ABSTRACT
Four new sesqui-lignans, (7R, 7'R, 7â³S, 8S, 8'S, 8â³S)-4',5â³-dihydroxy-3,5,3',4â³-tetramethoxy-7,9':7',9-diepoxy-4,8â³-oxy-8,8'-sesquineo-lignan-7â³,9â³-diol (1), (7R, 7'R, 7â³S, 8S, 8'S, 8â³S)-4',3â³-dihydroxy-3,5,3',5',4â³-pentamethoxy-7,9':7',9-diepoxy-4,8â³-oxy-8,8'-sesquineo-lignan-7â³,9â³-diol (2), (7R, 7'R, 7â³S, 8S, 8'S, 8â³S)-3',4â³-dihydroxy-3,5,4',5â³-tetramethoxy-7,9':7',9-diepoxy-4,8â³-oxy-8,8'-sesquineo-lignan-7â³,9â³-diol (3) and acanthopanax A (7) together with three known compounds (4-6) were isolated from the EtOAc-soluble extract of Acanthopanax senticosus. Their structures were elucidated on the basis of spectroscopic and physicochemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Among them, compounds 1-6 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values ranging from 61.1 ± 1.3 to 97.7 ± 1.1 µM and compound 7 showed selective inhibition of DGAT2 with IC50 value 93.2 ± 1.2.
Subject(s)
Diacylglycerol O-Acyltransferase/antagonists & inhibitors , Eleutherococcus/chemistry , Lignans/chemistry , Lignans/isolation & purification , Molecular Structure , Plant Stems/chemistryABSTRACT
Two new lignans were isolated from Saururus chinensis, along with eight known compounds. Their structures were elucidated on the basis of spectroscopic and physico-chemical analyses. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Among them, compounds 2, 3, 5 and 7 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values ranging from 44.3±1.5 to 87.5±1.3µM.