中山大学学报（医学科学版）2017，Vol.38Issue(6)：848-853,6.
99m锝标记前列腺癌PSMA适配体的制备和临床前研究
Preparation and Preclinical Study of 99mTc-labeled Prostate Cancer Aptamer
摘要
Abstract
[Objective]To radiolabel the PSMA aptamer A10-3.2 with 99mTc , and explore its biological characteristics in vivo and in vitro.[Methods]Using Succinimidyl 6-hydrazinonicotinate hydrochloride (SHNH) as the bifunctional chelating agent to label aptamer A10-3.2 with 99mTc, then tested for the stability in vitro, the specific uptake by prostate cancer LNCaP cells (PSMA+) , the characteristics of SPECT/CT imaging and biodistribution in LNCaP tumor-bearing NOD/SCID mice.[Results]The labeling rate and radiochemical purity of the products (99mTc-SHNH-A10-3.2) are(71.31 ± 6.78)% and 97.03%,respectively. 99mTc-SHNH-A10-3.2 had obvious target specificity for PSMA positive prostate cancer LNCaP cells, its uptake rate was significantly higher than PSMA nega?tive PC-3 cells (P<0.01). And in tumor-bearing mice, the tumor has a certain uptake and a high ratio of the tumor tissue to the mus?cle.[Conclusion]This study successfully constructed 99mTc-labeled PSMA-targeted aptamer A10-3.2, which has a good stability and targeting in vivo and in vitro, has a high tumor tissue/muscle ratio in tumor-bearing mice, which show that it may be a potential target?ed molecular imaging agent for prostate cancer.关键词
前列腺癌/前列腺特异性膜抗原/适配体/锝/SPECT/CT显像Key words
prostate cancer/PSMA/aptamer/99mTc/SPECT/CT imaging分类
医药卫生引用本文复制引用
杨婷,焦举,吕殷婷,邹琼,曹素娥,江淑琴,张勇..99m锝标记前列腺癌PSMA适配体的制备和临床前研究[J].中山大学学报（医学科学版）,2017,38(6):848-853,6.基金项目
广东省科技计划项目(2013B021800083、2014A020212153) （2013B021800083、2014A020212153）
广东省自然科学基金(2015A030313106) （2015A030313106）
教育部博士点基金(20130171110081) （20130171110081）
广东省医学科研基金(B2014147) （B2014147）
