Synthesis, radiolabeling and biological evaluation of butene amine oxime   containing nitrotriazole as a tumor hypoxia marker

doi:10.1007/s41365-016-0028-3

CORC > 北京大学 > 化学与分子工程学院

	Synthesis, radiolabeling and biological evaluation of butene amine oxime containing nitrotriazole as a tumor hypoxia marker
	Zhang, Qiang ; Chu, Tai-Wei
刊名	NUCLEAR SCIENCE AND TECHNIQUES
	2016
关键词	Tc-99m Butene amine oxime Hypoxia Nitrotriazole Radiolabeling COMPLEXES AK-2123 CANCER
DOI	10.1007/s41365-016-0028-3
英文摘要	Tc-99m-BnAO, as a nonnitroaromatic hypoxia marker, is the subject of intensive research in recent years. In this study, a butene amine oxime nitrotriazole (BnAO-NT) was synthesized and radiolabeled with Tc-99m in high yield. Cellular uptakes of Tc-99m-BnAO NT and Tc-99m-BnAO were tested using murine sarcoma S180 and hepatoma H22 cell lines. The highest hypoxic cellular uptake of Tc-99m-BnAO-NT was 27.11 +/- 0.73 and 14.85 +/- 0.83 % for the S180 and H22 cell lines, respectively, whereas the normoxic cellular uptake of the complex was about 4-8 % for both cell lines. For Tc-99m-BnAO, the highest hypoxic cellular uptake was 30.79 +/- 0.44 and 9.66 +/- 1.20 % for the S180 and H22 cell lines, respectively, while the normoxic cellular uptake was about 5 % for both cell lines. Both Tc-99m-BnAO NT and Tc-99m-BnAO complexes showed hypoxic/normoxic differentials in the two cell lines, but the results were more significant for the 5180 cell line. The in vitro results suggested that S180 may be better than H22 cell line in hypoxic biological evaluation of BnAO complexes. The biodistribution study was tested using a S180 tumor model. The complex Tc-99m-BnAO NT showed a selective enrichment in tumor tissues: At 4 h, the tumor-to-muscle ratio was 3.79 +/- 0.98 and the tumor-to-blood ratio was 2.31 +/- 0.34. Compared with the results of Tc-99m-BnAO, the latter was at the same level. In vitro and in vivo studies demonstrated that Tc-99m-BnAO NT could be a hypoxia-sensitive radiotracer for monitoring hypoxic regions in a sarcoma S180 tumor.; supported by the National Natural Science Foundation of China; SCI(E); 中国科学引文数据库(CSCD); ARTICLE; twchu@pku.edu.cn; 2; 37-45; 27
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/438330]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	Zhang, Qiang,Chu, Tai-Wei. Synthesis, radiolabeling and biological evaluation of butene amine oxime containing nitrotriazole as a tumor hypoxia marker[J]. NUCLEAR SCIENCE AND TECHNIQUES,2016.
APA	Zhang, Qiang,&Chu, Tai-Wei.(2016).Synthesis, radiolabeling and biological evaluation of butene amine oxime containing nitrotriazole as a tumor hypoxia marker.NUCLEAR SCIENCE AND TECHNIQUES.
MLA	Zhang, Qiang,et al."Synthesis, radiolabeling and biological evaluation of butene amine oxime containing nitrotriazole as a tumor hypoxia marker".NUCLEAR SCIENCE AND TECHNIQUES (2016).