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Comparison of radiolabeled choline and ethanolamine as probe for cancer detection.

机译:放射性标记胆碱和乙醇胺作为癌症检测探针的比较。

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OBJECTIVE: Recently [11C] or [18F] labeled choline has been developed as a promising tracer for cancer detection. However choline may not be best agent, as the development of in vivo 1H-decoupled, NOE-enhanced 31P- MRS enabled the resolution of the resonances of phosphorylethanolamine (PEt) and phosphorylcholine (PCho) peaks that normally overlap under the broad phosphomonoester peak (PME). In human non-Hodgkin's lymphoma in vivo, the PEt/PCho ratio was reported as 2.9 +/- 1.0 (n = 11). The objective of this work was to compare radiolabeled choline with ethanolamine as an agent for cancer detection using various cancer cell lines. RESULTS: Cell uptake of [14C] ethanolamine and [14C] N, N'-dimethyl ethanolamine was compared to [14C] choline uptake in a wide variety of different cancer cell lines. Our data clearly demonstrates that, ethanolamine and N, N'-dimethyl ethanolamine showed 2-7 fold more uptake than choline. We showed that proliferating fibroblasts have significantly higher uptake of ethanolamine and N, N'-dimethyl-ethanolamine, than does growth arrested fibroblasts. Time course studies in A172 cells indicate continuous linear uptake of ethanolamine after four hours of tracer exposure, which was halted if tracer containing, media was replaced with regular media after one hour. The androgen stimulated and depleted study with prostate cancer cell lines showed that increased trapping of radiotracers in cells is well correlated with their proliferation status. METHODS: We carried out comparison of radiolabeled choline and ethanolamine by cell uptake study using 8 different cancer cell lines. To evaluate the response of radiotracers towards proliferation we also carried out their cell uptake study of androgen dependent and androgen independent cells in androgen stipulated and deprived media. CONCLUSIONS: Our data demonstrate that ethanolamine and N, N'-dimethyl ethanolamine are taken up by a wide variety of tumor cells significantly better (2-7 fold) than the clinically utilized radiolabeled choline tracer.
机译:目的:最近已开发出[11C]或[18F]标记的胆碱作为一种有前途的癌症检测示踪剂。然而,胆碱可能不是最佳的治疗剂,因为体内1H去偶联,NOE增强的31P-MRS的发展使通常在宽的磷酸单酯峰下重叠的磷酸乙醇胺(PEt)和磷酸胆碱(PCho)峰的共振得以分离( PME)。在体内人类非霍奇金淋巴瘤中,PEt / PCho比据报道为2.9 +/- 1.0(n = 11)。这项工作的目的是比较放射性标记的胆碱和乙醇胺作为使用各种癌细胞系进行癌症检测的试剂。结果:在多种不同的癌细胞系中,将[14C]乙醇胺和[14C] N,N'-二甲基乙醇胺的细胞摄取与[14C]胆碱摄取进行了比较。我们的数据清楚地表明,乙醇胺和N,N'-二甲基乙醇胺的摄取量比胆碱高2-7倍。我们显示,与生长停滞的成纤维细胞相比,增殖的成纤维细胞对乙醇胺和N,N'-二甲基-乙醇胺的吸收明显更高。在A172细胞中进行的时程研究表明,暴露于示踪剂的四个小时后乙醇胺连续线性摄取,如果包含示踪剂的培养基在一小时后被常规培养基替代,则乙醇胺会停止。前列腺癌细胞系对雄激素的刺激和耗竭研究表明,放射性示踪剂在细胞中的捕获增加与其增殖状态密切相关。方法:我们通过使用8种不同癌细胞系的细胞摄取研究对放射性标记的胆碱和乙醇胺进行了比较。为了评估放射性示踪剂对增殖的反应,我们还在雄激素规定和缺乏的培养基中对雄激素依赖性和雄激素非依赖性细胞进行了细胞摄取研究。结论:我们的数据表明乙醇胺和N,N'-二甲基乙醇胺被多种肿瘤细胞吸收的效果(2-7倍)明显优于临床使用的放射性胆碱示踪剂。

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