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氟[~(18)F]标记黄连素衍生物(氟[~(18)F]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[~(19)F]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[~(19)F]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[~(18)F]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[~(19)F]HX01;课题组选取人正常肝细胞(HL-7702)与人肝癌细胞(Hep G2、SMMC-7721)为实验细胞材料,于荧光显微镜下观察[~(19)F]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[~(19)F]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[~(19)F]HX-01与人肝癌细胞Hep G2、SMMC-7721的结合能力明显高于人正常肝细胞HL-7702;(2)氟[~(19)F]HX-01对Hep G2、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[~(19)F]HX-01对人正常肝细胞HL-7702的毒性作用较SMMC-7721、Hep G2更低。上述体外研究结果表明:氟[~(19)F]HX-01对人肝癌细胞(Hep G2、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[~(18)F]HX-01有望进一步开发成为潜在肝癌PET显像分子探针。
Fluoro [~ (18) F] labeled berberine derivative (Fluoro [~ (18) F] HX-01) is a potential positron emission tomography (PET) tumor imaging agent with different energy states Non-radioactive reference standard (fluorine [~ (19) F] HX-01) physical and chemical properties exactly the same. In this study, we investigated whether there is a selective distribution of F (19) F] HX-01 in human hepatoma cells and human normal cells in vitro, PET imaging laid the foundation. In this paper, the use of berberine and 3-fluoropropanol in the base catalysis, the reaction of one step fluorine [~ (19) F] HX01; task group selected human normal hepatocytes (HL-7702) and human hepatoma cells (19) F] HX-01 cells were observed under a fluorescence microscope. The cell viability was measured by CCK-8, F] HX-01 on the proliferation of these cells and its cytotoxic effects. The results of this study showed that: (1) The binding ability of [19 F] HX-01 to human hepatocellular carcinoma cells Hep G2 and SMMC-7721 was significantly higher than that of human normal hepatocytes HL-7702; (2) 19) FXHX-01 could inhibit the cell proliferation of Hep G2, SMMC-7721 and HL-7702 in a dose-dependent manner. (3) Toxicity than SMMC-7721, Hep G2 lower. The results of in vitro studies showed that fluoro [19 F] HX-01 has higher selectivity and toxicity than human normal hepatocytes (HL-7702) in Hep G2 cells (SMMC-7721). On the basis of this, the radioactive reference fluoride [~ (18) F] HX-01 is expected to be further developed into a potential PET imaging molecular probe for liver cancer.