三羰基锝([^(99m)Tc(CO)_3(OH_2)_3]^+)标记Morpholino寡核苷酸  

Radiolabeling morpholino oligo with ^(99m)Tc tricarbonyl

作　　者：刘长滨[1] 田嘉禾[1] 邓敬兰[2] 乔宏庆[2] 汪静[2] 

机构地区：[1]解放军总医院核医学科,北京100853 [2]第四军医大学西京医院核医学科,西安710032

出　　处：《核技术》2005年第7期534-537,共4页Nuclear Techniques

基　　金：国家863课题(2002AA205081)部分资助

摘　　要：采用三羰基锝药盒制备三羰基锝([99mTc(CO)3(OH2)3]+),并以DTPA作为双功能螯合剂,标记人工合成的Morpholino寡核苷酸。高效液相色谱(HPLC)证实,此方法三羰基锝产率大于90%,且产率稳定;Morpholino寡核苷酸的标记率为(63±7)%,纯化后比活度为(9.62±1.26)GBq/μg;标记的Morpholino寡核苷酸在生理盐水及新鲜人血清中经过48h仍保持其稳定性(>90%),并保持与其互补链的杂交特性。总之,药盒法制备三羰基锝是一种简单而可靠的方法。Morpholino可以被三羰基锝成功标记并保持其生物活性。The preparation of [99 mTc(CO)3(OH2)3] + using carbonyl kits and the labeling of morpholinos (MORF), a DNA analogue, were described. A 25 mer MORF with a primary amine on the 3' equivalent end attached via a 10 member linker was conjugated with DTPA. The carbonyl kits were reconstituted according to the manufacturer's recommendation. The reversed phase and size exclusion HPLC indicate that the Tc-carbonyl intermediate's yield was more than 90%. The DTPA conjugated MORF was successfully radiolabeled, the labeling efficiency ranged (63±7)%, and the specific activity, which was dependent on the specific activity of [99 mTc(CO)3(OH2)3] +, was (9.62±1.26) GBq/μg. In saline at room temperature and in fresh human serum at 37°C, the radioactivity profile was unchanged over 48 h. This strategy for preparing [99 mTc(CO)3(OH2)3] + using carbonyl kits and labeling MORF with [99 mTc(CO)3(OH2)3] + therefore appears to be suitable for further applications.

关 键 词：Morpholino寡核苷酸 三羰基锝 放射性标记 

分 类 号：R817[医药卫生—影像医学与核医学]