Biodistribution and elimination study of fluorine-18 labeled Nε-carboxymethyl-lysine following intragastric and intravenous administration

PloS One
Hongzeng XuNaifeng Liu

Abstract

N(ε)-carboxymethyl-lysine (CML) is a major advanced glycation end-product (AGEs) widely found in foods. The aim of our study was to evaluate how exogenous CML-peptide is dynamically absorbed from the gastrointestinal tract and eliminated by renal tubular secretion using microPET imaging. The present study consisted of three investigations. In study I, we synthesized the imaging tracer (18)F-CML by reacting N-succinimidyl 4-(18)F-fluorobenzoate ((18)F-SFB) with CML. In study II, the biological activity of (18)F-CML was evaluated in RAW264.7 cells and HepG2 cells. In study III, the biodistribution and elimination of AGEs in ICR mice were studied in vivo following tail vein injection and intragastric administration of (18)F-CML. The formation of (18)F-CML was confirmed by comparing its retention time with the corresponding reference compound (19)F-CML. The radiochemical purity (RCP) of (18)F-CML was >95%, and it showed a stable character in vitro and in vivo. Uptake of (18)F-CML by RAW264.7 cells and HepG2 cells could be inhibited by unmodified CML. (18)F-CML was quickly distributed via the blood, and it was rapidly excreted through the kidneys 20 min after tail vein injection. However, (18)F-CML was only slightly absorbed followi...Continue Reading

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Citations

Dec 15, 2015·Journal of Agricultural and Food Chemistry·Mei LiJie Chen
Jun 14, 2017·Chemical Society Reviews·Dion van der BornDanielle J Vugts
Jan 27, 2016·Journal of Animal Science·C van RooijenW H Hendriks
Sep 30, 2020·Glycoconjugate Journal·Frederic J TessierMichael Howsam

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Methods Mentioned

BETA
acylation
reversed-phase chromatography

Software Mentioned

SPSS

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