| Literature DB >> 35100442 |
William J Behof1,2, Clayton A Whitmore1,2, Justin R Haynes1,2, Adam J Rosenberg1,2, Mohammed N Tantawy1,2, Todd E Peterson1,2, Fiona E Harrison3,4,5, Robert B Beelman6, Printha Wijesinghe7, Joanne A Matsubara7, Wellington Pham1,2,4,5,8,9,10,11.
Abstract
L-ergothioneine (ERGO) is a potent antioxidant with cytoprotective effects. To study ERGO biodistribution and detect oxidative stress in vivo, we report an efficient and reproducible preparation of [11 C]-labeled ERGO PET radioligand based on protecting the histidine carboxylic group with a methyl ester. Overall, this new protection approach using methyl ester improved the chemical yield of a 4-step reaction from 14% to 24% compared to the previous report using t-butyl ester. The [11 C]CH3 methylation of the precursor provided the desired product with 55 ± 10% radiochemical purity and a molar activity of 450 ± 200 TBq·mmol-1 . The [11 C]ERGO radioligand was able to detect threshold levels of oxidative stress in a preclinical animal model of Alzheimer's disease.Entities:
Keywords: PET imaging; ROS; alzheimer; ergothioneine; inflammation; oxidative stress
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Year: 2022 PMID： 35100442 PMCID： PMC9167250 DOI： 10.1002/1873-3468.14303
Source DB: PubMed Journal: FEBS Lett ISSN： 0014-5793 Impact factor: 3.864