中华核医学与分子影像杂志
中華覈醫學與分子影像雜誌
중화핵의학여분자영상잡지
Chinese Journal of Nuclear Medicine and Molecular Imaging
2014年
5期
370-373
,共4页
柳曦%张晓军%张锦明%李鹏%田嘉禾%刘伯里
柳晞%張曉軍%張錦明%李鵬%田嘉禾%劉伯裏
류희%장효군%장금명%리붕%전가화%류백리
鬼臼毒素%碳放射性同位素%同位素标记%药代动力学%小鼠
鬼臼毒素%碳放射性同位素%同位素標記%藥代動力學%小鼠
귀구독소%탄방사성동위소%동위소표기%약대동역학%소서
Podophyllotoxin%Carbon radioisotopes%Isotope labeling%Pharmacokinetics%Mice
目的 制备11C-鬼臼毒素(简称鬼臼)和11C-表鬼臼,研究两者在荷瘤鼠体内的生物学分布.方法 用11C-三氟甲基磺酰基甲烷(11C-Triflate-CH3)直接标记去甲基鬼臼和去甲基表鬼臼,产物经HPLC分离,测量11C-鬼臼和11C-表鬼臼的标记率和放化纯.取雌性荷EMT6乳腺癌小鼠30只,按随机数字表法分成2组,分别经尾静脉注射11C-鬼臼和11C-表鬼臼3.7 MBq,均于注射后5、10、30 min各处死小鼠5只,取血液、脑、心等组织测质量及放射性计数,计算放射性摄取值(％ID/g).采用配对t检验进行统计学比较.结果 用11C-Triflate-CH3直接标记去甲基鬼臼和表鬼臼的标记率均达90％以上,放化纯大于99％.11C-鬼臼和11C-表鬼臼在荷EMT6乳腺癌小鼠体内分布相似,血液清除慢,腹部放射性高.30 min时肿瘤对11C-鬼臼和11C-表鬼臼摄取分别为(3.16±0.27)和(3.63±0.98) ％ID/g,肿瘤/血液比仅为0.62和0.68,肿瘤/肌肉比为1.22和1.52;肿瘤对两者的摄取差异无统计学意义(t=0.47,P＞0.05).结论 荷瘤鼠肿瘤对11C-鬼臼摄取量不高,11C-鬼臼直接用于肿瘤的诊断价值有限.
目的 製備11C-鬼臼毒素(簡稱鬼臼)和11C-錶鬼臼,研究兩者在荷瘤鼠體內的生物學分佈.方法 用11C-三氟甲基磺酰基甲烷(11C-Triflate-CH3)直接標記去甲基鬼臼和去甲基錶鬼臼,產物經HPLC分離,測量11C-鬼臼和11C-錶鬼臼的標記率和放化純.取雌性荷EMT6乳腺癌小鼠30隻,按隨機數字錶法分成2組,分彆經尾靜脈註射11C-鬼臼和11C-錶鬼臼3.7 MBq,均于註射後5、10、30 min各處死小鼠5隻,取血液、腦、心等組織測質量及放射性計數,計算放射性攝取值(％ID/g).採用配對t檢驗進行統計學比較.結果 用11C-Triflate-CH3直接標記去甲基鬼臼和錶鬼臼的標記率均達90％以上,放化純大于99％.11C-鬼臼和11C-錶鬼臼在荷EMT6乳腺癌小鼠體內分佈相似,血液清除慢,腹部放射性高.30 min時腫瘤對11C-鬼臼和11C-錶鬼臼攝取分彆為(3.16±0.27)和(3.63±0.98) ％ID/g,腫瘤/血液比僅為0.62和0.68,腫瘤/肌肉比為1.22和1.52;腫瘤對兩者的攝取差異無統計學意義(t=0.47,P＞0.05).結論 荷瘤鼠腫瘤對11C-鬼臼攝取量不高,11C-鬼臼直接用于腫瘤的診斷價值有限.
목적 제비11C-귀구독소(간칭귀구)화11C-표귀구,연구량자재하류서체내적생물학분포.방법 용11C-삼불갑기광선기갑완(11C-Triflate-CH3)직접표기거갑기귀구화거갑기표귀구,산물경HPLC분리,측량11C-귀구화11C-표귀구적표기솔화방화순.취자성하EMT6유선암소서30지,안수궤수자표법분성2조,분별경미정맥주사11C-귀구화11C-표귀구3.7 MBq,균우주사후5、10、30 min각처사소서5지,취혈액、뇌、심등조직측질량급방사성계수,계산방사성섭취치(％ID/g).채용배대t검험진행통계학비교.결과 용11C-Triflate-CH3직접표기거갑기귀구화표귀구적표기솔균체90％이상,방화순대우99％.11C-귀구화11C-표귀구재하EMT6유선암소서체내분포상사,혈액청제만,복부방사성고.30 min시종류대11C-귀구화11C-표귀구섭취분별위(3.16±0.27)화(3.63±0.98) ％ID/g,종류/혈액비부위0.62화0.68,종류/기육비위1.22화1.52;종류대량자적섭취차이무통계학의의(t=0.47,P＞0.05).결론 하류서종류대11C-귀구섭취량불고,11C-귀구직접용우종류적진단개치유한.
Objective To synthesize podo-and epipodo-podophyllotoxin labeled with 11C and investigate their biodistribution in mice bearing EMT6 tumor by microPET.Methods 11 C-podo-or epipodopodophyllotoxin was synthesized by 11 C-CH3-Triflate mixed with 4'-methyl-demethmyl-podophyllotoxin (podo-and epipodo-) and purified using HPLC.The radiochemical purity (RCP) was analyzed by HPLC.Thirty mice bearing EMT6 tumor were divided into 2 groups and injected with 3.7 MBq 11C-podo-or epipodo-podophyllotoxin.The biodistribution of 11C-podo-or epipodo-podophyllotoxin was evaluated with microPET.The ID％/g was calculated.Paired t test was used to analyze the data.Results The yields of 11C-podo-and epipodo-podophyllotoxin were both ＞90％.The RCP was ＞99％.The biodistribution of 11C-podo-and epipodo-podophyllotoxin was similar with slow blood clearance and high uptake in abdomen.The tumor uptake of 11C-epipodophyllotoxin and 11C-podophyllotoxin at 30 min was (3.63±0.98) ％ID/g and (3.16±0.27) ％ID/g,respectively.The uptake ratio of tumor to blood and to muscle was 0.68 vs 0.62 and 1.52 vs 1.22,respectively.There was no significant difference between the tumor uptake of the two agents (t=0.47,P＞0.05).The result of microPET imaging was consistent with that of mice experiment.Conclusion 11C-podophyllotoxin has limited clinical value for tumor imaging.
