Dynamics of the cellular metabolism of leptosperin found in manuka honey.

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ID: 42666
2019
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Abstract
Leptosperin (methyl syringate β-D-gentiobioside) is abundantly found in manuka honey, which is widely used because of its antibacterial and possible anti-inflammatory activities. The aim of this study was to examine the molecular mechanism underlying the metabolism of leptosperin. Five phytochemicals [leptosperin, methyl syringate (MSYR), glucuronate conjugate of MSYR (MSYR-GA), sulfonate conjugate of MSYR (MSYR-S), and syringic acid (SYR)] were separately incubated with HepG2 and Caco-2 cells. After incubation, we found that the concentration of MSYR decreased, whereas the concentrations of SYR, MSYR-GA, and MSYR-S increased. By profiling with inhibitors and carboxylesterases (CES1, 2), we found that the conversion from MSYR to SYR was mediated by CES1. Lipopolysaccharide-stimulated RAW264.7 cells restored MSYR-GA to MSYR possibly by the secreted β-glucuronidase. All the mice administered with leptosperin, MSYR, or manuka honey showed higher MSYR (13.84 ± 11.51, 14.29 ± 9.19, or 6.66 ± 2.30 nM) and SYR (1.85 ± 0.66, 6.01 ± 1.20, or 8.16 ± 3.10 nM) levels in the plasma compared with that of the vehicle controls [3.33 ± 1.45 (MSYR) and 1.85 ± 0.66 (SYR) nM]. The findings of our study indicate that the unique metabolic pathways of these compounds may account for possible functionalities of manuka honey.
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Authors Kato, Yoji;Kawai, Masaki;Kawai, Shota;Okano, Yayako;Rokkaku, Natsumi;Ishisaka, Akari;Murota, Kaeko;Nakamura, Toshiyuki;Nakamura, Yoshimasa;Ikushiro, Shinichi;
Journal Journal of agricultural and food chemistry
Year 2019
DOI
10.1021/acs.jafc.9b03894
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