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

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 IC₅₀ 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.

Keywords: Akebia quinate; DGAT; Inhibitory activity; Lardizabalaceae; Sesquineolignans.