Design, Synthesis and Bioactivity of Core 1 O-glycan and its Derivative on Human Gut Microbiota

Author(s): Huanhuan Qu*, Baixue Li, Jingyi Yang, Huaiwen Liang, Meixia Li, Kan Ding*

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 12 , 2019

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Graphical Abstract:


Background: Disaccharide core 1 (Galβ1-3GalNAc) is a common O-glycan structure in nature. Biochemical studies have confirmed that the formation of the core 1 structure is an important initial step in O-glycan biosynthesis and it is of great importance for human body.

Objective: Our study will provide meaningful and useful sights for O-glycan synthesis and their bioassay. And all the synthetic glycosides would be used as intermediate building blocks in the scheme developed for oligosaccharide construction.

Methods: In this article, we firstly used chemical procedures to prepare core 1 and its derivative, and a novel disaccharide was efficiently synthesized. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR and MS. Then we employed three human gut symbionts belonging to Bacteroidetes, a predominantphyla in the distal gut, as models to study the bioactivity of core 1 and its derivative on human gut microbiota.

Results: According to our results, both core 1 and derivative could support the growth of B. fragilis, especially the core 1 derivative, while failed to support the growth of B. thetaiotaomicron and B. ovatus.

Conclusion: This suggested that the B. fragilis might have the specificity glycohydrolase to cut the glycosidic bond for acquiring monosaccharide.

Keywords: Bioactivity, core 1, derivative, human gut microbiota, O-glycan, synthesis.

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Year: 2019
Page: [1348 - 1353]
Pages: 6
DOI: 10.2174/1570180816666181218143207
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