新医学2016，Vol.47Issue(5)：308-312,5.DOI:10.3969/j.issn.0253-9802.2016.05.007
载125I 标记三螺旋形成寡核苷酸纳米粒的制备及初步应用
Preparation and primary application of 125 I labeled triplex-forming oligonucleotide loaded nanoparticles
摘要
Abstract
Objective Preparing the 1 25 I labeled anti-androgen receptor (AR)gene triplex-forming oligonucleotide loaded nanoparticles,To investigate the inhibitory effects on prostate cancer cells in vitro. Methods Synthesizing the 1 25 I labeled triplex-forming oligonucleotide by Bolton-Hunter Method,then prepar-ing the 1 25 I labeled triplex-forming oligonucleotide loaded nanoparticles (1 25 I-TFO-NP)by double emulsion sol-vent evaporation method.Its size,shape,embedding ratio and drug loading and release characteristics were i-dentified.The uptake of 1 25 I-TFO-NP by prostate cancer cells was measured by γradiation counter.The inhibi-tory effect on cells was test by CCK-8.AR gene expression was detected by Quantitative Real-time PCR and Western Blotting.Results The labeling efficiency and radiochemical purity were (86.87 ±0.45 )% and (96.21 ±0.97)% respectively.The size of 1 25 I-TFO-NP was(298.2 ±0.5)nm in average.The embedding ra-tio and drug loading were(70.6 ±6.6)% and (1 .89 ±0.1 3)μg/mg.The release test in vitro show signifi-cant controlled-release.The uptake of 1 25 I-TFO-NP by prostate cancer cells was significantly higher than that of non-embed 1 25 I-TFO (P <0.01 ).The cellular inhibitory rates of 1 25 I-TFO-NP were significant higher than that of blank control group (P <0.01 ).The AR mRNA expression level of 1 25 I-TFO-NP group were decreased sig-nificantly (P <0.05).Comparing with blank control group and TPO-NP group,the relative expression of AR 1 25 I-TFO-NP group were decreased significantly (P <0.01 ).Conclusions The character of 1 25 I-TFO labeled nanoparticles was fine.The nanoparticles are able to inhibit the proliferation the prostate cancer cells though in-hibiting androgen receptor relative gene and provide ideal carrier for genetic radiotherapy.关键词
前列腺癌/纳米粒/1 25 I标记三螺旋形成寡核苷酸Key words
Prostate cancer/Nanoparticle/125I labeled triplex-forming oligonucleotide引用本文复制引用
朱姝,曹素娥,杨婷,邹琼,焦举,张勇..载125I 标记三螺旋形成寡核苷酸纳米粒的制备及初步应用[J].新医学,2016,47(5):308-312,5.基金项目
国家自然科学基金（30970857）；广东省自然科学基金 （）
