氘及其标记化合物在生物医药研究中的应用进展

doi:10.19586/j.2095-2341.2024.0023

生物技术进展 ›› 2024, Vol. 14 ›› Issue (5): 785-792.DOI: 10.19586/j.2095-2341.2024.0023

• 进展评述 • 上一篇

氘及其标记化合物在生物医药研究中的应用进展

唐金格¹^,²(), 任巍², 蒋晴晴², 于宁¹()

^1.川北医学院，四川南充 637000
^2.解放军总医院第六医学中心耳鼻咽喉头颈外科医学部，北京 100853

收稿日期:2024-02-20 接受日期:2024-06-04 出版日期:2024-09-25 发布日期:2024-10-22
通讯作者: 于宁
作者简介:唐金格 E-mail: tangjinge6@163.com；
基金资助:
国家重点研发项目(2020YFC2004001);北京市自然科学基金项目(7222185)

Progress in the Application of Deuterium and its Labeled Compounds in Biomedical Research

Jinge TANG¹^,²(), Wei REN², Qingqing JIANG², Ning YU¹()

^1.North Sichuan Medical College，Sichuang Nanchong 637000，China
^2.Senior Department of Otolaryngology-head & Neck Surgery，the Sixth Medical Center of PLA General Hospital，Beijing 100853，China

Received:2024-02-20 Accepted:2024-06-04 Online:2024-09-25 Published:2024-10-22
Contact: Ning YU

摘要/Abstract

摘要：

稳定同位素因具有无放射性、稳定性好等特点，在医药、食品安全、生态环境等领域应用广泛。氘作为氢元素的一种稳定同位素，氘元素标记法具有简单、快捷、价格低等优点。研究发现，氘同位素标记在机体代谢机制、疾病预防及治疗靶点、药理学等生命科学领域具有巨大的应用潜力。综述从氘标记化合物的合成方法、检测技术、氘及其化合物在生物医药研究中的应用等方面进行总结，并对未来发展进行了展望，以期为相关领域的研究与应用提供参考。

关键词: 氘, 同位素, 生物医药, 临床研究

Abstract:

Stable isotopes are widely used in fields such as medicine， food safety， and ecological environment due to their characteristics of no radioactivity and good stability. Deuterium is a stable isotope of hydrogen element， and deuterium labeling method has the advantages of simplicity， speed， and low cost. Researches have shown that deuterium isotope labeling has enormous potential for application in the field of life sciences such as metabolic mechanisms， disease prevention and treatment targets， pharmacology， etc. The review summarized the synthesis methods， detection techniques， and applications of deuterium and its compounds in biomedical research， and prospected for the future development， in order to provide reference for researchers and applications in related fields.

Key words: deuterium, isotope, biomedicine, clinical study

中图分类号:

Q819

唐金格, 任巍, 蒋晴晴, 于宁. 氘及其标记化合物在生物医药研究中的应用进展[J]. 生物技术进展, 2024, 14(5): 785-792.

Jinge TANG, Wei REN, Qingqing JIANG, Ning YU. Progress in the Application of Deuterium and its Labeled Compounds in Biomedical Research[J]. Current Biotechnology, 2024, 14(5): 785-792.

图/表 8

图1 酸性条件下的氢同位素交换反应[4]

Fig. 1 H/D exchange under acidic conditions[4]

图2 正定向芳香族HIE选用铱(?Ⅰ?)作为催化剂[6]

Fig. 2 Selected iridium (Ⅰ?) catalysts for ortho-directed aromatic HIE[6]

图3 锰催化酮的三氘甲基化[16]

Fig. 3 Manganese-catalyzed trideuteromethylation of ketones[16]

图4 酰基肉毒碱的可调谐合成[17]注：NaCNBH3—氰基硼氢化钠；NaCNBD3—氰基硼氘化钠；MeOH—甲醇；AcOH—乙酸；DMF—二甲基甲酰胺；CH3I—甲基碘；CD3I—氘代碘甲烷；13CD3I—甲基碘-13C；Na2CO3—碳酸钠。

Fig. 4 Tuneable synthesis of acylcarnitines[17]

图5 氘丁苯那嗪[43]

Fig. 5 Deutetrabenazine[43]

图6 CTP-656 （氘代依伐卡托）、十八氘代依伐卡托和依伐卡托的结构[47]

Fig. 6 Structures of CTP-656 (d9-Ivacaftor), d18-Ivacaftor, and Ivacaftor[47]

图7 d4IFO的结构注：d4IFO的结构显示为氘位于α和α′碳上。

Fig. 7 The structure of d4IFO

图8 CTP-347的结构[51]

Fig. 8 Structure of CTP-347[51]

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氘及其标记化合物在生物医药研究中的应用进展

Progress in the Application of Deuterium and its Labeled Compounds in Biomedical Research

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