中华核医学杂志
中華覈醫學雜誌
중화핵의학잡지
CHINESE JOURNAL OF NUCLEAR MEDICINE
2011年
2期
121-124
,共4页
谢文晖%蔡小佳%刘慈懿%曾骏%张莉华%雷贝%黄钢
謝文暉%蔡小佳%劉慈懿%曾駿%張莉華%雷貝%黃鋼
사문휘%채소가%류자의%증준%장리화%뢰패%황강
肽类%锝%肿瘤%炎性反应%放射性核素显像%兔%小鼠,裸
肽類%锝%腫瘤%炎性反應%放射性覈素顯像%兔%小鼠,裸
태류%득%종류%염성반응%방사성핵소현상%토%소서,라
Peptides%Technetium%Isotope labeling%Neoplasms%Inflammation%Rabbits%Mice,nude
目的 进行99Tcm-精氨酸-谷氨酸-丝氨酸(RES)的亲肿瘤实验研究.方法 采用标准Fmoc固相合成法合成RES,在不同的试剂和温度(100 ℃或室温)条件下,以氯化亚锡为还原剂进行RES的99Tcm标记,优化标记条件.进行荷A549肺癌裸鼠99Tcm-RES显像并测定%ID/g,研究99TcmRES在荷瘤裸鼠体内的分布.比较兔炎性反应和肿瘤模型显像结果.结果 (1)酒石酸钠及氢氧化钠为缓冲剂,氯化亚锡为还原剂,100 ℃水浴10 min,RES放化纯最高达到85%;99Tcm-RES性能稳定,室温下放置6 h,放化纯仍达75%.(2)注射后0.5 h,99Tcm-RES多分布于心、肝、肾等血供丰富脏器,2 h血液的放射性(0.36%ID/g)降幅明显,仅相当于0.5 h(2.35%ID/g)的1/7;心、肝、肺的放射性降幅稍慢,但明显快于肿瘤;注射后0.5 h肿瘤放射性摄取为2.32%ID/g,6 h为1.54%ID/g,6 h后仍有超过60%的放射性滞留.99Tcm-RES注射后6 h肿瘤/血、肿瘤/心、肿瘤/肝、肿瘤/肺、肿瘤/脾和肿瘤/骨骼肌放射性比值分别为5.31,1.88,1.57,3.58,4.16和5.92.(3)荷瘤鼠显像发现肿瘤部位明显浓聚99Tcm-RES,而201Tl、99Tcm-MIBI在肿瘤部位未见明显浓聚.(4)兔炎性反应和肿瘤模型显像示肿瘤部位放射性明显浓聚,而炎性反应部位放射性无明显浓聚,注药后6 h肿瘤/炎性反应部位放射性比值为3.12.结论 用放射性组合化学文库筛选出的小分子RES是一种与肿瘤高亲和力的多肽,有望成为一种肿瘤显像剂.
目的 進行99Tcm-精氨痠-穀氨痠-絲氨痠(RES)的親腫瘤實驗研究.方法 採用標準Fmoc固相閤成法閤成RES,在不同的試劑和溫度(100 ℃或室溫)條件下,以氯化亞錫為還原劑進行RES的99Tcm標記,優化標記條件.進行荷A549肺癌裸鼠99Tcm-RES顯像併測定%ID/g,研究99TcmRES在荷瘤裸鼠體內的分佈.比較兔炎性反應和腫瘤模型顯像結果.結果 (1)酒石痠鈉及氫氧化鈉為緩遲劑,氯化亞錫為還原劑,100 ℃水浴10 min,RES放化純最高達到85%;99Tcm-RES性能穩定,室溫下放置6 h,放化純仍達75%.(2)註射後0.5 h,99Tcm-RES多分佈于心、肝、腎等血供豐富髒器,2 h血液的放射性(0.36%ID/g)降幅明顯,僅相噹于0.5 h(2.35%ID/g)的1/7;心、肝、肺的放射性降幅稍慢,但明顯快于腫瘤;註射後0.5 h腫瘤放射性攝取為2.32%ID/g,6 h為1.54%ID/g,6 h後仍有超過60%的放射性滯留.99Tcm-RES註射後6 h腫瘤/血、腫瘤/心、腫瘤/肝、腫瘤/肺、腫瘤/脾和腫瘤/骨骼肌放射性比值分彆為5.31,1.88,1.57,3.58,4.16和5.92.(3)荷瘤鼠顯像髮現腫瘤部位明顯濃聚99Tcm-RES,而201Tl、99Tcm-MIBI在腫瘤部位未見明顯濃聚.(4)兔炎性反應和腫瘤模型顯像示腫瘤部位放射性明顯濃聚,而炎性反應部位放射性無明顯濃聚,註藥後6 h腫瘤/炎性反應部位放射性比值為3.12.結論 用放射性組閤化學文庫篩選齣的小分子RES是一種與腫瘤高親和力的多肽,有望成為一種腫瘤顯像劑.
목적 진행99Tcm-정안산-곡안산-사안산(RES)적친종류실험연구.방법 채용표준Fmoc고상합성법합성RES,재불동적시제화온도(100 ℃혹실온)조건하,이록화아석위환원제진행RES적99Tcm표기,우화표기조건.진행하A549폐암라서99Tcm-RES현상병측정%ID/g,연구99TcmRES재하류라서체내적분포.비교토염성반응화종류모형현상결과.결과 (1)주석산납급경양화납위완충제,록화아석위환원제,100 ℃수욕10 min,RES방화순최고체도85%;99Tcm-RES성능은정,실온하방치6 h,방화순잉체75%.(2)주사후0.5 h,99Tcm-RES다분포우심、간、신등혈공봉부장기,2 h혈액적방사성(0.36%ID/g)강폭명현,부상당우0.5 h(2.35%ID/g)적1/7;심、간、폐적방사성강폭초만,단명현쾌우종류;주사후0.5 h종류방사성섭취위2.32%ID/g,6 h위1.54%ID/g,6 h후잉유초과60%적방사성체류.99Tcm-RES주사후6 h종류/혈、종류/심、종류/간、종류/폐、종류/비화종류/골격기방사성비치분별위5.31,1.88,1.57,3.58,4.16화5.92.(3)하류서현상발현종류부위명현농취99Tcm-RES,이201Tl、99Tcm-MIBI재종류부위미견명현농취.(4)토염성반응화종류모형현상시종류부위방사성명현농취,이염성반응부위방사성무명현농취,주약후6 h종류/염성반응부위방사성비치위3.12.결론 용방사성조합화학문고사선출적소분자RES시일충여종류고친화력적다태,유망성위일충종류현상제.
Objective To evaluate 99Tcm-Arg-Glu-Ser (99Tcm-RES) as a potential tumor imaging agent. Methods RES was synthesized using solid phase peptide synthesis. The optimal labeling conditions of RES were determined under different reagents and reacting temperatures using SnC12 as reducing agent.The biodistribution of 99Tcm-RES was studied in nude mice bearing human lung cancer A549. Results The radiochemical purity of 99Tcm-RES was up to 85% and the radiochemical purity was 75% ever after 6 h at room temperature. The tumor uptake of 99Tcm-RES was obvious and the radioactivity ratios of tumor/blood,tumor/heart, tumor/liver, tumor/lung, tumor/spleen and tumor/muscle were 5.31, 1.88, 1.57, 3.58,4. 16 and 5.92, respectively at 6 h after 99Tcm-RES injection. Gamma camera imaging showed that tumor uptake of 99Tcm-RES was negative in rabbits with inflammatory mass but positive in those bearing tumor.The radioactivity ratio of tumor/inflammation was 3.12 at 6 h after injection. Conclusion 99Tcm-RES might possibly become a potential tumor imaging agent.
