Synthesis and study of the pancreatic α-amylase inhibitory activity of methyl acarviosin and its derivatives

Kato, Eisuke; Chikahisa, Fumiaki; Kawabata, Jun

doi:10.1016/j.tetlet.2016.02.053


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Synthesis and study of the pancreatic α-amylase inhibitory activity of methyl acarviosin and its derivatives

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Please use this identifier to cite or link to this item:http://hdl.handle.net/2115/68675

Title:	Synthesis and study of the pancreatic α-amylase inhibitory activity of methyl acarviosin and its derivatives
Authors:	Kato, Eisuke Browse this author →KAKEN DB
	Chikahisa, Fumiaki Browse this author
	Kawabata, Jun Browse this author
Keywords:	Pancreatic　α-amylase
	α-amylase inhibitor
	diabetes mellitus
	acarviosin
	transglycosylation
Issue Date:	23-Mar-2016
Journal Title:	Tetrahedron Letters
Volume:	57
Issue:	12
Start Page:	1365
End Page:	1367
Publisher DOI:	10.1016/j.tetlet.2016.02.053
Abstract:	Pancreatic α-amylase is a target for type 2 diabetes mellitus treatment. However, small molecule inhibitors of α-amylase are currently scarce. In the course of developing small molecule α-amylase inhibitors, we designed and synthesized conjugates of glucose and acarviosin. The synthetic compounds showed mild α-amylase inhibitory activity with higher activity compared with non-glucose conjugated compounds, but lower activity compared to acarviosin. Comparison of these activities revealed transglycosylation of acarviosin during the enzyme reaction. Additionally, the α-amylase inhibitory activity of acarviosin is expressed through these transglycosylation products.
Rights:	© [2016]. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
Rights:	https://creativecommons.org/licenses/by-nc-nd/4.0/
Type:	article (author version)
URI:	http://hdl.handle.net/2115/68675
Appears in Collections:	農学院・農学研究院 (Graduate School of Agriculture / Faculty of Agriculture) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 加藤英介

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