mg时获得，使用氯胺 - T作为氧化剂，最佳量为25μg。标记反应在pH 5、室温下进行。本研究表明（125）I - 克罗米芬在体外和体内具有良好的稳定性。放射性标记化合物在注射后30分钟时腹水摄取率高，为18.12±0.27%。（125）I - 克罗米芬在注射后30分钟时实体瘤摄取率为12.48±0.32%。该数据揭示了示踪剂在肿瘤组织中的定位，其高百分比足以将（125）I - 克罗米芬用作诊断乳腺癌的有前景的工具。