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-  2017 

黄连素衍生物(氟[19F]HX-01)体外靶向肝癌的初步研究

DOI: doi:10.7507/1001-5515.201604025

Keywords: 氟[19F]HX-01, 黄连素, 人肝癌细胞, 人正常肝细胞, 正电子发射计算机断层显像

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Abstract:

氟[18F]标记黄连素衍生物(氟[18F]HX-01)是一种潜在的正电子发射计算机断层显像(PET)肿瘤显像剂,而能量状态不同、无放射性的标准对照品(氟[19F]HX-01)的物理性质及化学性质与其完全相同。本文通过研究氟[19F]HX-01 在体外人肝癌细胞和人正常细胞中有无选择性分布的现象,从而为进一步完成活体内氟[18F]HX-01 肝癌 PET 显像奠定基础。本文利用小檗红碱和 3-氟丙醇在碱催化作用下,一步反应制备氟[19F]HX-01;课题组选取人正常肝细胞(HL-7702)与人肝癌细胞(HepG2、SMMC-7721)为实验细胞材料,于荧光显微镜下观察[19F]HX-01 在细胞内的定位;用细胞增殖活性检测试剂盒(CCK-8)测定氟[19F]HX-01 对上述细胞的增殖抑制作用及其对细胞的毒性作用。本文研究结果显示:① 氟[19F]HX-01 与人肝癌细胞 HepG2、SMMC-7721 的结合能力明显高于人正常肝细胞 HL-7702;② 氟[19F]HX-01 对 HepG2、SMMC-7721 以及 HL-7702 的细胞增殖抑制作用具有剂量依赖效应;③ 氟[19F]HX-01 对人正常肝细胞 HL-7702 的毒性作用较 SMMC-7721、HepG2 更低。上述体外研究结果表明:氟[19F]HX-01 对人肝癌细胞(HepG2、SMMC-7721)较人正常肝细胞(HL-7702)具有更高选择性和更高毒性。以此为基础,放射性对照品氟[18F]HX-01 有望进一步开发成为潜在肝癌 PET 显像分子探针

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