放射性同位素氢标记血根碱全合成研究  

The Total Synthesis of Radioisotope Hydrogen-3 Labelled Sanguinarine

作　　者：王林 刘梦婷 董朕 王新昊 程辟[1,3] 曾建国 WANG Lin;LIU Meng-ting;DONG Zhen;WANG Xin-hao;CHENG Pi;ZENG Jian-guo(Hunan Key Laboratory of Traditional Chinese Veterinary Medicine,Hunan Agricultural University,Changsha 410128,China;College of Horticulture,Hunan Agricultural University,Changsha 410128,China;College of Veterinary Medicine,Hunan Agricultural University,Changsha 410128,China)

机构地区：[1]湖南农业大学中兽药湖南省重点实验室,长沙410128 [2]湖南农业大学园艺学院,长沙410128 [3]湖南农业大学动物医学院,长沙410128

出　　处：《中国兽药杂志》2025年第3期34-43,共10页Chinese Journal of Veterinary Drug

基　　金：“十四五”国家重点研发计划(2022YFD1801105)。

摘　　要：在饲用禁抗背景下,以血根碱为主要活性成分开发的国家二类新兽药博落回提取物作为抗生素替代品逐渐投入到养殖生产中,也同时面临长期使用潜在的食品安全风险。基于此,我们首次开展了放射性同位素[^(3)H]标记血根碱的全合成。以[^(3)H]碘甲烷为放射性同位素源,通过甲基化、氧化脱氢和还原酸化等反应制备得到放射性同位素^(3)H标记的血根碱,其结构经薄层色谱和高效液相色谱-串联四级杆质谱联用仪分析确认,反应总化学收率和放化收率36%和82%。经高效液体相色谱和ARC流式液体闪烁计数仪测定表明,标记物的化学纯度和放化纯度均大于97%,比活度为4 mCi/mg,十二个月内质量稳定。该标记物可作为放射性示踪剂,用于血根碱的代谢、残留和消除等研究。Under the context of the ban on antibiotic use in animal feed,the extract of Macleaya cordata,a newly developed national Class II veterinary drug with sanguinarine as its primary active component,has been increasingly adopted in breeding production as an alternative to antibiotics.However,its long-term use also raises potential food safety concerns.In light of this,we have successfully achieved the total synthesis of radioisotope[^(3)H]-labeled sanguinarine for the first time.Using[^(3)H]methyl iodide as the radioisotope source,[^(3)H]-labeled sanguinarine was synthesized through a series of reactions including methylation,oxidative dehydrogenation,and reductive acidification.The structure of the labeled compound was confirmed by thin-layer chromatography(TLC)and high-performance liquid chromatography/mass spectrometry(HPLC/MS)analysis.The overall chemical yield and radiochemical yield were 36%and 82%,respectively.The chemical purity and radiochemical purity of the labeled compound were determined using HPLC and an ARC liquid scintillation counter,with a specific activity of 4 mCi/mg.This labeled compound can serve as a radioactive tracer for studying the metabolism,residue,and elimination of sanguinarine in biological systems.

关 键 词：饲用禁抗 博落回提取物 血根碱 全合成 放射性同位素示踪技术 

分 类 号：S859.3[农业科学—临床兽医学]