Suppr超能文献

8-环戊二烯基三羰基99锝8-氧辛酸:一种用于评估肝脏中链脂肪酸代谢的新型放射性示踪剂。

8-cyclopentadienyltricarbonyl 99mtc 8-oxooctanoic acid: a novel radiotracer for evaluation of medium chain fatty acid metabolism in the liver.

作者信息

Lee Byung Chul, Choe Yearn Seong, Chi Dae Yoon, Paik Jin-Young, Lee Kyung-Han, Choi Yong, Kim Byung-Tae

机构信息

Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, 50 Ilwon-dong, Kangnam-ku, Seoul 135-710, Korea.

出版信息

Bioconjug Chem. 2004 Jan-Feb;15(1):121-7. doi: 10.1021/bc0341268.

Abstract

8-Cyclopentadienyltricarbonyl 99mTc 8-oxooctanoic acid (99mTc-CpTTOA; 1a) was synthesized for evaluation of medium chain fatty acid metabolism in the liver. 99mTc-CpTTOA was prepared in high radiochemical yield (50-63%) by a double ligand transfer reaction of methyl 8-ferrocenyl-8-oxooctanoate and Na99mTcO4 in the presence of CrCl3 and Cr(CO)6, followed by hydrolysis. This radiotracer was shown to be stable (>90% at 6 h) when incubated with human serum. Aqueous extraction of the radioactivity from the liver and blood samples of mice suggested that 99mTc-CpTTOA was mainly metabolized via beta-oxidation in the liver, and the radioactivity was retained longer in CCl4-treated mice than in control mice, possibly due to impaired beta-oxidation in the former. Planar images of rats injected with 99mTc-CpTTOA showed accumulation of the radioactivity in the liver, kidneys, and bladder with rapid hepatic clearance as a function of time. Analysis of the metabolites from the liver and urine samples of rats further supported that 99mTc-CpTTOA was metabolized to 4-cyclopentadienyltricarbonyl 99mTc 4-oxobutanoic acid (99mTc-CpTTBA; 1c) via beta-oxidation. The results suggested that this radiotracer might be of valuable use in the evaluation of fatty acid metabolism in the liver.

摘要

合成了8-环戊二烯基三羰基99mTc 8-氧代辛酸(99mTc-CpTTOA;1a)用于评估肝脏中中链脂肪酸代谢。通过8-二茂铁基-8-氧代辛酸甲酯与99mTcO4Na在CrCl3和Cr(CO)6存在下的双配体转移反应,然后水解,以高放射化学产率(50-63%)制备了99mTc-CpTTOA。该放射性示踪剂与人血清孵育时显示稳定(6小时时>90%)。从小鼠肝脏和血液样本中对放射性进行水相萃取表明,99mTc-CpTTOA主要在肝脏中通过β-氧化代谢,并且在CCl4处理的小鼠中放射性保留的时间比对照小鼠长,这可能是由于前者的β-氧化受损。注射99mTc-CpTTOA的大鼠的平面图像显示放射性在肝脏、肾脏和膀胱中积聚,肝脏清除迅速,呈时间函数关系。对大鼠肝脏和尿液样本中代谢物的分析进一步支持99mTc-CpTTOA通过β-氧化代谢为4-环戊二烯基三羰基99mTc 4-氧代丁酸(99mTc-CpTTBA;1c)。结果表明,这种放射性示踪剂可能在评估肝脏脂肪酸代谢方面具有重要价值。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验