Six new sesquineolignans from the stems of Akebia quinate and their diacylglycerol acyltransferase activity.

Authors :: Xu WH
Jiang YR
Bei TT
Xiao YX
Gao Y
Xu H
Wu XF
Lee HS
Cui L
Source :: Fitoterapia [Fitoterapia] 2024 Dec; Vol. 179, pp. 106221. Date of Electronic Publication: 2024 Sep 30.
Publication Year :: 2024
Abstract: Six new sesquineolignans (1-6), have been isolated and elucidated from the stems of Akebia quinate together with five known analogues (7-11). Their structures were elucidated on the basis of comprehensive analysis of UV, IR, NMR, HRESIMS and CD spectroscopy experiments. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Among them, compounds 1-11 were found to exhibit selective inhibitory activity on DGAT1 with IC <subscript>50</subscript> values ranging from 60.4 ± 1.3 to 84.6 ± 1.3 μM. Besides, the potential binding sites of 1 were predicted by molecular docking.<br />Competing Interests: Declaration of competing interest Wen-Hui Xu, Yi-Ran Jiang, Tian-Tian Bei, Ying-Xiao Xiao, Yuan Gao, Hao Xu, Xue-Feng Wu, Hyun-Sun Lee and Long Cui declare that they have no conflict of interest.<br /> (Copyright © 2024. Published by Elsevier B.V.)

Subjects :: Molecular Structure
Humans
China
Boraginaceae chemistry
Plant Stems chemistry
Diacylglycerol O-Acyltransferase antagonists & inhibitors
Lignans pharmacology
Lignans isolation & purification
Lignans chemistry
Molecular Docking Simulation
Phytochemicals pharmacology
Phytochemicals isolation & purification

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