DTPA 偶联 99mTc 标记氟他胺复合物([99mTc]DTPA-FLUT)作为一种潜在的癌症成像放射性示踪剂的放射性标记和临床前动物模型评估。

IF 1.1 4区 医学 Q3 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Acta radiologica Pub Date : 2024-08-01 Epub Date: 2024-05-15 DOI:10.1177/02841851241249161
Syed Ali Raza Naqvi, Ahmad Junaid Hassan, Muhammad Ramzan Saeed Ashraf Janjua, Naseem Abbas, Ameer Fawad Zahoor, Sadaf Ul Hassan, Amjad Hussain
{"title":"DTPA 偶联 99mTc 标记氟他胺复合物([99mTc]DTPA-FLUT)作为一种潜在的癌症成像放射性示踪剂的放射性标记和临床前动物模型评估。","authors":"Syed Ali Raza Naqvi, Ahmad Junaid Hassan, Muhammad Ramzan Saeed Ashraf Janjua, Naseem Abbas, Ameer Fawad Zahoor, Sadaf Ul Hassan, Amjad Hussain","doi":"10.1177/02841851241249161","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Advances in molecular imaging strategies have had an effect on precise diagnosis and treatment. Research has been intensified to develop more effective and versatile radiopharmaceuticals to uplift diagnostic efficiency and, consequently, the treatment.</p><p><strong>Purpose: </strong>To label the flutamide (FLUT) coupled with diethylenetriamine pentaacetate (DTPA) with technetium-99 m (<sup>99m</sup>Tc) and to evaluate its binding efficiency with rhabdomyosarcoma (RMS) cancer cells.</p><p><strong>Material and methods: </strong>Radiolabeling of FLUT with 185 MBq freshly eluted <sup>99m</sup>TcO<sub>4</sub><sup>-1</sup> was carried out via DTPA bifunctional chelating agent using stannous chloride reducing agent at pH 5. The labeled compound was assessed for its purity using chromatography analysis, stability in saline and blood serum, AND charge using paper electrophoresis. Normal biodistribution was studied using a mouse model, while binding affinity with RMS cancer cells was studied using an internalization assay. The in vivo accumulation of RMS cancer cells in a rabbit model was monitored using a SPECT gamma camera.</p><p><strong>Results: </strong>Radiolabeling reaction displayed a pharmaceutical yield of 97% and a stability assay showed >95% intact radiopharmaceutical up to 6 h in saline and blood serum. In vitro internalization studies showed the potential of [<sup>99m</sup>Tc]DTPA-FLUT to enter into cancer cells. This biodistribution study showed rapid blood clearance and minimum uptake by body organs, and scintigraphy displayed the [<sup>99m</sup>Tc]DTPA-FLUT uptake by lesion, induced by RMS cancer cell lines in rabbit.</p><p><strong>Conclusion: </strong>Stable, newly developed [<sup>99m</sup>Tc]DTPA-FLUT seeks its way to internalize into RMS cancer cells, indicating it could be a potential candidate for the diagnosis of RMS cancer.</p>","PeriodicalId":7143,"journal":{"name":"Acta radiologica","volume":" ","pages":"940-949"},"PeriodicalIF":1.1000,"publicationDate":"2024-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Radiolabeling and preclinical animal model evaluation of DTPA coupled <sup>99m</sup>Tc-labelled flutamide complex ([<sup>99m</sup>Tc]DTPA-FLUT) as a potential radiotracer for cancer imaging.\",\"authors\":\"Syed Ali Raza Naqvi, Ahmad Junaid Hassan, Muhammad Ramzan Saeed Ashraf Janjua, Naseem Abbas, Ameer Fawad Zahoor, Sadaf Ul Hassan, Amjad Hussain\",\"doi\":\"10.1177/02841851241249161\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Advances in molecular imaging strategies have had an effect on precise diagnosis and treatment. Research has been intensified to develop more effective and versatile radiopharmaceuticals to uplift diagnostic efficiency and, consequently, the treatment.</p><p><strong>Purpose: </strong>To label the flutamide (FLUT) coupled with diethylenetriamine pentaacetate (DTPA) with technetium-99 m (<sup>99m</sup>Tc) and to evaluate its binding efficiency with rhabdomyosarcoma (RMS) cancer cells.</p><p><strong>Material and methods: </strong>Radiolabeling of FLUT with 185 MBq freshly eluted <sup>99m</sup>TcO<sub>4</sub><sup>-1</sup> was carried out via DTPA bifunctional chelating agent using stannous chloride reducing agent at pH 5. The labeled compound was assessed for its purity using chromatography analysis, stability in saline and blood serum, AND charge using paper electrophoresis. Normal biodistribution was studied using a mouse model, while binding affinity with RMS cancer cells was studied using an internalization assay. The in vivo accumulation of RMS cancer cells in a rabbit model was monitored using a SPECT gamma camera.</p><p><strong>Results: </strong>Radiolabeling reaction displayed a pharmaceutical yield of 97% and a stability assay showed >95% intact radiopharmaceutical up to 6 h in saline and blood serum. In vitro internalization studies showed the potential of [<sup>99m</sup>Tc]DTPA-FLUT to enter into cancer cells. This biodistribution study showed rapid blood clearance and minimum uptake by body organs, and scintigraphy displayed the [<sup>99m</sup>Tc]DTPA-FLUT uptake by lesion, induced by RMS cancer cell lines in rabbit.</p><p><strong>Conclusion: </strong>Stable, newly developed [<sup>99m</sup>Tc]DTPA-FLUT seeks its way to internalize into RMS cancer cells, indicating it could be a potential candidate for the diagnosis of RMS cancer.</p>\",\"PeriodicalId\":7143,\"journal\":{\"name\":\"Acta radiologica\",\"volume\":\" \",\"pages\":\"940-949\"},\"PeriodicalIF\":1.1000,\"publicationDate\":\"2024-08-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Acta radiologica\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1177/02841851241249161\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/5/15 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q3\",\"JCRName\":\"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Acta radiologica","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1177/02841851241249161","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/5/15 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
引用次数: 0

摘要

背景:分子成像策略的进步对精确诊断和治疗产生了影响。目的:用锝-99 m (99mTc)标记氟他胺 (FLUT)和五乙酸二乙烯三胺 (DTPA),并评估其与横纹肌肉瘤 (RMS) 癌细胞的结合效率:在 pH 值为 5 的条件下,使用氯化亚锡还原剂,通过 DTPA 双功能螯合剂对 FLUT 进行 185 MBq 新鲜洗脱的 99mTcO4-1 放射性标记。利用小鼠模型研究了正常生物分布,同时利用内化试验研究了与 RMS 癌细胞的结合亲和力。使用 SPECT 伽玛相机监测了 RMS 癌细胞在兔子模型中的体内蓄积情况:结果:放射性标记反应的药物收率为97%,稳定性测定显示,在生理盐水和血清中6小时内,放射性药物的完整率大于95%。体外内化研究表明,[99mTc]DTPA-FLUT 有可能进入癌细胞。这项生物分布研究显示,[99mTc]DTPA-FLUT在血液中清除迅速,被身体器官摄取的量最少,闪烁成像显示,[99mTc]DTPA-FLUT被病变组织摄取,由兔RMS癌细胞株诱发:结论:新开发的稳定的[99mTc]DTPA-FLUT可内化到RMS癌细胞中,表明它可能成为诊断RMS癌的潜在候选物质。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Radiolabeling and preclinical animal model evaluation of DTPA coupled 99mTc-labelled flutamide complex ([99mTc]DTPA-FLUT) as a potential radiotracer for cancer imaging.

Background: Advances in molecular imaging strategies have had an effect on precise diagnosis and treatment. Research has been intensified to develop more effective and versatile radiopharmaceuticals to uplift diagnostic efficiency and, consequently, the treatment.

Purpose: To label the flutamide (FLUT) coupled with diethylenetriamine pentaacetate (DTPA) with technetium-99 m (99mTc) and to evaluate its binding efficiency with rhabdomyosarcoma (RMS) cancer cells.

Material and methods: Radiolabeling of FLUT with 185 MBq freshly eluted 99mTcO4-1 was carried out via DTPA bifunctional chelating agent using stannous chloride reducing agent at pH 5. The labeled compound was assessed for its purity using chromatography analysis, stability in saline and blood serum, AND charge using paper electrophoresis. Normal biodistribution was studied using a mouse model, while binding affinity with RMS cancer cells was studied using an internalization assay. The in vivo accumulation of RMS cancer cells in a rabbit model was monitored using a SPECT gamma camera.

Results: Radiolabeling reaction displayed a pharmaceutical yield of 97% and a stability assay showed >95% intact radiopharmaceutical up to 6 h in saline and blood serum. In vitro internalization studies showed the potential of [99mTc]DTPA-FLUT to enter into cancer cells. This biodistribution study showed rapid blood clearance and minimum uptake by body organs, and scintigraphy displayed the [99mTc]DTPA-FLUT uptake by lesion, induced by RMS cancer cell lines in rabbit.

Conclusion: Stable, newly developed [99mTc]DTPA-FLUT seeks its way to internalize into RMS cancer cells, indicating it could be a potential candidate for the diagnosis of RMS cancer.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Acta radiologica
Acta radiologica 医学-核医学
CiteScore
2.70
自引率
0.00%
发文量
170
审稿时长
3-8 weeks
期刊介绍: Acta Radiologica publishes articles on all aspects of radiology, from clinical radiology to experimental work. It is known for articles based on experimental work and contrast media research, giving priority to scientific original papers. The distinguished international editorial board also invite review articles, short communications and technical and instrumental notes.
期刊最新文献
Ultrasound-guided thrombin injection for cardiac catheterization pseudoaneurysms: efficacy, safety, and predictors. Development of a nomogram based on whole-tumor multiparametric MRI histogram analysis to predict deep myometrial invasion in stage I endometrioid endometrial carcinoma preoperatively. Development of a radiomic model for cervical cancer staging based on pathologically verified, retrospective metastatic lymph node data. Diffusion-weighted imaging based on intravoxel incoherent motion: correlation with molecular prognostic factors and subtypes in breast cancer. A combined model integrating radiomics and deep learning based on multiparametric magnetic resonance imaging for classification of brain metastases.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1