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Objective To synthesize 18F-AlF-1,4,7-triazacyclononane-l,4,7-triacetic acid (NOTA)-c (CGRRAGGSC),which could specifically bind to the α chain of interleukin (IL)-11 receptor (IL-11 R),and evaluate its targeting potential to IL-11 R-positive tumors.Methods Polypeptide c (CGRRAGGSC) was first coupled with NOTA and then labeled with 18F by AlF labeling method.The radiochemical purity and radiochemical yield of 18F-AlF-NOTA-c(CGRRAGGSC) were analyzed by high performance liquid chromatography,and the stability in vitro was evaluated.The tracer biodistribution in tumor-bearing mice (cell line SKOV3) was evaluated by the dynamic imaging with microPET 30 min,1 h,2 h after injection of 18F-AlF-NOTA-c (CGRRAGGSC).The tracer kinetics was performed in normal mice.Pharmacokinetics parameters were calculated using DAS2.0 software.Results The radiochemical purity of 18F-AlF-NOTA-c(CGRRAGGSC) was higher than 95％ and the radiochemical yield was (30.0±7.4)％.It could be stably maintained in phosphatebuffered solution and plasma for at least 2 h.MicroPET imaging showed that 18F-AlF-NOTA-c(CGRRAGGSC)had a good affinity to SKOV3 tumor.The tumor/muscle ratios at 30 min,1 h,2 h after the injection of 18F-AlF-NOTA-c(CGRRAGGSC) were 6.26±2.98,7.19±3.63 and 9.05±4.30,respectively.The tracer was cleared rapidly in blood and mainly excreted by the liver and kidneys.The T1/2α and T1/2β were (0.38±0.14) h and (2.64±0.28) h,respectively.Conclusions 18F-AlF-NOTA-c(CGRRAGGSC) is easy to be synthesized and has a good affinity to IL-11R-positive tumors.It will be a potential IL-11R-targeting imaging agent.
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Objective To investigate the expression of C-JUN activation domain binding protein 1(JAB1)and its relationship with expression of P27 protein in human hepatocellular carcinoma(HCC),and to determine whether JAB1 is associated with clinicopathological parameters and prognosis of HCC.Methods Immunohistochemical analysis was performed to investigate the expression of JAB1 and P27 in 76 cases of HCC and adjacent nontumorous tissues.Fresh tumor tissues and their adjacent nontumorous tissues from 8 cases of HCC were collected for Western blot and immunoprecipitation assays.Results The expression of JAB1 in HCC was significantly higher than that in adjacent nontumorous tissues.In contrast,P27 level was higher in nontumorous liver tissues than that in HCC.JAB1 overexpression was correlated with histological differentiation,serum alpha-fetoprotein(AFP)level and metastasis(P
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Objective To investigate the relationship between growth inhibiting effect of arsenic trioxide(As_2O_3) and phosphorylation of P27kip threonine residue 187(P27T187) in human hepatocellular carcinoma(HCC) cell line SMMC-7721.Methods SMMC-7721 were treated for 72 h with 2 ?mol/L As_2O_3.The cell growth inhibition was detected by cell counting and the cell cycle was detected by flow cytometry(FCM).The expression and localization of P27,T187 phosphorylated P27(p-P27T187) were detected by Subcellular Fractionation,Western blot and immunoflurescence.Results As_2O_3 significantly inhibited the proliferation of SMMC-7721 cell and cell cycle was arrested in G2/M.A significant decrease in p-P27T187 expression and a reciprocal increase in P27 expression were found in 2 ?mol/L As_2O_3-treated SMMC-7721 cell.Meanwhile,As_2O_3 decreased the protein levels of Cdk2 and cyclinE.The location of P27 was transferred from cytoplasm to nuclei and the expression of p-P27T187 was decreased in nuclei.Conclusion As_2O_3 inhibits the phosphorylation of P27T187,thereby promoting P27 accumu-lation in SMMC-7721 cell nuclei,inducing cel1 cycle arrest and growth inhibition.