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Real-Time Interrogation of Aspirin Reactivity, Biochemistry, and Biodistribution by Hyperpolarized Magnetic Resonance Spectroscopy.
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2019-02-20 , DOI: 10.1002/anie.201812759
Niki M Zacharias 1, 2 , Argentina Ornelas 1 , Jaehyuk Lee 1 , Jingzhe Hu 1 , Jennifer S Davis 3 , Nasir Uddin 1 , Shivanand Pudakalakatti 1 , David G Menter 4 , Jose A Karam 2 , Christopher G Wood 2 , Ernest T Hawk 5 , Scott Kopetz 4 , Eduardo Vilar 4, 5 , Pratip K Bhattacharya 1 , Steven W Millward 1
Affiliation  

Hyperpolarized magnetic resonance spectroscopy enables quantitative, non-radioactive, real-time measurement of imaging probe biodistribution and metabolism in vivo. Here, we investigate and report on the development and characterization of hyperpolarized acetylsalicylic acid (aspirin) and its use as a nuclear magnetic resonance (NMR) probe. Aspirin derivatives were synthesized with single- and double-13 C labels and hyperpolarized by dynamic nuclear polarization with 4.7 % and 3 % polarization, respectively. The longitudinal relaxation constants (T1 ) for the labeled acetyl and carboxyl carbonyls were approximately 30 seconds, supporting in vivo imaging and spectroscopy applications. In vitro hydrolysis, transacetylation, and albumin binding of hyperpolarized aspirin were readily monitored in real time by 13 C-NMR spectroscopy. Hyperpolarized, double-labeled aspirin was well tolerated in mice and could be observed by both 13 C-MR imaging and 13 C-NMR spectroscopy in vivo.

中文翻译:

通过超极化磁共振波谱实时询问阿司匹林反应性,生物化学和生物分布。

超极化磁共振波谱能够对成像探针的体内生物分布和代谢进行定量,非放射性的实时测量。在这里,我们调查和报告的超极化乙酰水杨酸(阿司匹林)的发展和表征及其作为核磁共振(NMR)探针的用途。合成了具有单和双13 C标签的阿司匹林衍生物,并分别通过极化为4.7%和3%的动态核极化来超极化。标记的乙酰基和羧基羰基的纵向弛豫常数(T1)约为30秒,支持体内成像和光谱学应用。超极化阿司匹林的体外水解,转乙酰化和白蛋白结合很容易通过13 C-NMR光谱实时监测。超极化
更新日期:2019-02-20
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