Long non-coding RNA (LncRNA) HOTAIR was amplified and overexpressed in many human carcinomas, which could serve as a useful target for cancer early detection and treatment. The 99mTc radiolabeled antisense oligonucleotides (ASON) could visualize the expression of HOTAIR and provide a diagnostic value for malignant tumors. | Ren et al. BMC Cancer 2022 22 79 https s12885-022-09170-7 RESEARCH Open Access Radiosynthesis of a novel antisense imaging probe targeting LncRNA HOTAIR in malignant glioma Jiongyu Ren1 2 Xiyuan Zhang3 Jiang Cao1 2 Jiali Tian1 2 Jin Luo1 2 Yaping Yu1 2 Fengkui Wang1 and Qian Zhao1 Abstract Background Long non-coding RNA LncRNA HOTAIR was amplified and overexpressed in many human carcino- mas which could serve as a useful target for cancer early detection and treatment. The 99mTc radiolabeled antisense oligonucleotides ASON could visualize the expression of HOTAIR and provide a diagnostic value for malignant tumors. The aim of this study was to evaluate whether liposome-coated antisense oligonucleotide probe 99mTc- HYNIC-ASON targeting HOTAIR can be used in in vivo imaging of HOTAIR in malignant glioma xenografts. Methods The ASON targeting LncRNA HOTAIR as well as mismatched ASON ASONM were designed and modified. The radiolabeling of 99mTc with two probes were via the conjugation of bifunctional chelator HYNIC. Then probes were purified by Sephadex G25 and tested for their radiolabeling efficiency and purity as well as stability by ITLC Instant thin-layer chromatography and gel electrophoresis. Then the radiolabeled probes were transfected with lipo- fectamine 2000 for cellular uptake test and the next experimental use. Furthermore biodistribution study and SPECT imaging were performed at different times after liposome-coated 99mTc-HYNIC-ASON ASONM were intravenously injected in glioma tumor-bearing mice models. All data were analyzed by statistical software. Results The labeling efficiencies of 99mTc-HYNIC-ASON and 99mTc-HYNIC-ASONM measured by ITLC were 91 and 90 respectively and both radiochemical purities were more than 89 . Two probes showed good stability within 12 h. Gel electrophoresis confirmed that the oligomers were successfully radiolabeled no significant degradation were found. Biodistribution study demonstrated that .
