Real‐Time Interrogation of Aspirin Reactivity, Biochemistry, and Biodistribution by Hyperpolarized Magnetic Resonance Spectroscopy
Abstract
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‐13C 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 13C‐NMR spectroscopy. Hyperpolarized, double‐labeled aspirin was well tolerated in mice and could be observed by both 13C‐MR imaging and 13C‐NMR spectroscopy in vivo.
Document Details
- Document Type
- Pub Defense Publication
- Publication Date
- Feb 20, 2019
- Source ID
- 10.1002/anie.201812759
Entities
People
- Argentina Ornelas
- Christopher G. Wood
- David G. Menter
- Eduardo Vilar
- Ernest T. Hawk
- Jaehyuk Lee
- Jennifer S Davis
- Jingzhe Hu
- Jose A. Karam
- Nasir Uddin
- Niki M. Zacharias
- Pratip K. Bhattacharya
- Scott Kopetz
- Shivanand M Pudakalakatti
- Steven W Millward
Organizations
- Cancer Prevention and Research Institute of Texas
- Congressionally Directed Medical Research Programs
- General Electric
- National Cancer Institute
- University of Texas at Austin