中国医药导刊
中國醫藥導刊
중국의약도간
CHINESE JOURNAL OF MEDICAL GUIDE
2014年
10期
1339-1342
,共4页
谢文晖%章斌%刘慈懿%常城%雷贝%王利华%吴翼伟
謝文暉%章斌%劉慈懿%常城%雷貝%王利華%吳翼偉
사문휘%장빈%류자의%상성%뢰패%왕리화%오익위
多肽%锝%肺癌%药代动力学%精氨酸-谷氨酸-苏氨酸
多肽%锝%肺癌%藥代動力學%精氨痠-穀氨痠-囌氨痠
다태%득%폐암%약대동역학%정안산-곡안산-소안산
Peptides%Technetium%Lung cancer%Pharmacokinetics%Arginine-glutamic-glutamic(RET)
目的:研究99mTc-RET(Arg-Glu-Thr)与肺癌细胞结合及其在正常小鼠体内分布和药代动力学。方法:采用99mTc直接法标记RET,行99mTc-RET与非小细胞肺癌细胞A549和H1299的结合实验。正常小鼠尾静脉注射99mTc-RET后不同时间处死,取主要脏器或组织,测定其每克组织百分注射剂量率(%ID/g)。另取尾静脉注射99mTc-RET后不同时间小鼠血液,测量放射性计数并计算药代动力学参数。结果:99mTc直接标记RET的标记率大于90%。99mTc-RET与非小细胞肺癌细胞A549和H1299的最高特异性结合率分别为(3.78±0.29)%和(3.56±0.37)%。体内分布提示99mTc-RET在小鼠血液中清除迅速,2h时放射性仅为注射5min时的26%,肝脏内放射性浓聚较多,且呈缓慢下降,肾脏、心、肺放射性摄取随时间逐渐下降,其余组织放射性呈低水平。结论:99mTcm-RET具有亲肺癌细胞的特性,有可能成为一种亲肺癌肿瘤显像剂。
目的:研究99mTc-RET(Arg-Glu-Thr)與肺癌細胞結閤及其在正常小鼠體內分佈和藥代動力學。方法:採用99mTc直接法標記RET,行99mTc-RET與非小細胞肺癌細胞A549和H1299的結閤實驗。正常小鼠尾靜脈註射99mTc-RET後不同時間處死,取主要髒器或組織,測定其每剋組織百分註射劑量率(%ID/g)。另取尾靜脈註射99mTc-RET後不同時間小鼠血液,測量放射性計數併計算藥代動力學參數。結果:99mTc直接標記RET的標記率大于90%。99mTc-RET與非小細胞肺癌細胞A549和H1299的最高特異性結閤率分彆為(3.78±0.29)%和(3.56±0.37)%。體內分佈提示99mTc-RET在小鼠血液中清除迅速,2h時放射性僅為註射5min時的26%,肝髒內放射性濃聚較多,且呈緩慢下降,腎髒、心、肺放射性攝取隨時間逐漸下降,其餘組織放射性呈低水平。結論:99mTcm-RET具有親肺癌細胞的特性,有可能成為一種親肺癌腫瘤顯像劑。
목적:연구99mTc-RET(Arg-Glu-Thr)여폐암세포결합급기재정상소서체내분포화약대동역학。방법:채용99mTc직접법표기RET,행99mTc-RET여비소세포폐암세포A549화H1299적결합실험。정상소서미정맥주사99mTc-RET후불동시간처사,취주요장기혹조직,측정기매극조직백분주사제량솔(%ID/g)。령취미정맥주사99mTc-RET후불동시간소서혈액,측량방사성계수병계산약대동역학삼수。결과:99mTc직접표기RET적표기솔대우90%。99mTc-RET여비소세포폐암세포A549화H1299적최고특이성결합솔분별위(3.78±0.29)%화(3.56±0.37)%。체내분포제시99mTc-RET재소서혈액중청제신속,2h시방사성부위주사5min시적26%,간장내방사성농취교다,차정완만하강,신장、심、폐방사성섭취수시간축점하강,기여조직방사성정저수평。결론:99mTcm-RET구유친폐암세포적특성,유가능성위일충친폐암종류현상제。
Objective: To investigate the biodistribution characteristics and pharmacokinetics in nomal mice and uptake in human lung cancer cells of99mTc labeled arginine-glutamic-glutamic(RET).Methods:RET was labeled directly with99mTc The biodistribution of99mTc-RET was studied at 2min,5 min,10min,30min,1h,2h,4h,8h,and 24h,respectively,after intravenous injection in normal mice. At different time points,the mice were sacrificed and organs of interest were excised,weighted and counted by a gamma counter. The organ uptake was calculated as a %ID/g.Results:The radiochemical purity of99mTc-RET were more than 90%,and the specific binding efficiency of99mTc-RET with A549 and H1299 cells was (3.78±0.29)% and (3.56±0.37)%. In the first 24h after injection,the biodistribution in mice showed rapid blood excretion and most of the radioactivity was observed in liver.Conclusion:99mTc-RET can be uptaked in human lung cancer cells,and might possibly become a potential lung cancer imaging agent.