CAJ | 학술논문

目的筛选99Tcm标记depreotide的最佳条件,并通过99Tmm-depreotide与人肺腺癌A549细胞结合特性的研究,评价其作为肿瘤生长抑素受体显像剂的可靠性.方法 ①采用直接标记法,在不同pH值(5.0、6.0、7.0)的磷酸缓冲溶液和不同温度(15 ℃、37 ℃、50 ℃)条件下对depreotide进行99Tcm标记,以纸层析法测定标记率,并通过对比分析,筛选出最佳标记条件.②采用受体放射分析法,分别在不同温度下将99Tcm-depreotide与A549细胞孵化,分析不同温度在A549细胞对99Tcm-depreotide摄取率和滞留率中的作用.结果 ①相同温度下,缓冲液pH=6.0时,99Tcm与depreotide的标记率高于pH=5.0和pH=7.0两组;随着反应温度由15℃逐渐升高到50 ℃,各pH实验组的标记率呈不同程度下降.②A549细胞对99Tcm-depreotide的摄取率随温度的升高逐渐增加,在37℃时,摄取峰值时间在60 min;对99Tcm-depreotide的清除速度不依赖于温度,37 ℃时的半清除时间为48 min.结论在低温(＜15℃)和弱酸性环境下,99Tcm直接标记depreotide的标记率高,稳定性好.在37 ℃时,A549细胞特异性结合99Tcm-depreotide,具有适于受体显像的摄取峰值时间和半清除时间.
목적 사선99Tcm표기depreotide적최가조건,병통과99Tmm-depreotide여인폐선암A549세포결합특성적연구,평개기작위종류생장억소수체현상제적가고성.방법 ①채용직접표기법,재불동pH치(5.0、6.0、7.0)적린산완충용액화불동온도(15 ℃、37 ℃、50 ℃)조건하대depreotide진행99Tcm표기,이지층석법측정표기솔,병통과대비분석,사선출최가표기조건.②채용수체방사분석법,분별재불동온도하장99Tcm-depreotide여A549세포부화,분석불동온도재A549세포대99Tcm-depreotide섭취솔화체류솔중적작용.결과 ①상동온도하,완충액pH=6.0시,99Tcm여depreotide적표기솔고우pH=5.0화pH=7.0량조;수착반응온도유15℃축점승고도50 ℃,각pH실험조적표기솔정불동정도하강.②A549세포대99Tcm-depreotide적섭취솔수온도적승고축점증가,재37℃시,섭취봉치시간재60 min;대99Tcm-depreotide적청제속도불의뢰우온도,37 ℃시적반청제시간위48 min.결론 재저온(＜15℃)화약산성배경하,99Tcm직접표기depreotide적표기솔고,은정성호.재37 ℃시,A549세포특이성결합99Tcm-depreotide,구유괄우수체현상적섭취봉치시간화반청제시간.
Objective To establish a simple and reliable method of making 99Tcm-depreotide by direct labeling. Furthermore, to investigate 99Tcm-depreotide's specific receptor binding properties in vitro with human lung adenocarcinoma cell line A549, and to evaluate the potentiality of 99Tcm-depreotide as a through a direct labeling using SnCl2 as reductant. Compared the labeling efficiency in different pH and temperature, then searched the best labeling method. Assessed the radiochemical purity and stability in uptake kinetics, then stagnation and half time were compared at different temperature and time points, and that 99Tcm-depreotide was incubated with A549 cell the internalization and surface-bound activity were group was higher than that of pH5.0 and pH7.0 groups. At the same pH,the labeling rate of all of the three The uptake rate increased with temperature at the same time point, and the peak time of maximum uptake was 60min at 37 ℃. The cleaning curves were similar at different temperature,and the half cleaning time at 37 ℃ was 48 min. Conclusions When depreotide was labeled with 99Tcm, the temperature could not be too high(＜15 ℃) and the pH would better be less than 6.0. 99Tcm-depreotid was a potential somatostatin receptor imaging agent with its appropriate the peak time of maximum uptake and the half cleaning time at 37 ℃.